Document Details

Document Type : Thesis 
Document Title :
FORMULATION AND EVALUATION OF CARVEDILOL ORODISPERSIBLE TABLETS
صياغة وتقييم أقراص الكارفيديلول القابلة للتفتت بالفم
 
Subject : Faculty of Pharmacy - Pharmaceutics 
Document Language : Arabic 
Abstract : Carvedilol (CAR) is used for treatment of essential hypertension, heart failure, and patients with systolic dysfunction after myocardial infarction. Due to its low aqueous solubility and extensive first-pass metabolism, its absolute bioavailability do not exceed 30%. To overcome these drawbacks of CAR, the objective of this work was to improve its solubility and bioavailability by complexation with HP-β-CD and formulating the complex in orodispersible tablets. Compatibility among CAR and all tablet excipients using DSC and FTIR, complexation of CAR with different polymers, and determination of the solubility of CAR in the prepared complexes were first performed. Box-Behnken design was used to study the effect of the tablet formulation variables on the characteristics of tablets and to optimize the preparation conditions. So, fifteen formulae of CAR-ODTs were prepared by direct compression using single punch machine then evaluated for their quality attributes. The relative bioavailability of the optimized CAR-ODTs was compared with the marketed tablet after oral administration of a single dose of CAR (2.5 mg/kg) to the New Zealand white rabbit using a double blind, randomized, cross-over design. The results revealed that the solubility of CAR was improved from 7.32 to 22.92 mg/mL by complexation with HP-β-CD in 1:2 molar ratio. The formulated CAR-ODTs showed satisfactory results concerning tablet hardness (5.35 kg/cm2), disintegration time (18 sec) and maximum amount of CAR released (99.72 %). Finally, the pharmacokinetic data of optimized CAR-ODTs showed increased Cmax significantly from 363.667 to 496.4 ng/mL, and hasten tmax to 2 h in comparison of 4 h for the marketed tablets indicating the improvement of the oral absorption of CAR and subsequently accelerate the onset of action which is favored for hypertensive and cardiac patients. 
Supervisor : Prof. Dr. Abdel-Raheem Mohammed El-Helw 
Thesis Type : Master Thesis 
Publishing Year : 1436 AH
2015 AD 
Co-Supervisor : Dr. Khalid Mohamed El-Say 
Added Date : Monday, May 4, 2015 

Researchers

Researcher Name (Arabic)Researcher Name (English)Researcher TypeDr GradeEmail
يزيد حسين الجماعيAljimaee, Yazeed HusseinResearcherMaster 

Files

File NameTypeDescription
 37951.pdf pdf 

Back To Researches Page