清咽滴丸中冰片和薄荷脑体外溶出及人口腔黏膜吸收规律研究

目的：由于滴丸类药物的载药量小,使得滴丸类制剂研究受到限制,因此本研究旨在考察清咽滴丸中冰片、薄荷脑体外溶出行为和人口腔黏膜吸收特性。方法：建立清咽滴丸中冰片和薄荷脑同时测定的气相色谱法。采用智能药物溶出仪研究清咽滴丸中冰片和薄荷脑的体外溶出规律,并对5名健康志愿者口腔黏膜吸收特性进行研究,以这两种成分在志愿者口腔黏膜的累积吸收百分率与其在体外试验中的累积溶出百分率进行相关性研究。结果：体外溶出实验结果表明,冰片、薄荷脑分别在10、20 min累积溶出百分率达到最大,分别为84.3%、79.7%;志愿者口腔黏膜吸收试验结果表明,冰片、薄荷脑分别在45、30 min累积吸收百分率达到最大,分别为90.3%、94.6%。对体外溶出及其口腔黏膜吸收试验结果进行相关性分析,结果表明清咽滴丸中冰片、薄荷脑体外溶出及口腔黏膜吸收之间具有良好的相关性,相关系数分别为r=0.890、r=0.907。结论：建立了灵敏、快速、准确的同时测定清咽滴丸中冰片和薄荷脑的气相色谱法,通过体外溶出实验及人口腔黏膜吸收试验均可以表明滴丸制剂中的主要成分冰片、薄荷脑具有溶出快、释药快、吸收快的特性，符合滴丸制剂的临床要求，并为指导临床用药提供理论依据。

Study on the rule of buccal absorption in human and the release discipline of borneol and menthol in Qingyan drop pills

AIM: Due to small amount of medica-ments contained in the drop pills of Chinese herbal medicine, the study of drop pills has been restricted, therefore, the aim of the study was to investigate the dissolution and human bueeal absorption characteristic of borneol and menthol in Qingyan drop pills in vitro. METHODS: The gas chromatograph (GC) method was established for simultaneous determination of borneol and menthol in Qingyan drop pills. The in vitro dissolution experiment of borneol and menthol was investigated with the instrument of drug dissolution, the human buccal absorption characteristic of borneol and menthol was performed in 5 healthy volunteers. The correlation between the cumulative human buccal ab-sorption rate and the in vitro cumulative dissolution rate of botneol and menthol were analyzed. RESULTS: The in vitro dissolution experiment indicated that the maximum cumulative dissolution rates of borneol and menthol were 84.3%, 79.7% in 10, 20 min respec-tively, and the human buccal absorption experiment in-dicated that the maximum cumulative absorption rates of borneol and menthol were 90.3%, 94.6% in 45, 30 min respectively. The correlation between in vivo and in vitro experiment was good, and the correlation coef-ficients were 0. 890, 0. 907 respectively. CONCLU-SION:A rapid, sensitive, and precise GC method has been established for the simultaneous determination of berneol and menthol in Qingyan drop pills. The results demonstrated that borneol and menthol, the main com-ponents of Qingyan drop pills, have the characteristic of rapid dissolution, fast release and absorption, which can meet the clinical demands of drop pills and provide theoretical basis for clinical medication.