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目的:检测SD大鼠经皮给予美洛昔康4h内的血药浓度和给药面皮肤浸出液中的浓度,以及荧光素钠(NaFI)在SD大鼠完整皮肤中的定位和荧光强度,探讨负极性驻极体对美洛昔康透皮的促渗作用以及驻极体促渗的主要途径。方法:利用药剂学方法和栅控恒压电晕充电技术制备驻极体美洛昔康贴剂;采用高效液相色谱法检测美洛昔康的浓度;以NaFI为探针,通过激光扫描共聚焦显微镜(LSCM)考察其在皮肤中的定位及透皮路径情况。结果:(1)负极性驻极体及其驻极体美洛昔康贴剂具有良好的电荷储存稳定性;(2)高效液相色谱检测表明经皮给药4h内驻极体对美洛昔康的透皮促进作用明显;(3)LSCM研究结果进一步验证了驻极体对小分子的促渗作用,同时证实了驻极体促进药物透皮的主要途径是角质层间脂和毛囊孔扩散。结论:负极性驻极体可以作为美洛昔康透皮吸收的一个促进因子。
OBJECTIVE: To detect the plasma concentration of meloxicam within 4 hours after transdermal administration to the skin of SD rats and the concentration of NaFI in the skin of leaching solution on the administration side, and to investigate the localization and fluorescence intensity of sodium fluorescein (NaFI) in intact skin of SD rats The Effect of Negative Polar Electret on the Permeability of Meloxicam Transdermal and the Major Pathway of Electret. Methods: The electret meloxicam patch was prepared by the method of pharmacy and the grid-controlled constant-voltage corona charging. The concentration of meloxicam was detected by high performance liquid chromatography. With NaFI as the probe, Confocal microscopy (LSCM) examines its localization in the skin and transdermal pathways. Results: (1) The negative electret and its electret meloxicam patch have good charge storage stability; (2) High performance liquid chromatography (HPLC) (3) LSCM results further verify the role of electret in promoting small molecules, and at the same time, it is confirmed that the main ways of electret promoting drug transdermal penetration are inter-cutaneous fat and hair follicle pores diffusion. Conclusion: The negative electrets can be used as a facilitator of meloxicam transdermal absorption.