INTRODUCTION TO PHARMACEUTICS 1 (PHYSICAL PHARMACY-DOSAGE FORM DESIGN).ppt

INTRODUCTION TO PHARMACEUTICS 1 (PHYSICAL PHARMACY-DOSAGE FORM DESIGN)
INTRODUCTION TO PHARMACEUTICS 1 (PHYSICAL PHARMACY-DOSAGE FORM DESIGN)
INTRODUCTION TO PHARMACEUTICS 1 (PHYSICAL PHARMACY-DOSAGE FORM DESIGN)

1. COLLEGE OF
PHARMACY
Dr. Mohammad Javed Ansari, PhD.
Contact info: [email protected]
PHARMACEUTICS-I
(PHT 232)
INTRODUCTION TO
Pharmaceeutics 1
(PhYSICAL PHarmacY -DOSAGE FORM design)

2. OBJECTIVES OF THE LECTURE
•At the end of this lecture, you will be able to know:
•The course specifications / topics of Pharmaceutics 1 (Physical
pharmacy).
•What is pharmacy and pharmaceutics?
•What is physical pharmacy?
•What are drugs, excipients and dosage forms?
•Why drugs are not used as such?
•Why formulation of dosage form is necessary?
•What are factors affecting dosage form design?
•What are various dosage forms?

3. Pharmaceutics 1-Course specifications

4. Pharmaceutics 1-Course specifications

5. Pharmaceutics 1-Course specifications

6. Pharmaceutics 1-Course specifications

7. Pharmaceutics 1-Course specifications

8. Pharmaceutics 1-Course specifications

9. Pharmaceutics 1-Course specifications

10. Pharmaceutics 1-Course specifications

11. Pharmaceutics 1-Course specifications

12. Pharmaceutics 1-Course specifications

13. Pharmaceutics 1-Course specifications

14. Pharmaceutics 1-Course specifications

15. Pharmaceutics 1-Course specifications

16. PHARMACY , PHARMACEUTICS & PHYSICAL
PHARMACY
•Pharmacy is the study of all aspects of drugs, both natural and
synthetic in origin, including- their chemistry, their uses in
medicines, and how they work within the body.
•Pharmaceutics is the study of all aspects of turning an active
pharmaceutical ingredient (API) into a Stable, Safe &
Effective (SSE) dosage form. It includes-
•Physicochemical factors (Pre-formulation studies),
•Biopharmaceutical factors (Formulation studies),
•Therapeutical factors (Patient’s age & disease)
•Suitable dosage forms (SSE) must be developed with
optimum dosing regimen (OD, BD and IV, IM) to overcome
barriers and optimize drug action (minimize adverse effects).
•Pharmacy is the science of drugs and Pharmaceutics is the
science of drug delivery (dosage form design).
•Physical pharmacy is application of physicochemical
principles in optimum dosage form design.

17. DRUG VERSUS DOSAGE FORMS: RATIONALE OF DOSAGE FORM
DESIGN
•Drug ?
•Active drug substance (active pharmaceutical ingredient - API)
•chemical compound with pharmacological (or other direct effect )
intended for used in diagnosis, treatment or prevention of diseases
•International non-proprietary names (INN / “generic“ names)
•Direct clinical use of the active drug substances is rare: Why??
•Rational behind drug formulation or dosage form design
•API handling and Accurate dosing can be difficult or impossible
(e.g., potent drugs: low mg and g doses)
•API administration can be impractical/unfeasible because of size,
shape, smell/odour, taste and low activity.
•Some API are chemically unstable in light, moisture, O
2
•API can be degraded at the site of administration (e.g., low pH in
stomach).
•API may cause local irritations or injury when they are present at
high concentrations at the site of administration.
•Administration of pure active substance would mean to have no
chance for modification (improvement) of its PK profile

18. •To provide for the safe and convenient delivery of
accurate dosage of potent drugs like Digoxin (0.25
mg) Thyroxin (0.05 mg) we can design tablets,
capsules, syrups, injections etc.
•For the protection of a drug substance from the
destructive influence of atmospheric oxygen or
moisture, we can design coated tablets, sealed
ampules.
•For the protection of a drug substance from the
destructive influence of gastric acid after oral
administration we can design enteric coated tablets.
•To conceal the bitter taste, salty obnoxious or odor
of a drug substance we can design capsules, coated
tablets, flavored syrups
Need of drug formulations : overcoming the
difficulties

19. •To provide liquid dosage forms of soluble drugs for
infants & children we can design solutions, syrups.
•To provide liquid preparations of drugs that are either
insoluble or unstable we can design suspension.
•To provide liquid preparations of oily drugs we can
design emulsions.
•To provide faster local effects with less side effects we
can design, inhalational aerosols, eye drops, ear drops,
ointments, enemas, rectal and vaginal suppositories.
•To provide very long duration of action for chronic
diseases we can design Implants.
•To deliver drugs with undesirable pharmacokinetic
profiles we can develop modified release or controlled
release formulations.
Need of drug formulations : overcoming the
difficulties

20. Definition: Dosage forms are the means by which drug molecules
/ APIs are delivered to sites of action within the body to produce
optimum desired effects and minimum adverse effect.
The need for dosage forms:
DRUG SAFETY/BENEFIT:
Protection from environment (light, moisture, O
2).
Protection from patients (gastric juice).
PATIENTS SAFETY/BENEFIT:
Accurate dose of potent drugs for children and elderly patients
Preventing local drug irritations/ ulcers.
Modifying PK of drug for optimum action(↑ benefits,↓ side effects)
Masking taste and odour of API.
Presenting API in desired / required forms. (Use of desired vehicle for
insoluble drugs, insertion of drugs into body cavities and placement of
drugs within body tissues like implants).
Need of drug formulations : overcoming the
difficulties

