ELECTROMERIC EFFECT – E effect + E effect Pharmacy Chemistry

July 28, 2023 by Renee

WHAT IS ELECTROMERIC EFFECT?
The complete transfer of shared pairs of π electrons of a double bond or multiple bond to one of the bonded atoms under the influence of the attacking reagent is known as electromeric effect.

Is Electromeric effect a temporary effect?

Since the effect involves complete transference of electrons, it lead to the development of full positive charge (+) and negative charges (-) within the molecule. Electromeric effect is a temporary effect and operates in presence of attacking reagent and vanishes as soon as the attacking reagent is withdrawn.
If a proton (H+) adds to C=C bond, the π bond will break and the electron pair will transferred completely to one of the C atoms.
The electromeric effect has no specific direction. Its direction is always that which favours the reaction.
The effect takes place in the direction of the more electronegative element. It can be represented by the symbol E and is of two types: (i) + E effect (ii) – E effect.

What is + E effect and – E effect?

+ E effect: When the displacement of an electron pair is away from the atom or group, it is called + E effect.
-E effect: When the displacement of an electron pair is towards the atom or group, it is called + E effect.

Electromeric Effect explanation with Examples and Mechanism

The Polarizability that is deformation of an unsaturated system on the close approach of a reagent is called electromeric effect. The region when the reagent is removed without allowing the reaction to take place the electronics system reverse to the original ground state of the molecule so this is a temporary effect which operates in the substrate molecule on the demand of the reagent.

This this effect causes complete transfer of those by electrons from one atom to another causing one end positively charged and other negatively charged and the reagent to attack.

Due to the electromeric effect complete transfer of π electrons take place from one carbon to another through cyclic halonium ion which combines with halide iron to form the product when the multiple bond is between two decimal atoms the shift of electrons takes place towards the more electronegative of the two example edition of reagents on carbonyl compound like aldehydes or ketones.
Example edition of hcn on ca=0 maybe shown as under

Addition of grignard reagent alcohol NaHSO3 on carbonyl compounds takes place also in this way.
Does the electromeric effect is strong effect than inductive effect since in its effect the loose π electron shift acompletely there by producing full charge + and – on the carbon atoms while in i effect the charge developed on carbon joined to the substituent is small shown as delta §+ § negative.

WHAT IS ELECTROMERIC EFFECT PDF PDF

FOR MORE PHARMACY NOTES please read here.

INDUCTIVE EFFECT

Polarisation of one bond by the influence of an adjacent bond or group is known as Inductive effect. It can be attributed to dipolar interactions through the bonds of a
molecule. Example-The Cl atom in ethyl chloride attracts electron density from C atom to which it is attached and creates a permanent dipole. A carbon chlorine dipole influences
the adjacent C atom by its electron withdrawing inductive effect (-I effect).

Characteristics of Inductive effect:
1. It always causes bond polarization.
2. In C-H, there is almost no inductive effect.
3. Inductive effect is a permanent effect.
4. Inductive influences decreases as the distance from the source increases.

Do You Know What is Phagocytosis?

June 23, 2023 by Renee

Phagocytosis What & How

Phagocytosis:

White blood cells internalize multimolecular particles such as bacteria or old red blood cells by extending pseudopods that wrap around and seal in the targeted material.

A lysosome fuses with and degrades the vesicle contents.

During phagocytosis is also known as “cell eating”. Large multimolecular particles are internalized. Most body cells perform pinocytosis, many carry out receptor-mediated endocytosis, but only a few specialized cells are capable of phagocytosis, the most notable being certain types of white blood cells that play an important role in the body’s defense mechanisms. When a white blood cell encounters a large particle, such as a bacterium or tissue debris, it extends surface projections known as pseudopods (“false feet”) that surround or engulf the particle and trap it within an internalized vesicle . A lysosome fuses with the membrane of the phagocytic vesicle and releases its hydrolytic enzymes into the vesicle, where they safely attack the bacterium or other trapped material without damaging the remainder of the cell. Th e enzymes largely breakdown the engulfed material into raw ingredients, such as amino acids, glucose, and fatty acids, that the cell can use.

Phagocytosis Mechanism or Steps in Diagram

Role and Function of Phagocytosis in a Fun Learning Way:

Phagocytosis is a tale of drama, deception, and deadly dinner parties, that’s happening right inside your body!

Imagine, if you will, a game of ‘Pac-Man’ – but in this version, Pac-Man is a white blood cell, and the ghosts are pesky pathogens. Just like in the game, our white blood cell, Mr. Pac-Man, can’t just cruise around ignoring all the invaders in his path. He’s got to face them, gobble them up, and do some cellular spring cleaning.

You see, phagocytosis is just like a microscopic version of Pac-Man. When Pac-Cell, our hero, encounters a shady-looking bacterium, he doesn’t just shake his nucleus at it and walk away. Oh no. He goes full glutton mode and engulfs the whole thing – gulp! It’s like the world’s most deadly dinner party, where the guests are the meals! Canapes, anyone?

Once inside, the bacterium isn’t left to just roam about freely. This isn’t a vacation inside a cushy, plush cell, after all. It’s prison! There, the bacterium is greeted by a ruthless welcoming committee – lysosomes. They are filled with digestive enzymes that start breaking the bacterium down. These enzymes are like the cell’s personal chefs – but they’re not cooking up something delicious, they’re cooking up death for the bacteria. It’s the cellular equivalent of putting a virus through a meat grinder – not a pleasant experience!

