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<p>Heart failure is a progressive cardiovascular disorder that significantly contributes to patient morbidity and mortality. Olmesartan, an angiotensin II receptor antagonist, is commonly prescribed to manage heart failure; however, its oral administration is hindered by poor solubility and variable bioavailability. This study aimed to develop a sublingual fast-dissolving Olmesartan tablet to bypass the gastrointestinal tract (GIT) and optimize its formulation using a Quality by Design (QbD) approach. A Box-Behnken Design (BBD) with three independent variables—Sodium Starch Glycolate (SSG), Crospovidone (CP), and Croscarmellose Sodium (CCS)—at two levels was employed to assess their influence on the dependent variables, namely disintegration time (DT) and cumulative drug release. The optimized formulation (OOSF-18) contained 9&#xa0;mg of SSG, 9&#xa0;mg of CP, and 6.44&#xa0;mg of CCS, yielding a rapid disintegration time of 33.33&#xa0;s and a cumulative drug release of 92.33%. Statistical analysis confirmed the robustness of the model, with an adjusted R² of 0.9961 for DT and 0.9806 for drug release, along with a desirability score of 0.998. The formulation was experimentally validated with minimal deviation from the predicted values. This optimized sublingual tablet formulation effectively addresses the limitations of oral administration, improving Olmesartan’s bioavailability and therapeutic efficacy. Additionally, the ex vivo permeation study of OOSF-18 demonstrated efficient drug release, reaching 89.76% permeation after 10&#xa0;min. Stability studies over 6 months indicated that the formulation maintained consistent physical appearance and drug content, affirming its stability and potential for long-term use. The developed sublingual Olmesartan tablet offers a promising alternative to traditional oral dosing, facilitating faster drug absorption and enhancing heart failure management through improved bioavailability.</p>

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Formulation and Optimization of Olmesartan Sublingual Tablets Using Box-Behnken Design: A QbD and Ex Vivo Study

  • 期刊论文

  • 发表日期：

    2025年10月17日

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  • Naveen K Choudhary,
  • Deepak Joshi

摘要

Heart failure is a progressive cardiovascular disorder that significantly contributes to patient morbidity and mortality. Olmesartan, an angiotensin II receptor antagonist, is commonly prescribed to manage heart failure; however, its oral administration is hindered by poor solubility and variable bioavailability. This study aimed to develop a sublingual fast-dissolving Olmesartan tablet to bypass the gastrointestinal tract (GIT) and optimize its formulation using a Quality by Design (QbD) approach. A Box-Behnken Design (BBD) with three independent variables—Sodium Starch Glycolate (SSG), Crospovidone (CP), and Croscarmellose Sodium (CCS)—at two levels was employed to assess their influence on the dependent variables, namely disintegration time (DT) and cumulative drug release. The optimized formulation (OOSF-18) contained 9 mg of SSG, 9 mg of CP, and 6.44 mg of CCS, yielding a rapid disintegration time of 33.33 s and a cumulative drug release of 92.33%. Statistical analysis confirmed the robustness of the model, with an adjusted R² of 0.9961 for DT and 0.9806 for drug release, along with a desirability score of 0.998. The formulation was experimentally validated with minimal deviation from the predicted values. This optimized sublingual tablet formulation effectively addresses the limitations of oral administration, improving Olmesartan’s bioavailability and therapeutic efficacy. Additionally, the ex vivo permeation study of OOSF-18 demonstrated efficient drug release, reaching 89.76% permeation after 10 min. Stability studies over 6 months indicated that the formulation maintained consistent physical appearance and drug content, affirming its stability and potential for long-term use. The developed sublingual Olmesartan tablet offers a promising alternative to traditional oral dosing, facilitating faster drug absorption and enhancing heart failure management through improved bioavailability.