Sinomenine Articular Injection Of Microspheres

Sinomenine Hydrochloride(SM), a pure alkaloid extracted from traditional Chinese medicine-Caulis Sinomenine, which has the Effectiveness of anti-inflammatory analgesic, anti-rheumatic and immune inhibition, has been mainly used for rheumatoid arthritis in clinical therapeutics. In this study, Sinomenine Hydrochloride gelatin microspheres (SM-GMS) were prepared by emulsification linkage for intra-articular injection.The method of UV was set up to determine the concentration of SM in the preparation and in vitro release. The formulation and process of the SM-GMS were studied according to investigating the basic physical characters of the drug. Applying appearance, particle size and drug-loading rate of microspheres to evaluate the quality of microspheres, the best formulation and process was screened by signal factor studies and orthogonal test.The physical and chemical characters of microspheres were evaluated by scanning electron microscope, laser size tester. The appearance was smooth without much adherence, the mean diameter was 6.40μm ,the loading amount was10.4%, the encapsulation efficiency was 73.3%. The stability study indicated that only the appearance of microspheres could be slight influenced by high temperature and high humidity.The release kinetics of microspheres in vitro could be characterized by Higuchi equation, the equation is Q=13.248 t^1/2+9.0044, R=0.9707, t₅₀=9.58 h. From the in vitro release curve it is obvious that the SM-GMS is a delayed-release preparation.The method of HPLC was developed for the analyzing of drug in rabbits plasma. The T_max of SM-GMS and control group were 24h and 4h respectively. The pharmacokinetics characters showed that the preparation of SM-GMS can keep the blood concentration on certain level longer than 50h, so it obviously delayed release.According to the Local biopsy identified by experts, there is no significantly Pathological and Physiological change between blank microspheres group and the saline group .That means the biocompatibility of the preparation is good, the organizations of the joint can not be damaged under long-term using .