Formulation of Effervescent Granules Based on Calotropis procera Ait Powder (Apocynaceae) and Zanthoxylum zanthoxyloides Lam (Rutaceae)

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Résumé

Introduction: Sickle cell disease is a genetic disease that affects nearly 5% of the world's population and is particularly prevalent in sub-Saharan Africa. The inaccessibility of modern treatment has led to the development of a phytomedicine called FACA® in Burkina Faso. It is formulated in capsule form and contains a mixture of powdered root barks of Zanthoxylum zanthoxyloides and Calotropis procera . This study aims to propose an alternative, easier-to-administer form for patients who have difficulty swallowing capsules by developing effervescent granules. Materials and methods: Pre-formulation studies focused on analyzing the physicochemical and pharmaco-technical properties of the powder mixture. These included macroscopic and organoleptic aspects, pH, residual moisture content, hygroscopicity, granulometry, and flow. Effervescent granules were formulated and manufactured by the wet granulation method. Five formulations (F1-F5) were produced. Citric acid and sodium bicarbonate were used as effervescent vehicles at a ratio of 1:1.25. PVP was used as a binding agent, sucrose as a sweetener, and cornstarch as a diluent. The granulation liquid was distilled water. The granules produced were evaluated for their physicochemical properties and disintegration time. Results and discussion: the results of the physicochemical and pharmaco-technical characteristics guided the choice of excipients and the manufacturing process. The formulations were beige in color and granular in appearance. THR values were <10%, pH ranged from 5.20 ± 0.29 to 5.91 ± 0.17. They were more or less hygroscopic and presented good rheological properties with an effervescence time satisfying the specifications of the European Pharmacopoeia 11th edition. Conclusion: F4 formulation had the best characteristics and could serve as an alternative to capsules. Indeed, being dispersed in water before administration, these granules could be well tolerated by the gastrointestinal tract and promote a more rapid action of the drug at a time of crisis.

Mots-clés

Sickle Cell Disease, Herbal Medicine, Formulation, Granules, Effervescent, Zanthoxylum zanthoxyloides, Calotropis procera