In the end, the bacterium’s components are digested and recycled by the cell. And Pac-Cell? He’s ready for his next round of the game, always hungry, always hunting. So, next time you’re feeling a bit under the weather, remember – you’ve got an army of miniature Pac-Men inside you, gobbling up invaders and keeping you safe. Game on! What do you say?

That’s all about Phagocytosis. Comment us your doubts.

Structure Physiology Anatomy of EYE

February 6, 2023 by Renee

The eye is a specialized sensory organ of photoreception. The eye is an easily accessible organ for local or systemic drug delivery.

Clinically, the eye can be considered to be composed of two segments:

1. Anterior segment – all structures from (and including) the lens forward.
2. Posterior segment – all structures posterior to the lens.

The anatomical and physiological characteristics of the eye are described are outlined in this section.

Structure of the eye; The eye can be divided into two compartments: the anterior and posterior segments.

An internal cross section of an eye is shown in Fig.1

Anterior segment; Externally, the anterior segment of eye is made up of cornea, conjunctiva, and sclera.

Internally, it consists of anterior chamber, iris/pupil, posterior chamber, and ciliary body.

The cornea, an optically transparent tissue that aids in refraction of light to the eye for focusing, is 1 mm thick at the periphery and 0.5 to 0.6 mm thick in the centre.

It is composed of squamous and basal columnar epithelium, Bowman’s membrane, substantia propria (stroma), limiting lamina, and the endothelium.

The conjunctiva is a thin, transparent, vascularised mucous membrane with an area of 18 cm2 covering the eye globe and the inner eyelids.

It maintains the precorneal tear film and protects the eye. It produces mucus and lubricates the surface of the eye.

It is made up of stratified columnar epithelium and lamina propria. The conjunctiva epithelium is divided into bulbar (covering the eyeball), fornix (covering the cornea), and palpebral (covering the eyelid) conjunctivae.

The sclera, the white outer coat of the eyeball, provides structural integrity, size, and shape to the eye.

There are three layers in the sclera, the anterior episclera, the middle scleral stroma, and the posterior lamina fusca.

The sclera is composed of gel like mucopolysaccharides, elastic fibers, bundles of dense collagen fibrils, and fibroblasts.

The iris is a diaphragm around the pupil (lens) and controls the amount of light entering the inner eye.

The ciliary body is made up of ciliary muscles, which aid in accommodation.
The anterior surface of the eye is constantly rinsed by tear fluid secreted at a flow rate of about 1 μL/min by the main lachrymal gland of the lachrymal apparatus.
Tears eventually drain into the nasal cavity through the nasolachrymal ducts.
Tear fluid contains mucin, lysozyme, lactoferrin, prealbumin, and serum proteins.

It functions as an antibacterial lubricant and aids in draining out foreign substances.

The normal volume of tear fluid is 5 to 10 μL.65

Posterior segment:

Externally, the posterior segment consists of the optic nerve and associated vasculature, and internally, it consists of the lens, vitreous, and rear ocular tissues. Vitreous is a colorless medium

Internal structure of the eye consisting of about 99 percent water, dissolved type II collagen, sodium hyaluronate, and proteoglycans.

The retina is the inner nervous layer of the eye responsible for the sensory function of sight.

The choroid is a dark brown vascular layer attached to the sclera and is believed to provide nourishment to the retina.

Basic Structure of the Eye

The eye has three layers or coats, three compartments and contains three fluids

1. The three coats of the eye are as follows:

(a) Outer fibrous layer:
• cornea
• sclera
• lamina cribrosa.
(b) Middle vascular layer (“uveal tract”):
• iris
• ciliary body – consisting of the pars
plicata and pars plana
• choroids.
(c) Inner nervous layer:
• pigment epithelium of the retina
• retinal photoreceptors
• retinal neurons.

2. The three compartments of the eye are as follows:

(a) Anterior chamber – the space between the cornea and the iris diaphragm.
(b) Posterior chamber – the triangular space between the iris anteriorly, the lens and zonule posteriorly, and the ciliary body.
(c) Vitreous chamber – the space behind the lens and zonule.

3. The three intraocular fluids are as follows:

(a) Aqueous humour – a watery, optically clear solution of water and electrolytes similar to tissue fluids except that aqueous humour has a low protein content normally.
(b) Vitreous humour – a transparent gel consisting of a three-dimensional network of collagen fibres with the interspaces filled with polymerised hyaluronic acid molecules and water. It fills the space between the posterior surface of the lens, ciliary body and retina.
(c) Blood – in addition to its usual functions, blood contributes to the maintenance of intraocular pressure. Most of the blood within the eye is in the choroid. The choroidal blood flow represents the largest blood flow per unit tissue in the body. The degree of desaturation of efferent choroidal blood is relatively small and indicates that the choroidal vasculature has functions beyond retinal nutrition. It might be that the choroid serves as a heat exchanger for the retina, which absorbs energy as light strikes the retinal pigment epithelium.

D Pharmacy 1st Year Notes PDF Download -ADME -Pharmacology

February 26, 2022 by Renee

ADME DEFINITION:

Absorption, distribution, metabolism, and excretion are sometimes referred to collectively as ADME processes. These processes determine when the drug appears in the blood stream and for how long it remains in the blood stream to give noticeable action.

Absorption, distribution, metabolism, and excretion
When & how long the drug appears in the blood stream
therapeutic response is dependent upon the ADME processes

In order for a drug to cause a therapeutic response, it must reach adequate concentrations in the blood so that it can reach and interact with drug receptors in adequate numbers to trigger a noticeable action. The course of drug action is, therefore, directly correlated with the concentration of the drug in the blood stream, and is dependent upon the ADME processes.

