Sustained and Controlled Release Preparations.pptVIP

Sustained and Controlled Release Preparations Chapter 17 I. Introduction A.Definition (1)sustained release preparation It constitutes any dosage form that provides medication over an extended time by providing drug in a slow first-order or Higuchi fashion. (2)controlled release preparation It denotes that the system is able to provide some actual therapeutic control (time and site) by obtaining zero-order release from the dosage form. B.properties (1)reduce the frequency of dosing and prolong the effective time in order to enhance the patient compliance (2)provide uniform C in order to reduce side-effects (3)increase the effectiveness of the drug and better the absorption of the drug (4)drug choice and higher cost II.Design mechanisms and methods Key: how to hinder the release of the drug from the dosage form A.control the dissolution rate Noyes-Whitney equation: dc/dt=DKA(CS-C)/(Vh) (1)difficultly soluble derivatives: ↓CS (2)polymer complex (3)increase size: ↓A (4)polymer matrix B.control the diffusion rate adjusting the thickness and porosity of the diffusion layer (1)water-insoluble coating: EC, acrylic resin RS,RL (2)water-insoluble polymer+water-soluble materials (Tween-80, lactose, salts etc) (3)polymer matrix (4)↑viscosity: used in the liquid preparations C.osmotically controlled release when C in the core is CS, ΔP is constant resulting in constancy of the release rate zero-order finally, C↓, ΔP ↓, V ↓ D.control the degradation rate polymer with biodegradability: PLA degradation release+diffusion release E.ion-exchange control ion-exchange resin containing salt-forming functional groups in repeating positions on the polymer chains resin+-drug-+X- resin+-X-+drug- resin--drug++Y+ resin--Y++drug+ III.Design A.drug choice (1)therapeutic range (2)physico-chemical properties: S0 (3)absorption site (4)first-effect (5)t1/2 B.design objectives (1)bioavailability: 80%-120% of common preparation (2)fluctuate coefficient lower than commo