Study on shedding particles from Chuanping Sustained-release Tablets based on multi-marker components balanced release / 中草药

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”.