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Current Pharmaceutical Analysis

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ISSN (Print): 1573-4129
ISSN (Online): 1875-676X

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Research Article

Assessment of Structural Compatibility of Saxagliptin in Physical Mixtures with some excipient by Using HPLC

Author(s): Sachin B. Gurav* and Neela M. Bhatia

Volume 16, Issue 8, 2020

Page: [1074 - 1082] Pages: 9

DOI: 10.2174/1573412915666190617153004

Price: $65

Abstract

Introduction: Saxagliptin hydrochloride is an oral hypoglycemic agent used for the treatment of type 2 diabetes mellitus. Saxagliptin is unstable because it undergoes an intra-molecular cyclisation reaction to form a cyclicamidine in both solution and solid states. In pharmaceutical development of saxagliptin it is important to select the excipients which are compatible and help to minimize the formation of cyclicamidine. In excipient compatibility study for saxagliptin it is essential to identify the formation of cyclicamidine and other related substances.

Materials and Methods: In the current work, the method for quantification of saxagliptin, cyclicamidine and its related substances by high performance liquid chromatographic was developed and validated. This method was used as screening technique for assessing the compatibility of saxagliptin with some pharmaceutical excipients. These were evaluated by analyzing the pure saxagliptin and saxagliptin- excipient in physical mixture, which were stored under different conditions at 40°C/75% Relative Humidity (RH) for one month. The method was successfully validated as per ICH guidelines.

Results and Conclusion: The results of compatibility study demonstrate the suitability of saxagliptin with Methocel, Polyethylene Glycol (PEG), Opadry Red, Opadry pink, Opadry white, and Opadry Pink.

Keywords: Compatibility, HPLC, saxagliptin hydrochloride, excipients, chromatography, pharmaceutical formulation.

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[1]
Fathima, N.; Mamatha, T.; Qureshi, H.K.; Anitha, N. Venka-teswara Rao, J. Drug-excipient interaction and its importance in dosage form development. J. Appl. Pharm. Sci., 2011, 1, 66-71.
[2]
Schmitt, E.A.; Peck, K.; Sun, Y.; Geoffroy, J. Rapid, practical and predictive excipient compatibility screening using isothermal microcalorimetry. Thermochimica. Acta., 2001, 380, 175-183.
[3]
Sachin, T.B.; Deodhar, M.N.; Prakya, V. Advances in analyti-cal techniques in predicting drug-excipients interactions. Int. J. Pharm. Technol., 2010, 2, 907-923.
[4]
Augeri, D.J.; Robl, J.A.; Betebenner, D.A.; Magnin, D.R.; Khanna, A.; Robertson, J.G.; Wang, A.; Simpkins, L.M.; Taunk, P.; Huang, Q.; Han, S.P.; Abboa-Offei, B.; Cap, M.; Xin, L.; Tao, L.; Tozzo, E.; Welzel, G.E.; Egan, D.M.; Marcinkeviciene, J.; Chang, S.Y.; Biller, S.A.; Kirby, M.S.; Parker, R.A.; Hamann, L.G. Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. J. Med. Chem., 2005, 48(15), 5025-5037.
[http://dx.doi.org/10.1021/jm050261p] [PMID: 16033281]
[5]
Brondi, A.M.; Garcia, J.S.; Trevisan, M.G. Development and Validation of a Chromatography Method Using Tandem UV / Charged Aerosol Detector for Simultaneous Determination of Amlodipine Besylate and Olmesartan Medoxomil: Application to Drug-Excipient Compatibility Study. J. Anal. Meth. Chem., 2017, 1-8.
[6]
da Silveira, L.M.; Fiorot, A.B.; Xavier, T.P.; Yoshida, M.I.; de Oliveira, M.A.; Oliveira, D. Drug-excipient compatibility assessment of solid formulations containing meloxicam. Eur. J. Pharm. Sci., 2018, 112, 146-151.
[http://dx.doi.org/10.1016/j.ejps.2017.11.015] [PMID: 29174987]
[7]
de Oliveira, G.G.; Feitosa, A.; Loureiro, K.; Fernandes, A.R.; Souto, E.B.; Severino, P. Compatibility study of paracetamol, chlorpheniramine maleate and phenylephrine hydrochloride in physical mixtures. Saudi Pharm. J., 2017, 25(1), 99-103.
[http://dx.doi.org/10.1016/j.jsps.2016.05.001] [PMID: 28223869]
[8]
Prathyusha, C.H.; Edu, J.A.P. Compatibility studies of Donepezil with different excipients by using HPLC and FTIR. J. Adv. Pharm. Educ. Res., 2013, 3(3), 273-278.
[9]
Agency, E.M. Onglyza; INN: saxagliptin, 2009.
[10]
ICH, Topic Q2 (R1) Validation of Analytical Procedures Text and Methodology. Int. Conf. Harmon 17, 2005.

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