Formulation and Evaluation of Gastro-retentive Microsphere of Saxagliptin Antidiabetic Agent

Purshottam Kumar Thakur; C K Tyagi; Neelesh Choubey

doi:10.24092/CRPS.2023.130302

Purshottam Kumar Thakur College of pharmacy, Sri Satya Sai university of Technology and Medical sciences, Sehore (M.P), India 466002
C K Tyagi College of pharmacy, Sri Satya Sai university of Technology and Medical sciences, Sehore (M.P), India 466002
Neelesh Choubey College of pharmacy, Sri Satya Sai university of Technology and Medical sciences, Sehore (M.P), India 466002

DOI https://doi.org/10.24092/CRPS.2023.130302

Abstract

The objective of this study was to develop a gastro-retentive microsphere of Saxagliptin. Saxagliptin is an orally active hypoglycemic drug of the newdipeptidylpeptidase-4(DPP4) inhibitor class of drug. Nine formulations of Saxagliptin microsphere are prepared by Emulsion solvent diffusion method using polymers like Eudragit RS 100 and Ethyl cellulose at different drug to polymer ratios and Polyvinyl Alcohol as Stabilizing agent by Emulsion Solvent Diffusion Method. The formulations were optimized on the basis of percent buoyancy and in vitro drug release. The prepared microspheres were evaluated for physicochemical parameters and found to be within range.

Keywords: Gastro retentive, Saxagliptin, Ethyl cellulose, Floating microsphere, Eudragit RS 100, Polyvinyl alcohol

References

Leon Lachman and Liberman A. The theory and practice of Industrial pharmacy Mumbai Varghese publishing house, 1987; 3: 329-5, 430.
2. Leon Lachman and Schwartz B. compression coated and layer tablets. Pharmaceutical dosage forms. Tablets, Mumbai: Varghese publishing House, 1989; 2:273-4.
3. Rajput GC, Majmudar D.F, Patel K.J, Patel N.K, Thakor S.R and Patel R.R. Floating Drug Delivery System- A Review. Pharm Ext. 2010; 1(1) 43-51.
4. Nasa P, Mahant S and Sharma D. Floating Systems: A Novel Approach towards Gastro retentive Drug Delivery System. 2010;2: 1-7.
Sharma V, Singh L, Sharma V. A Novel approach to combat regional variability: Floating drug delivery system. IJPSRR. 2011; 8(2):154-159.
6. Joshi VK, Jaimini M. Micro ballons drug delivery system: A review, AJPRD 2013;1(1);07-17.
7. Garg R and Gupta G.D. Progress in controlled Gastro retentive delivery. Trop J Phar Res. 2008; 7(3):1055-1066.
8. Pujara ND, Patel NV, Thacker AP, Raval BK, Doshi SM, Parmar RB. Floating microspheres: A novel approach for gastro retention. World journal of pharmacy and pharmaceutical sciences. 2012; 1(3): 872-89.
9. Yadav S, Nyola NK, Jeyabalan G, Gupta M. Gastro retentive drug delivery system: a concise review. Int J Res Pharm Sci 2016, 6(2); 19 –24.

10. Yamada T, Onishi H, Machida Y. Sustained release ketoprofen microparticles with ethyl cellulose and carboxymethyl ethyl cellulose. J Control Rel. 2001; 75: 271–282.
11. Shakya R, Thapa P, Saha.NR. In Vitro and In Vivo Evaluation of Gastro retentive Floating Drug Delivery System of Ofloxacin. Asian Journal of Pharmaceutical Sciences. 2013; 1(1): 91-98.
12. Ashtamkar J, Nangude S, Chugh N. Formulation and Evaluation of Controlled Release Tablets of Labetalol Hydrochloride using Hydrophobic Polymers, International Journal of Research in Pharmaceutical and Biomedical Sciences. 2013; 4(1): 380-384.
13. Rao GK, Mandapalli PK, Manthri RC, Reddy V, Reddy P. Development and In- Vivo Evaluation of Gastro retentive Delivery Systems for Cefuroxime Axetil, Saudi Pharmaceutical Journal.2013, 21: 53-59.
14. Padhye SG, Mangal S, Nagarsenker S. imva statin solid lipid nanoparticles for oral delivery: Formulation development and in vivo evaluation, Indian Journal of Pharmaceutical Science 2013; 75 (5): 591-598.
15. Ministry of Health and Family Welfare, Government of India, Indian Pharmacopoeia 2014; Ghaziabad, the Indian pharmacopoeia commission.
16. Suriya Kiran Vuddisa, Subramanian S, Sindu Raavi. Preparation and characterization of candesartan cilexetil solid lipid nano particvulate capsules. International Journal of Pharma Research and Review 2014; 3(12): 26-31.
17. Brahmankar DM, Sunil B. Jaiswal. Text book Biopharmaceutics and Pharmacokinetics -A treatise. 2nd ed. New delhi: Jaypee publishers; 2002.p. 243,397-510.
18. Swarupa Arvapally, Harini M, Harshitha G, Arunkumar A. Formulation and In vitro Evaluation of Glipizide Nanosponges. Amarican Journal of Pharm Tech Research. 2017;7(3):342-360.
19. Suvakanta Dash S, Padala, Narasimha Murthy K, Lilakanta Nath, Prasanth kumar Chowdhury RK inetic Modelling on Drug Release from Controlled Drug Delivery Systems, ActaPoloniae Pharmaceutica and Drug Research 2010; 67(3):217-223.