IMMEDIATE RELEASE SOLID DISPERSION TABLET OF AZILSARTAN: FORMULATION STRATEGY TO ENHANCE ORAL BIOAVAILABILITY

JAMEER A. TAMBOLI; SHRINIVAS K. MOHITE

doi:10.22159/ijap.2020v12i4.37695

Authors

JAMEER A. TAMBOLI Department of Pharmaceutics, Rajarambapu College of Pharmacy, Kasegaon, Tal Walwa, Dist Sangli MS India 415404
SHRINIVAS K. MOHITE Department of Pharmaceutics, Rajarambapu College of Pharmacy, Kasegaon, Tal Walwa, Dist Sangli MS India 415404

DOI:

https://doi.org/10.22159/ijap.2020v12i4.37695

Keywords:

Azilsartan, Soluplus, Solid dispersion, Immediate-release tablet, Bioavailability

Abstract

Objective: Objective of the present study was to develop an immediate release solid dispersion tablet to enhance oral bioavailability of Azilsartan.

Methods: Solid dispersion of azilsartan was developed using Soluplus® as a novel solubility enhancer by the solvent evaporation technique. 3²factorial design was used in a fully randomized order to study effect of amount of azilsartan and Soluplus on solubility (µg/ml) and % drug dissolved in 30 min. Prepared solid dispersion was evaluated for different micromeritic properties, saturation solubility, and wettability. Then solid dispersion of all the batches compressed into an immediate-release tablet using sodium starch glycolate as a super disintegrant. Developed tablet formulations were evaluated for various post-compression parameters and satisfactory formulation among these were further studied for Fourier-transform infrared spectroscopy (FTIR), Differential Scanning Colorimeter (DSC), X-Ray Diffraction (XRD), in vivo absorption and stability study.

Results: Results of micromeritic properties of solid dispersion showed that good flowability, compressibility, wettability, and saturation solubility. Post compression parameters of immediate-release tablets were found to be in acceptable limits. Batch ASD2 containing 40 mg Diacerein and 80 mg of Soluplus showed maximum drug release i.e. 99.82 % within 30 min. Compatibility study using FTIR, DSC, and XRD showed that drug is compatible with Soluplus. In vivo absorption study showed that, 2.67 fold increase in Area Under Curve (AUC) as compared to plain Azilsartan. Relative bioavailability was found to be 267.11 %. Results of stability study indicate that developed formulations were stable at accelerated temperature and humidity conditions.

Conclusion: Study concluded that solid dispersion using Soluplus as a solubility enhancer is a suitable formulation strategy to enhance solubility, dissolution, and bioavailability of poorly water-soluble drug-like Azilsartan.

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References

Deshmukh DB, Gaikwad PD, Bankar VH, Pawar SP. Dissolution enhancement of poorly water soluble diacerein by solid dispersion technique. J Pharm Sci Res 2010;2:734-39.

Patil AN, Shinkar DM, Saudagar RB. Solubility enhancement by solid dispersion. Int J Curr Pharm Res 2017;9:15-8.

Tachibana T, Nakamura A. A method for preparing an aqueous colloidal dispersion of organic materials by using water-soluble polymers: dispersion of B-carotene by polyvinylpyrrolidone. Kolloid-Zeitschrift Zeitschrift Polym 1965;203:130-3.

Shamma RN, Basha M. Soluplus®: a novel polymeric solubilizer for optimization of carvedilol solid dispersions: formulation design and effect of method of preparation. Powder Tech 2013;237:406-14.

Sum L. Azilsartan a newly approved angiotensin ii receptor blocker. Cardiol Rev 2011;19:300-4.

Fernanda SL, Lavinia SF, Corinna WS. Heart and blood medications. In: Christof S, Paul P, Richard KM. Drugs during pregnancy and lactation treatment options and risk assessment. 3rd ed. Academic Press: United States; 2015. p. 193-223.

Tamboli JA, Mohite SK. Self microemulsifying immediate release tablet of azilsartan for enhanced dissolution. Res J Pharm Tech 2020;13:197-202.

Naykode MD, Bhagwat DA, Jadhav SD, More HN. Analytical and bioanalytical method for quantification of pure azilsartan, not its salts by RP-HPLC. Res J Pharm Tech 2017;10:708-14.

