Preformulation: The use of FTIR in compatibility studies
Abstract
Studies of active pharmaceutical ingredient (API) - excipient compatibility represent an important study in the preformulation stage of the development of new dosage forms. The potential physical and chemical interactions between an API and the excipients can affect the chemical nature, the stability and bioavailability of the former and, consequently, its therapeutic efficacy and safety. Solid dosage forms are generally less stable than their API components. Despite the importance of API-excipient compatibility testing, there is no universally accepted protocol to assess such interactions. Fourier Transform Infrared Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), Isothermal Stress Testing-Fourier Transform Infrared Spectroscopy (IST-FT-IR), Isothermal Stress Testing-High Performance Liquid Chromatography (IST-HPLC), are commonly used as screening techniques for assessing the compatibility of an active pharmaceutical ingredient (API) with some currently employed excipients. Through the assignment of spectral bands, FTIR provides information on chemical reactions taking place between the API and the excipient. Thus, this procedure gives formulation scientists information on which chemical groups to avoid in the excipients, favoring the development of more stable blends.
Keywords:
Compatibility studies, Preformulation, Fourier Transform Infrared Spectroscopy, Differential Scanning Calorimetry, Isothermal Stress Testing-Fourier Transform Infrared Spectroscopy, Isothermal Stress Testing-High Performance Liquid Chromatography
Downloads
Download data is not yet available.
References
1. Bharate SS, Bharate SB, Bajaj AN: Interactions and incompatibilities of pharmaceutical excipients with active pharmaceutical ingredients: a comprehensive review. J. Excip. Food. Chem. 2010; 1:3-26.
2. Moyano MA, Broussalis AM, Segall A: Thermal analysis of lipoic acid and evaluation of the compatibility with excipients. J. Therm. Anal. Cal. 2010; 99: 631-637.
3. Ceresole R, Han Y, Rosasco MA, Orelli LR, Segall AI: Drug-excipient compatibility studies in binary mixtures of Avobenzone. J. Cosmet. Sci. 2013; 64: 317-328.
4. Chadha R, Bhandari S: Drug–excipient compatibility screening—Role of thermoanalytical and spectroscopic techniques J. Pharm. Biomed. Anal. 2014; 87: 82-97.
5. McDaid FM, Barker SA, Fitzpatrick S, Petts C, Craig DQM: Further investigations into the use of high sensitivity differential scanning calorimetry as a means of predicting drug–excipient interactions. Int. J. Pharm. 2003; 252:235-240.
6. O’Neill MA, Gaisford S: Application and use of isothermal calorimetry in pharmaceutical development. Int. J. Pharm. 2011; 417:83-93.
7. Ferraz Pinto M, Afonso de Moura E, Santos de Souza F, Oliveira Macêdo R:Thermal compatibility studies of nitroimidazoles and excipients. J. Therm. Anal. Cal. 2010; 102:323-329.
8. Oliveira Santos AF, Basilio Jr ID, Souza FS,Medeiros AFD, Ferraz Pinto M, de Santana DP: Application of thermal analysis of binary mixtures with metformin. J. Therm. Anal. Cal. 2008; 93:361-364.
9. Chou YP, Huang JY, Tseng JM, Cheng Y, Shu CM: Reaction hazard analysis for the thermal decomposition of cumene hydroperoxide in the presence of sodium hydroxide. J. Therm. Anal. Cal. 2008; 93:275-280.
10. Sashima ES, Janowska G, Zaborski M, Vnuchkin AV: Compatibility of fibroin/chitosan and fibroin/cellulose blends by thermal analysis. J. Therm. Anal. Cal. 2007; 89:887-891.
11. Medeiros AFD, Santos AFO, de Souza FS, Júnior IDB, Valdilȃnio J, Procópio JVV, de Santana DP, Macêdo RO: Thermal studies of pre-formulates of metronidazole obtained by spray drying technique. J. Therm. Anal. Cal. 2007; 89: 775-781.
