Thermal analysis studies on the compatibility of furosemide with solid state and liquid crystalline excipients

Main Article Content

Marilena Vlachou
Natassa Pippa
Angeliki Siamidi
Aimilia Kyrili

Abstract

In the context of the present study, the thermal behavior of furosemide and the solid state excipients, sodium alginate, poly(ethylene oxide), poly(vinylpyrrolidone), lactose mono­hydrate and magnesium stearate, using Differential Scanning Calorimetry (DSC), was probed. It was found that the thermal behavior of these solid-state pharmaceutical excipients and furosemide correlates nicely with the literature relevant data. Regarding the furosemide-excipients mixtures, the DSC scans appear as a compilation of the thermal curves of each excipient. This suggests that the formulations containing these mixtures, may retain their stability over time. This information, which arises from the cooperativity of materials, their thermal stability and behavioris very helpful for the research and development of safe and effective pharmaceutical formulations. DSC experiments were also carried out with chimeric bilayers (called "liposomes"), composed of hydrogenated soy phosphatidylcholine (HSPC) and poly(n-butylacrylate)-b-poly(acrylic acid) block copolymer with 70 % content of poly(acrylic acid (PnBA-b-PAA 30/70) with the addition of furosemide at the molar ratio of 9:0.1:1.0 in the system HSPC:PnBA-b-PAA 30/70:furosemide. Chimeric liposomal systems were characterized as "fluid-like" by their DSC curves, which may be potentially translated as an easy way for release of furosemide from the advanced delivery system. 

Downloads

Download data is not yet available.

Article Details

How to Cite
Vlachou, M., Pippa, N., Siamidi, A., & Kyrili, A. (2020). Thermal analysis studies on the compatibility of furosemide with solid state and liquid crystalline excipients. HEMIJSKA INDUSTRIJA (Chemical Industry), 74(1), 15–23. https://doi.org/10.2298/HEMIND190910002V
Section
Chemical Engineering - Pharmaceutical Engineering

References

Strauch S, Jantratid E, Dressman JB, Junginger HE, Kopp S, Midha KK, Shah VP, Stavchansky S, Barends DM. Biowaiver monographs for immediate release solid oral dosage forms: mefloquine hydrochloride. J Pharm Sci. 2011; 100: 11-21.

Vlachou M and Papaïoannou G. Preparation and characterization of the inclusion complex of furosemide with hydroxypropyl-β-cyclodextrin. J Biomater Appl. 2003; 17: 197–206.

Efentakis M and Vlachou M. Evaluation of high molecular weight poly(oxyethyle) (polyox) polymer: studies of flow properties and release rates of furosemide and captopril from controlled-release hard gelatin capsules. Pharm Dev Technol. 2000; 5: 339-346.

Vlachou M, Geraniou E., Siamidi A, Modified release of furosemide from Eudragits® and poly(ethylene oxide)-based matrices and dry-coated tablets Acta Pharm. 2020; 10: 49-61 https://doi.org/10.2478/acph-2019-0043

Bruylants G, Woutres J, Michaux C. Differential scanning calorimetry in life science: thermodynamics, stability, molecular recognition and application in drug design. Curr Med Chem. 2005; 12: 2011-2020.

Narang AS, Desai D, Badawy S. Impact of excipient interactions on solid dosage form stability. Pharm Res. 2012; 29: 2660-2683.

Chadha R, Bhandari S. Drug-excipient compatibility screening-Role of thermoanalytical and spectroscopic techniques. J Pharm Biom Anal. 2014; 87: 82-97.

Soares JP, Santos JE, Chierice GO, Cavalheiro ETG. Thermal behavior of alginic acid and its sodium salt. Eclética Quimica. 2004; 29: 57-63.

Freire F.D., Aragão, C.F.S., de Lima e Moura, T.F.A. et al. Compatibility study between chlorpropamide and excipients in their physical mixtures. J Therm Anal Calorim. 2009; 97: 355. https://doi.org/10.1007/s10973-009-0258-2

Rus LM, Tomuta I, Iuga C, Maier C, Kacso I, Borodi G, Bratu I, Bojita M. Compatibility studies of indapamide/pharmaceutical excipients used in tablet reformulation. Farmacia. 2002; 60: 92-101.

Lima NGPB, Lima IPB, Barros DMC, Oliveira TS, Raffin FN, Moura TFA, Medeiros ACD, Gomes APB, Aragão CSF. Compatibility studies of trioxsalen with excipients by DSC, DTA, and FTIR. J Therm Anal Calorim 2014; 115: 2311-2318.