Yan Xie, Guowen Li, Xiurong Yuan, Zhenzhen Cai, Rong Rong. Preparation and in vitro evaluation of solid dispersions of total flavones of hippophae rhamnoides L. AAPS PharmSciTech 2009;10:631-40.

Alireza Homayouni, Fatemeh Sadeghi, Ali Nokhodchi, Jaleh Varshosaz, Hadi Afrasiabi Garekanif. Preparation and characterization of celecoxib dispersions in soluplus®: comparison of spray drying and conventional methods. Iran J Pharm Sci 2015;14:35-50.

Rao MRP, Chandanshive PA. Preparation and characterization of solid dispersions for solubility enhancement of BCS class II drug. WJPPS 2017;6:1852-69.

Aulton ME. Pharmaceutics: the science of dosage form design. Second Edn. Livingstone C. Elsevier Science Ltd; 2002. p. 315-20.

More HN, Hajare AA. Practical physical pharmacy. Career Prakashan, Nashik. 2nd; 2010. p. 29-131.

Chaulang G, Patil K, Ghodke D, Khan S, Yeole P. Preparation and characterization of solid dispersion tablet of furosemide with crospovidone. Res J Pharm Tech 2008;1:20-7.

Lefebvre C, Barthelemy AM, Hermann G. An attempt at bringing to light a ‘‘phase inversion’’ in a binary mixture of two-dimensional rounded particles. Drug Dev Ind Pharm 1988;14:2443–65.

Kang MJ. Immediate release of ibuprofen from fujicalin®-based fast dissolving self-emulsifying tablets. Drug Dev Ind Pharm 2011;37:1298-305.

Panigrahi R, Chowdary KA, Mishra G, Bhowmik M, Behera S. Formulation of fast dissolving tablets of Lisinopril using combination of synthetic superdisintegrants. Asian J Pharm Tech 2012;2:94-8.

Lachman L, Liberman HA. Theory and practice of industrial pharmacy. 3rd. Varghese publishing house, Mumbai; 1990. p. 171-94.

Banker GS, Anderson NR. Tablet. In: Leon Lachman, HA Lieberman, JL Kanig. 3rd ed. The theory and practice of industrial pharmacy. Varghese publishing house, Mumbai; 1990. p. 296-302.

Indian Pharmacopoeia Government of India, Ministry of Health and Family Welfare. Vol. II. The controller of publications. New Delhi; 1996. p. 734-6.

Budiman A, Sopyan I, Riyandi DS. Enhancement of glibenclamide dissolution rate by solid dispersion method using HPMC and PVP. Int J Appl Pharm 2019;11:19-24.

Tianshu L, Yinghua S, Dawei D, Qi Z, Rui F, Zhonggui H, et al. Study on enhanced dissolution of azilsartan-loaded solid dispersion, prepared by combining wet milling and spray-drying technologies. AAPS PharmSciTech 2017;18:473-80.

Lesinski L, Duschmale UJ. Differential scanning calorimetry, physical chemistry. Wintersemester 2006;7:1-8.

Aggarwal AK, Singh S. Physicochemical characterization and dissolution study of solid dispersions of diacerein with polyethylene glycol 6000. Drug Dev Ind Pharm 2011;37:1181-91.

Chopra DK, Kar DM, Sahu PK. Improvement of oral bioavailability of azilsartan medoxomil by lipid based liquisolid compacts: in vitro and in vivo evaluation. Int Res J Pharm 2018;9:134-9.

Linn M, Collnot EM, Djuric D, Hempel K, Fabian E, Kolter K, et al. Soluplus® as an effective absorption enhancer of poorly soluble drugs in vitro and in vivo. Eur J Pharm Sci 2012;45:336-43.

Shah I, Bhatt S, Yadav A. Enhancement of solubility and dissolution of nebivolol by solid dispersion technique. Int J Pharm Pharm Sci 2014;6:566-71.

Najmuddin M, Khan T, Mohsin AA, Shelar S, Patel V. Enhancement of dissolution rate of ketoconazole by solid dispersion technique. Int J Pharm Pharm Sci 2010;2:132-6.

Guntaka Pr, Lankalapalli S. Solubility and dissolution enhancement of ivacaftor table ts by using solid dispersion technique of hot-melt extrusion-a design of experimental approach. Asian J Pharm Clin Res 2019;12:356-63.