ABSTRACT
Objective: To study on the changes of shedding particles, drug loading and release of Chuanping Sustained-release Tablets (CST) which were made by the different sustained-release excipients in vitro, so as to elucidate the mechanism about balanced release of multi-marker components on Chinese materia medica compound sustained-release preparation. Methods: Using Chuanping Prescription (Ephedra Herba and Datura Flos) as model drug, improved Peach Gum and HPMC was used as sustained release materials, the release test combinied with underwater video observation were applied to shot external forms at different time point, and the laser particle sizer was applied to determinate particle size, and HPLC was applied to determine the accumulated release rate of the index components (ephedrine, pseudoephedrine, and scopolamine) to calculate the cumulative release curve slope K value, and to evaluate the balance release of the different components. Results: CST which were made by the improved peach gum and HPMC sustained-release excipient, which particles were dropped at 0.5 h after contacting the dissolution medium. At the same time, the particles were obviously shedding with the passage of time. In contrast, CST that was made by the improved peach gum, its balanced release of multi-marker components was better (K of ephedrine was 12.18, K of pseudoephedrine was 12.30, and K of scopolamine was 12.40), and particles dropped faster (it was significantly at 1 h), and particle size was bigger (D50 was 53.37—70.33 μm and D90 was 100.3—196.5 μm), and drug loading was more (ephedrine 30.63%, pseudoephedrine 32.97%, and scopolamine 31.67%), and release time of drug was longer (60—120 min). Conclusion: The shedding particles were important part of balance release of multi-marker components about CST which was made by the improved peach gum sustained-release excipient, and also was the embodiment of the drug release mode of “corrosion-dissolution”.
ABSTRACT
OBJECTIVE: To establish a method for the quality control of Lonicerae Japonicae Flos by multi-components quantitative fingerprint. METHODS: Chlorogenic acid was selected as the marker of ingredients to establish the HPLC fingerprint and as the internal reference standard to determine the contents of other eight components(neochlorogenic acid, cryptochlorogenic acid, chiratin, rutin, galuteolin, isochlorogenic acid B, isochlorogenic acid A and isochlorogenic acid C) according to the relative correction factor of quantitative analysis of multi-components by single marker(QAMS) by slope correction method. At the same time, the nine components were determined by external standard method. The accuracy and feasibility of QAMS were evaluated by comparison of the results between external standard method and QAMS. RESULTS: The fingerprint of Lonicerae Japonicae Flos was established, 21 common peaks were identified in all the tested samples, nine of which were verified, the similarities of 20 batches of Lonicerae Japonicae Flos samples were in the range of 0.959-0.997, and there was no significant difference between the quantitative test results of nine ingredients in 20 batches by the QAMS method and external standard method. CONCLUSION: The method of multi-marker components quantitative fingerprint is feasible and accurate for the quality control of Lonicerae Japonicae Flos, and it might be a new quality evaluation pattern for Traditional Chinese medicine.