12. Silva MAS, Kelmann RG, Foppa T, Cruz AP, Bertol CD Sartori T, Granada A, Carmignan F, Murakami FS: Thermoanalytical study of fluoxetine hydrochloride. J. Therm. Anal. Cal. 2007; 87:463-467.
13. Lira AM, Araújo AAS, Basílio IDJ, Santos BLL, Santana DP, Macêdo RO:Compatibility studies of lapachol with pharmaceutical excipients for the development of topical formulations. Thermochim. Acta. 2007; 457:1-6.
14. Mura P, Furlanetto S, Cirri M, Maestrelli F, Marras AM, Pinzauti S:Optimization of glibenclamide tablet composition through the combined use of differential scanning calorimetry and d-optimal mixture experimental design. J. Pharm. Biomed. Anal. 2005; 37:65-71.
15. Araújo AAS, Storpirtis S, Mercuri LP, Carvalho FMS, dos Santos Filho M, Matos JR:Thermal analysis of the antirretroviral zidovudine (AZT) and evaluation of the compatibility with excipients used in solid dosage forms. Int. J. Pharm. 2003; 260: 303-314.
16. Matos APS, Costa JS, Boniatti J, Seiceira RC, Pitaluga Jr A, Oliveira DL, Visçosa AL, Holandino C: Compatibility study between diazepam and tablet excipients. J. Therm. Anal. Cal. 2017; 127:1675-1682.
17. Liltorp K, Larsen TG, Willumsen B, Holm R: Solid state compatibility studies with tablet excipients using non thermal methods. J. Pharm. Biomed. Anal. 2011; 55:424-428.
18. Verma RK, Garg S: Selection of excipients for extended release formulations of glipizide through drug–excipient compatibility testing. J. Pharm. Biomed. Anal. 2005; 38:633-644.
19. Verma RK, Garg S: Compatibility studies between isosorbide mononitrate and selected excipients used in the development of extended release formulations. J. Pharm. Biomed. Anal. 2004; 35:449-458.
20. Silva LAD, Teixeira FV, Serpa RC, Esteves NL, dos Santos RR, Lima EM, da Cunha-Filho MSS, de Souza Araújo AA, Taveira SF, Marreto RN: Evaluation of carvedilol compatibility with lipid excipients for the development of lipid-based drug delivery systems. J. Therm. Anal. Cal. 2016; 123:2337-2344.
21. Veiga A, Oliveira PR, Bernardi LS, Mendes C, Silva MAS, Sangoi MS, Janissek PR, Murakami FS: Solid-state compatibility studies of a drug without melting point. J. Therm. Anal. Cal. 2018;131:3201-3209.
22. 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 preformulation. Farmacia. 2012; 60:92-101.
23. Tomassetti M, Catalani A, Rossi V, Vecchio S: Thermal analysis study of the interactions between acetaminophen and excipients in solid dosage forms and in some binary mixtures. J. Pharm. Biomed. Anal. 2005; 35:949-955.
24. Ding T, Chen L, Zhai LH, Fu Y, Wang-Sun B: Compatibility study of rivaroxaban and its pharmaceutical excipients. J. Therm. Anal. Cal. 2017; 130: 1569-1573.
25. Pires SA, Mussel WN, Yoshida MI: Solid-state characterization and pharmaceutical compatibility between citalopram and excipients using thermal and non-thermal techniques. J. Therm. Anal. Cal. 2017; 127:535-542.
26. Joshi BV, Patil VB, Pokharkar VB: Compatibility studies between carbamazepine and tablet excipients using thermal and non-thermal methods. Drug Devel. Ind. Pharm. 2002; 28:687–694.
27. Stulzer HK, Rodrigues PO, Cardoso TM, Matos JSR, Silva MAS: Compatibility studies between captopril and pharmaceutical excipients used in tablets formulations. J. Therm. Anal. Cal. 2008; 9:323-328.
28. Reddy RA, Ramesh B. Kishan V: Drug-excipient interaction during formulation development in vitro and in vivo evaluation of gastroretentive drug delivery system for nizatidine. Int. J. Pharm. Sci. Nanotech. 2013; 6: 2281-2293.
