二氢杨梅素胃内漂浮片处方研究

Formula Study on Gastric-retention Tablets of Dihydromyricetin

关键词:  二氢杨梅素  胃内漂浮片  制备工艺

Key words:  dihydromyricetin  gastric-retention tablets  preparation technology

摘要:

目的 为了延长二氢杨梅素在胃内停留的时间，延缓药物的释放，将其制备成胃内漂浮片。方法 采用粉末直接压片法制片，运用单因素的平行实验和L₉(3⁴)正交设计，以起漂时间、漂浮持续时间及释放度为指标选择最佳处方。结果 最佳处方：片剂重量为300 mg，其他各成分的含量分别为：HPMC K4M 75 mg，PVP K30 40 mg，NaHCO₃ 40 mg，主药 80 mg，乳糖 65 mg，该制剂在37 ℃的人工胃液中立即起漂，12 h释放>90%，持漂时间>10 h。结论 制备的胃漂浮片具有优良的漂浮能力和释药行为，可增加二氢杨梅素在胃部的滞留时间，提高药物的稳定性，增强保肝作用。

Abstract:

OBJECTIVE To prepare and characterize gastric-retention sustained-release tablets of dihydromyricetin which is expected to prolong its floating time in stomach. METHODS Direct compression was used to prepare tablets, single factor experiment and orthogonal experimental design were used to optimize of the formulation based on the index such as the time to start floating, lasting time and the drug release rate. RESULTS The optimum formulation of 300 mg included: HPMC K4M 75 mg, PVP K30 40 mg, NaHCO₃ 40 mg, dihydromyricetin 80 mg, lactose 65 mg. In the artificial gastric juice of 37 ℃, the results showed that the products could immediately float, the drug released more than 90% within 12 h and the durative floating time was more than 10 h. CONCLUSION These prepared gastric-retention tablets show a good continual floating property and sustained-release, it could increase residence time and improve the stable of drug, also improve the efficacy for liver protection.