کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2485612 | 1114361 | 2011 | 14 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Tadalafil Inclusion in Microporous Silica as Effective Dissolution Enhancer: Optimization of Loading Procedure and Molecular State Characterization
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Tadalafil Inclusion in Microporous Silica as Effective Dissolution Enhancer: Optimization of Loading Procedure and Molecular State Characterization Tadalafil Inclusion in Microporous Silica as Effective Dissolution Enhancer: Optimization of Loading Procedure and Molecular State Characterization](/preview/png/2485612.png)
چکیده انگلیسی
Tadalafil is an efficient drug used to treat erectile dysfunction characterized by poor water solubility, which has a negative influence on its bioavailability. Utilization of microporous silica represents an effective and facile technology to increase the dissolution rate of poorly soluble drugs. Our strategy involved directly introducing tadalafil as guest molecule into microporous silica as host material by incipient wetness impregnation method. To optimize tadalafil inclusion, response surface methodology (RSM) using 33 factorial design was utilized. Furthermore, to investigate the molecular state of tadalafil, Fourier-transform infrared spectroscopy, differential scanning calorimetery, thermal gravimetrical analysis, nitrogen adsorption, and powder X-ray diffraction (PXRD) were carried out. The results obtained pointed out that the quantity of microporous silica was the predominant factor that increased the loading efficiency. For the optimized formula, the loading efficiency was 42.50Â wt %. Adsorption-desorption experiments indicated that tadalafil has been introduced into the micropores. Powder XRD and differential scanning calorimetry analyses revealed that tadalafil is arranged in amorphous form. In addition, the dissolution rate of tadalafil from the microporous silica was faster than that of free drug. Amorphous tadalafil occluded in microporous silica did not crystallize over 3Â months. These findings contributed in opening a new strategy concerning the utilization of porous silica for the dissolution rate enhancement.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 100, Issue 5, May 2011, Pages 1805-1818
Journal: Journal of Pharmaceutical Sciences - Volume 100, Issue 5, May 2011, Pages 1805-1818
نویسندگان
Mohammed M. Mehanna, Adel M. Motawaa, Magda W. Samaha,