ABSORPTION:

Absorption is the transfer of a drug from its site of administration to the bloodstream. The rate and extent of absorption depends on the route of administration, the formulation and chemical properties of the drug, and physiologic factors that can impact the site of absorption.

Transfer of a drug from site to the blood
route of administration, Drug properties
IV route is fastest and effective for ABSORPTION
Highly water-soluble drugs absorb more readily than fat-soluble drugs
Drugs with smaller particle sizes ABSORB easily

When a drug is administered intravenously, absorption is not required because the drug is transferred from the administration device directly into the bloodstream. In the case of intravenous administration, the entire dose of the drug is available to move to the sites of drug action. Administration by other routes may result in less availability due to incomplete absorption. When this occurs, less of the drug is delivered by the bloodstream to the site of action. When a tablet or capsule is swallowed it must dissolve before it can be absorbed. The dissolving of a tablet or capsule is referred to as dissolution. Manufacturing processes and the water solubility of the drug affect dissolution rates. Highly water-soluble medications dissolve more readily in the gastrointestinal (GI) tract, while fat-soluble drugs dissolve more slowly. Drugs with smaller particle sizes go into solution more readily. The inert ingredients added to formulations can also affect their dissolution

DISTRIBUTION

Distribution is a process when a drug is absorbed into the bloodstream it can be carried throughout the body. This process specifically carrying is called distribution. It is a reversible process; while some molecules may be interacting with receptors on cell membranes or inside of cells, other molecules may move back into the bloodstream.

Process of distribution of a drug from the bloodstream to the site of absorption.
Factors influencing distribution are blood flow, capillary permeability, the degree of binding and its solubility.
Blood-brain barrier protects the brain from entering high concentrations of drugs to CNS central nervous system.

The delivery of a drug from the bloodstream to the site of drug action primarily depends on blood flow, capillary permeability, the degree of binding (attachment) of the drug to blood and tissue proteins, and the relative lipid-solubility of the drug molecule. Blood flow to different organs of the body is not equal. The most vitally important organs of the body receive the greatest supply of blood. These organs include the brain, liver, and kidneys. Skeletal muscle and bone receive less blood, and adipose tissue (fat) receives the least. If blood flow were the only factor affecting distribution, it would be reasonable to expect that high concentrations of administered medications would always appear in the brain and liver. In reality, few drugs exhibit good penetration of the central nervous system. The anatomical structure of the capillary network in the brain creates a significant barrier to the passage of many drugs and is commonly referred to as the blood-brain barrier. This barrier is an adaptation that for the most part protects brain tissue from invasion by foreign substances. To readily penetrate into the brain, drugs must be fairly small and lipidsoluble or must be picked up by the carrier-mediated transport mechanism in the central nervous system. This explains why the small and highly fat-soluble anesthetic gases quickly and easily penetrate the brain to cause anesthesia, while other larger and water soluble molecules like penicillin antibiotics penetrate the central nervous system to a much lesser degree.

METABOLISM

Drugs are eliminated from the body either unchanged through the kidneys and bile, or they may undergo chemical changes that allow them to be more easily excreted. The process of undergoing chemical changes is called biotransformation, or metabolism. As previously noted, anything absorbed through the GI tract goes directly into the portal circulaextracellular Outside of the cell or cells. interstitial Situated within or between parts of a particular organ or tissue. intracellular Existing or functioning inside a cell or cells. hydrophilic Having an affinity for, readily absorbing, or mixing with water. lipophilic Having an affinity for, or ability to absorb or dissolve in, fats. biotransformation Chemical alterations of a compound that occur within the body, as in drug metabolism. prodrug An inactive drug precursor that is converted in the body to the active drug form. Absorption that feeds into the liver. The liver is adapted to clear toxins from the body and is the major site for drug metabolism, but specific drugs may undergo biotransformation in other tissues. The kidneys cannot efficiently excrete highly fat-soluble drugs that readily cross cell membranes because they are reabsorbed in the last stages of filtration. These compounds must first be metabolized in the liver to more water-soluble compounds and then removed. There are two types of metabolic processes drugs undergo in the liver. Most undergo one or both types of reactions. In the first type of reaction drugs are made more polar through oxidation-reduction reactions or hydrolysis. These reactions use metabolic enzymes, most often those of the cytochrome P450 enzyme system, to catalyze the biotransformation.

Metabolism is the process of undergoing chemical changes to get excreted easily is called metabolism
Biotransformation is also known as metabolism
Major site for drug metabolism is liver and Kidney
two types of metabolic processes
hydrolysis an enzyme-catalyzed reactions
conjugation reactions with glucuronic acid, sulfuric acid, acetic acid, or an amino acid like Glucuronidation.
Metabolism converts the prodrug to the active form. Example: Fosphenytoin is a prodrug of phenytoin,

In enzyme-catalyzed reactions, the rate of the reaction is accelerated by the presence of enzymes. A limited amount of enzyme is present at any given time in the liver. Since the rate of enzyme-catalyzed drug metabolism is limited by the quantity of available enzyme, metabolism in these cases is considered a saturable process. This means that the rate of conversion will only continue at the normal pace until the available supply of enzyme is used. At that point, metabolism is slowed until enzyme becomes available again. For the usual doses of most drugs, these reactions never reach saturation. There are a few drugs where doses may reach the saturation point of the enzymes. Once enzymes become saturated, blood levels increase exponentially toward toxicity. Examples include metabolism of alcohol and phenytoin. The second type of metabolism involves conjugation reactions. In this type of reaction the drug undergoing change is joined with another substance, such as glucuronic acid, sulfuric acid, acetic acid, or an amino acid. Glucuronidation is the most common conjugation reaction. The result of conjugation is a more water-soluble compound that is easier for the kidneys to excrete. These metabolites are most often therapeutically inactive. Some agents are initially administered as an inactive compound (prodrug) in order to improve availability or reduce side effects. Metabolism converts the prodrug to the active form. Fosphenytoin, for example, is a prodrug of phenytoin, a drug used for seizure disorders. Fosphenytoin is more completely and quickly absorbed when given by IM injection than phenytoin and can be used in critical situations with greater ease because it dose not require insertion of an intravenous catheter.

