Objective: The objective of this study is to develop a controlled release matrix tablet of candesartan cilexetil to reduce the frequency of administration, enhance bioavailability and improve patient compliance; a once daily sustained release formulation of candesartan cilexetil is desirable.
Methods:The prepared tablets from F1 to F24 were evaluated with different evaluation parameters like weight variation, drug content, friability, hardness, thickness and swelling ability. In vitro release for all formulas were studied depends on the type and amount of each polymer, i.e. (16 mg, 32 mg and 48 mg) respectively beside to the combination effect of polymers on the release of the drug from the tablet.
Results:In vitro release showed that formula 13 had the faster release (100% after 4 h) which contained acacia (1:1) and the lowest sustain release was showed for F7 (73% after 8 h) which contained HPMC K100M (1:1). Formula 1 was an 89 % release after 8 h which contain eudragit RS100; F4 was a 100 % release after 5 h which contain Na CMC, F10 was a 100% after 8 h which contain xanthan gum and F16 was a 100 % release after 5 h which contain tragacanth polymer. Formula 9 had a lower release than F7 and F8 respectively. Formula 7 can be used for sustain oral drug delivery of candesartan cilexetil while Formula 13 can be used in contrary as fast release tablets for faster response.
Conclusion:Controlled drug delivery system is promising for less dosing and higher patient compliance.
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Objective: Matrix tablet approach is one of the delivery systems intended for poorly water-soluble drugs like candesartan cilexetil. Candesartan cilexetil is a class II drug used for the treatment of hypertension.
Methods: Matrix tablets from (F1x to F18z) were prepared in the presence of β-cyclodextrin. Matrix tablet formulation ensures control release of the drug and higher dissolution by β-cyclodextrin. Fourier transform infrared spectroscopy and differential scanning calorimetry were used to study compatibility.
Results:The angle of repose determination showed good flow for most of the formulas besides having good compressibility. Weight variation test for all formulas showed accepted value. Drug content measurement showed accepted values. Friability and hardness of tablets were within the allowed values. Higher tablet swelling was obtained for the formulas containing hydroxy propyl methyl cellulose (HPMC) K100M (F3x and F15z) in which the ratio of the polymer was (1:1) and (1:3) respectively. In vitro release showed that F1x to F13z were studied depends on the type and amount of polymer i.e. (1:1), (1:2) and (1:3) respectively. F1x release after 8h was 95% which contain (1:1) polymer ratio in compare to F3x, which showed 85% after 8h, Which include 1:3 (drug: HPMC K100). Kinetic studies showed a zero-order model.
Conclusion: The use of β-cyclodextrin modify the release profile of the drug, and control the sustained release formulas. The lower the time of the release but in a range that a sustained release of the drug was observed in compare with the formulas prepared without β-cyclodextrin.
Diabetes is a metabolic condition that affects how the body utilizes digested food for growth and energy. The majority of the food we consume is broken down into glucose, which is the form of sugar in our blood. Glucose is the body's primary fuel source. The solubility of glibenclamide (glibenclamide), metformin, and sitagliptin were evaluated in triplicate in different pH using a water bath shaker at 37oC using the shake-flask technique. The quantity of medicine accessible for absorption is determined by the drug release. Each drug's physiochemical characteristics substantially impact release along the G.I.T. For each medication, a calibration curve and solubility measurement were performed. In the duodenum and the small intestine, glibenclamide was released more efficiently and fast than metformin and sitagliptin, which had higher pKa values than glibenclamide, i.e., the metformin and sitagliptin were released more quickly and efficiently in pH 1.2 and pH 5.8. Glibenclamide is absorbed from the stomach, if not completely.
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