A Pharmaceutical study on improving the oral bioavailability of an antihypertensive drug / Doaa Mohamed Elsegaie Morsi ; Supervised Mohamed Ahmed Elnabarawi , Mina Ibrahim Tadros , Mahmoud Hassan Teaima

Thesis (M.Sc.) - Cairo University - Faculty of Pharmacy - Department of Industrial Pharmacy

In this thesis Candesartan Cilexetil bioavailability was successfully improved through its formulation as a LS-SNEDDS. A calibration curve was done using Phosphate buffer PH 6.8 and Methanol to detect the nmax. Several oils, surfactants and co-surfactants were screened for their ability to solubilize the drug and as a result Capryol 90®, Tween 80 and Transcutol HP® were chosen as an oil, surfactant and co-surfactant respectively. Only 5 formulas (F1,F2,F9,F10,F16) out of the 36 stayed clear after the addition of drug and then they went through further examination tests like self-emulsification time, viscosity, content uniformity, Globule size, Polydispersity index (PDI) and zeta potential Determinations. F16 which consisted of 10 % oil, 30% Surfactant, 60% Co-surfactant was chosen as it enabled 99.55% of the drug to be dissolved within 9 minutes in phosphate buffer pH6.8 which would lead to improving the drug bioavailability. Then the transformation of liquid lipid systems into oral dosage forms has been attempted through adsorption to solid carriers using Avicel PH102, Aerosil 200, and croscarmilose sodium as carrier, coating material and super disintegrating agent respectively, Six formulae were prepared using two liquid load factors LF of 0.22 and 0.25, as well as three excipient rations R of 10, 20 and 30. Then the characterization of the prepared Candesartan Cilexetil LS-SNEDDS Formulae was done using Angle of repose, Hausner{u201F}s ratio and carr{u201F}s index. The free flowing powders of the successful formulae were compressed into tablets and then the tablets were evaluated in accordance to their weight variation, Hardness, friability, Disintegration, Drug content uniformity and in-vitro drug release. Angle of repose was found to be below 25 indicating excellent flow properties

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