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Pharmaceutics:西地那非体外溶解动力学揭示以用于新制剂的开发

2020-04-25 MedSci原创 MedSci原创

本研究旨在建立一个生理学相关的体外-体内相关(IVIVIVC)模型,反映西地那非的溶出动力学。

本研究旨在建立一个生理学相关的体外-体内相关(IVIVIVC)模型,反映西地那非的溶出动力学。

 

通过湿法制粒法制备了速释(IR,20 mg)和三种缓释(SR,60 mg)西地那非片剂。采用桨叶法在pH 1.2、4.5和6.8介质中测定体外溶出度。口服制备的IR和SR配方给Beagle犬(n = 12)后,评估其体内药代动力学。

 

结果显示,SR制剂中西地那非在pH值6.8时溶解不完全,而在pH值1.2和pH值4.5时没有观察到。相对生物利用度随着溶解率的降低而降低。此外,在血浆浓度-时间曲线中观察到了次生峰,这可能是由于位置依赖性溶解导致的。因此,建立了POP-PK模型,通过分别描述溶解和吸收过程,反映出了西地那非的体内溶解情况。最后,建立了一个IVIVC,并通过体外和体内溶解率的相关性来验证。

 

总之,本方法可用于建立具有复杂溶解动力学的各种药物的IVIVC,以开发新的制剂。

 

原始出处:

 

Tae Hwan KimSoyoung Shin, et al., Physiologically Relevant In Vitro-In Vivo Correlation (IVIVC) Approach for Sildenafil with Site-Dependent Dissolution. Pharmaceutics. 2019 Jun; 11(6): 251.  doi: 10.3390/pharmaceutics11060251

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    2020-08-18 jj000001
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    2020-07-15 yb6560
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    2020-06-24 shanyongle
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    2020-04-27 lfyang

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