EXCRETION

When a drug is taken into and distributed throughout the body, it must be subsequently removed, or concentrations of the drug would continue to rise with each successive dose. The complete removal of the drug from the body is referred to as elimination. Elimination of the drug encompasses both the metabolism of the drug, and excretion of the drug through the kidneys, and to a much lesser degree into the bile. Excretion into the urine is one of the most important mechanisms of drug removal. The kidneys act as a filter for the blood and create urine as a vehicle for removal of waste. Blood enters the kidney through renal arteries and then is filtered by the glomerulus.

The complete removal of the drug from the body is referred to as elimination.
Excretion of the drug through the kidneys into the urine is one of the most important mechanisms of drug removal aside of liver.
the amount being taken in by the patient is equal to the amount being removed by the liver and kidneys. This state of equilibrium is called steady state

The glomerular filtrate becomes concentrated and substances are removed as it passes through the renal tubule and eventually becomes urine. Drug molecules in the bloodstream that are not bound to albumin are also filtered out into the glomerular filtrate. When drugs have not been converted to water soluble compounds in the liver, they are likely to be reabsorbed back into the bloodstream at the end of the filtration process, and will cycle through the body again. If they are water soluble, they will end up in the urine and be excreted. When a medication is given repeatedly, as most are in real patients, the total amount of drug in the body will increase up to a point and then stabilize. At this point, the amount being taken in by the patient is equal to the amount being removed by the liver and kidneys (Fig. 3.7). This state of equilibrium is called steady state, and drug levels will remain fairly constant unless there is a dose change, an interruption in treatment, or failure of the organs of elimination. The therapeutic effects of many drugs are closely correlated to a specific range of steady state serum drug levels, and physicians or clinical pharmacists will monitor these levels and adjust doses when necessary so that patients obtain the appropriate drug response.

What are Non Patentable Inventions? Types & Examples

July 28, 2021June 29, 2021 by Renee

THE PATENTS ACT, 1970 is an Act to amend and consolidate the law relating to patents.

INVENTIONS NOT PATENTABLE

What are not inventions.
The following are not inventions within the meaning of this
Act,—
(a) an invention which is frivolous or which claims anything obviously contrary to well established natural laws;
(b) an invention the primary or intended use or commercial exploitation of which could be contrary public order or morality or which causes serious prejudice to human, animal or
plant life or health or to the environment;
(c) the mere discovery of a scientific principle or the formulation of an abstract theory or discovery of any living thing or non-living substance occurring in nature;
(d) the mere discovery of a new form of a known substance which does not result in the enhancement of the known efficacy of that substance or the mere discovery of any new property or new use for a known substance or of the mere use of a known process, machine or apparatus unless such known process results in a new product or employs at least one new reactant.
Explanation.—For the purposes of this clause, salts, esters, ethers, polymorphs,metabolites, pure form, particle size, isomers, mixtures of isomers, complexes, combinations and other derivatives of known substance shall be considered to be the same substance, unless they differ significantly in properties with regard to efficacy;
(e) a substance obtained by a mere admixture resulting only in the aggregation of the properties of the components thereof or a process for producing such substance;
(f) the mere arrangement or re-arrangement or duplication of known devices each functioning independently of one another in a known way;
(g) Omitted by the Patents (Amendment) Act, 2002
(h) a method of agriculture or horticulture;
(i) any process for the medicinal, surgical, curative, prophylactic diagnostic, therapeutic or other treatment of human beings or any process for a similar treatment of animals to render them free of disease or to increase their economic value or that of their products.
(j) plants and animals in whole or any part thereof other than micro organisms but including seeds, varieties and species and essentially biological processes for production or propagation of plants and animals;
(k) a mathematical or business method or a computer programme per se or algorithms;
(l) a literary, dramatic, musical or artistic work or any other aesthetic creation whatsoever including cinematographic works and television productions;
(m) a mere scheme or rule or method of performing mental act or method of playing game;
(n) a presentation of information;
(o) topography of integrated circuits;
(p) an invention which in effect, is traditional knowledge or which is an aggregation or duplication of known properties of traditionally known component or components.
4. Inventions relating to atomic energy not patentable.—No patent shall be granted in respect of an invention relating to atomic energy falling within sub section (1) of section 20 of the
Atomic Energy Act, 1962 (33 of 1962).
5. Inventions where only methods or processes of manufacture patentable: [Omitted by the Patents (Amendment) Act, 2005]

For more information. please visit pharmawiki regularly.

