Preparation Of The Components Capsule Of Hedyotis Diffusa And Correlation Between In Vivo Absorption And In Vitro Release

The topic according to the present common liver diseases that endanger human body health, on the basis of the preliminary experiment study, quercetin, oleanolic acid, stigmasterol of three kinds of difficult soluble drugs are developed capsules. In order to improve the solubility and bioavailability in vivo, drug preparation into solid dispersions, filling capsules, obtain two kinds components capsule of Hedyotis diffusa has efficacy of liver, and the two capsules efficacy in vitro dissolution, in vivo pharmacokinetics studies and other aspects. And the efficacy, dissolution in vitro and in vivo pharmacokinetics of two kinds capsules were studied.With quercetin, oleanolic acid, stigmasterol, on the basis of the physical and chemical properties to establish content determination method, lay the foundation for the study of capsule preparation process.According to the preliminary experiment to optimization the prescription, preparation of two kinds of capsules, cumulative dissolution rate as index, through the carrier type inspect single factor experiment, carried out study on preparation process of solid dispersion capsule. The optimized process for:With PEG6000 as a carrier, the drug and carrier 1:1 mass ratio, freezing 30min prepared solid dispersion have the best dissolution effect.To study the dissolution in vitro of conventional capsule and solid dispersion capsule by absorbance-wavelength curve(AUAWC) combined with high performance liquid chromatography(HPLC), the results by AUAWC of ordinary capsule and solid dispersions capsule dissolubility within 10h mixed drug accumulation were 101.41 mg,129.19 mg, High performance liquid chromatography (HPLC) is used to measure quercetin, oleanolic acid, stigmasterol single ingredient additive in two capsules and cumulative dissolution rate within 10h were 101.24 mg,128.26 mg, the results show that two methods are basically consistent,date under two methods have a good affinity, explated combination of AUAWC and HPLC for total composition and individual components dissolution determination provide good methodological guidance, for research and development of new formulations to provide a theoretical basis.In pharmacokinetic study, with method of AUAWC-HPLC, two capsules mixed total of drugs and individual components conformed to one-compartement model in rats, Tmax are 0.5h,two capsules after drug preparation to solid dispersions, Cmax and AUC0-∞both increase, t1/2 decrease; Common capsule method of AUAWC AUC0-24 and AUC0-∞, are 20.748mg·h·L-1, 51.590mg·h·L-1, method of HPLC three kinds of single component add AUC0-24 and AUC0-∞ are16.258 mg·h·L-1,20.474 mg·h·L-1; Solid dispersion capsule method of AUAWC AUC0-24 and AUC0-∞ are 30.017 mg-h-L-1,62.360 mg·h·L-1, method of HPLC three kinds of single component add AUC0-24 and AUC0-∞ are28.657 mg·h·L-1,34.629 mg·h·L-1.In vitro and in vivo correlation results show that AUAWC of the total composition of Hedyotis diffusa Willd solid dispersion capsule of the correlation coefficient r=0.7656 prompt it had a good correlation between the in vitro dissolution and the in vivo absorption percentage.