盐酸倍他洛尔温敏型眼用原位凝胶的制备及其含量测定

摘要

Poloxamer 407(F127) and poloxamer 188(F68) were used to prepare the in situ gel, and the formulation was optimized by determining the gelation temperature. HPLC method was established to determine the content of betaxolol hydrochloride in the gel. The separation was performed on a Zorbax SB-C18 column and the mobile phase consisted of acetonitrile and pH 3.0 phosphate buffer in the ratio of 45:55 ( v/v). "Hie UV detector wavelength was set at 280 run with a flow rate of 0.8 ml/min. The results suggested that the best composition of the gel formulation was 20% F127 and 5% F68. The gelation temperature before and after simulated tear fluid dilution was 28.2℃ and 33.4℃, respectively. The linear range was from 11.0 μg · mL-1 to 440.0μg · mL-1 (r =0.9997) and the average recovery rate was 99.5% . The method showed high precision of within-day and between-day for determination. The thermosensitive in situ, gel showed a potential for the ocular drug delivery system. The established method was simple, accurate and reliable for the determination of betaxolol hydrochloride in the gel.%以泊洛沙姆407(F127)和泊洛沙姆188(F68)作为原位凝胶载体材料,研究胶凝温度优化处方,并采用高效波相色谱法测定原位凝胶中盐酸倍他洛尔的含量(色谱柱为ZorbaxSB-C18柱,流动相为乙腈-pH3.0磷酸盐缓冲液(45∶55,(V/V)),检测波长为280nm,流速0.8mL/min).结果表明:原位凝胶最佳处方组成为20％F127和5％F68,经人工泪液稀释前后的胶凝温度分别为28.2℃和33.4℃；盐酸倍他洛尔在浓度11.0-440.0μg/mL范围内呈良好的线性相关性(r=0.9997),日内和日间精密度良好,平均回收率为99.5％.