[C program code] Demonstration of Backslash Characters or Escape sequences

September 3, 2020 by Renee

First year of B- Pharmacy has a subject Remedial Maths & Computers in which C language is the important topic. This is one of the important questions of it “[C program code] Demonstration of Backslash Characters or Escape sequences”

Backslash or escape characters

/*Demonstration of Backslash Characters or
Escape sequences
*/
#include<stdio.h>
main ()
{int i;
clrscr();
printf(“this is formfeed\t\t Example\f (\\f)\n”);
getch();
printf(“this is audible alert\t\t Example\a (\\a)\n”);
getch();
printf(“this is Backspace\t\t Example\b (\\b)\n”);
getch();
printf(“this is NULL\t\t Exam\n\0ple (\\0)\n”);
getch();
printf(“this is newline\t\t \n Example (\\n)\n”);
getch();
printf(“this is horizontal tab\t\t Exam\tple (\\t)\n”);
getch();
printf(“this is Vertical tab\t\t Example\v (\\v)\n”);
getch();
printf(“this is formfeed\t\t Example\f (\\f)\n”);
getch();
printf(“this is carriage return\t\t \rExample(\\r)”);
getch();
}

[/code]

🤦‍♀️3rd B-PHARM D- Pharm Juris Notes=Narcotic Drugs & Psychotropic Act,1985

August 20, 2020 by Renee

3rd B-PHARM Notes for Pharmaceutical Jurisprudence on Narcotic Drugs and Psychotropic Substances Act,1985 and Rules, 1985

Narcotic drugs and psychotropic substances are the habit forming substances which may produce a sleep. At higher concentration, those substances proved to be toxic and therefore, there is a restriction for the cultivation, collection, import, manufacture, purchase, sale, transportation of narcotic drugs and psychotropic substances. Psychotropic substances are substance, salt or any preparation which is included in the list of narcotic substance as specified in the Schedules to the Act.

Cannabis

Charas :

separated resin whether crude or purified obtained from Cannabis plant and also includes concentrated preparations and resin known as hashish oil or liquid hashish.

Ganja:

Flowering and fruiting tops of Cannabis plant excluding from seeds and leaves, or

Any mixture with or without neutral material of any above forms of Cannabis or any drink prepared from them.

Coca derivatives:

Crude cocaine which can be used directly or indirectly for the manufacture of cocaine; or

b) Ecgonine and all the derivatives of ecgonine from which it can be recovered; or
c) Cocaine i.e. methyl ester of benzoyl ecgonine; or
d) All the preparations containing more than 0.1% cocaine

Opium poppy

The plant of species Papaver somniferum or the plant of any other species of Papaver from which opium or any other phenanthrene alkaloids can be extracted and Central Government may declare to be Opium poppy.

Poppy straw

Parts of Opium poppy after harvesting them in their original form, cut or rushed and whether or not the juice has been extracted therefrom.

Poppy straw concentrate

Material arising when the poppy straw has entered into processes for the concentration of its alkaloids

Coca Leaf

Leaf of coca plant except a leaf from which cocaine and all the derivatives of ecgonine have been removed and any mixture with or without neutral material but does not include any preparation containing not more than 0.1% cocaine.

Coca Plant

Plant of any species of the genus Erythroxylon.

Medicinal Cannabis (hemp) is Extract or tincture of Cannabis (hemp).

Prepared opium

Opium which is obtained by any series of operations design to transform opium into an extract suitable for smoking and the dross or other residue remaining after the opium is being smoked.

Medicinal opium

Opium which has undergone the processes necessary to adopt it for its medicinal use in accordance with the requirements of Indian Pharmacopoeia or any other Pharmacopoeia notified, whether in powder form or granulated or mixed with the neutral material.

*only for educational purpose

Dry Granulation – STEPS METHOD USES PPT PDF

July 26, 2020June 29, 2020 by Renee

Dry granulation is a powder agglomeration process used in the pharmaceutical industry to improve the flowability of powders by increasing the particle size (granules). This operation is achieved using a roller press, which can have different configurations and equipment designs.
In simple terms Granulation is the process in which primary powder particles are made to adhere to form larger multiparticle entities called granules.

Dry Granulation Advantages & Limitations:

(Slugging of rollercompaction)
Advantages:
* Eliminates exposure to moisture and drying.
* Dusty procedure.

This is also called double compression or slugging method, this is valuable alternative to direct compression,
where the dose of drug is too high or to wet granulation when the drug is sensitive to heat, moisture or both.
This method is also used when other methods of granulation yield granules with poor flow or compression
properties, because there are less chances of segregation of drug and excipients.

Limitations:
* Not suitable for all compounds.
* Slow process.

Long processing time, a relatively high capital investment on heavy duty presses or compactors.

Steps involved in dry granulation process

I. Milling of drugs and excipients
II. Mixing of milled powders
III. Compression into large, hard tablets to make slug
IV. Screening of slugs
V. Mixing with lubricant and disintegrating agent
VI. Tablet compression

In dry granulation method the primary powder particles are aggregated at high pressure. There are two main processes – either a large tablet (known as slug) is produced in a heavy duty tableting press( known as slugging) or the powder is squeezed between two rollers to produce a sheet of material (roller compaction) . The two different types are illustrated in below:

Slugging process

how well a material may slug will depend on the below terms

Compressibility or cohesiveness of the matter,
Compression ratio of powder
Density of the powder
Machine type
Punch and die size
Slug thickness
Speed of compression
Pressure used to produce slug

Granulation by slugging is the process of compressing dry powder of tablet formulation with tablet press having die cavity large enough in diameter to fill quickly. The accuracy or condition of slug is not too important. Only sufficient pressure to compact the powder into uniform slugs should be used. Once slugs are produced they are reduced to appropriate granule size for final compression by screening and milling

Slugging (Old Method)Slugging (Old Method) • material to be granulized is first made into a large compressed mass or “slug” typically by way of a tablet press using large flat-faced too long.

