Study on shedding particles from Chuanping Sustained-release Tablets based on multi-marker components balanced release
(2.Jianmin Pharmaceutical Group Co., Ltd., Wuhan, China 430000)
【Abstract】 Objective To study 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 medicinal compound sustained-release preparation. Methods Using Chuanping Prescription (Herba Ephedraeand Flos Daturae) as model drug and improved peach gum and HPMC as sustained release materials, the release test combinied with underwater video observation were applied to shot external forms at different time points, and the laser particle analyzer was applied to determinate particle size. 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 balanced release of the different components. Results For CST which were made by the improved peach gum and HPMC sustained-release excipient, particles were dropped at 0.5 h after contacting the dissolution medium. At the same time, the particles were obviously shedded over time. In contrast, for CST that were 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); particle size was larger (D50 was 53.37–70.33 μm and D90 was 100.3–196.5 μm), and drug loading was higher (ephedrine 30.63%, pseudoephedrine 32.97%, and scopolamine 31.67%); besides, the release time of drug was longer (60–120 min). Conclusion The shedding particles were important part of balanced release of multi-marker components about CST which were made by the improved peach gum sustained-release excipient, and also were the embodiment of the drug release mode of “corrosion–dissolution”.
【Keywords】 shedding particles; balanced release; multi-marker components; improved peach gum; HPMC; sustained release; in vitro release; particle size; laser particle analyzer; HPLC;
(Translated by ZHAO B)
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