Enhancement of Solubility, Dissolution Rate, and Bioavailability of Azilsartan Medoxomil Using the Solid Dispersion Technique

Authors

  • Sanjeev Kumar
  • Tanveer Naved
  • Sanjar Alam
  • Reeta Chauhan

DOI:

https://doi.org/10.52783/jns.v14.3493

Keywords:

Azilsartan Medoxomil, Solid dispersion, Solubility enhancement, Pharmacokinetic, Bioavailability

Abstract

For increasing bioavailability and solubility of Azilsartan Medoxomil (AZM), a modified dosage form was developed in this study. Solid dispersion of Azilsartan Medoxomil was prepared through physical mixture and kneading method with β-cyclodextrin. Characterization is done by two main methods, Differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FTIR). The results confirmed that the use of solid dispersion in the modified dosage forms greatly enhanced the antihypertensive medications solubility and dissolution, which were previously weakly soluble in water. Furthermore, the pharmacokinetic study was performed on Wistar rats after oral administration of pure suspension and Azilsartan solid dispersion. The pharmacokinetic parameters i.e., Cmax and AUC for solid dispersions were reported to be significantly increased (p < 0.05) than that of pure API suspension. The formulation of SD-3 solid dispersion was shown best in improving solubility and dissolution. Overall, the study showed how altered dose forms may enhance the bioavailability and effectiveness of medications that are poorly soluble in water, which may result in better treatment outcomes for hypertension patients

Downloads

Download data is not yet available.

Metrics

Metrics Loading ...

References

Mills KT, Stefanescu A, He J. The global epidemiology of hypertension. Nat. Rev. Nephrol. 2020;16(4):223-3. doi: 10.1038/S41581-019-0244-2. PMID: 32024986.

Mills KT, Bundy JD, Kelly TN, Reed JE, Kearney PM, Reynolds K, Chen J, He J. Global Disparities of Hypertension Prevalence and Control: A Systematic Analysis of Population-Based Studies From 90 Countries. Circulation 2016:134:441-450. doi: 10.1161/CIRCULATIONAHA.115.018912. PMID 27502908.

Kario K, Hoshide S, Mogi M. Lifetime home BP-centered approach is the core from onset to aggravation of hypertension. Hypertens. Res.2023:46:553–555. doi: 10.1038/s41440-023-01174-5.

Ražem D, Katušin-Ražem B. The effects of irradiation on controlled drug delivery/controlled drug release systems. Radiat. Phys. Chem.2007: 77:288–344. doi:.org/10.1016/j.radphyschem.2007.06.006.

Pradhan A, Tiwari A, Sethi R. Azilsartan: Current Evidence and Perspectives in Management of Hypertension. Int. J. Hypertens 2019:2019:1824621. doi: 10.1155/2019/1824621.

“Azilsartan: Side Effects, Dosage & Uses - Drugs.com.” https://www.drugs.com/azilsartan-Medoxomil l.html (accessed Mar. 25, 2023).

Kurtz TW, Kajiya T. Differential pharmacology and benefit/risk of azilsartan compared to other sartans. Vasc. Health Risk Manag 2012:8(1):133–143. doi: 10.2147/VHRM.S22595.

Chand SP, Debnath S, Rahimi M, Ashraf MS, Bhatt P, Rahin SA. Contextualization of Trait Nexus and Gene Action for Quantitative and Qualitative Characteristics in Indian Mustard. J. Food Qual 2022:2022(2). doi: 10.1155/2022/4387318.

Mei JQ, Zhou DN, Jin ZY, Xu XM, Chen HQ. Effects of citric acid esterification on digestibility, structural and physicochemical properties of cassava starch. Food Chem 2015:187:378–384. doi: 10.1016/j.foodchem.2015.04.076.

De Caterina AR, Harper AR, Cuculi F. Critical evaluation of the efficacy and tolerability of azilsartan. Vasc. Health Risk Manag 2012:8:299–305. doi: 10.2147/VHRM.S22589. PMID: 22661897.

Al-Snafi AE, Singh S, Bhatt P, Kumar V. A review on prescription and non-prescription appetite suppressants and evidence-based method to treat overweight and obesity. GSC Biol. Pharm 2022:19(03):148–155. doi: 10.30574/gscbps.2022.19.3.0231.

[Gao Q, Xu L, Cai J. New drug targets for hypertension: A literature review. Biochim. Biophys 2021(03):1867:166037. doi: 10.1016/j.bbadis.2020.166037.

Bhatt P, Kumar V, Goel R, Sharma SK, Kaushik S, Sharma S, Shrivastava A, Tesema M. Structural Modifications and Strategies for Native Starch for Applications in Advanced Drug Delivery. Biomed Res. Int 2022:2022:1–14. doi: 10.1155/2022/2188940. PMID: 35993055.

Bhatt P, Singh S, Sharma SK, Rabiu S. Development and Characterization of Fast Dissolving Buccal Strip of Frovatriptan Succinate Monoydrate for Buccal Delivery. Int. J. Pharm. Investig 2021:11(1):69–75. doi: 10.5530/ijpi.2021.1.13.

Beneš M, Pekárek T, Beránek J, Havlíček J, Krejčík L, Šimek M, Tkadlecová M, Doležal P. Methods for the preparation of amorphous solid dispersions – A comparative study. J. Drug Deliv. Sci. Technol 2017:38:125–134. 10.1016/j.jddst.2017.02.005.

Veseli A, Žakelj S, Kristl A. A review of methods for solubility determination in biopharmaceutical drug characterization. Drug Dev. Ind. Pharm 2019:45(11):1717–1724. doi: 10.1080/03639045.2019.1665062. PMID: 31512934.

Kanojiya PS, Charde YM, Wadetwar RN. Solid Dispersion of Artemether in Fast Disintegrating Tablet to Enhance Dissolution Rate and Oral Bioavailability. Indian J of Pharmaceutical Education and Research.2022;56(1):153-65. doi: 10.5530/ijper.56.1.18.

Atef E, Belmonte AA. Formulation and in vitro and in vivo characterization of a phenytoin self-emulsifying drug delivery system (SEDDS). Eur J Pharm Sci. 2008;35(4):257–263. doi: 10.1016/j.ejps.2008.07.004. PMID: 18706499.

Mohan A, Madhavi M, Swetha G, Jyosthna P. Preparation, in vitro and in vivo characterization of solid dispersions of lamotrigine using solvent evaporation technique. IOSR J Pharm. 2015;5(1):54–59.

Aher SS, Saudagar RB, Kothari H. Development and validation of rp-hplc method for simultaneous estimation of azilsartan medoxomil and chlorthalidone in bulk and tablet dosage form. Int J Curr Pharm Res 2018:10(6):21-24. doi: 10.22159/ijcpr.2018v10i6.30967.

Downloads

Published

2025-04-11

How to Cite

1.
Kumar S, Naved T, Alam S, Chauhan R. Enhancement of Solubility, Dissolution Rate, and Bioavailability of Azilsartan Medoxomil Using the Solid Dispersion Technique. J Neonatal Surg [Internet]. 2025Apr.11 [cited 2025Apr.24];14(15S):119-33. Available from: https://jneonatalsurg.com/index.php/jns/article/view/3493