Disadvantages of Slugging:

single batch processing
frequent maintenance changeover
poor process control
poor economies of scale
low manufacturing output per hour
excessive air and sound pollution,
Increased use of storage containers,
more energy and time required to produce

Roller compaction:

In a roller compactor material particles are consolidated and densified by passing the material between two high-pressure rollers. The densified material from a roller compactor is then reduced to a uniform granule size by milling.
Roller compaction dry granulation process is capable of handling a large amount of material in a short period of time. As a special subtype briquetting utilizes special designed compaction rolls which divides the compacted powder in pieces (briquettes).
For dry granulation the compaction force in extend and uniformity of distribution is essential in regard to uniformity of granules porosity to ensure uniform hardness and disintegration of the final product. Because of its advantages, roll compaction is being increasingly used as a granulation technique, but it is not a simple process and may involve many variables for example roll pressure, roll speed, horizontal/vertical feed screw speed, roller gap, screen size. These parameters need to be optimized depending on the materials and the type of equipment used in order to obtain products of desirable quality.

Pneumatic Dry Granulation:

The pneumatic dry granulation process is a new and patent pending technology. The granulation process is based on the
use of roller compaction with very low compaction force together with a proprietary air classification method. The method enables production of granules with extraordinary combination of flow ability and compressibility. The granules produced by Pneumatic Dry Granulation and tablets produced show fast disintegration properties, offering the potential for fast
release dosage forms, and Release time can be tailored to requirements.
PDG technology can achieve, high drug loading, even with difficult APIs and combinations along with Taste masking and Excellent stability

References:

Ankit Sharma, Pooja sethi, Dinesh pawar. “Granulation techniques and innovations”, Inventi Rapid: Pharmtech, Vol.10, 2011
Himanshu.K.Solanki, Tarashankar Basuri, Jalaram H.Thakkar, “Recent advances in granulation technology, International Journal of Pharmaceutical Sciences Review and Research, 3(5), 48,2010 . 11.
Nidhi Prakash Sapkal, Vaishali A. Kilor, Minal Nandkumar Bonde. Application of a convenient and cost and effective granulation technology for the formulation of tablets using conventional excipients, Asian Journal of Pharmaceutics – 225-254, 2014.
Rudnic EM, Schwartz JD. Oral solid dosage forms In: Remington: The science and practice of pharmacy Gennaro, Lippincott Williams and Wilkins, USA, 2000: 858.
Gohel MC. A review of co-processed directly compressible excipients. J Pharm Pharmaceut Sci 2005; 8: 76-93.
Schwartz JB, Fonner DE, Anderson NR, Banker GS. Granulation and tablet characteristics, Lieberman HA, Lachman L, eds. Pharmaceutical Dosage Forms: Tablets. Vol. 2, New York, Marcel Dekker, 1981:201.

Oxytocin: Functions Drugs Side Effects Contraindications Pharmacokinetics Dynamics

July 26, 2020September 2, 2019 by Renee

Oxytocin is a hormone, predominately belonging to mammalian family; it is secreted by the posterior pituitary gland. After its release in the blood stream it cannot re-enter the brain due to the presence of blood brain barrier .Oxytocin is a hormone that has both peripheral and central actions. y are synthesized in the magnocellular neurons present in the supra–optic and Para –ventricular nucleus present in the hypothalamus. The universally known functions would include its role at the time of labour and ejection of milk. The functions which remain partially unknown are in erectile responses, ejaculation, bonding, and feeling of love and maintenance of eye contact during a conversation.

Functions and roles of Oxytocin:

Oxytocin plays a key role in establishing trust , falling in love , parturition , milk ejection, mother – child bond , erection and ejaculatory response in males. Oxytocin insuffiency is leads to increased stress and sleep disturbances. The solution to the above mentioned problem lies in creating a drug which can mimic the functional properties of Oxytocin, which was achieved. Oxytocin has been widely used in the field of gynaecology to induce labour. It is also administered to patients i.e. mothers who are unable to produce milk after parturition. The invention of Oxytocin nasal sprays is not unknown. Recommended doses when administered to autism patients are proven to increase the sense of trust at the time of communication.

Mechanism of OXYTOCIN

Oxytocin is a naturally occurring nonapeptide hormone which acts through a G-protein coupled cell surface receptor to stimulate contractions of the uterus. A synthetic version of this hormone is used to induce contractions of the uterus which are indistinguishable from spontaneous labour.

Pharmacokinetics

Oxytocin is administered as a slow intravenous infusion (to induce or augment labour), or as a single intramuscular or intravenous injection to help prevent and treat uterine atony and postpartum haemorrhage. In pregnant women, oxytocin is metabolised very quickly in the maternal circulation by an aminopeptidase enzyme which cleaves the protein leaving it without biological function. This oxytocinase activity is also seen within the placenta and uterine tissue, and activity increases throughout pregnancy where at term the half -life of oxytocin is between 2 and 20 minutes.

Adverse effects

The main side effects are related to overstimulation of the uterus which can compromise the placental blood supply and fetal well-being, and can also contribute to rupture of the uterus especially in women who have had a previous caesarean delivery. Oxytocin is similar in structure to Vasopressin which is also produced by the posterior pituitary, and prolonged administration with intravenous fluids may lead to fluid overload, pulmonary oedema and water intoxication.

Oxytocin Molecular Formula

It has a molecular formula of C43H66N12O12S 2.

