Excipients are inactive substances formulated with active pharmaceutical ingredients to create drug products. They serve important purposes like bulking up formulations, ensuring consistent drug release and stability, and determining properties of the final dosage form like tablet size and dissolution rate. Common excipients include diluents, binders, disintegrants, lubricants, and glidants. Diluents increase volume and include substances like lactose, starch and calcium phosphate. Binders promote adhesion while disintegrants facilitate breaking of tablets. Lubricants prevent adhesion during compression and glidants promote powder flow. Proper excipient selection is crucial for an efficacious and robust drug product.
The chapter deals with the preformulation studies that have to be considered while designing a dosage form and developing a formulation that is suitable for a patient. Here, physical and chemical properties of a drug substance are studied along with biopharmaceutical classification of drugs. Also a detailed study on the application of preformulation studies in different dosage forms are also studied.
The chapter deals with the preformulation studies that have to be considered while designing a dosage form and developing a formulation that is suitable for a patient. Here, physical and chemical properties of a drug substance are studied along with biopharmaceutical classification of drugs. Also a detailed study on the application of preformulation studies in different dosage forms are also studied.
Preformulation Studies: Introduction to preformulation, goals and objectives, study of
physicochemical characteristics of drug substances.
a. Physical properties: Physical form (crystal & amorphous), particle size, shape, flow
properties, solubility profile (pKa, pH, partition coefficient), polymorphism.
b. Chemical Properties: Hydrolysis, oxidation, reduction, racemisation, polymerization
BCS classification of drugs & its significant
Application of preformulation considerations in the development of solid, liquid oral and
parenteral dosage forms and its impact on stability of dosage forms.
A detailed study on every aspects of parenteral :- introduction, preformulation factors, essential requirements, vehicles and additives, isotonicity, production procedure, facilities, and controls, container and closure selection and finally the quality control evaluation of parenterals.
Hard gelatin capsules - a detailed studyTeny Thomas
The presentation involves a descriptive study on hard gelatin capsules which includes the production of the hard gelatin capsule shell, size of the capsules, capsule filling machines and the finishing techniques. The presentation also involves the special techniques of capsule formulation and the quality control tests of hard gelatin capsules
Pharmaceutical excipients are pharmacologically inert substances which are included in the manufacturing process or are contained in a finished pharmaceutical product dosage form to alter the functions.
Preformulation Studies: Introduction to preformulation, goals and objectives, study of
physicochemical characteristics of drug substances.
a. Physical properties: Physical form (crystal & amorphous), particle size, shape, flow
properties, solubility profile (pKa, pH, partition coefficient), polymorphism.
b. Chemical Properties: Hydrolysis, oxidation, reduction, racemisation, polymerization
BCS classification of drugs & its significant
Application of preformulation considerations in the development of solid, liquid oral and
parenteral dosage forms and its impact on stability of dosage forms.
A detailed study on every aspects of parenteral :- introduction, preformulation factors, essential requirements, vehicles and additives, isotonicity, production procedure, facilities, and controls, container and closure selection and finally the quality control evaluation of parenterals.
Hard gelatin capsules - a detailed studyTeny Thomas
The presentation involves a descriptive study on hard gelatin capsules which includes the production of the hard gelatin capsule shell, size of the capsules, capsule filling machines and the finishing techniques. The presentation also involves the special techniques of capsule formulation and the quality control tests of hard gelatin capsules
Pharmaceutical excipients are pharmacologically inert substances which are included in the manufacturing process or are contained in a finished pharmaceutical product dosage form to alter the functions.
Role and requirements of excipients in pharmaceuticals. Summary of new EU guideline published in March 2015 concerning risk assessment of excipients and excipient manufacturers.
drug execipent compatibilty studies is of prime importance for the better formulation of the new drug and also for reducing cost by verfication of the data at the earlier atage.
this presentation will give the brief explanation of the goal, importance, dteps involve to studi the drug execient compatibility studies with different examples suitable accordiingly.
These are the substances which are added in the formulation along the therapeutic agent so as to impart specific qualities in the formulation.
These are have very little or no therapeutic value but are necessary in the manufacture of various dosage forms.
Purposes served by Additives:
Provide bulk to the formulation.
Facilitate drug absorption or solubility and other pharmacokinetic considerations.
Aid in handling of “API” during manufacturing .
Provide stability and prevent from denaturation etc
An excipient is a pharmacologically inactive/ inert substance formulated alongside the active pharmaceutical ingredient of a medication. Drug products contain both drug substance (commonly referred to as active pharmaceutical ingredient or API) and excipients.
The most common tablet manufacturing process techniques are wet granulation, dry granulation, and direct compression.
Your active pharmaceutical ingredients’ (APIs) physical and chemical stability influences manufacturing.
