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Module 3
Pharmaceutics Part II
Objectives
Biopharmaceutics
Involves the formulation, dissolution, stability, and controlled release of drugs.
Biopharmaceutics — Relationship with Pharmacokinetics and Pharmacodynamics
Integrates with pharmacokinetics (ADME) and pharmacodynamics (concentration-effect relationships).
Dosage Formulation
A combination of an active ingredient with excipients to create a specific dosage form.
Dosage Form — Importance
Determines the route of administration and influences drug efficacy and safety.
Pharmacokinetic-Pharmacodynamic (PK-PD) Models
Link between drug concentration in systemic circulation and receptor interaction.
PK-PD Models — Purpose
Provide the basis for dose optimization to achieve desired therapeutic outcomes.
Challenges in Veterinary Drug Delivery
Species diversity, body size variations, husbandry practices, seasonal changes, and economic factors.
Innovative Solutions in Veterinary Drug Delivery
Topical spot-on formulations, microencapsulation, and controlled-release systems for ruminants.
Oral Route of Administration
Widely used in companion animals (dogs, cats) and food animals (cattle, pigs, poultry).
Oral Dosage Forms — Liquids
Solutions, suspensions, emulsions, elixirs, and syrups.
Oral Dosage Forms — Semisolids
Pastes.
Oral Dosage Forms — Solids
Tablets, capsules, powders, granules, premixes, and medicated blocks.
Advantages of Oral Dosage Forms
Convenient administration and systemic effects through GI absorption.
Oral Dosage Forms — Examples
Tablets for dogs, granules in rations for horses, and premixes for poultry.
Challenges and Considerations of Oral Dosage Forms
Absorption variability, drug stability problems, and the need for careful pharmaceutical formulation to ensure efficacy.
Absorption — Oral Dosage Forms
Absorption rates can vary.
Drug Stability — Oral Dosage Forms
Acid-labile drugs may be destroyed in the stomach.
Formulation Requirements — Oral Dosage Forms
Careful pharmaceutical formulation is needed to ensure efficacy.
Parenteral Route
Any non-oral route of administration.
Four Main Parenteral Routes
Intravenous (IV), Intramuscular (IM), Subcutaneous (SC), and Intra-articular (IA).
Injectable Preparations — Sterile Solutions
Use water for injection or alternative solvents.
Injectable Preparations — Excipients
Antioxidants, antimicrobial preservatives, buffers, chelating agents, inert gases, and tonicity-adjusting agents.
Injectable Preparations — Sterility
Injectable preparations require sterility and avoidance of pyrogens.
Suspensions — Injectable Dosage Form
An injectable dosage form; example: procaine penicillin G.
Factors Influencing Drug Release from Injectable Suspensions
Viscosity and particle size.
Emulsions — Injectable Dosage Form
Can be oil-in-water or water-in-oil emulsions.
Propofol
Example of an injectable emulsion.
Dry Powders — Injectable Dosage Form
Require reconstitution before administration.
Dry Powders — Common Use
Commonly used in vaccines through freeze-drying (lyophilization).
Intramammary Infusions
Used in treating mastitis in lactating and nonlactating cows.
Intramammary Infusions — Key Consideration
There are key differences between formulations used for intramammary infusion.
Intravaginal Devices
Include Controlled Internal Drug Release (CIDR) devices, Progesterone-Releasing Intravaginal Devices (PRIDs), and vaginal sponges.
Intravaginal Devices — Use
Used in estrus synchronization in sheep, goats, and cattle.
Implants — Examples
Weight gain and feed conversion implants; reproductive performance enhancers.
Reproductive Performance Enhancers — Examples
Deslorelin for mares and testosterone for wethers.
Implants — Legal Consideration
Extralabel use for growth promotion is not legal in the US.