Research Article
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Year 2025, Volume: 29 Issue: 3, 1256 - 1264, 04.06.2025

Emine Betül Kadıoğlu , Oya Kerimoğlu

https://doi.org/10.12991/jrespharm.1624425

Abstract

References

  • [1] Larochelle P, Tobe SW, Lacourcière Y. β-Blockers in hypertension: studies and meta-analyses over the years. Can J Cardiol. 2014;30(5 Suppl):S16-22. http://dx.doi.org/10.1016/j.cjca.2014.02.012
  • [2] Lin ZP, Dong M, Liu J. Bisoprolol improved endothelial function and myocardium survival of hypertension with stable angina: a randomized double-blinded trial. Eur Rev Med Pharmacol Sci. 2013;17(6): 794-801.
  • [3] Metra M, Nodari S, Bordonali T, Milani P, Lombardi C, Bugatti S, Dei Cas L. Bisoprolol in the treatment of chronic heart failure: from pathophysiology to clinical pharmacology and trial results. Ther Clin Risk Manag. 2007;3(4):569-578.
  • [4] Poldermans D, Boersma E, Bax JJ, Thomson IR, Paelinck B, Van de Ven LLM, Roelandt JRTC. Bisoprolol reduces cardiac death and myocardial infarction in high-risk patients as long as 2 years after successful major vascular surgery. Eur Heart J. 2001; 22(15): 1353-1358. https://doi.org/10.1053/euhj.2000.2555
  • [5] Saini-Chohan HK, Hatch GM. Biological actions and metabolism of currently used pharmacological agents for the treatment of congestive heart failure. Curr Drug Metabo. 2009; 10(3): 206-219. https://doi.org/10.2174/138920009787846314
  • [6] Ahad A, Al-Jenoobi FI, Al-Mohizea AM, Akhtar N, Raish M, Aqil M. Systemic delivery of β-blockers via transdermal route for hypertension. Saudi Pharm J. 2015; 23(6): 587-602. http://dx.doi.org/10.1016/j.jsps.2013.12.019
  • [7] Panainte AD, Gafitanu C, Stoleriu I, Tarțău LM, Popescu MC, Lisa G, Popa EG. New modified release tablets of bisoprolol fumarate for the treatment of hypertension: characterization and in vitro evaluation. J Drug Deliv Sci Technol. 2019; 50: 402-409. https://doi.org/10.1016/j.jddst.2018.11.011
  • [8] Lee Y, Kim K, Kim M, Choi DH, Jeong SH. Orally disintegrating films focusing on formulation, manufacturing process and characterization. J Pharm Invest. 2017; 47(3): 183–201. https://doi.org/10.1007/s40005-017-0311-2 [9] Borges AF, Silva C, Coelho JF, Simões S. Oral films: Current status and future perspectives: I- Galenical development and quality attributes. J Control Release. 2015; 206:1–19. https://doi.org/10.1016/j.jconrel.2015.03.006
  • [10] Charoo NA, Shamsher AA, Lian LY, Abrahamsson B, Cristofoletti R, Groot DW, Dressman J. Biowaiver monograph for immediate-release solid oral dosage forms: bisoprolol fumarate. J Pharm Sci. 2014; 103(2): 378-391. https://doi.org/10.1002/jps.23817
  • [11] Irfan M, Rabel S, Bukhtar Q, Qadir MI, Jabeen F, Khan A. Orally disintegrating films: a modern expansion in drug delivery system. Saudi Pharm J. 2016; 24(5): 537–546. https://doi.org/10.1016/j.jsps.2015.02.024
  • [12] Mayerhöfer TG, Pipa AV, Popp J. Beer's Law-Why Integrated Absorbance Depends Linearly on Concentration. Chemphyschem. 2019;20(21):2748-2753. https://doi.org/10.1002/cphc.201900787
  • [13] Shakar AAM, Hossain MJ, Kayesh R, Rahman A, Sultan MZ. Incompatibility of Bisoprolol Fumarate with Some Super-disintegrating Agents. J Pharm Res Int. 2014; 5(2): 137–145. https://doi.org/10.9734/BJPR/2015/13956
  • [14] Dixit RP, Puthli SP. Oral strip technology: overview and future potential. J Control Release. 2009; 139(2): 94–107. https://doi.org/10.1016/j.jconrel.2009.06.014
  • [15] Nagaraju T, Gowthami R, Rajashekar M, Sandeep S, Mallesham M, Sathish D, Kumar YS. Comprehensive review on oral disintegrating films. Curr Drug Deliv. 2013; 10(1): 96–108. https://doi.org/10.2174/1567201811310010016
  • [16] Özen, MI. Master’s Thesis. Preparation and evaluation of orally disintegrating films containing donepezil hydrochloride. Department of Pharmaceutical Technology, Faculty of Pharmacy, Marmara University, Başıbüyük, İstanbul, Türkiye, 2023.
