提升溶解性的蒂卡格勒尔片的自微乳化系统的组合和表征
Rajagopal Kumaravelrajan1, Narayanan Naresh2, Guru Prasad Mohanta3
1Department of Pharmaceutics, C. L. Baid Metha College of Pharmacy, affiliated with T. N. Dr. M. G. R. Medical University, Chennai, Tamil Nadu, India. rkumaravelrajan@gmail.com.
International journal of pharmaceutical compounding
|May 20, 2024
概括
这项研究开发了一种以格为载的自微乳化药物输送系统 (SMEDDS),以药片形式进行优化. 新的SMEDDS显著提高了蒂卡格勒罗的溶解性和溶解性,以改善急性冠状动脉综合征的治疗.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 制定 发展 制定 发展
背景情况:
- 提卡格雷勒对急性冠状动脉综合征至关重要,但具有较差的溶性和较低的生物可用性.
- 这些局限性阻碍了其体内疗效和治疗结果.
- 开发先进的药物输送系统对于克服这些挑战至关重要.
研究的目的:
- 为了制定和优化Ticagrelor装载的自微乳化药物输送系统 (SMEDDS) 到药片形式.
- 为了提高蒂卡格勒的可溶性和溶解率.
- 评估优化配方的物理化学特性和体外药物释放.
主要方法:
- 使用中链甘油油,表面活性剂和表面活性剂制备含有蒂卡格洛尔的SMEDDS.
- 使用伪三极相图和简单格子混合设计来优化配方.
- 使用气溶作为吸附剂,将微乳液转化为颗粒,然后压缩片.
- 颗粒和片剂的表征,包括颗粒大小,泽塔潜力,表面形态和体外药物释放研究.
主要成果:
- 优化的蒂卡格勒罗尔SMEDDS配方显示可溶性显著增加,达到221.37 mg/mL.
- 颗粒的表征和平板电脑的压缩是令人满意的,气溶使用高达30%.
- 实验室研究显示,在30分钟内,药物释放超过80%,这表明溶解的增强.
结论:
- 开发的装有蒂卡格洛尔的SMEDDS药片提供了一种有效的策略,可以提高蒂卡格洛尔的溶解性和溶解性.
- 优化的配方,包括特定比例的油,表面活性剂和表面活性剂,显示了改善治疗疗效的承诺.
- 这种方法代表了在临床实践中克服蒂卡格勒罗的生物可用性限制的可行方法.
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