Studies Of Propranolol Hydrochloride Drug-resin Liquid Sustained-release System

In this paper, beta-adrenoceptor antagonists Propranolol hydrochloride(PNH)was used as model drug. New style excipient-strong acidic cationic exchange resin AMBERLITT IRP69 was used as drug carrier, drug resin liquid sustained-release delivery system was prepared. And we made systematic studies on PNH sustained-release suspension based on ion exchange resin. The studies were as follows:1) In the preformulation research, the analysis methods for dissolution and contents tests for PNH-resinates(microcapsules) were established, which were proved sensitive and reliable. The solubilities of PNH in different media were determined.2) The drug-resinates were prepared by bath method and column method. The influence of formulations and process on the rate and equilibrium of ion exchange reaction were investigated, and the optimal preparation method was defined. The studies of the drug release in vitro showed that the release rate was increased with the enhancement of the ionic concentration of the releasing media. The diffusion of PNH from the resin particles was controlled by a particle diffusion process according to Viswanathan's equation.3) Coated with Surelease(?) aqueous dispersions by a new reformed bottom spray fluidized bed, the microcapsules of PNH-resinates were prepared using the drug-resinates as capsule cores. Through investigation of the drug release, the final formulation and procedure were defined. The optimal microcapsule was able to maintain a sustained release in vitro, which was not disturbed by the pH of the releasing medium. With the increase of the ionic concentration and rotate speed, the release speed increased. The release of PNH from the microcapsules followed first order kinetics, which belonged to Fickian diffusion.4) The suspension medium was screened with stability parameters as evaluating criterias, and the suspension with good redispersibility was obtained. The accelerating testing and long-term testing for the suspension were investagated, which indicated that the prepared suspension had a good stability.5) The behaviors in vivo of PNH-resinates sustained-release suspension and the...