Wang Y, Luo YH, Zhao J, Sun BW. Selection of excipients for dispersible tablets of itraconazole through the application of thermal techniques and Raman spectroscopy. J Therm Anal Calorim. 2014; 115: 2391-2400.

Τeleginski LK, Maciel AB, Mendes C, Segatto Silva MA, Bernardi LS, Oliveira PR. Fluconazole – excipient compatibility studies as the first step in the development of formulation candidate for biowaiver. J Therm Anal Calorim. 2015; 120: 771-781.

Marian E, Jurca T, Kacso I, Borodi J, Rus LM, Bratu I. Compatibility study between simvastatin and excipients in their physical mixtures. Revistance de Chimie (Bucharest), 2015; 66: 803-807.

Chaves LL, Rolim LA, Gonçalves MLCM, Vieira ACC, Alves LDS, Soares MFR, Soares-Sobrinho JL, Lima MCA, Rolim-Neto PJ. Study of stability and drug-excipient compatibility of diethylcarbamazine citrate. J Therm Anal Calorim. 2013; 111: 2179-2186.

Lavor EP, Navarro MVM, Freire FD, Aragão CFS, RaffinFN, Barbosa EG, Moura TFA, Application of thermal analysis to the study of antituberculosis drugs-excipient compatibility. J Therm Anal Calorim. 2014; 115: 2303-2309.

GombÁs, Á., Szabó-Révész, P., Kata, M. et al. Quantitative Determination of Crystallinity of α-lactose monohydrate by DSC . J Therm Anal Calorim. 2002; 68: 503. https://doi.org/10.1023/A:1016039819247

Júlio TA, Zâmara IF, Garcia JS, Trevisan MG. Compatibility of sildenafil citrate and pharmaceutical excipients by thermal analysis and LC-UV. J Therm Anal Calorim. 2013; 111: 2037-2044.

Munavirov BV, Filippov AV, Rudakova MA, Antzutkin ON. Polyacrylic acid modifies local and lateral mobilities in lipid. membranes. J Dispers Sci technol..2014; 35:6, 848-858. doi:10.1080/01932691.2013.823096

Pires, S.A., Mussel, W.N., Oliveira, M.A. and Yoshida, M.I. Compatibility studies of ciprofibrate with excipients by DSC, XRPD, and FTIR. In: IX Congresso Brasileiro de AnáliseTérmica e Calorimetria. Serra Negra. 2014; 1 doi:10.13140/2.1.3578.4640 Conference: IX Brazilian Congress in Thermal Analysis and Calorimetry, At Serra Negra - São Paulo.

Li J, Zhao J, Tao L, Wang J, Waknis V, Pan D, Hubert M, Raghavan K. Patel J. the effect of polymeric excipients on the physical properties and performance of amorphous dispersions: Part I, Free volume and glass transition. Pharm Res. 2015; 32: 500-515.

Craig DQM. A review of thermal methods used for the analysis of the crystal form, solution thermodynamics and glass transition behaviour of polyethylene glycols. Thermochimica Acta. 1995; 248: 189-203.

Pielichowski K, Flejtuch K. Differential scanning calorimetry studies on poly(ethylene glycol) with different molecular weights for thermal energy storage materials. Polym Adv Technol. 2002 ;13: 690-696.

Seongok H, Chongyoup K, Dongsook K. Thermal degradation of poly(ethylene Glycol). Polym Degrad Stab. 1995; 47: 203-208.

Cássia R, Semaan FS. Thermal behavior of furosemide. J Therm Anal Calorim. 2013; 111: 1933-1937.

Kyrili A, Choutoulesi M, Pippa N, Meristoudi A, Pispas S, Demetzos C. Design and development of pH-sensitive liposomes by evaluating the thermotropic behavior of their chimeric bilayers. J Therm Anal Calorim. 2017; 127: 1381-1392.

Chen J, He C, Lin A, Xu F, Wang F, Zhao B, Liu X, Chen Z, Cai B. Brucine-loaded liposomes composed of HSPC and DPPC at different ratios: in vitro and in vivo evaluation. Drug Dev Ind Pharm. 2014; 40(2): 244-251.

Di Foggia M, Bonora S, Tinti A, Tugnoli V. DSC and Raman study of DMPC liposomes in presence of Ibuprofen at different pH. J Therm Anal Calorim. 2016; 127(2): 1407-1417. doi:10.1007/s10973-016-5408-8.

Pippa N, Gardikis K, Pispas S. Demetzos C. The physicochemical/thermodynamic balance of advanced drug liposomal delivery systems. J Therm Anal Calorim. 2014; 116: 99–105.