Cerchiara T, Luppi B, Bigucci F, Zecchi V
Department of Pharmaceutical Sciences, Via S. Donato 19/2, 40127 Bologna, Italy.
J Pharm Pharmacol. 2003 Dec;55(12):1623-7. doi: 10.1211/0022357022322.
The aim of this study was to describe a sustained drug release system based on chitosan salts for vancomycin hydrochloride delivery. Chitosan lactate, chitosan aspartate, chitosan glutamate and chitosan hydrochloride were prepared by spray-drying technique. Vancomycin hydrochloride was used as a model peptidic drug, the nasal sustained release of which should avoid first-pass metabolism in the liver. This in-vitro study evaluated the influence of chitosan salts on the release behaviour of vancomycin hydrochloride from the physical mixtures at pH 5.5 and 7.4. In-vitro release of vancomycin was retarded by chitosan salts and, in particular, chitosan hydrochloride provided the lowest release of vancomycin.
本研究的目的是描述一种基于壳聚糖盐的用于盐酸万古霉素递送的持续药物释放系统。通过喷雾干燥技术制备了乳酸壳聚糖、天冬氨酸壳聚糖、谷氨酸壳聚糖和盐酸壳聚糖。盐酸万古霉素用作模型肽类药物,其鼻腔持续释放应避免肝脏的首过代谢。这项体外研究评估了壳聚糖盐对盐酸万古霉素在pH 5.5和7.4条件下从物理混合物中释放行为的影响。壳聚糖盐可延缓万古霉素的体外释放,特别是盐酸壳聚糖使万古霉素的释放量最低。