29. Prathyusha CH, Murthy TEGK: Compatibility studies of Donepezil with different excipients by using HPLC and FTIR. J. Adv. Pharm. Tech. Res. 2013; 3:273-278.
30. Jangde R, Singh D: Compatibility studies of quercetin with pharmaceutical excipients used in the development of novel formulation. Research J. Pharm. and Tech. 2014; 7:1101-1105.
31. Tiwari SP, Vidyasagar G: Identification, characterization, and drug-excipient compatibility of diltiazem hydrochloride by physico-chemical techniques UK. J. Pharm. Biosci. 2014; 2:49-53.
32. Gupta A, Kar HK: Solid state compatibility studies of miconazole using thermal and spectroscopic methods. Adv. Anal. Chem. 2015; 5:51-55.
33. Khan MI, Madni A, Ahmad S, Khan A, Rehman M, Mahmood MA: ATR-FTIR based pre and post formulation compatibility studies for the design of niosomal drug delivery system containing nonionic amphiphiles and chondroprotective drug. J. Chem. Soc. Pak. 2015; 37:527-534.
34. da Silva EP, Pereira MAV, de Barros Lima IP, Barros Lima NGP, Barboza EG, Aragã CFS, Gomes APB: Compatibility study between atorvastatin and excipients using DSC and FTIR. J. Therm. Anal. Cal. 2016; 123:933-939.
35. Amir IM, Amir ME, Osama AA, Suzan A, Alaa IM: Investigation of drug–polymer compatibility using chemometric-assisted UV-Spectrophotometry. Pharmaceutics 2017; 9:1-13.
36. Canbay HS, Doğantürk M: Application of differential scanning calorimetry and Fourier Transform Infrared Spectroscopy to the study of metoprolol-excipient and lisinopril-excipient compatibility. Eurasian. J. Anal. Chem. 2018; 13:1-7.
37. Gomes EC de L, Mussel WN, Resende JM, Fialho SL, Barbosa J, Yoshida MI:Chemical interactions study of antiretroviral drugs efavirenz and lamivudine concerning the development of stable fixed-dose combination formulations for AIDS treatment. J. Braz. Chem. Soc. 2013; 24:573-579.
38. Monajjemzadeh F, Hassanzadeh D, Valizadeh H, Siahi-Shadbad MR, Mojarrad JS, Robertson TH, Roberts MS: Compatibility studies of acyclovir and lactose in physical mixtures and commercial tablets. Eur. J. Pharm. Biopharm. 2009; 73: 404-413.
39. Mura P, Manderioli A, Bramanti G, Furlanetto S, Pinzauti S: Utilization of differential scanning calorimetry as a screening technique to determine the compatibility of ketoprofen with excipients. Int. J. Pharm. 1995; 119:71-79.
40. Malan CEP, de Villiers MM, Lötter AP: Application of differential scanning calorimetry and high performance liquid chromatography to determine the effects of mixture composition and preparation during the evaluation of niclosamide-excipient compatibility. J. Pharm. Biomed. Anal. 1997; 15:549-557.
41. Daniel JSP, Veronez IP, Lopez Rodriguez L, Trevisan MG, García JS: Risperidone – Solid-state characterization and pharmaceutical compatibility using thermal and non-thermal techniques. Thermochim Acta. 2013; 568:148-155.
42. Lima NGPB, Lima IP., Barros DMC, Oliveira TS, Raffin FN, de Lima e Moura TFA, Medeiros ACD, Gomes APB, Aragão CFS:Compatibility studies of trioxsalen with excipients by DSC, DTA, and FTIR. J. Therm. Anal. Cal. 2014; 115: 2311-2318.
43. Rosasco MA, Bonafede SL, Faudone SN, Segall AI: Compatibility Study Between Tobramycin and Pharmaceutical Excipients Using Differential Scanning Calorimetry, FT-IR, DRX and HPLC. J. Therm. Anal. Cal. 2018; 134: 1929-1941.
