直接凝血酶抑制剂冻干循环的研制及循环中辅料和工艺参数的影响。

S. Panda, Subas C. Dinda
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引用次数: 0

摘要

本研究的目的是开发稳定的比伐鲁定冻干产品,比伐鲁定是一种直接凝血酶抑制剂,具有良好的重组时间,良好的小瓶收率和饼质量。用DSC法测定膨化剂冷冻干燥后结晶学变化的结晶度损失百分比。5% w/v比伐鲁定、3% w/v甘露醇和0.03%醋酸钠的玻璃化转变温度约为- 31℃,崩溃温度约为-28℃。发现管状小瓶在冷冻干燥过程中经受住了热转变。含水量与初级干燥设定点成反比。重构时间与退火温度和真空设定点成反比。好瓶收率和饼质量与退火时间和初级干燥设定点成正比。DSC的结晶度损失百分比与所有因素无关,与退火时间成正比。-10°C干燥导致β型甘露醇转变,-7.5°C和-5°C干燥分别导致α和δ型甘露醇转变。在-7℃下退火54分钟,在-6.5℃下干燥215mT,冻干产物含水量小于2%,重构时间小于10秒,收率高达95%以上,得到饼质量最好的小瓶。DOI: http://dx.doi.org/10.3329/icpj.v3i5.18533国际现代医药杂志,2014年4月,3(5):259-264
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development of lyophilization cycle for direct thrombin Inhibitor and influence of excipients and process parameter during the cycle.
The objective of this study was to develop stable lyophilized product of Bivalirudin, a direct thrombin inhibitor with good reconstitution time, % yield of good vials and cake quality. The % loss of crystallinity was determined by DSC for any crystallographic changes of the bulking agent after freeze drying. The glass transition temperature of 5% w/v of Bivalirudin, 3% w/v of mannitol and 0.03% of sodium acetate was approximately ‑31°C and the collapse temperature was approximately -28°C. Tubular vials were found to withstand the thermal transition during freeze drying. Water content was inversely proportional to the primary drying set point. Reconstitution time was inversely proportional to annealing temperature and vacuum set point. The % yield of good vials and cake quality was directly proportional to annealing time and primary drying set point. The % loss of crystallinity by DSC was independent of all factors and directly proportional to annealing time. Drying at -10°C results in transition of β form of mannitol, whereas drying at -7.5°C and -5°C results in α and δ form of mannitol respectively. On annealing at -7°C for 54 minutes and drying at -6.5°C at 215mT lyophilized product with less than 2% water content, reconstitution time less than 10 seconds, with high yield of more than 95% yield of good vials with best cake quality was obtained. DOI:  http://dx.doi.org/10.3329/icpj.v3i5.18533 International Current Pharmaceutical Journal, April 2014, 3(5): 259-264
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