  • [17] Zhang L, Aloia M, Pielecha-Safira B, Lin H, Rajai PM, Kunnath K, Davé RN. Impact of superdisintegrants and film thickness on disintegration time of strip films loaded with poorly water-soluble drug microparticles. J Pharm Sci. 2018; 107(8): 2107–2118. https://doi.org/10.1016/j.xphs.2018.04.006
  • [18] Visser JC, Dohmen WM, Hinrichs WL, Breitkreutz J, Frijlink HW, Woerdenbag HJ. Quality by design approach for optimizing the formulation and physical properties of extemporaneously prepared orodispersible films. Int J Pharm. 2015; 485(1-2): 70-76. https://doi.org/10.1016/j.ijpharm.2015.03.005
  • [19] Gökay Y. Master’s Thesis. Preparation and evaluation of orally dispersing films containing verapamil hydrochloride. Department of Pharmaceutical Technology, Faculty of Pharmacy, Marmara University, Haydarpaşa, İstanbul, Türkiye, 2020.
  • [20] Özen MI, Kerimoğlu O. Evaluation and characterization of orally disintegrating films loaded donepezil hydrochloride for Alzheimer’s disease. J Res Pharm. 2023; 27(2):893-902. http://dx.doi.org/10.29228/jrp.369
  • [21] Baranowski P, Karolewicz B, Gajda M, Pluta J. Ophthalmic drug dosage forms: characterisation and research methods. Sci World J. 2014; (1): 861904. https://doi.org/10.1155/2014/861904
  • [22] Karki S, Kim H, Na SJ, Shin D, Jo K, Lee J. Thin films as an emerging platform for drug delivery. Asian J Pharm Sci. 2016; 11(5): 559-574. https://doi.org/10.1016/j.ajps.2016.05.004
  • [23] Bala, R., Pawar, P., Khanna, S., Arora, S. Orally dissolving strips: A new approach to oral drug delivery system. Int J Pharm Invest. 2013; 3(2): 67–76. https://doi.org/10.4103/2230-973X.114897
  • [24] Kapadia YD, Trambadiya DA, Patel AV, Patel VP. Formulation and Evaluation of Fast Dissolving Sublingual Film of Metoprolol Succinate. Pharma Science Monitor. 2013; 3(3): 140–154.
  • [25] Manohara C, Sanganal S, Prem KG, Swamy KB, Phani AR. Improved Dissolution Rate of Piroxicam by Fusion Solid Dispersion Technique. Sci Technol Arts Res J. 2014; 3: 44-47. http://dx.doi.org/10.4314/star.v3i1.8
  • [26] Bánfai B, Ganzler K, Kemény S. Content uniformity and assay requirements in current regulations. J Chromatogr A. 2007; 1156(1-2): 206-212. https://doi.org/10.1016/j.chroma.2006.10.067
  • [27] European Pharmacopoeia, 2.9.6. Uniformity of Content of Single-Dose Preparations, seventh ed., France, Council of Europe, 2011.
  • [28] Alaei S, Omidian H. Mucoadhesion and Mechanical Assessment of Oral Films. Eur J Pharm Sci. 2021; 159: 105727. https://doi.org/10.1016/j.ejps.2021.105727 .
  • [29] Alopaeus JF, Hellfritzsch M, Gutowski T, Scherließ R, Almeida A, Sarmento B, Škalko-Basnet N, Tho I. Mucoadhesive buccal films based on a graft co-polymer–A mucin-retentive hydrogel scaffold. Eur J Pharm Sci. 2020; 142: 105142. https://doi.org/10.1016/j.ejps.2019.105142 .
  • [30] European Pharmacopoeia, 4.1.3. Buffer Solutions, seventh ed., France, Council of Europe, 2011.
  • [31] Rathod AC, Dudhe AR, Gajare KH. Development of Analytical Technique for Dichlofenac Sodium and Ibuprofen Utilizing UV Visible Spectroscopy and AUC Method. Int J Multidisc Res. 2023 5(2): IJFMR23022570. https://doi.org/10.36948/ijfmr.2023.v05i02.2570.
  • [32] Kumari B, Khansili A. Analytical method development and validation of UV-visible spectrophotometric method for the estimation of vildagliptin in gastric medium. Drug Res (Stuttgart). 2020; 70(9): 417-423. https://doi.org/10.1055/a-1217-0296.
  • [33] Mishra P. Development and validation of Q-absorbance ratio UV spectrophotometric method for simultaneous determination of bisoprolol fumarate and cilnidipine in marketed formulation Besicor C5. Asian J Pharm. 2022; 16(3). https://doi.org/10.22377/ajp.v16i3.4484.
  • [34] Verma M, Pandey S, Gidwani B, Pandey RK, Shukla SS. Bisoprolol Fumarate: An Exploration on its Properties and Analytical Methods. Palestinian Med Pharm J. 2024; 9(4): 6. https://doi.org/10.59049/2790-0231.1272

