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

Received: 26 February 2025     Accepted: 12 March 2025     Published: 14 May 2025
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Abstract

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.

Published in Pharmaceutical Science and Technology (Volume 9, Issue 1)
DOI 10.11648/j.pst.20250901.13
Page(s) 17-26
Creative Commons

This is an Open Access article, distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution and reproduction in any medium or format, provided the original work is properly cited.

Copyright

Copyright © The Author(s), 2025. Published by Science Publishing Group

Keywords

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

References
[1] Ouattara B, Jansen O, Angenot L, Guissou I, Frédérich M, Fondu P, et al. Antisickling properties of divanilloylquinic acids isolated from Fagara zanthoxyloides Lam. (Rutaceae). Phytomedicine. 2009; 16(2-3): 125-9.
[2] Traore A, Lompo M, Some N, Sana B, Guissou I. Vasodilator effect of Zanthoxylum zanthoxyloïdes, Calotropis procera and FACA, a mixture of these two plants. International Journal of Biological and Chemical Sciences. 2011; 5(4): 1351-7.
[3] Guissou I, Sawadogo M, Sawadogo A, Ouattara A. Study of the anti-sickle cell efficacy of FACA® capsules in children in a hospital setting in Ouagadougou (chn-yo). Pharm Méd trad afro. 1995: 29-36.
[4] Ouédraogo S, Traoré S, Ouédraogo JCW, Koala M, Belemnaba L, Ouédraogo N, et al. Quality control and standardization Of FACA® syrup. Int J Drug Deliv. 2018; 9(4): 101.
[5] Ouédraogo JCW, Kini FB, Belemnaba L, Ouédraogo S, Guissou IP. Standardization of bark root powder of Zanthoxylum zanthoxyloides for the production of pediatric phytomedecine against Sickle Cell Disease. Journal of the West African Chemical Society. 2015; 40: 24.
[6] Aslani A, Jahangiri H. Formulation, characterization and physicochemical evaluation of ranitidine effervescent tablets. Advanced pharmaceutical bulletin. 2013; 3(2): 315.
[7] AL-MOUSAWY J, AL-HUSSAINY Z, ALAAYEDI M. Formulation and evaluation of effervescent granules of ibuprofen. International Journal of applied pharmaceutics. 2019: 66-9.
[8] Bhattacharyya S, Swetha G. Formulation and evaluation of effervescent granules of Fexofenadine hydrochloride. The Pharma Innovation. 2014; 3(3, Part A): 1.
[9] Ph. Eur. European Pharmacopoeia 10th edition 10.0, 10.1, 10.2- edqm / council of europe 2019.
[10] Fonteneau J-M. The Pharmacopoeia 11th edition. Pharmaceutical News. 2024; 63(637): 30-2.
[11] Adi-Dako O, Kumadoh D, Egbi G, Okyem S, Addo PY, Nyarko A, et al. Strategies for formulation of effervescent granules of an herbal product for the management of typhoid fever. Heliyon. 2021; 7(10).
[12] Rowe RC, Sheskey P, Quinn M. Handbook of pharmaceutical excipients: Libros Digitales-Pharmaceutical Press; 2009.
[13] Allen L, Ansel HC. Ansel's pharmaceutical dosage forms and drug delivery systems: Lippincott Williams & Wilkins; 2013.
[14] Parikh DM. Handbook of pharmaceutical granulation technology. Drugs and the pharmaceutical sciences. 2005; 81.
[15] Aulton ME. Pharmaceutics: The science of dosage form design. (No Title). 2002.
[16] Alburyhi MM, El-Shaibany A. Formulation and Evaluation of Effervescent Granules of Artemisia Arborescence Herbal Product for Foodborne Illness. World Journal of Pharmacy and Pharmaceutical Sciences. 2023; 12(12): 1429-44.
[17] Le Hir A. Life of a drug, from design to good manufacturing practices. Abstracts of galenic pharmacy good manufacturing practices for drugs 9th edition Masson. 2001: 4-8.
[18] Jassim ZE, Rajab NA, Mohammed NH. Study the effect of wet granulation and fusion methods on preparation, characterization, and release of lornoxicam sachet effervescent granules. Drug Invention Today. 2018; 10(9): 1612-6.
Cite This Article
  • APA Style

    Salfo, O., Constantin, A. B., Kadiatou, T. T., Martin, R. T. S., Safiatou, T., et al. (2025). Formulation of Effervescent Granules Based on Calotropis procera Ait Powder (Apocynaceae) and Zanthoxylum zanthoxyloides Lam (Rutaceae). Pharmaceutical Science and Technology, 9(1), 17-26. https://doi.org/10.11648/j.pst.20250901.13

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    ACS Style

    Salfo, O.; Constantin, A. B.; Kadiatou, T. T.; Martin, R. T. S.; Safiatou, T., et al. Formulation of Effervescent Granules Based on Calotropis procera Ait Powder (Apocynaceae) and Zanthoxylum zanthoxyloides Lam (Rutaceae). Pharm. Sci. Technol. 2025, 9(1), 17-26. doi: 10.11648/j.pst.20250901.13

