苯巴比妥钠包合物的制备及其在液体制剂中的稳定性

Preparation of inclusion compound of phenobarbital sodium and the stability in liquid pharmaceutical preparations

目的:制备苯巴比妥钠包合物并考察其稳定性。方法:采用β-环糊精作为包合剂制备苯巴比妥钠包合物,应用等温加热法,选择40,50,60,70,80℃进行加速稳定性试验考察其在水溶液中的稳定性,应用动力学数据估算有效期,以紫外分光光度法测定苯巴比妥钠含量。结果:选择β-环糊精与苯巴比妥钠的摩尔比为1∶2投料进行包合物制备,各温度下苯巴比妥钠及其包合物的消除量时间函数呈线性关系,预测室温下包合物有效期(含量下降5%)为苯巴比妥钠的3.5倍。结论:β-环糊精包合后提高了苯巴比妥钠稳定性。

OBJECTIVE To prepare the inclusion compounds of phenobarbital sodium and observe their stability.METHODS β-cyclodextrin was used to prepare inclusion compounds. An accelerated stability test was carried out to study the stability of the inclusion compounds in water by isothermal heating method （at 40,50,60,70,80℃）. Data obtained in the kinetic information were applied to predict shelf-lives at room temperature. UV difference spectrophotometry was used for phenobarbital sodium determination. RESULTS The inclusion compound was made in 1：2 molar ratio of β-cyclodextrin to phenobarbital sodium. The decrease in stability at different temperatures as a function of time was possible to describe by linear dependence. The predict shelf-lives of the inclusion compound in which phenobarbital sodium content mean value failed by 5 % of the initial one at room temperatures was 3. 5 times of phenobarbital sodium. CONCLUSION The stability of phenobarbital sodium is increased when it was included by β-cyclodextrin.