Compatibility study between diazepam and tablet excipients
Tóm tắt
Compatibility between diazepam (DZP), a benzodiazepine drug used for the treatment of anxiety, and tablet excipients has been investigated by thermal analysis (differential scanning calorimetry—DSC and thermogravimetry—TG) and infrared (IR) spectroscopy. In order to investigate possible interactions, the components were prepared in 1:1 (w/w) mixtures. Moreover, individual samples as well as physical mixtures were stored in accelerated conditions at 40 °C/75 % RH for 3 months. Mixtures, which showed possible interactions, were also investigated in other ratios based on typical pharmaceutical solid formulation. DSC curves of DZP have shown an endothermic peak at 132 °C, which corresponds to the melting process in agreement with the literature. DSC curves of the mixtures containing DZP and colloidal silicon dioxide (CSD) indicated a possible interaction due to enthalpy values lower than expected. However, as this interaction was not confirmed by IR and TG, this suggests that these techniques are not sensitive enough to identify such interaction. These results suggest that there is a possible interaction, but not an incompatibility between DZP and CSD. For all other mixtures, it was not possible to identify significant interactions, suggesting that there are no compatibility issues.
Tài liệu tham khảo
Bosmann HB, Case KR, Distefano P. Diazepam receptor characterization: specific binding of a benzodiazepine to macromolecules in various areas of rat brain. FEBS Lett. 1977;82(2):368–72.
Moros J, Garrigues S, de La Guardia M. Quality control Fourier transform infrared determination of diazepam in pharmaceuticals. J Pharm Biomed Anal. 2007;43:1277–82.
Mielcarek J, Nowak DM, Pajzderska A, Peplinska B, Wąsicki J. A hybrid method for estimation of molecular dynamics of diazepam-density functional theory combined with NMR and FT-IR spectroscopy. Int J Pharm. 2011;404:19–26.
Sylaja B, Srinivasan S. Experimental and theoretical investigation of spectroscopic properties of diazepam. Int J ChemTech Res. 2012;4(1):361–76.
Cunha-Filho MSS, Pacheco RM, Landín M. Compatibility of the antitumoral β-lapachone with different solid dosage forms excipients. J Pharm Biomed Anal. 2007;45:590–8.
Liltorp K, Larsen TG, Willumsen B, Holm R. Solid state compatibility studies with tablet excipients using non thermal methods. J Pharm Biomed Anal. 2011;55:424–8.
Tita B, Fulias A, Bandur G, Marian E, Tita D. Compatibility study between ketoprofen and pharmaceutical excipients used in solid dosage forms. J Pharm Biomed Anal. 2011;56:221–7.
Shantikumar S, Sreekanth G, SurendraNath KV, JaferValli S, Satheeshkumar N. Compatibility study between sitagliptin and pharmaceutical excipients used in solid dosage forms. J Therm Anal Calorim. 2014;115(3):2423–8.
Mura P, Faucci MT, Manderioli A, Bramanti G, Ceccarelli L. Compatibility study between ibuproxam and pharmaceutical excipients using differential scanning calorimetry, hot-stage microscopy and scanning electron microscopy. J Pharm Biomed Anal. 1998;18:151–63.
Macedo RO, do Nascimento TG, Veras JWE. Comparison of generic hydrochlorothiazide formulations by means of TG and DSC coupled to a photovisual system. J Therm Anal Calorim. 2011;64:757–63.
Dousa M, Gibala P, Havlícek J, Placek L, Tkadlecová M, Brichác J. Drug-excipient compatibility testing—Identification and characterization of degradation products of phenylephrine in several pharmaceutical formulations against the common cold. J Pharm Biomed Anal. 2011;55:946–56.
Silva LAD, Teixeira FV, Serpa RC, Esteves NL, dos Santos RR, Lima EM, Cunha-Filho MSS, Araújo AAS, Taveira SF, Marreto RN. Evaluation of carvedilol compatibility with lipid excipient for the development of lipid-based drug delivery systems. J Therm Anal Calorim. 2015;. doi:10.1007/s10973-015-5022-1.
Monajjemzadeh F, Hassanzadeh D, Valizadeh H, Siahi-shadbad MR, Mojarrad JS, Robertson TA, Roberts MS. Compatibility studies of acyclovir and lactose in physical mixtures and commercial tablets. Eur J Pharm Biopharm. 2009;73:404–13.
Chadha R, Bhandari S. Drug-excipient compatibility screening—role of thermoanalytical and spectroscopic techniques. J Pharm Biomed Anal. 2014;87:82–97.
Thomas VH, Naath M. Design and utilization of the drug-excipient chemical compatibility automated system. Int J Pharm. 2008;359:150–7.
Maswadeh HM. Incompatibility study of ibuprofen in ternary interactive mixture by using differential scanning calorimetry. J Therm Anal Calorim. 2015;. doi:10.1007/s10973-015-4773-z.
Clas SD, Dalton CR, Hancock BC. Differential scanning calorimetry: applications in drug development. Pharm Sci Technol Today. 1999;2(8):311–20.
Botha SA, Lötter AP. Compatibility study between oxprenolol hydrochloride, temazepam and tablet excipients using differential scanning calorimetry. Drug Dev Ind Pharm. 1990;16(2):331–45.
Zayed MA, Fahmey MA, Hawash MF. Investigation of diazepam drug using thermal analyses, mass spectrometry and semi-empirical MO calculation. Spectrochim Acta A. 2005;61:799–805.
Desai SR, Shaikh MM, Dharwadkar SR. Preformulation compatibility studies of etamsylate and fluconazole drugs with lactose by DSC. J Therm Anal Calorim. 2003;71:651–8.
Schmitt EA, Peck K, Sun Y, Geoffroy JM. Rapid, practical and predictive excipient compatibility screening using isothermal microcalorimetry. Thermochim Acta. 2001;380:175–83.
Verma RK, Garg S. Compatibility studies between isossorbide mononitrate and selected excipients used in the development of the extended release formulations. J Pharm Biomed Anal. 2004;35:449–58.
Choudhari KB, Sanghavi NM. Dissolution behaviour and characterization of diazepam-Pullulan coground mixtures. Int J Pharm. 1993;89:207–11.
Abdelbary G, Fahmy RH. Diazepam-loaded solid lipid nanoparticles: design and characterization. AAPS PharmSciTech. 2009;10:211–9.
Neville GA, Shurvell HF. Fourier transform Raman and infrared vibrational study of diazepam and four closely related 1,4 benzodiazepines. J Raman Spectrosc. 1990;21:9–19.
Gunasekaran S, Thilak Kumar R, Ponnusamy S. Vibrational spectra and normal coordinate analysis of diazepam, phenytoin and phenobarbitone. Spectrochim Acta A. 2006;65:1041–52.
Ledeţi I, Vlase G, Vlase T, Şuta LM, Todea A, Fuliaş A. Selection of solid-state excipients for simvastatin dosage forms through thermal and nonthermal techniques. J Therm Anal Calorim. 2015;121:1093–102.