Document Details

Document Type : Thesis 
Document Title :
DEVELOPMENT AND OPTIMIZATION OF ORAL LYOPHILIZED FLASH TABLETS LOADED WITH FEBUXOSTAT SELF-NANOEMULSIFYING SYSTEM
تطوير واستمثال أقراص مجفدة سريعة الذوبان بالفم ومحملة بمستحلب متناهي الصغر لعقار الفيبوكسوستات
 
Subject : faculty of Pharmacy 
Document Language : Arabic 
Abstract : Gout is the most familiar inflammatory arthritis condition caused by the elevation of uric acid in the bloodstream. Febuxostat (FBX) is the latest drug developed approved by the United States Food and Drug Administration (US FDA) for treatment and management of gout and hyperuricemia. FBX is characterized by low solubility and high permeability which considered as a Class Ⅱ compound regarded the Biopharmaceutics Classification System. As a consequences FBX bioavailability is poor and variable. The aim of this thesis was to improve the poor bioavailability issue of FBX by incorporation of FBX in self nanoemulsifing drug delivery system (SNEDDS) formulation with minimum globule size and maximum stability index followed by loading into a large surface area carrier system to be lyophilized as orally disintegrating tablets for oral transmucosal delivery affording porous tablet characterized by minimum disintegration time and, maximum drug release. The solubility of FBX was studied in various oils, surfactants, and cosurfactants. Mixture design was successfully utilized to prepare FBX-SNEDDS with minimum globule size (Y1) and maximum stability index (Y2). The optimized FBX-SNEDDS was developed into lyophilized tablets after the incorporation of the appropriate additives. The experimental design known as Box Behnken design was successfully utilized to study and optimized the level of the independent factor: croscarmellose sodium percentage (X1), gelatin solution concentration (X2), and hydroxypropyl methylcellulose percentage (X3), to develop FBX-self nanoemulsifing lyophilized tablets (SNELTs) with minimum disintegration time (Y1), and maximum drug release (Y2). The pharmacokinetic parameters of the optimized FBX-SNELTs were tested in healthy human volunteers and compared with marketed FBX tablets. The results showed that the optimized FBX-SNELTs increased the maximum plasma concentration (Cmax) and decreased the time to reach Cmax (Tmax) with a larger area under the curve (AUC) as a result enhanced the relative bioavailability of FBX-SNELTs to 146.4 % in comparison to the marketed FBX tablets. The marked enhancement of FBX bioavailability encourages its use in the treatment and management of gout due to its superiority in the enhancing FBX bioavailability compared to marketed FBX tablets. 
Supervisor : Prof. Dr. Khalid Mohamed Mohamed El-Say 
Thesis Type : Master Thesis 
Publishing Year : 1441 AH
2020 AD 
Co-Supervisor : Dr. Khaled Mohamed Hosny Omar 
Added Date : Saturday, June 13, 2020 

Researchers

Researcher Name (Arabic)Researcher Name (English)Researcher TypeDr GradeEmail
ياسر علي العاموديAl-Amodi, Yasir AliResearcherMaster 

Files

File NameTypeDescription
 46377.pdf pdf 

Back To Researches Page