球形晶体聚合技术,以改善阿扎纳维尔硫酸盐的流动性和口服生物可用性
Darpan Shah1, Jatin Rawat1, Hetal Thakkar1
1Center for Post-Graduate Studies & Research in Pharmaceutical Sciences, Shri GH Patel Pharmacy building, Faculty of Pharmacy, The Maharaja Sayajirao University of Baroda, Vadodara, Gujarat, 390002, India.
Therapeutic delivery
|June 21, 2023
概括
阿扎纳维尔硫酸的球形晶体聚合物 (SCA) 是为了提高药物的溶解性和流量而开发的. 与市场上销售的产品相比,这些SCA片显示出更好的溶解和生物可用性.
科学领域:
- 制药技术 制药技术 制药技术
- 药物输送系统 药物输送系统
- 材料科学 材料科学 材料科学
背景情况:
- 阿塔萨纳维尔硫酸盐具有较差的溶解性和流动性,阻碍了有效的口服剂型的开发.
- 改善阿塔扎纳维尔硫酸盐的生物制药性质对于提高治疗疗效至关重要.
- 球形晶体聚合物 (SCA) 为克服配方挑战提供了一个潜在的策略.
研究的目的:
- 为了制备阿塔萨纳维尔硫酸盐的球形晶体聚合物 (SCA).
- 为了增强阿塔萨纳维尔硫酸盐的溶解性和微米性质.
- 为了评估SCA在直接压缩片中的性能.
主要方法:
- 使用准乳化溶剂扩散技术制备了球形晶体聚合物 (SCA).
- 甲醇,水和二甲分别被用作好的溶剂,坏的溶剂和桥梁液.
- 配方的SCA被直接压缩成药片进行进一步评估.
主要成果:
- 配方的SCA表现出更好的溶解性和优良的微米质性质.
- 从SCA制造的药片表现出明显更高的溶解率,而不是普通药物和市场上的一种配方.
- 在体内药理动力学研究表明,相比于市场上销售的产品,SCA的相对生物利用率增加了1.74倍,Cmax和AUC0-t更高.
- 该SCA配方在三个多月内保持稳定,药物含量或溶解没有显著变化.
结论:
- 准乳化溶剂扩散方法成功地产生了具有增强可溶性和流量特性的阿塔萨纳维尔硫酸球形晶体聚合物 (SCA).
- 由SCA制成的直接压缩片显示出优异的溶解概况和改善的体内药理学参数,包括生物可用性.
- 开发的SCA配方是稳定的,并代表了一种有前途的方法来改善阿扎纳维尔硫酸盐的口服输送.
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