Preparation and characterization of disintegrating film formulations containing bisoprolol fumarate for the treatment of hypertension

Year 2025, Volume: 29 Issue: 3, 1256 - 1264, 04.06.2025

Emine Betül Kadıoğlu , Oya Kerimoğlu

https://doi.org/10.12991/jrespharm.1624425

Abstract

Since oral administration is the most preferred route of drug administration, innovative and effective oral pharmaceutical dosage forms are being investigated. Among these new pharmaceutical forms, orally disintegrating films (ODFs) play an important role. This study aims to create optimum ODF formulations containing bisoprolol fumarate using solvent casting method. While pullulan and lycoat were used as polymers in the structure of the films, plasticizers such as polyethylene glycol 400 (PEG-400) and glycerin were used to provide flexibility. Characterization studies on the obtained films are determination of morphological characteristics, folding determination, thickness determination, determination of swelling behaviour, determination of disintegration time, in vitro release determination, mass uniformity determination, determination of content uniformity, tensile strength, elastic modulus and elongation percentage determinations. UV-Vis spectroscopy studies were performed to confirm bisoprolol fumarate. The complete disintegration time for the F-14 films with optimum characteristics was found to be 38 seconds on average in the petri dish method and 16 seconds on average using the dispersion time analyzer. These values revealed that pullulan polymer exhibited better film-forming capacity when used in close amounts with lycoate polymer. ODFs containing bisoprolol fumarate have provided an effective, safe, innovative and easy to use treatment for hypertension.

Keywords

orally disintegration films bisoprolol fumarate pullulan lycoat

Supporting Institution

Marmara University Health Sciences Institute

Thanks

The authors are thankful to Prof. Dr. Timuçin Uğurlu for supplying Bisoprolol fumarate and other excipients. Authors are also thankful to Ali Raif Pharmaceutical Industry Co., Ltd. for supplying pullulan and lycoat.

