Version  1.0
 File Size  02.90 mb
 File Count  1
 Create Date  July 13, 2022
 Update Date  July 13, 2022
 Telegram  Join Now

You have to wait 15 seconds.

Syllabus of Unit 1 :-

Preformulation Studies : Introduction to preformulation, goals and objectives, study of physicochemical characteristics of drug substances.
  • Physical properties : Physical form (crystal & amorphous), particle size, shape, flow properties, solubility profile (pKa, pH, partition coefficient), polymorphism
  • Chemical Properties : Hydrolysis, oxidation, reduction, racemization, 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.

1. Preformulation Studies

It is defined because the phase of research and development in which preformulation studies characterize physical and chemical properties of a drug molecule so as to develop safe, effective and stable dosage form.

Objectives :-
  1. To establish the physio-chemical parameters of a brand new drug entity
  2. To determine its kinetics and stability
  3. To establish its compatibility with common excipients
  4. It provides insights into how drug products should be processed and stored to confirm their quality.

2. Powder Flow Properties

Powder flow properties are often laid low with change in particle size, shape & density.
The flow properties depends upon following
  1. Force of friction.
  2. Cohesion between one particle to a different.
  • Fine particle posses poor flow by filling void spaces between larger particles causing packing & densification of particles.
  • By using glidant we are able to alter the flow properties. e.g. Talc

3. BCS classification of drugs

The Biopharmaceutical organization (BCS) has been a prognostic tool for assessing the potential effects of formulation on the human drug oral bioavailability. When utilized in conjunction with in vitro dissolution tests, the BCS can suppaort the prediction of in vivo product performance and also the development of mechanistic models that support formulation assessments through the generation of “what if” scenarios. To date, the applicability of existing human BCS criteria has not been evaluated in dogs, thereby limiting its use in canine drug development.

Within the framework of human pharmaceuticals, drugs will be classified into one in all the subsequent four BCS categories :-
  1. Class I : high solubility, high permeability: generally very well-absorbed compounds
  2. Class II : low solubility, high permeability: exhibits dissolution rate-limited absorption
  3. Class III : high solubility, low permeability: exhibits permeability-limited absorption
  4. Class IV : low solubility, low permeability: very poor oral bioavailability