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    AMA Style

    Salfo O, Constantin AB, Kadiatou TT, Martin RTS, Safiatou T, et al. Formulation of Effervescent Granules Based on Calotropis procera Ait Powder (Apocynaceae) and Zanthoxylum zanthoxyloides Lam (Rutaceae). Pharm Sci Technol. 2025;9(1):17-26. doi: 10.11648/j.pst.20250901.13

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  • @article{10.11648/j.pst.20250901.13,
      author = {Ouédraogo Salfo and Atchadé Boladé Constantin and Traoré Tata Kadiatou and Rouamba Téyindé Songré Martin and Traoré Safiatou and Goumbri Wendinmi Bertrand Florent and Yaméogo Boumbéwendin Gérard Josias and Ouédraogo Sylvin and Semdé Rasmané},
      title = {Formulation of Effervescent Granules Based on Calotropis procera Ait Powder (Apocynaceae) and Zanthoxylum zanthoxyloides Lam (Rutaceae)
    },
      journal = {Pharmaceutical Science and Technology},
      volume = {9},
      number = {1},
      pages = {17-26},
      doi = {10.11648/j.pst.20250901.13},
      url = {https://doi.org/10.11648/j.pst.20250901.13},
      eprint = {https://article.sciencepublishinggroup.com/pdf/10.11648.j.pst.20250901.13},
      abstract = {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.
    },
     year = {2025}
    }
    

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  • TY  - JOUR
    T1  - Formulation of Effervescent Granules Based on Calotropis procera Ait Powder (Apocynaceae) and Zanthoxylum zanthoxyloides Lam (Rutaceae)
    
    AU  - Ouédraogo Salfo
    AU  - Atchadé Boladé Constantin
    AU  - Traoré Tata Kadiatou
    AU  - Rouamba Téyindé Songré Martin
    AU  - Traoré Safiatou
    AU  - Goumbri Wendinmi Bertrand Florent
    AU  - Yaméogo Boumbéwendin Gérard Josias
    AU  - Ouédraogo Sylvin
    AU  - Semdé Rasmané
    Y1  - 2025/05/14
    PY  - 2025
    N1  - https://doi.org/10.11648/j.pst.20250901.13
    DO  - 10.11648/j.pst.20250901.13
    T2  - Pharmaceutical Science and Technology
    JF  - Pharmaceutical Science and Technology
    JO  - Pharmaceutical Science and Technology
    SP  - 17
    EP  - 26
    PB  - Science Publishing Group
    SN  - 2640-4540
    UR  - https://doi.org/10.11648/j.pst.20250901.13
    AB  - 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.
    
    VL  - 9
    IS  - 1
    ER  - 

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Author Information
  • Research and Development Laboratory for Phytomedicines and Drugs (LR-D/PM), Institute for Research in Health Sciences (IRSS/CNRST), Ouagadougou, Burkina Faso; Laboratory of Drug Development (LADME), Doctoral School of Health, Joseph Ki-Zerbo University, Ouagadougou, Burkina Faso

  • Research and Development Laboratory for Phytomedicines and Drugs (LR-D/PM), Institute for Research in Health Sciences (IRSS/CNRST), Ouagadougou, Burkina Faso; Laboratory of Drug Development (LADME), Doctoral School of Health, Joseph Ki-Zerbo University, Ouagadougou, Burkina Faso

  • Research and Development Laboratory for Phytomedicines and Drugs (LR-D/PM), Institute for Research in Health Sciences (IRSS/CNRST), Ouagadougou, Burkina Faso

  • Laboratory of Drug Development (LADME), Doctoral School of Health, Joseph Ki-Zerbo University, Ouagadougou, Burkina Faso

  • Research and Development Laboratory for Phytomedicines and Drugs (LR-D/PM), Institute for Research in Health Sciences (IRSS/CNRST), Ouagadougou, Burkina Faso; Laboratory of Drug Development (LADME), Doctoral School of Health, Joseph Ki-Zerbo University, Ouagadougou, Burkina Faso

  • Research and Development Laboratory for Phytomedicines and Drugs (LR-D/PM), Institute for Research in Health Sciences (IRSS/CNRST), Ouagadougou, Burkina Faso; Laboratory of Drug Development (LADME), Doctoral School of Health, Joseph Ki-Zerbo University, Ouagadougou, Burkina Faso

  • Laboratory of Drug Development (LADME), Doctoral School of Health, Joseph Ki-Zerbo University, Ouagadougou, Burkina Faso

  • Research and Development Laboratory for Phytomedicines and Drugs (LR-D/PM), Institute for Research in Health Sciences (IRSS/CNRST), Ouagadougou, Burkina Faso

  • Laboratory of Drug Development (LADME), Doctoral School of Health, Joseph Ki-Zerbo University, Ouagadougou, Burkina Faso

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