Bioavailablity prodrugs and drug delivery

This is a short ppt about prodrugs and Drug delivery.

1. Name:-Umangi Thakkar Roll no:-062 Topic:- BiOAVAIBLITY , Prodrugs and Drug Delivery

2. What is Bioavailability Bioavailability, indicates measurement of the rate and extent(amount)of therapeutically active drug that reaches the systemic circulation and is available at the site of action. Concept of Bioavailability:- Rate and extent at which therapeutically active drug reaches systemic circulation. The fraction of administrated dose that reaches the systemic circulation in contrast to that stated on label. Rate and extent of absorption of unchanged drug from its dosage form.

3. Objectives Development of new formulations. Determination of influence of excipients, patient related factors and possible interaction with other drugs on rhe efficiency of absorption. Control of quality of a drug product during the early stages of marketing in order to determine the influence of processing factors,storage,stability on drug absorption. Primary stages of the development of a suitable dosage from for a new drug entity.

4. Prodrugs The concept of prodrug is first introduced by Adrian albert in 1958 to describe the compound undergo biotransformation prior to eliciting their pharmacological effect. Prodrug is defined as a biologically inactive derivative of a parent drug molecule that usually requires a chemical or enzymatic transformation within the body to release the active drug,and possess improved delivery properties over the parent molecule The development of prodrugs is now well established as a strategy to improve the physicochemical,biopharmaceutical or pharmacokinetic properties of pharmacologically potent compounds,and thereby increase usefullness of a potential drug.

5. Rational for prodrug design A)Improving formulation and adminstration. B)Enhancing permeability and absorption. C)Changing the distribution profile. D)Protecting from rapid metabolism. E)Overcoming toxicity problems

6. Properties of ideal prodrug

7. Classification of Prodrug.

8. A)Carrier linked prodrug Carrier linked prodrug consists of the attachment of a carrier group to the active drug to alter its physicochemical properties. The subsequent enzymatic or non-enzymatic mechanism release active drug moiety.

9. 1.Bipartite prodrug It is composed of one carrier(group)attached to the drugs. Such prodrugs have greatly modified lipophicity due to the attached carrier.The active drug is released by hydrolytic cleavage either chemically or enzymetically. Eg.Tolmetin-Glycine prodrug.

10. Tripartite prodrug. The carrier group ia attached via linker to drug.

11. Drug delivery Drug delivery systems refers to approaches,formulations,technologies, and systems for transporting a pharmaceutical compound in the body as needed to safely achieve its desired therapeutic effect. Based on two basic parameters: Route of entery. Dosage form. Method of drug delivery:-significant effect on efficacy. Current trend :-Targeted delivery & Sustained release formulations.