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 clarify the influence of the different combinations (consumption, fillers) of Improved Peach Gum to the balance release of complex components. Methods: Use Chuanping Prescription as model drug, Improved Peach Gum as sustained release materials, the release test companied with HPLC was applied to determine the accumulated release rate of the index components (ephedrine, pseudoephedrine, scopolamine) in Chuanping Sustained-release Tablets, calculate the cumulative release curve slope K value, and to evaluate the balance release of the different components. Results: The study on different combinations, when the filler is starch, starch/dextrin, and starch/MCC, the index component cumulative release curves were close to slope K value and can achieve the balance release; match with dextrin and MCC, the slope K values are different and can not achieve the balance release. With increasing the amount of Improved Peach Gum, release time prolonged, cumulative release slope K values of index components are basically same and can achieve balance release. Conclusion: Different fillers match with Improved Peach Gum can affect the balance release of complex components of Chinese materia medica; Different amount of Improved Peach Gum will affect the drug release time, but not affect on balance release.