21. •Active drug substance (active pharmaceutical ingredient - API)
•Excipients (inactive pharmaceutical ingredients)
•Diluents/fillers, binders, lubricants, disintegrants, coatings,
preservantives and stabilizers, colorants and flavourings.
•Technological, biopharmaceutical and/or stability reasons
•Pharmaceutical dosage form
•is a drug delivery system which is formed by technological
processing (drug formulation)
•determines the physical form of the final pharmaceutical
preparation
•Pharmaceutical preparation (PP)
•particular pharmaceutical product containing active and inactive
pharmaceutical ingredients formulated into the particular
dosage form.
•Packed and labelled appropriately
•Two major types of PP according the origin:
•Manufactured in large scales by pharmaceutical industry
(original and generic preparations)
•Compounded individually in compounding pharmacies
From drug substance to Pharmaceutical Dosage
forms

22. •Drug substances /API are seldom administered in their
natural or pure state, but rather as part of a formulation in
combination with one or more excipients such as
diluents/fillers, binders, lubricants, disintegrants, coatings,
preservantives / stabilizers, solublizers, colors and flavors.
•It is the pharmaceutical excipients that serves to
solubilize, suspend, thicken, dilute, emulsify, stabilize,
preserve, provide color, flavor and fashion the drug
substances (API) into safe, stable, effective and appealing
pharmaceutical preparations.
•Therefore these excipients are also called as
pharmaceutical aids / pharmaceutical ingredients /,
pharmaceutical adjuncts / pharmaceutical necessities.
•Through selective use of these excipients we can design
and develop various type of dosage forms or
pharmaceutical preparations as per requirement.
From drug substance to Pharmaceutical Dosage
forms

23. Factors affecting Dosage Form Design
1. Drug Consideration In Dosage Form Design
•Organoleptic considerations such as physical appearance,
taste, smell, tactility, size, & “Pharmaceutical elegance”.
•Physicochemical properties of drug substance such as type
(crystalline/ polymorphs/ amorphous / hygroscopic), melting
point, boiling point, solubility, pKa, lipophilicity, reactivity,
flow properties, rheological behaviour etc.
•Stability of drug substance. Oxidation / hydrolysis,
photolysis, rate of degradation (pH stability profile).
•Determining Drug Formulation Stability – Compatibility
Active vs. active vs. excipients vs Container.
•Prevention Against Microbial Contamination
From drug substance to Pharmaceutical Dosage
forms

24. Factors affecting Dosage Form Design
2. Therapeutic Considerations In Dosage Form Design
2.1 Nature of the disease or illness. Chronic / acute
2.2 Age of the Patient: Infants /children / adults.
3. Biopharmaceutics Considerations
3.1 PK profile of drug:
Where/how well is the drug absorbed?
Where/how the drug is distributed, metabolized & excreted?
What is biological half life of drug?
3.2 Intended site of action: Systemic / local
3.3 Intended onset of action: Immediate / sustained /delayed.
From drug substance to Pharmaceutical Dosage
forms

25. They are classified according to:
Route of administration Physical form
Oral Solid
Topical Semisolid
Transdermal Liquid
Parenteral Gases
Inhalation
Buccal & sublingual
Ophthalmic
Otic
Rectal
Vaginal


TYPES OF DOSAGE FORMS

26. TYPES OF DOSAGE FORMS: Physical
Semi-solid dosage forms
Shaped Suppositories (for rectal administration)
Pessaries (vaginal suppositories)
Unshaped Gels, Creams, Ointments, Pastes
Solid dosage forms
Shaped Tablets, Capsules, Implants, Transdermal patches
Unshaped powders for external/internal use
Liquid dosage forms
MonophasicSolutions (syrups, spirits, elixirs, Tinctures)
Biphasic Emulsions, Suspension
External solutions: Lotions, Liniments, Collodions etc
Gaseous dosage forms
Medicinal gases Aerosols: Inhalation/volatile anaesthetics
Aerodispersions Antiasthmatics sprays

27. TYPES OF DOSAGE FORMS: Route of Administration
Enteral
Oral Tablets, Capsules, syrups, suspension, emulsion etc.
Dry Powder Inhaler (DPI) pressurized Metered Dose Inhaler
(pMDI) • Nebulizer • Vaporizer
Sub-lingual
Buccal
Orally Disintegrating Tablet (ODT) • Lozenges • Chewing
tablets, Mouthwash • Toothpaste • Ointment • Oral spray
Rectal Ointment • Suppository • Enema • Nutrient enema
Topical
DermalOintment
 • Liniment • Paste • Cream • Lotion • Lip balm •
Medicated shampoo
 • Dermal patch •
MucosalEar drops • Eye drops • Nasal spray • Ointment • Hydrogel •
Nanosphere suspension • Mucoadhesive microdisc
(microsphere tablet), pessaries.
Percutaneous: Transdermal patch
 etc
Parenteral (injections & infusions)
Intravenous • Intramuscular • Intracardiac • Intraosseous •
Intraperitoneal • Intracerebral • Intrathecal • Intradermal • Subcutaneous

28. TEST YOUR KNOWLEDGE
•Compare pharmacy, pharmaceutics & physical pharmacy?
•Compare drugs, excipients and dosage forms?
•Why drugs are not used as such?
•Why formulation of dosage form is necessary?
•What are various factors that affect design of dosage forms?
•What are various dosage forms?
•What are different classification of dosage forms?

29. THANK YOU
FOR
YOUR ATTENTION..
Questions?