Oxytocin drugs:

Oxytocin is also known as Pitocin, Syntocinon, Ocytocin, Endopituitrina, Oxitocina, Oxytocine, Oxytocinum, Oxytocic hormone and Orasthin.

It has a molecular formula of C43H66N12O12S 2. They are commercially available as intravenous and intramuscular injections , nasal sprays and sublingual tablets .The commonly used Anirudha kabilan /J. Pharm. Sci. & Res. Vol. 6(4), 2014, 220-223 221 drug types are pitocin and syntocinon, the chemical resemblance to Oxytocin makes them an ideal drug of choice for various cases for example at time if parturition . Pitocin is composed of oxtocic acid/ml along with chlorobutanol , a chloroform derivative. However medical supervision is mandatory to rule out the onset of complications (20,31). The general uses of these Oxytocin drugs would include induction of labour .Under appropriate level , at the time delivery, Oxytocin binds to the receptors present in the myometrium , activates the pathway of hydrolysis of phoshotidyl inositol and diacyl glycerol, there by activating the same. This activation causes the release of intracellular Ca+ which causes contraction of the uterus .In conditions associated with low level of Oxytocin production this process is carried out by Oxytocin drugs (29, 27) Incase of people suffering from autism, administration of pitocin is said to reduce repetitive behaviour and also enhances speech. Few researches have proved the improvement of trust in people affected by autism when they were given pitocin nasal sprays. It also enhances eye to eye contact in these individuals. Pitcoin helps in social interaction in people who suffer from schizophrenia . So pitocin may not only combat hallucinogens and psychosis, but also make human interaction easier . Being a new field if research there is not enough evidence to prove the role pitocin in both autism and schizophrenia. Further, they are also used to cure problems in erectile responses, ejaculation, depression, anxiety, and stress management

Dosage of Oxytocin:

10 units by intravenous route or 20-40 mUnit/min by Intramuscular route are injected for post partum haemorrhage. 0.5-1 mUnit/min by intravenous route for the induction of labour.10-20 mUnit/min is administered along with other drugs for termination of pregnancy.

Pharmacodynamics

Uterine contractions are seen after 3-5 minutes and approx 1 minute of aministration through intramuscular and intravenous routes respectively. A steady state of the drug is reached after 40 mins of parenteral route of administration. It is distributed throughout extracellular fluid compartment of the mother; small amounts may cross the placental barrier and reach foetus. Metabolism takes place rapidly via the liver and plasma by the enzyme oxytocinase a few steps of metabolism also takes place via mammary gland. It has a half-life of 1-5 minute. Kidney and liver help in the elimination of Oxytocin drugs( 9) unchanged form of this drug is rarely excreted in urine (30). Overdose can cause titanic uterine contractions, impaired blood flow to the uterus, uterine ruptures, seizures and amniotic fluid embolism contractions, impaired blood flow to the uterus, uterine ruptures, seizures and amniotic fluid embolism.

Contraindications:

Significant cephalopelvic disproportion
Unfavourable foetal positions
Obstetric emergencies which favours surgery
Hyperactive or hypertonic uterus
When vaginal delivery is contraindicated,
Anaphylactic patients, Foetal distress
Polyhydramnios
Partial placenta pervia
Elective labour induction

Side effects

 Nausea or vomiting
 Memory problems or confusion
 Runny nose, sore throat, or coughing
 severe headaches
 hallucinations
 vomiting
 confusion
 Seizures and severe hypertension

Clinical Scenario 1

Which of the following abnormalities of labor is associated with a significantly increased incidence of neonatal
morbidity?
a. Prolonged latent phase
b. Protracted descent
c. Secondary arrest of dilation
d. Protracted active-phase dilation
Answer: c (Secondary arrest of dilation)
Explanation:
Three significant advances in the treatment of uterine dysfunction have reduced the risk of perinatal morbidity (PNM) and
mortality: (1) the avoidance of undue prolongation of labor, (2) the use of intravenous oxytocin in the treatment of some patterns
of uterine dysfunction, and (3) the liberal use of cesarean section (rather than midforceps) to affect delivery when oxytocin fails.

Clinical Scenario 2

Management of obstructed labor includes all, except:
[AIIMS May 2004]
a. IV fluids
b. Oxytocin use
c. Antibiotics
d. Cesarean section
Answer: b (Oxytocin use)
Explanation:
Two main principles in management of obstructed labor are:
1. Never wait and watch.
2. Never use oxytocin.
In patients of obstructed labor, the uterine contractions (power) are always adequate.
There is a problem with the passage or the passenger.
By increasing the power (by giving oxytocin) we are increasing the risk of rupture uterus.
It is like flogging a dead horse. Uterus is already contracting, and there is no point in increasing the contractions further in
a case of obstructed labor.
The patient should be given IV fluids to correct the dehydration and ketoacidosis, which usually develops due to prolonged
labor. Patient should be given antibiotics to prevent infection, and then steps should be taken to immediately relieve
the obstruction either by instrumental deliver or by LSCS. LSCS may have to be done even if the baby is dead and if vaginal
delivery is not possible, or else rupture uterus will occur.
NOTE: In cases of prolonged labor where there are hypotonic uterine contractions, oxytocin is justified.

LABELING -Pharmaceutical Labeling Requirements Theory PPT PDF

July 26, 2020July 17, 2019 by Renee

Labeling:

The term “labeling” designates all labels and other written, printed, or graphic matter upon an immediate container of an article or upon, or in, any package or wrapper in which it is enclosed, except any outer shipping container.

Labeling?

