Liver Soviet Sustained-release Formulations

Gansu granule has been proved effective by a number of clinicalpractices in the treatment of chronic active hepatitis, B tyPe hepatitisand acute viral hepatitis. But probIems stilI exist in the present Gansupreparation like l) unclear substantial basis and pharmacologicalmechanisms of the raW material--Penthorum Chinense Pursh, 2)out-dated preparational technology, 3) inconvenience fOr patients'intake, such as relatively high dosage, too many daily intake times anduneasy preparation. In order to meet the need fOr modernization ofChinese herb preparation and improve the compatibility fOrintemational competition, the present study was designed to develop arelease caPsule of Gansu granule. It is aimed to elucidate thepharmacological basis of Gansu granule in the treatment of hepaticdisorders, explore its action mechanism such as antivirus,hepatoprotection and lowering enzyme, and also try to fOund amethodological system for evaluation the research and development ofreleased preparation of Chinese herb medicine.By using systematic solvent method and absorptive resin separatingmethod, the active extraction component of Penthorum ChinensePursh has been proved to be the ethanol elution from the big pore resinabsorbed water extraction. Seven chemical compounds have beenisolated from Penthorum Chinense Pursh by chemical analysis.Chemical structUre of six from the seven has been identified. Analysisand comParison of the fingerprint of differeflt extraction from varioussolvents were carried out with liquid chromatograPhy. Dimensionalfingerprint and liquid chromatograPhy combined withmass-spectrogram have been employed for the observation andanalysis of the active extraction. These works have fOund a solid basisfOr the study of the substantial basis of Gansu.Study on released preparation of Gansu has been carried out onthe basis of the defined active extraction. By using ultravioletspectrophotometry with gallic acid and quercetin as the referenceparametef, the extraction teclmology and the resin refine technologywas optimized, the tyPes and amount of adjuvant and the method forreleased-preparation has been clarified. Comparison between the invitro release rate of Gansu released capsule with common GansucaPsule showed that the release rate of release capsule was obviouslyslower than that of the common capsule, which suggested the effectsof the released preparation.In vitro release rate measured by ultraviolet spectrophotometry wasemployed fOr the quality control of Gansu release caPsule. In vivopharmacokinetics and pharmacodynamics of Gansu release capsulewere measured in dogs. The evaluation parameters were bloodconcentration-time relation (blood concentration of garlic acid as theindex) and the efficacy-time relation (inhibition rate of the elevatedSGPT as the index). Results suggested that Gansu release capsulecould maintain a relatively long and stable in vivo b1ood concentrationand efficacy.In the mean time, HPLC method for determining garlic acid andquercetin concentration in Gansu release caPsule has been fOunded inthis study Routine examinations and safety evaluations for caPsulepreparation were also perfOrmed.Wth the screening out active extractions of Gansu and developing therelease caPsule in this study, a research route for screening extractionsfrom Chinese herb medicine and a relative complete developing andevaluation system for release herb preparations have been explored.These provide a scientific basis for further research on release herbpreparation.