44. Rojek B, Wesolowski M: Fourier transform infrared spectroscopy supported by multivariate statistics in compatibility study of atenolol with excipients. Vib. Spectrosc. 2016; 86:190–197.
45. de Barros Lima IP, Lima NPGB, Barros DMC, Oliveira TS, Barbosa EG, Gomes APB, Ferrari M, do Nascimento TG, AragãoCFS: Compatibility study of tretinoin with several pharmaceutical excipients by thermal and non-thermal techniques. J. Therm. Anal. Cal. 2015; 120:733-745.
2. Moyano MA, Broussalis AM, Segall A: Thermal analysis of lipoic acid and evaluation of the compatibility with excipients. J. Therm. Anal. Cal. 2010; 99: 631-637.
3. Ceresole R, Han Y, Rosasco MA, Orelli LR, Segall AI: Drug-excipient compatibility studies in binary mixtures of Avobenzone. J. Cosmet. Sci. 2013; 64: 317-328.
4. Chadha R, Bhandari S: Drug–excipient compatibility screening—Role of thermoanalytical and spectroscopic techniques J. Pharm. Biomed. Anal. 2014; 87: 82-97.
5. McDaid FM, Barker SA, Fitzpatrick S, Petts C, Craig DQM: Further investigations into the use of high sensitivity differential scanning calorimetry as a means of predicting drug–excipient interactions. Int. J. Pharm. 2003; 252:235-240.
6. O’Neill MA, Gaisford S: Application and use of isothermal calorimetry in pharmaceutical development. Int. J. Pharm. 2011; 417:83-93.
7. Ferraz Pinto M, Afonso de Moura E, Santos de Souza F, Oliveira Macêdo R:Thermal compatibility studies of nitroimidazoles and excipients. J. Therm. Anal. Cal. 2010; 102:323-329.
8. Oliveira Santos AF, Basilio Jr ID, Souza FS,Medeiros AFD, Ferraz Pinto M, de Santana DP: Application of thermal analysis of binary mixtures with metformin. J. Therm. Anal. Cal. 2008; 93:361-364.
9. Chou YP, Huang JY, Tseng JM, Cheng Y, Shu CM: Reaction hazard analysis for the thermal decomposition of cumene hydroperoxide in the presence of sodium hydroxide. J. Therm. Anal. Cal. 2008; 93:275-280.
10. Sashima ES, Janowska G, Zaborski M, Vnuchkin AV: Compatibility of fibroin/chitosan and fibroin/cellulose blends by thermal analysis. J. Therm. Anal. Cal. 2007; 89:887-891.
11. Medeiros AFD, Santos AFO, de Souza FS, Júnior IDB, Valdilȃnio J, Procópio JVV, de Santana DP, Macêdo RO: Thermal studies of pre-formulates of metronidazole obtained by spray drying technique. J. Therm. Anal. Cal. 2007; 89: 775-781.
12. Silva MAS, Kelmann RG, Foppa T, Cruz AP, Bertol CD Sartori T, Granada A, Carmignan F, Murakami FS: Thermoanalytical study of fluoxetine hydrochloride. J. Therm. Anal. Cal. 2007; 87:463-467.
13. Lira AM, Araújo AAS, Basílio IDJ, Santos BLL, Santana DP, Macêdo RO:Compatibility studies of lapachol with pharmaceutical excipients for the development of topical formulations. Thermochim. Acta. 2007; 457:1-6.
14. Mura P, Furlanetto S, Cirri M, Maestrelli F, Marras AM, Pinzauti S:Optimization of glibenclamide tablet composition through the combined use of differential scanning calorimetry and d-optimal mixture experimental design. J. Pharm. Biomed. Anal. 2005; 37:65-71.
15. Araújo AAS, Storpirtis S, Mercuri LP, Carvalho FMS, dos Santos Filho M, Matos JR:Thermal analysis of the antirretroviral zidovudine (AZT) and evaluation of the compatibility with excipients used in solid dosage forms. Int. J. Pharm. 2003; 260: 303-314.