The term “label” designates that part of the labeling upon the immediate container. A shipping container containing a single article, unless such container is also essentially the immediate container or the outside of the consumer package, is labeled with a minimum of product identification (except for controlled articles), lot number, expiration date, and conditions for storage and distribution. Articles in these compendia are subject to compliance with such labeling requirements as may be promulgated by governmental bodies in addition to the compendial requirements set forth for the articles.

Label: Amount of Ingredient Per Dosage Unit:

The strength of a drug product is expressed on the container label in terms of micrograms or milligrams or grams or percentage of the therapeutically active moiety or drug substance, whichever form is used in the title, unless otherwise indicated in an individual monograph. Both the active moiety and drug substance names and their equivalent amounts are then provided in the labeling. Official articles in capsule, tablet, or other unit dosage form shall be labeled to express the quantity of each active ingredient or recognized nutrient contained in each such unit; except that, in the case of unit-dose oral solutions or suspensions, whether supplied as liquid preparations or as liquid preparations that are constituted from solids upon addition of a designated volume of a specific diluent, the label shall express the quantity of each active ingredient or recognized nutrient delivered under the conditions prescribed in Deliverable Volume 〈698〉. Official drug products not in unit dosage form shall be labeled to express the quantity of each active ingredient in each milliliter or in each gram, or to express the percentage of each such ingredient (see 8.140., Percentage Concentrations), except that oral liquids or solids intended to be constituted to yield oral liquids may, alternatively, be labeled in terms of each 5-mL portion of the liquid or resulting liquid. Unless otherwise indicated in a monograph or chapter, such declarations of strength or quantity shall be stated only in metric units.

Labeling: Use of Leading and Terminal Zeros

To help minimize the possibility of errors in the dispensing and administration of drugs, the quantity of active ingredient when expressed in whole numbers shall be shown without a decimal point that is followed by a terminal zero (e.g., express as 4 mg [not 4.0 mg]). The quantity of active ingredient when expressed as a decimal number smaller than 1 shall be shown with a zero preceding the decimal point (e.g., express as 0.2 mg [not .2 mg]).

Labeling of Salts of Drugs

It is an established principle that official articles shall have only one official title. For purposes of saving space on labels, and because chemical symbols for the most common inorganic salts of drugs are well known to practitioners as synonymous with the written forms, the following alternatives are permitted in labeling official articles that are salts: HCl for hydrochloride; HBr for hydrobromide; Na for sodium; and K for potassium. The symbols Na and K are intended for use in abbreviating names of the salts of organic acids, but these symbols are not used where the word Sodium or Potassium appears at the beginning of an official title (e.g., Phenobarbital Na is acceptable, but Na Salicylate is not to be written).

Labeling Vitamin-Containing Products

The vitamin content of an official drug product shall be stated on the label in metric units per dosage unit. The amounts of vitamins A, D, and E may be stated also in USP Units. Quantities of vitamin A declared in metric units refer to the equivalent amounts of retinol (vitamin A alcohol). The label of a nutritional supplement shall bear an identifying lot number, control number, or batch number. 10.40.50. Labeling Botanical-Containing Products The label of an herb or other botanical intended for use as a dietary supplement bears the statement, “If you are pregnant or nursing a baby, seek the advice of a health professional before using this

Labeling Parenteral and Topical Preparations

The label of a preparation intended for parenteral or topical use states the names of all added substances (see 5.20., Added Substances, Excipients, and Ingredients and see Labeling under Injections 〈1〉), and, in the case of parenteral preparations, also their amounts or proportions, except that for substances added for adjustment of pH or to achieve isotonicity, the label may indicate only their presence and the reason for their addition.

Labeling Electrolytes:

The concentration and dosage of electrolytes for replacement therapy (e.g., sodium chloride or potassium chloride) shall be stated on the label in milliequivalents (mEq). The label of the product shall indicate also the quantity of ingredient(s) in terms of weight or percentage concentration.

Labeling Alcohol:

The content of alcohol in a liquid preparation shall be stated on the label as a percentage (v/v) of C2H5OH.

Symbols Commonly Employed for SI Metric Unit

Symbols commonly employed for SI metric units and other units
are as follows:
Bq = becquerel dL = deciliter
kBq = kilobecquerel L = liter
MBq = megabecquerel mL = milliliterc
GBq = gigabecquerel μL = microliter
Ci = curie Eq = gram-equivalent weight
mCi = millicurie mEq = milliequivalent
μCi = microcurie mol = gram-molecular weight (mole)
nCi = nanocurie Da = dalton (relative molecular mass)
Gy = gray mmol = millimole
mGy = milligray Osmol = osmole
m = meter mOsmol = milliosmole
dm = decimeter Hz = hertz
cm = centimeter kHz = kilohertz
mm = millimeter MHz = megahertz
μm = micrometer (0.001mm) V = volts
nm = nanometera MeV = million electron volts
kg = kilogram keV = kilo-electron volt
g = gram mV = millivolt
mg = milligram psi = pounds per square inch
μg; mcg = microgramb Pa = pascal
ng = nanogram kPa = kilopascal
pg = pictogram g = gravity (in centrifugation)
fg = femtogram
a Previously the symbol mμ (for millimicron) was used.
b One milliliter (mL) is used herein as the equivalent of one cubic centimeter (cc).
c The symbol μg is used in the USP and NF to represent micrograms, but micrograms
may be represented as “mcg” for labeling and prescribing purposes. The term
“gamma,” symbolized by γ, frequently is used to represent micrograms in biochemical
literature