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卡马西平(Ⅰ)是水不溶的,作者应用两个普通的水溶助溶剂苯甲酸钠(Ⅱ)和水杨酸钠(Ⅲ)可增加(Ⅰ)的溶解度。23±1℃时,在50％(w/v)的(Ⅱ)和(Ⅲ)溶液存在下,可使(Ⅰ)的溶解度分别增加98.6和112倍。例如,(Ⅰ)在23±1℃无助溶剂时,其溶解度只有36.5μg/ml,而当(Ⅰ)溶解在含50％ (w/v)(Ⅱ)和(Ⅲ)的溶液时,(Ⅰ)的溶解度则分别增加为3600μg/ml 和4012μg/ml。由此可制得3.6mg/ml(Ⅰ)的注射水溶液。作者还研究了此水溶液的稳定性,发现在8℃时最稳定,其分解速度随温度升高而加
Carbamazepine (I) is water-insoluble. The authors used two common water-soluble cosolvent sodium benzoate (II) and sodium salicylate (III) to increase the solubility of (I). At 23 ± 1 ° C, the solubilities of (I) were increased by 98.6 and 112 fold, respectively, in the presence of 50% (w / v) solutions of (II) and (III) For example, (I) has a solubility of only 36.5 μg / ml at 23 ± 1 ° C without solvent and (I) when dissolved in a solution containing 50% (w / v) of I) increased to 3600 μg / ml and 4012 μg / ml, respectively. Thus, an aqueous injection solution of 3.6 mg / ml (I) was obtained. The authors also studied the stability of this aqueous solution and found that it is the most stable at 8 ° C and its decomposition rate increases with increasing temperature