References

  • [1] Larochelle P, Tobe SW, Lacourcière Y. β-Blockers in hypertension: studies and meta-analyses over the years. Can J Cardiol. 2014;30(5 Suppl):S16-22. http://dx.doi.org/10.1016/j.cjca.2014.02.012
  • [2] Lin ZP, Dong M, Liu J. Bisoprolol improved endothelial function and myocardium survival of hypertension with stable angina: a randomized double-blinded trial. Eur Rev Med Pharmacol Sci. 2013;17(6): 794-801.
  • [3] Metra M, Nodari S, Bordonali T, Milani P, Lombardi C, Bugatti S, Dei Cas L. Bisoprolol in the treatment of chronic heart failure: from pathophysiology to clinical pharmacology and trial results. Ther Clin Risk Manag. 2007;3(4):569-578.
  • [4] Poldermans D, Boersma E, Bax JJ, Thomson IR, Paelinck B, Van de Ven LLM, Roelandt JRTC. Bisoprolol reduces cardiac death and myocardial infarction in high-risk patients as long as 2 years after successful major vascular surgery. Eur Heart J. 2001; 22(15): 1353-1358. https://doi.org/10.1053/euhj.2000.2555
  • [5] Saini-Chohan HK, Hatch GM. Biological actions and metabolism of currently used pharmacological agents for the treatment of congestive heart failure. Curr Drug Metabo. 2009; 10(3): 206-219. https://doi.org/10.2174/138920009787846314
  • [6] Ahad A, Al-Jenoobi FI, Al-Mohizea AM, Akhtar N, Raish M, Aqil M. Systemic delivery of β-blockers via transdermal route for hypertension. Saudi Pharm J. 2015; 23(6): 587-602. http://dx.doi.org/10.1016/j.jsps.2013.12.019
  • [7] Panainte AD, Gafitanu C, Stoleriu I, Tarțău LM, Popescu MC, Lisa G, Popa EG. New modified release tablets of bisoprolol fumarate for the treatment of hypertension: characterization and in vitro evaluation. J Drug Deliv Sci Technol. 2019; 50: 402-409. https://doi.org/10.1016/j.jddst.2018.11.011
  • [8] Lee Y, Kim K, Kim M, Choi DH, Jeong SH. Orally disintegrating films focusing on formulation, manufacturing process and characterization. J Pharm Invest. 2017; 47(3): 183–201. https://doi.org/10.1007/s40005-017-0311-2 [9] Borges AF, Silva C, Coelho JF, Simões S. Oral films: Current status and future perspectives: I- Galenical development and quality attributes. J Control Release. 2015; 206:1–19. https://doi.org/10.1016/j.jconrel.2015.03.006
  • [10] Charoo NA, Shamsher AA, Lian LY, Abrahamsson B, Cristofoletti R, Groot DW, Dressman J. Biowaiver monograph for immediate-release solid oral dosage forms: bisoprolol fumarate. J Pharm Sci. 2014; 103(2): 378-391. https://doi.org/10.1002/jps.23817
  • [11] Irfan M, Rabel S, Bukhtar Q, Qadir MI, Jabeen F, Khan A. Orally disintegrating films: a modern expansion in drug delivery system. Saudi Pharm J. 2016; 24(5): 537–546. https://doi.org/10.1016/j.jsps.2015.02.024
  • [12] Mayerhöfer TG, Pipa AV, Popp J. Beer's Law-Why Integrated Absorbance Depends Linearly on Concentration. Chemphyschem. 2019;20(21):2748-2753. https://doi.org/10.1002/cphc.201900787
  • [13] Shakar AAM, Hossain MJ, Kayesh R, Rahman A, Sultan MZ. Incompatibility of Bisoprolol Fumarate with Some Super-disintegrating Agents. J Pharm Res Int. 2014; 5(2): 137–145. https://doi.org/10.9734/BJPR/2015/13956
  • [14] Dixit RP, Puthli SP. Oral strip technology: overview and future potential. J Control Release. 2009; 139(2): 94–107. https://doi.org/10.1016/j.jconrel.2009.06.014
  • [15] Nagaraju T, Gowthami R, Rajashekar M, Sandeep S, Mallesham M, Sathish D, Kumar YS. Comprehensive review on oral disintegrating films. Curr Drug Deliv. 2013; 10(1): 96–108. https://doi.org/10.2174/1567201811310010016
  • [16] Özen, MI. Master’s Thesis. Preparation and evaluation of orally disintegrating films containing donepezil hydrochloride. Department of Pharmaceutical Technology, Faculty of Pharmacy, Marmara University, Başıbüyük, İstanbul, Türkiye, 2023.
