ZuoJin sustained-release tablets (ZJSRT), which consist of Rhizoma coptidis-Evodia rutaecarpa powder (6:1, g/g), have been widely used for a long time as a treatment of gastrointestinal disorders in China. Because ZJSRT is a kind of Chinese medicine prescription (CMP), it comprises many components, which makes the quality control studies more difficult. The main aim of this paper was to evaluate the release of four alkaloids using kinetic models and to assess the dissolution behaviors of ZJSRT using total quantum statistical moment (TQSM). The release data generated during in vitro release studies were fitted to zero-order, first-order, Higuchi, Hill, Weibull, and Michaelis-Menten models. The dissolution behavior data were obtained by calculating the TQSM parameters. The release kinetics of ZJSRT from most formulations follow a classical Fickian diffusion mechanism but do not follow an empirical model. The data from the TQSM parameters demonstrate that all components in ZJSRT released at nearly the same ratio and the same time. Therefore, the study should contribute to the quality control for CMP such as ZJSRT.
中国药学会药物安全评价研究专业委员会(Drug Safety Evaluation & Studu Special Committee,Chinese Pharmaceutical Association)、中国药理学会药物毒理专业委员会(Drug Toxicology Special Committee,Chinese Pharmacologic Society)、中国毒理学会药物毒理与安全性评价专业委员会(Drug Toxicology & Safety Evaluation Special Committee,Chinese Society of Toxicology)
Aim of the study: The inhibitive effect of BuYang HuanWu Decoction (BYHWD) and its major components on vascular intimal hyperplasia and the expressions of cell cycle protein and extracellular matrix protein. Materials and methods: Sprague-Dawley rats were randomly divided into sham-operated, control, alkaloid, glycoside, BYHWD and atorvastatin groups. Rat aorta intima in all groups were injured by insesion of domestic balloon catheter into the aortae except sham-operated rats. Drugs were administrated orally from the second day after vascular injury and continued for 14 days. The injured segments of aortae were collected on the sixteenth day after operation to observe the morphological changes of vascular structure and to examine the expressions of proteins in vascular cells associated with cell cycle including proliferating cell nuclear antigen(PCNA), cyclinD(1) and cyclinE, and extracellular matrix(ECM) proteins including collagen I (Col-1) and fibronectin (FN), further to discover the involved biologically active substances and the potential mechanisms. Results: Alkaloid and glycosid isolated from BYHWD were more effective than BYHVVD in the inhibition of intimal hyperplasia and the expressions of PCNA, cyclinD(1), cychnE, Col-I and FN, suggesting that alkaloid and glycoside may be the main components of BYHWD responsible for the observed inhibition of excessive hyperplasia of vascular intima. Conclusions: The mechanism associated with the anti-hyperplasia activity of BYHVVD and its effective components may be related to the blockage of cell cycles of VSMC, and the inhibition of the ECM protein synthesis, even the increased degradation of ECM proteins. (C) 2009 Elsevier Ireland Ltd. All rights reserved.