16. Matos APS, Costa JS, Boniatti J, Seiceira RC, Pitaluga Jr A, Oliveira DL, Visçosa AL, Holandino C: Compatibility study between diazepam and tablet excipients. J. Therm. Anal. Cal. 2017; 127:1675-1682.
17. Liltorp K, Larsen TG, Willumsen B, Holm R: Solid state compatibility studies with tablet excipients using non thermal methods. J. Pharm. Biomed. Anal. 2011; 55:424-428.
18. Verma RK, Garg S: Selection of excipients for extended release formulations of glipizide through drug–excipient compatibility testing. J. Pharm. Biomed. Anal. 2005; 38:633-644.
19. Verma RK, Garg S: Compatibility studies between isosorbide mononitrate and selected excipients used in the development of extended release formulations. J. Pharm. Biomed. Anal. 2004; 35:449-458.
20. Silva LAD, Teixeira FV, Serpa RC, Esteves NL, dos Santos RR, Lima EM, da Cunha-Filho MSS, de Souza Araújo AA, Taveira SF, Marreto RN: Evaluation of carvedilol compatibility with lipid excipients for the development of lipid-based drug delivery systems. J. Therm. Anal. Cal. 2016; 123:2337-2344.
21. Veiga A, Oliveira PR, Bernardi LS, Mendes C, Silva MAS, Sangoi MS, Janissek PR, Murakami FS: Solid-state compatibility studies of a drug without melting point. J. Therm. Anal. Cal. 2018;131:3201-3209.
22. 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 preformulation. Farmacia. 2012; 60:92-101.
23. Tomassetti M, Catalani A, Rossi V, Vecchio S: Thermal analysis study of the interactions between acetaminophen and excipients in solid dosage forms and in some binary mixtures. J. Pharm. Biomed. Anal. 2005; 35:949-955.
24. Ding T, Chen L, Zhai LH, Fu Y, Wang-Sun B: Compatibility study of rivaroxaban and its pharmaceutical excipients. J. Therm. Anal. Cal. 2017; 130: 1569-1573.
25. Pires SA, Mussel WN, Yoshida MI: Solid-state characterization and pharmaceutical compatibility between citalopram and excipients using thermal and non-thermal techniques. J. Therm. Anal. Cal. 2017; 127:535-542.
26. Joshi BV, Patil VB, Pokharkar VB: Compatibility studies between carbamazepine and tablet excipients using thermal and non-thermal methods. Drug Devel. Ind. Pharm. 2002; 28:687–694.
27. Stulzer HK, Rodrigues PO, Cardoso TM, Matos JSR, Silva MAS: Compatibility studies between captopril and pharmaceutical excipients used in tablets formulations. J. Therm. Anal. Cal. 2008; 9:323-328.
28. Reddy RA, Ramesh B. Kishan V: Drug-excipient interaction during formulation development in vitro and in vivo evaluation of gastroretentive drug delivery system for nizatidine. Int. J. Pharm. Sci. Nanotech. 2013; 6: 2281-2293.
29. Prathyusha CH, Murthy TEGK: Compatibility studies of Donepezil with different excipients by using HPLC and FTIR. J. Adv. Pharm. Tech. Res. 2013; 3:273-278.
30. Jangde R, Singh D: Compatibility studies of quercetin with pharmaceutical excipients used in the development of novel formulation. Research J. Pharm. and Tech. 2014; 7:1101-1105.
31. Tiwari SP, Vidyasagar G: Identification, characterization, and drug-excipient compatibility of diltiazem hydrochloride by physico-chemical techniques UK. J. Pharm. Biosci. 2014; 2:49-53.
32. Gupta A, Kar HK: Solid state compatibility studies of miconazole using thermal and spectroscopic methods. Adv. Anal. Chem. 2015; 5:51-55.
33. Khan MI, Madni A, Ahmad S, Khan A, Rehman M, Mahmood MA: ATR-FTIR based pre and post formulation compatibility studies for the design of niosomal drug delivery system containing nonionic amphiphiles and chondroprotective drug. J. Chem. Soc. Pak. 2015; 37:527-534.
