Tapia Cristián, Montezuma Víctor, Yazdani-Pedram Mehrdad
Laboratorio de Operaciones Unitarias, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Casilla 233, Santiago 1, Chile.
AAPS PharmSciTech. 2008;9(4):1198-206. doi: 10.1208/s12249-008-9164-3. Epub 2008 Dec 11.
The aim of this work was to develop a procedure for encapsulation of diltiazem HCl by spray coagulation. Factors affecting the formulations such as the effect of NaCl on the solubility of diltiazem in alginate solution, surface tension, pH, viscosity of the coagulation medium, and the effect of drug load on drug release were studied. The drug load was increased substantially from 10 up to 320 mg/mL by adding 1.2% w/v NaCl in 1% w/v alginate solution. More stable microcapsules were obtained at pH 4.6 (acetate buffer) than at a pH 2.8 (lactic acid), and the microencapsulation process was favored by the type of chitosan that produced low turbidity and viscosity in the coagulation medium. A dose of 50 mg/mL of diltiazem HCl, 1.2% w/v NaCl, and chitosan CS allowed higher amount of drug to be encapsulated. The high water solubility of diltiazem HCl leads to fast release from the microcapsules.
本研究旨在开发一种通过喷雾凝固法包封盐酸地尔硫䓬的工艺。研究了影响制剂的因素,如氯化钠对盐酸地尔硫䓬在藻酸盐溶液中溶解度的影响、表面张力、pH值、凝固介质的粘度以及药物载量对药物释放的影响。通过在1% w/v藻酸盐溶液中添加1.2% w/v氯化钠,药物载量从10 mg/mL大幅提高至320 mg/mL。在pH 4.6(醋酸盐缓冲液)下获得的微胶囊比在pH 2.8(乳酸)下更稳定,并且微囊化过程更倾向于使用在凝固介质中产生低浊度和低粘度的壳聚糖类型。50 mg/mL的盐酸地尔硫䓬剂量、1.2% w/v氯化钠和壳聚糖CS可实现更高的药物包封量。盐酸地尔硫䓬的高水溶性导致其从微胶囊中快速释放。