| Houpowenzhongtang consists of Cortex Magnoliae Officinalis, Semen Alpiniae katsumadai, Pericarpium Citri Reticulatae, Radix Aucklandiae, Radix Glycyrrhizae, Poria and Rhizoma Zingiberis. This paper is about the pharmcodynamics of Houpowenzhongtang with the optimized extraction process, investigation on formulation process of capsule, quality assessment on Houpowenzhong capsules, and pharmacokinetics of magnolol in Houpowenzhong capsules.Pharmacodynamic actions on gastric ulcer of Houpowenzhongtang with optimized extraction process with 95% ethanol were studied. Ulcer index and ulcer inhibition ratio were chosen as indicator. Results showed that 1/10 of the traditional dose of the extract with optimized process had significant preventive effect on gastric ulcer.Formulation process was investigated. For convenience in taking, the traditional decoction was transformed into capsule. The mean capsule content is about 0.35 g. The water content, weight variation and dissolution rate were investigated and all of them were in conformity with Chinese Pharmacopoeia.A high performance liquid chromatography (HPLC) method was developed for the simultaneous determination of seven effective components in Houpuwenzhong capsules. The separation was performed on a Scienhome C18 column (250 mm×4.6 mm,5μm) with methanol-acetonitrile-0.06% phosphonic acid (38:27:35, v/v/v) as the mobile phase at 30℃. The flow rate was 1.0 mL·min-1.The detective wavelength was set at 235 nm. There were good linear relationships between the mass concentrations and the peak areas of alpinetin, glycyrrhizic acid, honokiol, cardamonin, costunolide, dehydrocostus lactone and magnolol in the range of 0.885-17.7×10-3 mg·mL-1,0.107-2.140 mg·mL-1,8.850-177.0×10-3 mg·mL-1,1.035-20.70×10-3 mg·mL-1,4.850-97.00×10-3 mg·mL-1,5,900-118.0×10-3 mg·mL-1 and 0.0175-0.350 mg·mL-1, respectively. The recoveries were found to be in the range of 96.9%-101.1%,96.0%-100.5%,100.3%-100.8%,97.7%-101.4%,100.4%-102.3%,96.0%-102.3% and 96.2%-100.6%, respectively. This method is rapid, simple and suitable for the quality control of Houpowenzhong capsules. An HPLC method was developed to determine magnolol in rat plasma with adran as internal standard. After intragastric administration of Houpowenzhong capsule and extract of Cortex Magnoliae Officinalis respectively, pharmacokinetic behaviors of magnolol in rat plasma were compared. Acetoacetate solvent extraction was used to precipitate protein. The HPLC separation was achieved on a Scienhome C18 (200 mm×4.6 mm,5μm) column at 25℃. The mobile phase consisted of methanol-0.5% glacial acetic acid solution (80:20, v/v) at a flow rate of 1.0 mL·min-1. The UV detection wavelength was set at 225 nm. The extraction recoveries exceeded 82.9%. Linear calibration plot was obtained in the concentration range from 0.16 to 16μg·mL-1 (r>0.991). Intra-day RSD and inter-day RSD were no more than 4.5%. After intragastric administration of Houpowenzhong capsule and extract of Cortex Magnoliae Officinalis respectively, magnolol showed two-compartment model.Tmax was 0.43 and 0.85 h, Cmax was 2.53 and 1.82μg·mL-1, AUC0→t was 8.39 and 7.66 mg·h·L-1, AUC0→∞was 11.60 and 9.44 mg·h·L-1, t1/2αwas 0.268 and 0.769 h, and t1/2βwas 9.90 and 11.2 h respectively. |