For successful tablet manufacturing, you need granulators, mixing equipment, drying machinery, and coating systems.
Even if you’re using the right equipment to manufacture your product, there is a wide range of common tablet defects that can occur that affect quality.
There are several goals to aim for during the tablet manufacturing process:
Develop tablets that are strong and hard enough to hold up against mechanical shock during manufacturing, packaging, shipping, and dispensing
Formulate tablets that are uniform in weight and drug content
Manufacture bioavailable products according to indication requirements
Create chemically and physically stable tablets that last over long periods
Formulate products that are free of defects and have an elegant finish
These are diluents or fillers designed to make up the required bulk of the tablet.
These are inactive ingredients that are added to tablets in addition to the active drug.
Some very common diluents in tablet include lactose their derivatives, starch, cellulose derivatives.
Used in the direct compression the tablets.
Excipients..different types of excipients and its applications in pharmacetical industry for manufacturing of dosage forms.
few examples of commercially available excipients in the market for the manufacturing purpose of intended dosage forms.
Nutraceutical market, scope and growth: Herbal drug technologyLokesh Patil
As consumer awareness of health and wellness rises, the nutraceutical market—which includes goods like functional meals, drinks, and dietary supplements that provide health advantages beyond basic nutrition—is growing significantly. As healthcare expenses rise, the population ages, and people want natural and preventative health solutions more and more, this industry is increasing quickly. Further driving market expansion are product formulation innovations and the use of cutting-edge technology for customized nutrition. With its worldwide reach, the nutraceutical industry is expected to keep growing and provide significant chances for research and investment in a number of categories, including vitamins, minerals, probiotics, and herbal supplements.
Professional air quality monitoring systems provide immediate, on-site data for analysis, compliance, and decision-making.
Monitor common gases, weather parameters, particulates.
THE IMPORTANCE OF MARTIAN ATMOSPHERE SAMPLE RETURN.Sérgio Sacani
The return of a sample of near-surface atmosphere from Mars would facilitate answers to several first-order science questions surrounding the formation and evolution of the planet. One of the important aspects of terrestrial planet formation in general is the role that primary atmospheres played in influencing the chemistry and structure of the planets and their antecedents. Studies of the martian atmosphere can be used to investigate the role of a primary atmosphere in its history. Atmosphere samples would also inform our understanding of the near-surface chemistry of the planet, and ultimately the prospects for life. High-precision isotopic analyses of constituent gases are needed to address these questions, requiring that the analyses are made on returned samples rather than in situ.
This pdf is about the Schizophrenia.
For more details visit on YouTube; @SELF-EXPLANATORY;
https://www.youtube.com/channel/UCAiarMZDNhe1A3Rnpr_WkzA/videos
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Richard's aventures in two entangled wonderlandsRichard Gill
Since the loophole-free Bell experiments of 2020 and the Nobel prizes in physics of 2022, critics of Bell's work have retreated to the fortress of super-determinism. Now, super-determinism is a derogatory word - it just means "determinism". Palmer, Hance and Hossenfelder argue that quantum mechanics and determinism are not incompatible, using a sophisticated mathematical construction based on a subtle thinning of allowed states and measurements in quantum mechanics, such that what is left appears to make Bell's argument fail, without altering the empirical predictions of quantum mechanics. I think however that it is a smoke screen, and the slogan "lost in math" comes to my mind. I will discuss some other recent disproofs of Bell's theorem using the language of causality based on causal graphs. Causal thinking is also central to law and justice. I will mention surprising connections to my work on serial killer nurse cases, in particular the Dutch case of Lucia de Berk and the current UK case of Lucy Letby.
Richard's entangled aventures in wonderlandRichard Gill
Since the loophole-free Bell experiments of 2020 and the Nobel prizes in physics of 2022, critics of Bell's work have retreated to the fortress of super-determinism. Now, super-determinism is a derogatory word - it just means "determinism". Palmer, Hance and Hossenfelder argue that quantum mechanics and determinism are not incompatible, using a sophisticated mathematical construction based on a subtle thinning of allowed states and measurements in quantum mechanics, such that what is left appears to make Bell's argument fail, without altering the empirical predictions of quantum mechanics. I think however that it is a smoke screen, and the slogan "lost in math" comes to my mind. I will discuss some other recent disproofs of Bell's theorem using the language of causality based on causal graphs. Causal thinking is also central to law and justice. I will mention surprising connections to my work on serial killer nurse cases, in particular the Dutch case of Lucia de Berk and the current UK case of Lucy Letby.
Cancer cell metabolism: special Reference to Lactate PathwayAADYARAJPANDEY1
Normal Cell Metabolism:
Cellular respiration describes the series of steps that cells use to break down sugar and other chemicals to get the energy we need to function.
