Objective: In the present research work, the aim was to prepare the bilayer tablet of atenolol for biphasic drug release to improve its bioavailability and absorption in the lower gastrointestinal tract. Methods: In the formulation of immediate release crospovidone, croscarmellose sodium, and sodium starch glycolate was used as super disintegrate and was directly compressed. For a sustained release portion different grade hydroxypropyl methylcellulose (HPMC) K4M, HPMC K15M, gum tragacanth, gum acacia, guar gum, and ethyl cellulose. Preformulation studies were performed before compression. The compressed bilayer tablets were evaluated for weight variation, dimension, hardness, friability, drug content, disintegration time, and in vitro drug release using USP dissolution apparatus type 2 (paddle). Results: The formulation IR3 showed 95% drug release in 30 min, and regression coefficient value (r2) value was found to be 0.994 suggesting first-order drug release kinetics. The F9 formulation using HPMC K15M and gum acacia (1:1) showed 91.20% drug release at the end of 12 h, and regression coefficient value (r2) was 0.992 suggesting zero-order drug release kinetics. Formulation IR3F9 showed faster drug release for bilayer tablet containing 5%w/w crospovidone in immediate release layer and HPMC and guar gum (1:1) in sustained release. Formulation IR3F9 showed swelling index 206%, floating lag time was found to be 2 min and total floating time up to 12 h. Conclusion: The formulation IR3F9 showed a faster drug release profile among the others in the preparation of the atenolol bilayer tablet. Hence, it was considered as an optimized formulation.
Objective: The current study aimed to optimize the bioavailability and absorption of olmesartan in the lower gastrointestinal tract by creating a bilayer tablet for biphasic drug release. Methods: Microcrystalline cellulose was combined and direct compression the requirement for an early response to address an undesirable defect or condition. In the current instance, 5 mg of olmesartan must be released immediately, and the remaining 10 mg of olmesartan must be released gradually to maintain the therapeutic concentration. In order to adjust the release pattern of the olmesartan sustained release tablet in accordance with the needs of therapy and IP guidelines. Result: The best cumulative drug release was demonstrated by formulation. All formulations for immediate release support the first-order kinetics. As a result, all three formulations were chosen for additional research. Dissolution rate for long-term release Cumulative drug release from the SR1 to SR3 formulations using HPMC K15M and gum acacia was up to 24 hours. Utilizing HPMC K15M and guar gum, the formulations SR1, SR2, and SR3 demonstrated cumulative drug releases of 72.66, 69.19, and 92.66%, respectively. The best cumulative release of the drug was demonstrated by formulations SR1, SR2, and SR3. Consequently, everyone was chosen for additional research. The cumulative drug release for the IR1-SR1, IR2-SR2, and IR3-SR3 bilayer tablet formulations was 95.24, 90.15, and 91.09%. Up to 12 hours of cumulative drug release from the formulation was observed. As a result, it was determined that IR1-SR1 was the best formulation out of all of them due to its strong correlation between the total cumulative percentage of medication releases and time, which was 95.24% up to 12 hours.
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