| Fagopyrum dibotrys(D. Don)Hara is one of perennial herbs of the genus Polygonaceae in the Fagopyrum family. Fagopyrum dibotrys(D. Don)Hara is listed in the Chinese Pharmacoepia and the tablets and capsules made of its extracts had been approved as medicaments in China.The efficient compositions isolated from Fagopyrum dibotrys(D. Don)Hara are named as procyanidins, the majority of which are the polyphenol coupounds in plants and the chemical structure of its major constituent is 5,7,3’,4’-tetrarydroxyflavon-3-ol C4-C8 dimers,i.e. procyanidins B2.Modern pharmacological studies showed that Fagopyrum dibotrys(D. Don)Hara has a wide range of pharmacological activity that clearing away heat and toxic,drainaging Septic,excluding congestion,it is primary applied to treat disease such as Lung abscess, Measles pneumonia, Peritonsillar abscess and so on.This subject mainly deal with:(1) establishment of a method for determing the content of princepal component; (2)extraction technology of crude drug; (3) Pharmacodynamics research; (4)preparation technology of soft capsule; (5)quality standard and stability of prepatation.According to literature and experiments, the HPLC method was employed in this paper to determine the content of (-)epicatechins and the UV spectrophotometry was employed to determine the content of total flavone as well as its dissolution. The TLC method was used to identify the herb.The extraction process of the active constituents is studied by the criterion of transference rate of (-)epicatechins, the content of total flavone and the extraction rate of the solid.The extraction methods,extracting solvents, the size that the herbal is comminuted, the soaking time, times of solvent, extracting hours are studied to investigate the influence on the typical principles’ extraction. Orthogonal tests are used to optimize ethanol concentration, the decoction time, decoction times and solvent volume.the transference rate of (-)epicatechins is 47.5%, the content of total flavone is 104.53 mg/g and the extraction rate of solid is 15%.The optimun method of extraction and purification process has a good repeatability.The pharmacodynamical experimentation of extract of Jin Qiaomai which is gotton by using the optimun extraction process indicates that Jin Qiaomai soft gelatin capsule has definite treatment on the anti-inflammation, antitussive, expectorant pharmacological effects with definite therapeutic effectiveness and neglectable side effects.The ratio between extract and diluent, the size of extract powder, the kinds of suspending agent and wetting agent were studied to test the influences on the physical stability of the content with the sedimentation ratio of the content suspension as the test index. The final formulation of content was determined as follows:the ratio between extract and soybean oil was 1:1.5. Glyceryl monostearate was used as the suspending agent, accounting for 1% of soybean oil. Span-80 was used as the wetting agent, accounting for 0.5% of soybean oil. With the results of pharmacodynamics and constituents of prescription,the final dose of JQM is four capsules at a time and every capsule has 0.66mL matter.The contents quality is 0.70 g.With the dissolution rate of lemon yellow added in the capsule shell as the index, ratio between gelatin and glycerin, storage temperature, supplements added were investigated to test their influence on the solubility of capsule shell. The final formulation of capsule shell was fixed as follows:gelatin:glycerin:water:butenedioic acid:titanium dioxide preservatives (1:1.2:1.0: 0.032:0.0064:0.0064, w/w). With own control method the dissolution of Jin QiaoMai total flavone were measured in PBS 6.8, water and chlorhydric acid solution (0.1 mol/L),0.5%SDS solution respectively. The 0.5%SDS solution was selected as the dissolution medium in vitro. The dissolution of total flavone reached 80% within 45 min.Preliminary stability tests showed that the stability of this product is good. |
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