Document Details

Document Type : Thesis 
Document Title :
Development and optimization of taste masked vardenafil oral disintegrating tablets
صياغة و استمثال عقار الفاردينافيل في صورة أقراص مقبولة الطعم سريعة التفتت بالفم
 
Subject : faculty of Pharmacy 
Document Language : Arabic 
Abstract : Vardenafil (VRD) is used for the treatment of erectile dysfunction. Because of the poor aqueous solubility of VRD as well as the considerable first-pass metabolism, the absolute bioavailability of VRD does not exceed 15%. So the aim of this study was to increase the solubility, hasten the onset of action, and mask the unpleasant taste of VRD by using β-cyclodextrin as complexing agent. And then formulate the VRD inclusion complex as oral disintegrating tablets (ODTs). The compatibility of VRD with the excipients has been studied by utilizing Fourier transform infrared spectroscopy (FTIR). Moreover, the complexation of VRD with β-cyclodextrin in various ratios and the solubility of VRD in the resulting complexes have been studied. A Box-Behnken design was utilized to investigate the influence of formulation variables on the prepared tablet properties and to improve the preparation conditions. The optimized VRD-ODTs were compared with the marketed VRD tablets utilizing the relative pharmacokinetic parameters. The solubility of VRD was improved after using β-cyclodextrin as complexing agent at 1:2 of drug: β-cyclodextrin ratio from 0.13 to 13.7 mg/ml. The formulated VRD-ODTs exhibit satisfying results including tablet hardness which ranged from 36.46 to 65.86 N and disintegration time which ranged from 36.33 to 97.67 seconds. In addition, in vivo taste masking and disintegration time showed improved results. Where the scores of taste masking equal or less than 1 which indicate the formulation has acceptable taste and the disintegration time has a mean result 62.33 seconds. The pharmacokinetic results for the optimized VRD–ODTs exhibit a significant, p < 0.05, improvement in the maximum plasma concentration (Cmax) from 12.2 to 18.2 ng/ml and reduction in the time needed to reach maximum plasma concentration (Tmax) from 2.0 to 1.0 h when compared with the marketed tablets. Finally, the optimized VRD-ODTs exhibited increased oral absorption of VRD, subsequent decreasing the time of onset of clinical effect and masking the unpleasant taste, which is favored for erectile dysfunction patients. 
Supervisor : Prof. Dr. Khalid Mohamed El-Say 
Thesis Type : Master Thesis 
Publishing Year : 1440 AH
2019 AD 
Co-Supervisor : Dr. Osama Abdelhakim Ahmed 
Added Date : Sunday, July 14, 2019 

Researchers

Researcher Name (Arabic)Researcher Name (English)Researcher TypeDr GradeEmail
هيثم أحمد القثميAl-Gethmy, Hytham AhmedResearcherMaster 

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