肿瘤抑素T7肽溶液的稳定性研究

Study on the stability of tumstatin T7 peptide solution

目的考察水溶性肿瘤抑素T7肽在脂质体制备及贮存条件下的稳定性。方法将T7肽溶液置于室温下,HPLC法测定6 h内峰面积减小百分比,确定溶剂。再将T7肽溶液分别置于4℃和25℃下,绘制降解曲线,确定贮存条件。最后将不同pH值、含不同缓冲盐的T7肽溶液于65℃下保温1 h,检测保温前后溶液中T7肽含量,优化制备条件。结果以重蒸水和灭菌注射用水为溶剂的T7肽溶液在6 h内峰面积减少分别为79.66%和18.31%,于4℃或25℃贮存6 h后的降解率分别约为10%与20%,在pH值4.0～9.0的溶剂中降解率分别为39.67%、42.55%、37.71%、13.44%、7.34%和23.76%,与各种缓冲液接触后质量浓度均降至初始质量浓度的40%以下。结论 T7肽溶液应以弱碱性的灭菌注射用水为溶剂,现用现配,制剂制备过程中应避免与缓冲液接触,并于4℃下贮存。

Objective To investigate the stability of water soluble tumstatin T7 peptide under the condition in which liposomes were prepared and storage. Method Firstly, T7 peptide was dissolved in redistilled water and sterile water for injection, and the solution was kept at room temperature for 6 h.Then T7 solution was kept at 4 ℃ and 25 ℃ for 6 h, and the degradation curves were obtained.Finally, T7 peptide was dissolved in solvents with different pH and buffer salts, with the concentration of 100 mg·L-1 P P, and these solutions were kept at 65 ℃ for 1 h. Contents of T7 peptide were detected by HPLC. Result The percentage degradation of T7 peptide dissolved in redistilled water and sterile water for injection after 6 h was 79.66% and 18.31%, respectively. Degradation of T7 solutions kept at 4 ℃and 25 ℃ for 6 h were about 10% and 20%, respectively. Degradation rate of T7 solution dissolved in solvents with different pH 4.0-9.0 were 39.67%, 42.55%, 37.71%, 13.44%, 7.34% and 23.76%,respectively. Contents of T7 solution falled below 40% after dissolved in general buffers. Conclusion T7 peptide should be dissolved in sterile water for injection when it was needed, isolated from buffers,and stored at 4℃.