Control Drug Delivery System
Control Drug Delivery System
Control Drug Delivery System
II. Gen. The release is under control of the drug delivery system Advantages:
Avoids fluctuations of plasma drug concentration p better safety and efficacy Decreased frequency of drug administration (often once daily admin) p better compliance May overcome some problems with BAV Can be much more economical (better cost-effectiveness)
Sustained release (SR) release of the initial API dose & further prolonged release
Biopharmaceutical consideration
1. Release from formulation 2. Movement within body during its passage to site of action
Drug in dosage form
Release
Absorption
Drug in body
Biopharmaceutical properties
Molecular weight of drug Aqueous solubility of the drug Apparent partition coefficient of drug Drug pKa and pH Drug stability in G.I.T. Mechanism of absorption Route of administration
Approaches
A. Continuous release system
1. Dissolution Controlled drug release system a. Matrix Dissolution Controlled system b. Encapsulation/coating Dissolution Controlled drug release system 2. Diffusion Controlled drug release system a. Matrix Diffusion system b. Reservoir devices 3. Dissolution and diffusion Controlled drug release system 4. 5. 6. 7. 8. Ion exchange resin drug complexes Slow dissolving salts and complexes pH depending formulation Osmotic pressure Controlled system Hydrodynamic pressure Controlled system
Dosage forms for systemic administration Parenteral route dosage forms Implants
Controlled drug delivery for over a long time (months/years) Principle Reservoir (Osmotic/diffusion) systems Matrix systems
Non-biodegradable Biodegrable polymeric materials with dispersed drug
Advantages largely overcomes problems with individual compliance Disadvantages mini-surgery is needed, uneasy to simply discontinue the therapy, local reactions
Examples: hormones/contraception
Disadvantages
Not feasible for all API ! Mr < 500 Well balanced lipohilicity High potency (high doses can not be accommodated and delivered) p Penetration enhancers can help! Local relations (irritation, disruption of barrier skin function) Need not be practical/comfortable Need not be cost-effective
Examples of clinical use: hormones (HRT, contraceptives), opioid analgesics (e.g., fentanyl), nitroglycerine, nicotine (RT), clonidine or scopolamine
Liposome's
Niosomes
Evaluation testing