34. da Silva EP, Pereira MAV, de Barros Lima IP, Barros Lima NGP, Barboza EG, Aragã CFS, Gomes APB: Compatibility study between atorvastatin and excipients using DSC and FTIR. J. Therm. Anal. Cal. 2016; 123:933-939.
35. Amir IM, Amir ME, Osama AA, Suzan A, Alaa IM: Investigation of drug–polymer compatibility using chemometric-assisted UV-Spectrophotometry. Pharmaceutics 2017; 9:1-13.
36. Canbay HS, Doğantürk M: Application of differential scanning calorimetry and Fourier Transform Infrared Spectroscopy to the study of metoprolol-excipient and lisinopril-excipient compatibility. Eurasian. J. Anal. Chem. 2018; 13:1-7.
37. Gomes EC de L, Mussel WN, Resende JM, Fialho SL, Barbosa J, Yoshida MI:Chemical interactions study of antiretroviral drugs efavirenz and lamivudine concerning the development of stable fixed-dose combination formulations for AIDS treatment. J. Braz. Chem. Soc. 2013; 24:573-579.
38. Monajjemzadeh F, Hassanzadeh D, Valizadeh H, Siahi-Shadbad MR, Mojarrad JS, Robertson TH, Roberts MS: Compatibility studies of acyclovir and lactose in physical mixtures and commercial tablets. Eur. J. Pharm. Biopharm. 2009; 73: 404-413.
39. Mura P, Manderioli A, Bramanti G, Furlanetto S, Pinzauti S: Utilization of differential scanning calorimetry as a screening technique to determine the compatibility of ketoprofen with excipients. Int. J. Pharm. 1995; 119:71-79.
40. Malan CEP, de Villiers MM, Lötter AP: Application of differential scanning calorimetry and high performance liquid chromatography to determine the effects of mixture composition and preparation during the evaluation of niclosamide-excipient compatibility. J. Pharm. Biomed. Anal. 1997; 15:549-557.
41. Daniel JSP, Veronez IP, Lopez Rodriguez L, Trevisan MG, García JS: Risperidone – Solid-state characterization and pharmaceutical compatibility using thermal and non-thermal techniques. Thermochim Acta. 2013; 568:148-155.
42. Lima NGPB, Lima IP., Barros DMC, Oliveira TS, Raffin FN, de Lima e Moura TFA, Medeiros ACD, Gomes APB, Aragão CFS:Compatibility studies of trioxsalen with excipients by DSC, DTA, and FTIR. J. Therm. Anal. Cal. 2014; 115: 2311-2318.
43. Rosasco MA, Bonafede SL, Faudone SN, Segall AI: Compatibility Study Between Tobramycin and Pharmaceutical Excipients Using Differential Scanning Calorimetry, FT-IR, DRX and HPLC. J. Therm. Anal. Cal. 2018; 134: 1929-1941.
44. Rojek B, Wesolowski M: Fourier transform infrared spectroscopy supported by multivariate statistics in compatibility study of atenolol with excipients. Vib. Spectrosc. 2016; 86:190–197.
45. de Barros Lima IP, Lima NPGB, Barros DMC, Oliveira TS, Barbosa EG, Gomes APB, Ferrari M, do Nascimento TG, AragãoCFS: Compatibility study of tretinoin with several pharmaceutical excipients by thermal and non-thermal techniques. J. Therm. Anal. Cal. 2015; 120:733-745.
Published
30/09/2019
Statistics
28 Views | 30 Downloads
Citatons
How to Cite
Segall, A. I. (2019). Preformulation: The use of FTIR in compatibility studies. Journal of Innovations in Applied Pharmaceutical Science (JIAPS), 4(3), 01-06. Retrieved from https://www.saap.org.in/journals/index.php/jiaps/article/view/198
Issue
Section
Review Article(S)
Copyright © Author(s) retain the copyright of this article.
.