Study On Qingxin Ling PH - Controlled Sustained - Release Pellets

Wanshi Niuhuang Qingxin pills are recorded in ChP(2005 Edition). It consists of six medicines which are bezoar, cinnabar, coptis chinensis, scutellaria, gardenia and curcumae. However due to torpidity action and comparatively large dose, it was restricted in clinical use. Based on Wanshi Niuhuang Qingxin pills and inspired by successful prescription change of Angong Niuhuang Boluses, Qingxinling is a new preparation of Chinese Materia Medica conducted by the method of modern pharmacology. It is made up of bezoar, berberine hydrochloride, baicalin, extracts of cape jasmine (content of jasminoidin above 50%)and aetherolea of Curcuma(enclosed byβ-CD). Qingxinling pellets choose active component and active part for drug use, greatly reduce dosage, increase function of velocity and provide another new preparation for clinical drug use.The qualitative and quantitative determination of index component-berberine hydrochloride, baicalin and jasminoidin was obtained by HPLC. To determine the content of pellets, a method was developed for the detection of berberine hydrochloride and baicalin by HPLC simultaneously. The method is simple and available,and it is suitable for the quality control of the preparationOptimization of extraction of Gardenia by Orthogonal Design, the content of extracted jasminoidin reached over 50%; The Study was developed on Inclusion Complex ofβ-CD with extracted aetherolea and optimal conditions of inclusion technology ofβ-CD was obtained by the method of Orthogonal Design.This experiment used coating pan system for Qingxinling pellets. Apply blank pill core for coating pan, adjusting the speed of coating pan 35r·min-1 and the temperature 30℃, then injected into the right amount of water to the surface, which of surface wettability not agglomeration, uniformly sprinkle into medicamental pulverata,and then consperge into sufficient water, alternate progress. Results of such an alteration of the operation show that the preparation was of good fresh spirit pellets, the pellets rounded appearance of berberine hydrochloride dissolution with preparations.Under the condition of different pH in dissolved bingxisuan resin as coating material, prepared by three kinds of coated pellets in vitro simulated human gastrointestinal tract pH conditions of the release of the determination of berberine hydrochloride, the results show that the drug release showed it clear that various components with different properties are released synchronously.Through the pH control sustained-release pellets preliminary stability test results show that the coating of pellets, in the conditions of wet, heat and light relatively stable. After three months of acceleration experiments of berberine hydrochloride, showed no obvious changes release.Pharmacokinetic studies, determined by HPLC method for six rats oral home-made pills and home-made pH-control sustained-release pellets and spirit of berberine hydrochloride after drug concentration. The result show that the peak of berberine hydrochloride Cmax blood concentrations decreased obviously, the role of time significantly extend, body also presents the gradient pulse medicine expected.