Energy is stored in the bonds of glucose and when glucose is broken down, much of that energy is released.
Cell utilize energy in the form of ATP.
The first step of respiration is called glycolysis. In a series of steps, glycolysis breaks glucose into two smaller molecules - a chemical called pyruvate. A small amount of ATP is formed during this process.
Most healthy cells continue the breakdown in a second process, called the Kreb's cycle. The Kreb's cycle allows cells to “burn” the pyruvates made in glycolysis to get more ATP.
The last step in the breakdown of glucose is called oxidative phosphorylation (Ox-Phos).
It takes place in specialized cell structures called mitochondria. This process produces a large amount of ATP. Importantly, cells need oxygen to complete oxidative phosphorylation.
If a cell completes only glycolysis, only 2 molecules of ATP are made per glucose. However, if the cell completes the entire respiration process (glycolysis - Kreb's - oxidative phosphorylation), about 36 molecules of ATP are created, giving it much more energy to use.
IN CANCER CELL:
Unlike healthy cells that "burn" the entire molecule of sugar to capture a large amount of energy as ATP, cancer cells are wasteful.
Cancer cells only partially break down sugar molecules. They overuse the first step of respiration, glycolysis. They frequently do not complete the second step, oxidative phosphorylation.
This results in only 2 molecules of ATP per each glucose molecule instead of the 36 or so ATPs healthy cells gain. As a result, cancer cells need to use a lot more sugar molecules to get enough energy to survive.
Unlike healthy cells that "burn" the entire molecule of sugar to capture a large amount of energy as ATP, cancer cells are wasteful.
Cancer cells only partially break down sugar molecules. They overuse the first step of respiration, glycolysis. They frequently do not complete the second step, oxidative phosphorylation.
This results in only 2 molecules of ATP per each glucose molecule instead of the 36 or so ATPs healthy cells gain. As a result, cancer cells need to use a lot more sugar molecules to get enough energy to survive.
introduction to WARBERG PHENOMENA:
WARBURG EFFECT Usually, cancer cells are highly glycolytic (glucose addiction) and take up more glucose than do normal cells from outside.
Otto Heinrich Warburg (; 8 October 1883 – 1 August 1970) In 1931 was awarded the Nobel Prize in Physiology for his "discovery of the nature and mode of action of the respiratory enzyme.
WARNBURG EFFECT : cancer cells under aerobic (well-oxygenated) conditions to metabolize glucose to lactate (aerobic glycolysis) is known as the Warburg effect. Warburg made the observation that tumor slices consume glucose and secrete lactate at a higher rate than normal tissues.
2. Excipient
An excipient is an inactive substance formulated
alongside the active ingredient of a medication, for the
purpose of bulking-up formulations that contain
potent active ingredients.
Drug products contain both drug substance
(commonly referred to as active pharmaceutical
ingredient or API) and excipients. Formulation of API
with excipients is primarily to ensure an efficacious
drug product with desired properties and a robust
manufacturing process
3. The resultant biological, chemical and physical properties
of the drug product are directly affected by the excipients
chosen, their concentration and interactions with the API:
Consistency of drug release and bioavailability
Stability including protection from degradation
Ease of administration to the target patient
population(s) by the intended route
Excipients determine the bulk of the final product in
dosage forms such as tablet, capsule, etc., the speed of
disintegration, rate of dissolution,release of drug,
protection against moisture, stability during storage,
and compatibility . Excipients should have no
bioactivity, no reaction with the drug substance, no
effect on the functions of other excipients, and no
support of microbiological growth in the product .
4. Ideal properties of excipient
No interaction with drug
Cost effective
Pharmacologically inert
Stable for handling
Feasible
5. Excipients are inactive ingredients used as carriers for
the active ingredients in a pharmaceutical product.
These may be classified into the following categories:
Antiadherents
Binders
Coatings
Disintegrants
Fillers and Diluents
Coloring Agents
Glidants
Lubricants
Preservatives
Sorbents
Sweeteners
6. DILUENTS
Diluents increase the volume to a formulation to prepare tablets of the
desired size. Widely used fillers are lactose, dextrin, microcrystalline
cellulose, starch, pregelatinized starch, powdered sucrose, and calcium
phosphate.
The diluent is selected based on various factors, such as the
experience of the manufacturer in the preparation of other
tablets, its cost, and compatibility with other formulation
ingredients. For example, in the preparation of tablets or
capsules of tetracycline antibiotics, a calcium salt should
not be used as a diluent since calcium interferes with
absorption of the antibiotics from the GI tract.
