Study On TWH Release Sustained Dropping Pills

Traditional Chinese medicine(TCM)can reduce administration frequency and adverse drug reactions,enhance drug bioavailability,improve patients' compliance.Chinese medicine treatment of Chinese medicine and only realize various components synchronous sustained-release,while acting on the target site,in order to achieve synergies between the various components of the role,to play its multi-level,multi-target integrated advantages efficacy.So,an herbal medicine may be defined as a collection of active components in relatively steady ratios.Insoluble Tripterygium wilfordii Hook(TWH)was chosen as model drug and the self-made quality-controllable TWH extract was chosen as bulk pharmaceutical chemicals(BPC)to develop TCM preparation of TWH sustained-release dropping pills on the basic of solid dispersion theory.Through carrier controlled drug release,synchronous sustained-release of TWH multicomponents was intended to be achieved.HPLC in vitro analytical method of TWH extractive was established to determine the basic physiochemical properties of TWH,the dissolution rate and assay of TWH solid dispersions and the in vitro release and assay of dropping pills.After investigating the influence of different carriers and different ratios of drug to carrier on TWH dissolution rate,polyethylene glycol 6000(PEG 6000)and poloxamer 188(F68)were ultimately chosen as carrier materials to prepare TWH solid dispersions,drug: PEG6000:F86=1:2:1.Physiochemical property investigation suggested that the solubility of TWH effective components was increased apparently in different dissolution matrix in comparison with BPC.The triptonide lactone ketone in the water solubility of 30 times.main component of TWH,which cumulative dissolution was 80% in 60 minutes.X-ray diffraction(XRD),differential scanning calorimetry(DSC)and scanning electron microscope showed that drug may exist as amorphous state in solid dispersion.With the solubilization of solid dispersion,the sustained-release dropping pills of Tripterygium Wilfordii Hook was successfully made.Taking feed liquid temperature,condensate temperature,dripping speed and dripping gap as investigation factors,appearance quality and pill weight variation as investigation indexes,orthogonal design method was employed to optimize the preparation technics of dropping pills,the final optimized technics was: drug liquid temperature: 80°C,condensate temperature: 10°C,dripping rate: 30 d·min-1,dripping gap: 6 cm.Taking drug content,the ratio of water-soluble matrix to insoluble matrix and the ratio of stearic acid to glycerin monostearate as investigation factors,orthogonal design method was applied,the parameters of dropping pills were determined as: drug content 15%,the ratio of water-soluble matrix to insoluble matrix was 3:1,the ratio of stearic acid to glycerin monostearate was 3:1,in accordance with in vitro synchronism.The in vitro release degree test indicated that every effective component in dropping pills met sustained-release property and their similarity factor f2 were all greater than 50,satisfying the requirements of synchronous release.The in vitro drug release equation suggested that the drug release mechanism was the combination of dissolution and corrosion.For TWH dropping pill with high temperature,high humidity and strong light irradiation experiment,show that Humidity and temperature has certain influence to the stability of the preparation,should be in a dry and low temperature conditions preserve.