Compatibility Studies of Sildenafil with Different Excipients by Using TGA, DSC, XRD and FTIR

Study of drug–excipient interactions is a crucial step in preformulation stage of drug development to achieve consistent chemical, physical, bioavailability, manufacturability and stability of the dosage form. In pre-formulation studies, it is important to use thermoanalytical and spectroscopic methods. These are important systems for achieving a suitable formulation. Sildenafil is a well-tolerated and highly effective treatment for erectile dysfunction. erectile dysfunction was revolutionized with the development of a selective inhibitor of cyclic guanosine monophosphate-specific phosphodiesterase type 5. , Fourier Transform Infrared Spectroscopy, and X-ray Powder Diffraction systems were used in the investigation and to determine the possible interactions between sildenafil and some excipients like butylated hydroxyanisole, cellulose, sodium carboxymethyl cellulose, ascorbic acid, and citric acid. Binary mixtures of drug:excipient=1:1 (mass/mass) have been analyzed. According to the results, there is incompatibility with butylated hydroxyanisole, ascorbic acid, and citric acid.

Keywords:

Sildenafil, compatibility, excipient, TGA FTIR, DSC,

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1. Lue, T.F, Erectile dysfunction, The New England Journal of Medicine, 2000, 342, 1802-1813.
2. McMahon, C.G, High dose sildenafil citrate as a salvage therapy for severe erectile dysfunction. International Journal of Impotence Research, 2002, 14, 533-538.
3. Özgür, C.Ö, Gonenc, F, Yazicioglu, A.H, Sildenafil or vardenafil nonresponders’ erectile response to Tadalafil, Urology Journal, 2009(6), 267-271.
4. Boolell, M, Allen, M.J, Ballard, S.A, Gepi-Attee, S, Muirhead, G.J, Naylor, A.M, Osterloh, I.H, Gingell, C, Sildenafil: an orally active type 5 cyclic GMP-specific phosphodiesterase inhibitor for the treatment of penile erectile dysfunction. International Journal of Impotence Research, 1996, 8, 47–52.
5. Webb, D.J, Freestone, S, Allen, M.J, Muirhead, G.J, Sildenafil citrate and blood-pressure–lowering drugs: Results of drug interaction studies with an organic nitrate and a calcium antagonist, The American Journal of Cardiologyt, 1999, 83(5A), 21C-28C.
6. Verma, R.K, Garg, S, Selection of excipients for extended release formulations of glipizide through drug–excipient compatibility testing, Journal of Pharmaceutical and Biomedical Analysis, 2005, 38(4), 633-44.
7. Fathima, N, Mamatha, T, Qureshi, H.K, Anitha, N, Rao, J.V, Drug-excipients interaction and its importance in dosage form development, Journal of Applied Pharmaceutical Science, 2011, 1(6), 66-71.
8. Bozag Pehlivian, S, Subaşi, B, Vural, I, Unlü, N, Capan, Y, Evaluation of drug-excipient interaction in the formulation of celecoxib tablets. Acta Poloniae Pharmaceutica, 2011, 68, 423-433.
9. Murthy, T.E.G.K, Bala Vishnu Priya M, Suresh Babu V.V, Compatibility studies of Acetazolamide with excipients by using High performance liquid chromatography, Indian drugs, 2012, 49(05), 39-45.
10. Prathyusha, C.H, Murthy. T.E.G.K. Compatibility studies of Donepezil with different excipients by using HPLC and FTIR, Journal of Advanced Pharmacy Education & Research, 2013, 3(3), 273-278.
11. Tulasi Baru, R, Bitla, P, Cyclobenzaprine drug assay and cyclobenzaprine-excipient interaction studyby chromatography, thermal and spectral analysis, Journal of Pharmaceutical Chemistry & Chemical Science, 2017, 1(1), 1-9.
12. McDaid FM, Barker SA, Fitzpatrick S, Petts, C.R, Craig, D.Q.M, Further investigations into the use of high sensitivity differential scanning calorimetry as a means of predicting drug–excipient interactions, The International Journal of Pharmaceutics, 2003, 252(1), 235-240.
13. Thomas, V.H, Naath, M, Design and utilization of the drug–excipient chemical compatibility automated system, The International Journal of Pharmaceutics, 2008, 359(1), 150-157.
14. Monajjemzadeh, F, Hassanzadeh, D, Valizadeh, H, Siahi-Shadbad, M.R, Mojarrad, J.S, Robertson, T.A, Roberts, M.S, Compatibility studies of acyclovir and lactose in physical mixtures and commercial tablets, The European Journal of Pharmaceutics and Biopharmaceutics, 2009, 73, 404–413.
15. Verma, R.K, Garg, S, Selection of excipients for extended release formulations of glipizide through drug – excipient compatibility testing, Journal of Pharmaceutical and Biomedical Analysis, 2005, 38, 633–644.
16. Wakasawa, T, Sano, K, Hirakura, Y, Toyooka, T, Kitamura, S, Solid-state compatibility studies using a high-throughput and automated forced degradation system, The International Journal of Pharmaceutics, 2008, 355, 164–173.
17. Madejová, J, FTIR techniques in clay mineral studies, Vibrational Spectroscopy, 2003, 31(1), 1–10.
18. Ohannesian, L, Streeterhandbook, A.J, Handbook of Pharmaceutical Analysis, Marcel Dekker, New York, NY, USA, 2002.
19. Melnikov, P, Corbi, P.P, Cuin, A, Cavicchioli, M, Guimarães, W.R, Physicochemical properties of sildenafil citrate (Viagra) and sildenafil base, Journal of Pharmaceutical Sciences, 2003, 92, 2140-43.
20. Júlio, T.A, Zâmara, I.F, Garcia, J.S, Trevisan, M.G, Compatibility of sildenafil citrate and pharmaceutical excipients by thermal analysis and LC-UV, Journal of Thermal Analysis and Calorimetry, 111(3), 2037-2044.
21. Yathirajan, H.S, Nagaraj, B, Nagaraja, P, Bolte, M, Sildenafil citrate monohydrate, Acta Crystallographica Section E, 2005, E61, o489-o491.
22. Sawatdee, S, Pakawatchai, C, Nitichai, K, Srichana, T, Phetmung, H, Why sildenafil and sildenafil citrate monohydrate crystals are not stable?, Saudi Pharmaceutical Journal, 2015, 23, 504-514.

Celal Bayar Üniversitesi Fen Bilimleri Dergisi-Cover

ISSN: 1305-130X
Başlangıç: 2005
Yayıncı: Manisa Celal Bayar Üniversitesi Fen Bilimleri Enstitüsü

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