Solid Dispersion System Candesartan-cilexetil Mannitol Co-Grinding Method
DOI:
https://doi.org/10.30595/pharmacy.v0i0.16667Keywords:
Candesartan-cilexetil, Co-grinding, Solid dispersionAbstract
Research on solid dispersion systems had been done to improve physicochemical characteristics and the dissolution rate of candesartan-cilexetil a had been conducted. Candesartan cilexetil is included in BCS (Biopharmaceutical Classification System) class II, which has low solubility and high permeability which causes poor absorption of drugs in the digestive tract. Solid dispersions were prepared through the grinding method using mannitol. The formula with 3 comparisons between candesartan-cilexetil and mannitol 1:1, 1:3, and 1:5. A mixture of physics of candesartan cilexetil-mannitol was made without a solid dispersions system which was 1:1 as a comparison. Solid dispersion formed was characterized by particle size distribution analysis, Fourier transforms infrared (FT-IR), X-ray diffraction, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), determination rate, and dissolution test. The result particle size distribution analysis showed grinding method there were solid dispersions mixed perfectly. The FT-IR of this analysis showed no interaction between candesartan-cilexetil mannitol in solid dispersion powder. The result of X-ray diffraction showed a decrease in crystallization degree. The DSC result showed a shift in endothermic peak candesartan-cilexetil. The manufacture of a solid dispersion system of candesartan-cilexetil mannitol can improve the physicochemical characteristics and the dissolution rate of candesartan-cilexetil compared with physical mixtures. The result in the dissolution was solid dispersion 1 = 53.1990 %, solid dispersion 2 = 54.3621 %, and solid dispersion 3 = 62.3621 %. The statistical result of dissolution efficiency using the Kruskal-Willis test with significant = 0.009(< 0.05) showed the difference among the dissolution efficiency of candesartan-cilexetil, physical mixture, and each solid dispersion.
References
Ali, HA., Omer, HK. 2022. Solubility Enhancement of a Poorly Water-Soluble Drug Using Hydrotropy and Mixed Hydrotropy-Based Solid Dispersion Techniques. Hindawi Advances in Pharmacological and Pharmaceutical Sciences, https://doi.org/10.1155/2022/7161660.
Althanoon, ZA., Thanoon, IAJ. 2022. Comparative Effects of Amlodipine and Candesartan on Blood Pressure and Metabolic Profile in Non-Diabetic Hypertensive Patients. Pharmacogn J. 14(1): 141-147.
Azharshekoufeh, L., Shokri, J., Jalali, MB., Javadzadeh, Y. 2017. Liquiground Technique: a New Concept for Enhancing Dissolution Rate of Glibenclamide by Combination of Liquisolid and C0-grinding Technologies. BioImpacts, 7(1), 5-12.
Bertoni, S., Albertini, B., Passerini, N. 2020. Different BCS Class II Drug-Gelucire Solid Dispersions Prepared by Spray Congealing: Evaluation of Solid State Properties and In Vitro Performances. Pharmaceutics, 12, 548; doi:10.3390/pharmaceutics12060548.
Japanesa Pharmacopeia Committee. (2011). The Japanese Pharmacopeia. Edisi XVI. Tokyo: The Ministry of Health, Labour and Welfare.
Kondoros, BA., Berkesi, O., Toth, Z., Aigner, Z., Ambrus, R., Csoka, I. 2022. Cyclodextrin Complexation of Fenofibrate by Co-Grinding Method and Monitoring the Process Using Complementary Analytical Tools. Pharmaceutics, https://doi.org/10.3390/pharmaceutics14071329.
Mannem, V., Suryadevara, V., Doppalapudi, S. 2018. Formulation and Evaluation of Telmisartan Solid Dispersions Using Entada Scandens Seed Starch and Poloxamer-188 as Superdisintegrants. Asian Journal of Pharmaceutical and Clinical Research, 11(9), 474-481.
Martau, GA., Coman, V., Vodnar, DC. 2020. Recent Advances in The Biotechnological Production of Erythritol and Mannitol. Critical Reviews in Biotechnology, https://doi.org/10.1080/07388551.2020.1751057.
Nazem, NM., Shokri, J., Nourani, N., Rajabi, A., Javadzadeh, Y. 2022. Combining Liquidsolid and Co-grinding Techniques to Enhance the Dissolution Rate of Celecoxib. Journal of Pharmaceutical Innovation, https://doi.org/10.1007/s12247-022-09641-1.
Pansuriya, K., Shelat, P., Patel, H. 2020. Preformulation Study For Candesartan Cilexetil Buccal (Effervescent) Tablet. International Journal of Pharmaceutical Sciences and Research, 11(6):2868-2874.
Shargel, L., Wu-Pong, S., Yu, A. B. C. 2004. Applied Biopharmaceutics and Pharmacokinetics. 5th ed. New York: McGraw-Hill Medical Google Scholar.
Shi, Q., Chen, H., Wang, Y., Wang, R., Xu, J., Zhang, C. 2022. Amorphous Solid Dispersions: Role of the Polymer and Its Importance in Physical Stability and In Vitro Performance. Pharmaceutics, https://doi.org/10.3390/pharmaceutics14081747.
Shittu, AO., Njinga, NS., Orshio, SD. 2022. Development and Characterization of Ibuprofen Solid Dispersion for Solubility and Dissolution Improvement Using a Binary Carrier System Consisting of D- Mannitol – Polyethylene Glycol 600. The Nigerian Journal of Pharmacy. 56(1):109-118.
Thakral, S., Sonje, J., Munjal, B., Bhatnagar, B., Suryanarayanan, R. 2022. Mannitol as an Excipient for Lyophilized Injectable Formulations. Journal of Pharmaceutical Sciences, 112 (2023) 19-35.
The United States Pharmacopeial Convention. (2016). Revision Bulletin. Candesartan Cilexetil Tablets (C181881_M12275-CHM22015, Rev. 0 20161118). Chemical Medicines Monographs 2.
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