The Pharmaceutical Research Of Caragana Sinica Tablet

Toluylene glycosides from Caragana sinica (Buc’hoz) Rehd.(TGC), which is mainly active site of Caragana sinica (Buc ’hoz) Rehd, shows a wide range of physiological activity on the basis of modern pharmacological researches, such as the stimulation of osteoblast proliferation, promoting bone growth and adjusting bone metabolism. There have not been any formulations of TGC on the market yet. The aimof this project is to extract and purify TGC, which has therapeutic effects on osteoporosis, from Caragana sinica (Buc’hoz) Rehd, to make formulation of TGC, to optimize the production process of TGC, to establish its pharmaceutical quality and thus to prepare for the new drug application of TGC. The research mainly includes the following five parts:1. Quality standards of Caragana sinica.The quality standards of Caragana sinica.was established, which mainly includes identification and assayof CKV (carasinol B-kobophenol A (+)-a-viniferin).2. Optimization of extraction and purification process for effective ingredients (TGC)(1) The extraction process for effective ingredients in Caragana sinica was optimized. Three extraction methods were investigated, including soaking, hot refluxing and decoction with water. The orthogonal test design was used in the optimization, and the synthetic score based on the extraction rate of CKV was used as the assessment indices.(2) TGC were purified from Caragana sinica. by macroreticular resin. Purification is the key step to guarantee the quality of TGC extract. The best resin was selected by comparison of the adsorption capacity, elutive ratio and purity of CKV in the product. The technical procedure for purification of CKV with the optimum macroreticular resin was screened by content and transferring rate of CKV in product. A orthogonal test methodology was also employed to study the technological parameters of the purification process with AB-8type macroreticular resin. Similarity index of10batches of TGC was more than0.98, which showed the preparation process was stable and repeatable. 3. Quality standards of TGCThe quality standards of TGC was established, which mainly includes identification and the assay of CKV (carasinol B、kobophenol A、(+)-α-viniferin).4. Formulation and preparation of tablet of TGC.TGC tablets were prepared by direct powder compression. The excipients were selected on the basis of flowability and compressibility of the powder. The appearance, hardness, disintegration time and tablet weight variations were investigated by single-factor method.5. Quality standards of TGC tabletThe quality standards of tablet Caragana sinica.was established, which mainly includes character identification, tests on variation of the tablet weight and disintegration limit. The method of the assay and the dissolution test of carasinol B、kobophenol A、(+)-α-viniferin, which are the key ingredients in the tablet of TGC, were set up and validated.