physical and chemical behavior of drug products

1. Physical and Chemical Behavior of Drug Products

This part is about how drugs behave in different conditions (solid, liquid, or solution form) and how their stability can be affected.

🔹 Physical Behavior

  • Solubility – A drug must dissolve before it can act. Poor solubility = poor absorption.
    Example: Griseofulvin is poorly soluble, so micronization improves absorption.
  • Polymorphism – A drug can exist in more than one crystal form. Different forms = different solubility & stability.
    Example: Ritonavir tablets failed once because of a new polymorph appearing.
  • Hygroscopicity – Some drugs absorb moisture from the air (e.g., calcium chloride). This affects stability.
  • Particle size – Affects dissolution rate, absorption, and even the texture of creams/ointments.
  • Partition coefficient – Shows how a drug distributes between water and lipid phases (important for crossing membranes).

🔹 Chemical Behavior

  • Hydrolysis – Breakdown due to water.
    Example: Aspirin → Salicylic acid + Acetic acid.
  • Oxidation – Drug reacts with oxygen, losing potency.
    Example: Adrenaline (oxidizes to pink/brown color).
  • Photolysis – Drug degrades in light.
    Example: Riboflavin, nitroprusside.
  • Racemization – Conversion of active enantiomer to inactive one.
    Example: L-epinephrine → D-epinephrine (less active).
  • Polymerization – Small molecules join to form inactive complexes.

👉 Why it matters? If you don’t understand these, you can’t predict drug stability, packaging, or shelf-life.


2. Rationale Underlying Their Formulation

Here we ask: Why do we make a drug in a specific dosage form (tablet, injection, suspension, cream, etc.) instead of another?

🔹 Key Reasons

  • Stability – Some drugs are unstable in liquid form → made as dry powder for reconstitution (e.g., amoxicillin).
  • Bioavailability – Poorly soluble drugs need formulations like nanosuspensions, solid dispersions, or use of surfactants.
  • Patient convenience – Syrups for kids, injections for emergencies, transdermal patches for chronic use.
  • Drug release control – Immediate release vs. controlled/extended release vs. targeted release.
  • Taste masking – Bitter drugs (e.g., metronidazole) formulated with flavors/coatings.
  • Compatibility – Excipients are chosen so they don’t chemically react with the drug.

👉 Example: Nitroglycerin is explosive and unstable → formulated in tablets with excipients or transdermal patches for safe, controlled release.


3. Compounding Techniques of Pharmaceutical Preparations

This is the art + science part where pharmacists prepare customized medications when commercial products are not suitable.

🔹 Major Compounding Techniques

  1. Solutions

    • Simple solution: Dissolve drug in solvent.
    • Syrups, elixirs, tinctures.
    • Key concern: Solubility + preservation.
  2. Suspensions

    • Insoluble drug dispersed in liquid.
    • Must use suspending agents (e.g., methylcellulose).
    • Example: Antacid suspensions.
  3. Emulsions

    • Oil + water stabilized with emulsifiers.
    • Types: O/W (creams, lotions) and W/O (ointments).
    • Example: Castor oil emulsion.
  4. Ointments & Creams

    • Drug incorporated into a base.
    • Levigation (grinding drug with small amount of base/liquid).
  5. Powders

    • Simple mixing or geometric dilution for potent drugs.
    • Example: Oral rehydration salts (ORS).
  6. Capsules & Tablets (Extemporaneous)

    • Filling powders in capsules manually.
    • Making small-scale tablets with compression or molding.
  7. Sterile Preparations

    • Aseptic techniques for injections, eye drops.
    • Filtration, autoclaving, lyophilization.

👉 Modern compounding also includes:

  • Bio-identical hormone replacement (custom dosing).
  • Pediatric formulations (liquid forms when only tablets are available).
  • Oncology (dose adjustments, sterile prep).

🌟 Summary in One Line

  • Physical & chemical behavior → tells us how drugs degrade/act.
  • Rationale of formulation → explains why a drug is made in a certain dosage form.
  • Compounding techniques → shows how pharmacists prepare customized medicines safely and effectively.

 MCQs like:

  • Why is aspirin unstable in water?
  • Which excipient is used to mask bitter taste?
  • Which method is used to prepare ointments with insoluble drugs?

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