注射用琥珀酰明胶的制备

目的制备注射用琥珀酰明胶,以提高其稳定性及运输贮藏的便易性。方法合成琥珀酰明胶,并用IR、1H-NMR及UV光谱方法对其进行表征,采用喷雾干燥和冷冻干燥工艺制备注射用琥珀酰明胶,同时对所制备产品的再分散性质进行了初步考察。结果合成条件为:明胶质量浓度为200 mg.L-1,琥珀酸酐质量浓度为10 mg.L-1,pH值为10,温度90℃,时间2 h。冷冻干燥法制备的注射用琥珀酰明胶与琥珀酰明胶对照品的1H-NMR、IR及UV谱图均相符。以质量浓度50 mg.L-1的甘露醇为冻干保护剂制备的产品外观蓬松饱满,复溶时间短。配成输液后渗透压为288 mmol.L-1,pH值为7.19。结论运用丁二酰化法合成琥珀酰明胶,以质量浓度50 mg.L-1甘露醇为冻干保护剂,利用冷冻干燥法可相对较稳定地制备拥有较好外观及溶解度的注射用琥珀酰明胶,且配制成输液后渗透压及pH值符合静脉用药要求。

Preparation of succinylated gelatin for injection

Objectives To prepare succinylated gelatin for injection. Methods Succinylated gelatin was synthesized and then characterized using IR, ¹H-NMR and UV. Succinylated gelatin for injection was prepared by spray drying and freeze-drying. The redispersion properties of succinylated gelatin for injection were investigated. Results Succinylated gelatin could be synthesized under the conditions as follows: the concentration of gelatin was 200 mg·L^-1, the concentration of succinic anhydride was 10 mg·L^-1, pH was 10, temperature was 90 ℃ and reaction time was 2 hours. The ¹H-NMR, IR and UV spectra of succinylated gelatin prepared by freeze-drying and reference substance were basically identical. The succinylated gelatin for injection prepared with mannitol in concentration of 50 mg·L^-1 as protective agent had a bulky and plump appearance and short dissolving time. After being prepared to infusion, its osmotic pressure was 288 mol·L^-1 and its pH was 7.19. Conclusions Succinylated gelatin for injection can be prepared relatively stably with good appearance and solubility by freeze-drying with 50 mg·L^-1 mannitol as protective agent. The osmotic pressure value and pH value of the prepared infusion meet the qualification for intravenous use.