  • [17] Zhang L, Aloia M, Pielecha-Safira B, Lin H, Rajai PM, Kunnath K, Davé RN. Impact of superdisintegrants and film thickness on disintegration time of strip films loaded with poorly water-soluble drug microparticles. J Pharm Sci. 2018; 107(8): 2107–2118. https://doi.org/10.1016/j.xphs.2018.04.006
  • [18] Visser JC, Dohmen WM, Hinrichs WL, Breitkreutz J, Frijlink HW, Woerdenbag HJ. Quality by design approach for optimizing the formulation and physical properties of extemporaneously prepared orodispersible films. Int J Pharm. 2015; 485(1-2): 70-76. https://doi.org/10.1016/j.ijpharm.2015.03.005
  • [19] Gökay Y. Master’s Thesis. Preparation and evaluation of orally dispersing films containing verapamil hydrochloride. Department of Pharmaceutical Technology, Faculty of Pharmacy, Marmara University, Haydarpaşa, İstanbul, Türkiye, 2020.
  • [20] Özen MI, Kerimoğlu O. Evaluation and characterization of orally disintegrating films loaded donepezil hydrochloride for Alzheimer’s disease. J Res Pharm. 2023; 27(2):893-902. http://dx.doi.org/10.29228/jrp.369
  • [21] Baranowski P, Karolewicz B, Gajda M, Pluta J. Ophthalmic drug dosage forms: characterisation and research methods. Sci World J. 2014; (1): 861904. https://doi.org/10.1155/2014/861904
  • [22] Karki S, Kim H, Na SJ, Shin D, Jo K, Lee J. Thin films as an emerging platform for drug delivery. Asian J Pharm Sci. 2016; 11(5): 559-574. https://doi.org/10.1016/j.ajps.2016.05.004
  • [23] Bala, R., Pawar, P., Khanna, S., Arora, S. Orally dissolving strips: A new approach to oral drug delivery system. Int J Pharm Invest. 2013; 3(2): 67–76. https://doi.org/10.4103/2230-973X.114897
  • [24] Kapadia YD, Trambadiya DA, Patel AV, Patel VP. Formulation and Evaluation of Fast Dissolving Sublingual Film of Metoprolol Succinate. Pharma Science Monitor. 2013; 3(3): 140–154.
  • [25] Manohara C, Sanganal S, Prem KG, Swamy KB, Phani AR. Improved Dissolution Rate of Piroxicam by Fusion Solid Dispersion Technique. Sci Technol Arts Res J. 2014; 3: 44-47. http://dx.doi.org/10.4314/star.v3i1.8
  • [26] Bánfai B, Ganzler K, Kemény S. Content uniformity and assay requirements in current regulations. J Chromatogr A. 2007; 1156(1-2): 206-212. https://doi.org/10.1016/j.chroma.2006.10.067
  • [27] European Pharmacopoeia, 2.9.6. Uniformity of Content of Single-Dose Preparations, seventh ed., France, Council of Europe, 2011.
  • [28] Alaei S, Omidian H. Mucoadhesion and Mechanical Assessment of Oral Films. Eur J Pharm Sci. 2021; 159: 105727. https://doi.org/10.1016/j.ejps.2021.105727 .
  • [29] Alopaeus JF, Hellfritzsch M, Gutowski T, Scherließ R, Almeida A, Sarmento B, Škalko-Basnet N, Tho I. Mucoadhesive buccal films based on a graft co-polymer–A mucin-retentive hydrogel scaffold. Eur J Pharm Sci. 2020; 142: 105142. https://doi.org/10.1016/j.ejps.2019.105142 .
  • [30] European Pharmacopoeia, 4.1.3. Buffer Solutions, seventh ed., France, Council of Europe, 2011.
  • [31] Rathod AC, Dudhe AR, Gajare KH. Development of Analytical Technique for Dichlofenac Sodium and Ibuprofen Utilizing UV Visible Spectroscopy and AUC Method. Int J Multidisc Res. 2023 5(2): IJFMR23022570. https://doi.org/10.36948/ijfmr.2023.v05i02.2570.
  • [32] Kumari B, Khansili A. Analytical method development and validation of UV-visible spectrophotometric method for the estimation of vildagliptin in gastric medium. Drug Res (Stuttgart). 2020; 70(9): 417-423. https://doi.org/10.1055/a-1217-0296.
  • [33] Mishra P. Development and validation of Q-absorbance ratio UV spectrophotometric method for simultaneous determination of bisoprolol fumarate and cilnidipine in marketed formulation Besicor C5. Asian J Pharm. 2022; 16(3). https://doi.org/10.22377/ajp.v16i3.4484.
  • [34] Verma M, Pandey S, Gidwani B, Pandey RK, Shukla SS. Bisoprolol Fumarate: An Exploration on its Properties and Analytical Methods. Palestinian Med Pharm J. 2024; 9(4): 6. https://doi.org/10.59049/2790-0231.1272
There are 33 citations in total.

