Study On Microencapsulation Of Sinomenine And Its Sustained-Release Tablet

Sinomenine as an active ingredient of acutum, it has anti-inflammatory, anti-rheumatic and immunosuppressive effect, commonly clinical used to treat rheumatism and arthritis, and also with in the treatment of chronic nephritis. But sinomenine has short half-life, and has stomach irritation, so it is necessary to study it in pharmaceutics.Established in vitro UV-visible spectrophotometry to determine the content. The detection wavelength was265nm. At this wavelength, excipient have no interference to the determination. The regression equation is:A=0.012C+0.0264, r=0.9998, within15～60μg·ml-1showed a good linear relationship between absorbance. Methodological study, the intra-day precision were good, and the relative standard deviation (RSD) values were less than equal to1.31%; low, medium, and high concentrations of the average recoveries were100.28%,99.67%,99.84%, and the relative standard deviation (RSD) values were less than1.08%.The paper chosen spray drying to prepare sinomenine microcapsules, use encapsulation efficiency for examine indicators, through single factor for the preparation of microcapsules prescription and screening process to determine the composition and microcapsules prescription dosage of each ingredient and spray the parameters of the drying apparatus. On the basis of a single factor, orthogonal design experiments to establish the optimal prescription:the capsule material is ethyl cellulose, the amount of4%; plasticizer as castor oil, the amount of1%; anti-viscosity of talc, the amount of0.4%; optimum process:inlet air temperature150℃, injection speed7ml·min-1, air velocity4.1m·s-1.Optimal process and get the best prescription for preparing microcapsules by the average encapsulation efficiency was90.2%, the average drug loading was16.7%, an average particle size of7.2μm, process reproducibility is good.Microcapsules prepared for further formulation studies, through the type and amount of excipients screening to determine the prescription hydrochloride sustained-release tablets Sinomenine composition. Tablets relative microcapsules, easy packing, transport and storage, but also improve patient compliance. Preparation of sustained-release tablets do stability study, the results meet the quality requirements. Established Sinomenine in vivo analysis of the content, and methodology are validated, recovery and precision are good, specific, and meet pharmacokinetic analysis requires the use of high performance liquid chromatography. Commercially available Zhengqingfengtongning release tablets for the reference formulation, homemade hydrochloride sustained-release tablets of Sinomenine test preparation, choice of coffee as the internal standard, regression equation Y=2.6211C+0.0119, r=0.9992, within0.1～3.2μg·ml-1range, a good linear relationship. Use3P97pharmacokinetic software for data processing, relevant pharmacokinetic parameters and the plasma concentration curve plotted against time, analyze the experimental results. The results show that self-release tablets Sinomenine microcapsules compared with commercially available formulations are bioequivalent and delayed time to peak plasma concentration is relatively stable, has a good release effect.