Document Details

Document Type : Thesis 
Document Title :
Preparation of Injectable Rosuvastatin in Situ Gel Formulation with Minimum Initial Drug Burst
تحضير مستحضر هلامي من الروزوفاستاتين يتصلب داخل الجسم معد للحقن و يتميز بإنطلاق أولي منخفض من الدواء
 
Subject : Faculty of Pharmacy 
Document Language : Arabic 
Abstract : Injectable in situ gel (ISG) system suffers from high initial drug release which may result in toxic effect. The rationale behind this work was to develop an optimized injectable rosuvastatin (RSV) ISG formulation characterized by minimum initial burst. Six formulation parameters have been screened, using the Plackett Burman design (PB), for their effect on RSV release in the first 24 h. Poly lactic acid-co-Ɛ-caprolactone (PLCL) concentration, poly lactic acid: poly caprolactone ratio, polyethylene glycol (PEG) molecular weight, PEG concentration, surfactant hydrophilic lipophilic balance (HLB) and surfactant concentration were screened. The most significant formulation factors were optimized using Box-Behnken design to achieve minimum RSV release after 0.5, 2 and 24 h. Physicochemical characterization for the optimized formulation components was studied. Pharmacodynamic effects of the optimized ISG formulation were studied and compared to ISG formulation containing 45 % PLCL (25: 75) loaded with raw RSV and to an oral marketed drug product. Result of the screening study revealed that PLCL (25: 75) concentration, surfactant HLB and surfactant: PEG 400 ratio were significantly affecting RSV release and their optimized levels are 45 %, 14.25 and 80:20, respectively. Physicochemical characterization demonstrated complete entrapment of RSV in the polymeric matrix and confirmed drug transformation to the amorphous state. Pharmacodynamic study revealed sustained reduction in the lipid profile that lasts for 21 days with a marked decrease in the lipid level during the first 24 h from the ISG system loaded with raw RSV. In conclusion, the optimized RSV ISG formulation can be considered as an alternative for the marketed drug oral daily tablets. 
Supervisor : Dr. Tariq Abdulnabi 
Thesis Type : Master Thesis 
Publishing Year : 1440 AH
2019 AD 
Added Date : Monday, May 20, 2019 

Researchers

Researcher Name (Arabic)Researcher Name (English)Researcher TypeDr GradeEmail
محمد عبدالرحمن مصيريMussari, Mohammed AbdulrahmanResearcherMaster 

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 44456.pdf pdf 

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