9. LACTOSE :
• solubility – water soluble
Forms
Hydrous
Anhydrous
used in wet granulation
shows fast disintegration, good friability,
practically no sticking, binding and
capping
• most widely used diluent
hydrous form undergoes maillard reaction discoloration of certain drugs
( amine drug )
• Problem of browning due to contamination of 5-hydroxyfurfural which was
accelerated in the presence of basic amine drugs and catalyzed by tartarate, citrate
and acetate ions
10. BINDERS
Binders promote the adhesion of particles of the
formulation. Such adhesion enables preparation of
granules and maintains the integrity of the final
tablet. Commonly used binding agents include:
starch, gelatin and sugars ( sucrose, glucose,
dextrose, and lactose).
12. Binders
Binders add mechanical strength to the
tablet or granules.
Starch
(1,4-alpha-glycosidic linkages)
Cellulose
(1,4-beta-glycosidic linkages)
Gellatin Polyethylene glycol (PEG)
13. Disintegrants
( Added to a tablet formulation to facilitate its breaking or
disintegration when it contact in water in the GIT).
• Example: Starch- 5-20% of tablet weight.
• Starch derivative – Primogel and Explotab (1-8%)
• Clays- Veegum HV, bentonite 10% level in colored tablet only
• Cellulose
• Cellulose derivatives- Ac- Di-Sol (sodium carboxy methyl cellulose)
• Alginate
• PVP (Polyvinylpyrrolidone), cross-linked
14. Mode of action:
In many cases water uptake alone will cause disintegration, by
rupturing the intra-particle cohesive forces that hold the tablet
together and resulting in subsequent disintegration.
If swelling occurs simultaneously with water uptake, the
channels for penetration are widened by physical rupture and the
penetration rate of water into the dosage form increased.
15. Superdisintegrants
• Swells upto ten fold within 30 seconds when contact water.
• Example: Crosscarmellose- cross-linked cellulose, Crosspovidone- cross-
linked povidone (polymer), Sodium starch glycolate- cross-linked starch.
• These cross-linked products swell upto ten fold within 30 seconds when in
contact with water.
• A portion of disintegrant is added before granulation and a portion before
compression, which serve as glidants or lubricant. Evaluation of carbon
dioxide in effervescent tablets is also one way of disintegration
16. Lubricant and Glidants
Lubricants are intended to prevent adhesion of the tablet
materials to the surface of dies and punches, reduce inter
particle friction and may improve the rate of flow of the tablet
granulation.
Glidants are intended to promote flow of granules or powder material
by reducing the friction between the particles.
Example: Lubricants- Stearic acid, Stearic acid salt - Stearic acid,
Magnesium stearate, Talc, PEG (Polyethylene glycols), Surfactants
Glidants- Corn Starch – 5-10% conc., Talc-5% conc., Silica derivative -
Colloidal silicas such as Cab-O-Sil, Syloid, Aerosil in 0.25-3% conc.
17. Compression lubricants prevent adherence of granule/powder to
punch die/faces and promote smooth ejection from the die after
compaction:
Magnesium stearate is by far the most extensively used tableting
lubricant
Lubricants tend to be hydrophobic, so their levels (typically 0.3 – 2%) need
to be optimised:
Under-lubricated blends tend to flow poorly and show compression
sticking problems
Over-lubricated blends can adversely affect tablet hardness and
dissolution rate
18. Lubricants can also be used when compression isn’t involved,
e.g.
In powder blends for filling into capsules to prevent adherence of
granule/powder to equipment surfaces and dosator mechanisms
Coating the surface of multi-particulate dosage forms (including
intermediate product) to inhibit agglomeration of individual particles
19. Glidants
Glidants promote flow of the tablet granulation or
powder materials by reducing friction between
particles.
The commonly used glidants are talcum, starch,
colloidal silica, silicates, stearates, calcium phosphate
etc.
The effect of glidants on the flow of the granules
depends on the shape and size of the particles of the
glidants and the granules
20. As a general rule hydrophilic materials act better on
hydrophilic granules and lipophilic ones on the
lipophilic granules.
The glidants in a particular formulation ensure
increasing flow of granules up to a certain optimum
concentration . If the concentration of the glidant is
taken beyond this, a drag action may come into
operation
bringing down the rate of flow.
21. Most commonly; colloidal silicon dioxide (traditionally, talc was
used)
Good bulk powder flowability is especially important during
high speed processing
Glidants improve flow by adhering to particles and so reducing
inter-particulate friction
Most common in dry powder formulations, e.g. direct compression tablets
Can also be added to granules to improve flow prior to compression
NB: can get undesirable “flooding” if flow is too good
Very low levels required (ca. <0.2%)
Control can be challenging with blends sensitive to levels
Very low bulk density (0.03 – 0.04g/cm3)
Difficult to work with (very voluminous) – not a standard excipient, only
added if needed
Issues with dust exposure