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Document Type |
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Thesis |
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Document Title |
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IMPROVING THE BIOAVAILABILITY OF VALSARTAN VIA ITS FORMULATION IN TABLETS LOADED WITH A SELF-NANOEMULSIFYING SYSTEM تحسين التوافر البيولوجي لفالسارتان من خلال تركيبته في أقراص محملة بنظام التنقية الذاتية للنانو |
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Subject |
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faculty of Pharmacy |
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Document Language |
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Arabic |
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Abstract |
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Valsartan (VST) is a poorly soluble antihypertensive drug that is characterized by an unstable dissolution rate and low bioavailability. So, this study aims to improve VST solubility and dissolution rate, improving its bioavailability via developing liquisolid tablets (LSTs) containing a self-nanoemulsifying drug delivery system (SNEDDS) and investigating their quality attributes. Optimized SNEDDS was prepared using sesame oil, tween 80 as a surfactant, and polyethylene glycol 400 as a co-surfactant. Various liquisolid systems were developed and optimized using a 32 3-level factorial design. Several LS formulations were prepared using the SNEDDS-loaded VST and Neusilin®US2 as a carrier and fumed silica as a coating material. The flowability and compressibility index of powder mixtures were studied. The effect of using different excipient ratios (X1) and various types of super-disintegrants (X2) were also emphasized in developing the optimized VST-LSTs. The in vitro dissolution studies of VST from the LSTs were compared with the marketed product (Diovan®). Non-compartmental analysis of plasma data after extravascular input with the linear trapezoidal method was used to calculate the pharmacokinetic parameters of the optimized VST-LSTs compared with the marketed tablet on rats. The optimized SNEDDS compromised 24.9% sesame oil, 33.3% surfactant, and 41.8% cosurfactant, giving 173.9 nm size and 63.9 mg/ml loading capacity. Also, the LST-loaded SNEDDS revealed good quality attributes with the release of 75% of its content in 5 min and 100% within 15 min. On the other hand, the marketed product took a full hour for the entire amount of drug to be released entirely. Moreover, the maximum plasma concentration (Cmax) of the optimized VST-LST was 6585.33 ng/ml within one hour (Tmax), compared to 2884.67 ng/ml within two hours of the marketed tablet. These findings confirm that our approach to developing VST in LST loaded with SNEDDS improved its bioavailability by 213.7% more than the marketed tablet. The VST-LST appears to be a promising method for increasing solubility, dissolution behavior in GIT, and the bioavailability of poorly water-soluble drugs.
Keywords: Bioavailability; Drug development; liquisolid technique; SNEDDS; Valsartan |
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Supervisor |
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Prof. Dr. Khalid Mohamed El-Say |
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Thesis Type |
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Master Thesis |
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Publishing Year |
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1444 AH
2023 AD |
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Co-Supervisor |
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Prof. Dr. Tarek Abdelnapy Ahmed |
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Added Date |
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Wednesday, March 15, 2023 |
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Researchers
| سامي هديبان العمري | Alamri, Sami Hudayban | Researcher | Master | |
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