Details

Primary Language English
Subjects Pharmaceutical Sciences, Pharmacology and Pharmaceutical Sciences (Other)
Journal Section Articles
Authors

Emine Betül Kadıoğlu 0009-0003-5230-0427

Oya Kerimoğlu 0000-0003-2619-0490

Publication Date June 4, 2025
Submission Date January 21, 2025
Acceptance Date March 26, 2025
Published in Issue Year 2025 Volume: 29 Issue: 3

Cite

APA Kadıoğlu, E. B., & Kerimoğlu, O. (2025). Preparation and characterization of disintegrating film formulations containing bisoprolol fumarate for the treatment of hypertension. Journal of Research in Pharmacy, 29(3), 1256-1264. https://doi.org/10.12991/jrespharm.1624425
AMA Kadıoğlu EB, Kerimoğlu O. Preparation and characterization of disintegrating film formulations containing bisoprolol fumarate for the treatment of hypertension. J. Res. Pharm. June 2025;29(3):1256-1264. doi:10.12991/jrespharm.1624425
Chicago Kadıoğlu, Emine Betül, and Oya Kerimoğlu. “Preparation and Characterization of Disintegrating Film Formulations Containing Bisoprolol Fumarate for the Treatment of Hypertension”. Journal of Research in Pharmacy 29, no. 3 (June 2025): 1256-64. https://doi.org/10.12991/jrespharm.1624425.
EndNote Kadıoğlu EB, Kerimoğlu O (June 1, 2025) Preparation and characterization of disintegrating film formulations containing bisoprolol fumarate for the treatment of hypertension. Journal of Research in Pharmacy 29 3 1256–1264.
IEEE E. B. Kadıoğlu and O. Kerimoğlu, “Preparation and characterization of disintegrating film formulations containing bisoprolol fumarate for the treatment of hypertension”, J. Res. Pharm., vol. 29, no. 3, pp. 1256–1264, 2025, doi: 10.12991/jrespharm.1624425.
ISNAD Kadıoğlu, Emine Betül - Kerimoğlu, Oya. “Preparation and Characterization of Disintegrating Film Formulations Containing Bisoprolol Fumarate for the Treatment of Hypertension”. Journal of Research in Pharmacy 29/3 (June 2025), 1256-1264. https://doi.org/10.12991/jrespharm.1624425.
JAMA Kadıoğlu EB, Kerimoğlu O. Preparation and characterization of disintegrating film formulations containing bisoprolol fumarate for the treatment of hypertension. J. Res. Pharm. 2025;29:1256–1264.
MLA Kadıoğlu, Emine Betül and Oya Kerimoğlu. “Preparation and Characterization of Disintegrating Film Formulations Containing Bisoprolol Fumarate for the Treatment of Hypertension”. Journal of Research in Pharmacy, vol. 29, no. 3, 2025, pp. 1256-64, doi:10.12991/jrespharm.1624425.
Vancouver Kadıoğlu EB, Kerimoğlu O. Preparation and characterization of disintegrating film formulations containing bisoprolol fumarate for the treatment of hypertension. J. Res. Pharm. 2025;29(3):1256-64.