Preparation and Evaluation of Telmisartan Solid Dispersion as Sublingual Tablets
DOI:
https://doi.org/10.32007/jfacmedbagdad.2145Keywords:
Solid dispersion, Soluplus, Sublingual tablet, Potassium carbonate, TelmisartanAbstract
Background: Telmisartan is an antihypertensive angiotensin II receptor antagonist drug commonly used to treat hypertension and renal disease. Based on the Biopharmaceutical Classification System, it’s a Class II poorly soluble drug.
Objective: To prepare a sublingual tablet by increasing the dissolution and solubility of Telmisartan utilising the solid dispersion method.
Methods: Three methods were obtained to prepare the solid dispersion of telmisartan: solvent evaporation, kneading, and microwave method. Each method uses soluplus as a hydrophilic carrier in different ratios of 1%, 2%, and 3%. Preparation of ternary solid dispersion by adding potassium carbonate salt to the binary solid dispersion. After that, the preparation of the sublingual tablets was done by applying a direct compression method, using different types and ratios of super disintegrants such as crospovidone, croscarmellose, and sodium starch glycolate in 5% and 10%.
Study the evaluation tests of sublingual tablets, such as friability, hardness, disintegration time, and dissolution time.
Results: The solid dispersion showed an improvement in solubility over the pure medication. The best result was obtained with the formula (Telmisartan, Soluplus, and K2CO3 salt at a 1:1:0.3 ratio) prepared by the microwave method. In this method and the high ratio of soluplus, the solubility increased more than in the solvent evaporation and kneading methods. The selected tablet is prepared using crospovidone 10% as a super disintegrant that appears disintegration time in 5 seconds and releases in 1 min in dissolution media.
Conclusion: The solubility and dissolution of Telmisartan were improved by microwave-based ternary solid dispersion using hydrophilic carriers and salt in a ratio of 1:1:0.3 (drug: carrier: salt). The analysis exerts the increases in wettability, enhanced solubility, and dissolution due to conversion from crystal to amorphous state.
Received May. 2023
Revised: July 2023
Accepted Aug. 2023
Published Jan. 2024
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References
1. Savjani KT, Gajjar AK, Savjani JK. Drug solubility: importance and enhancement techniques. ISRN. 2012. https://doi.org/10.5402/2012/195727.
2. Abdulqader AA, Al-Khedairy EB. Formulation and valuation of fast dissolving tablets of taste-masked ondansetron hydrochloride by solid /dispersion. IJPS. 2017;26(1):50-60. https://doi.org/10.31351/vol26iss1pp50-60.
3. Ismail MY, Ghareeb MM. Enhancement of the solubility a10.5530/srp.2020.3.29nd dissolution rate of rebamipide by using solid dispersion technique (Part I). IJPS. 2018:55-65. https://doi.org/10.31351/vol27iss2pp55-65.
4. Alkufi HK, Kassab HJ. Formulation and evaluation of sustained release sumatriptan mucoadhesive intranasal in-situ gel. IJPS. 2019;28(2):95-104. https://doi.org/10.31351/vol28iss2pp95-104.
5. Sabri LA, Hussien AA. Formulation and In-Vitro Characterization of Solidified Nebivolol Self-Nanoemulsion using Liquisolid Technique. Sys Rev Pharm..2020;11 (3). https://doi.org/10.5530/srp.2020.3.29.
6. Ahmed KK, Al-Jumaili AA, Mutlak SH, Hadi MK. Determinants of national drug products acceptance across patients, pharmacists, and manufacturers: A mixed method study. JGM. 2021;17(3):139-153. https://doi.org/10.1177/1741134320926625.
7. Yas LS. Effects of hypertension with and without smoking on salivary electrolytes concentration. JFacMed Baghdad. 2023;65(1).59-64. https://doi.org/10.32007/jfacmedbagdad.6512046.
8. Destro M, Cagnoni F, Dognini GP, Galimberti V, Taietti C, Cavalleri C, Galli E. Telmisartan: just an antihypertensive agent? A literature review. Expert opinion on pharmacotherapy. 2011;12(17):2719-35. https://doi.org/10.1517/14656566.2011.632367.
9. Zou Z, Xi GL, Yuan HB, Zhu QF, Shi XY. Telmisartan versus angiotensin-converting enzyme inhibitors in the treatment of hypertension: a meta-analysis of randomized controlled trials. JHH. 2009;23(5):339- 49. https://doi.org/10.1038/jhh.2008.132.
10. Kadam S, Boppana SS, Manna S, Datta S, Karande S. Management of hypertension: Comparison of Telmisartan with other antihypertensive drugs. MEDRECH. 2022;9(2):88-93. https://doi.org/10.26838/MEDRECH.2022.9.2.584.
11. Al-Akayleh F, Al-Naji I, Adwan S, Al-Remawi M, Shubair M. Enhancement of curcumin solubility using a novel solubilizing polymer Soluplus®. JPI. 2022; 17:142-154. https://doi.org/10.1007/s12247-020-09500-x.
12. Prajapati ST, Patel MV, Patel CN. Preparation and evaluation of sublingual tablets of zolmitriptan. Int J Pharm Investig. 2014 Jan;4(1):27-31. https://doi.org/10.4103/2230-973X.127737.
13. Aghera NJ, Shah SD, Vadalia KR. Formulation and evaluation of sublingual tablets of Losartan potassium. Asian Pacific J TroP. Dis. 2012;2:S130-5. https://doi.org/10.1016/S2222-1808(12)60138-8.
14. Toma NM, Khalil YI. Formulation and evaluation of bilayer tablets containing immediate release aspirin layer and floating clopidogrel layer. IJPS. 2013;22(1):40-9. https://doi.org/10.31351/vol22iss1pp40-49.
15. Alkhalidi MM, Jawad FJ. Enhancement of Aqueous Solubility and Dissolution Rate of Etoricoxib by Solid Dispersion Technique. IJPS. 2020;29(1):76-87. https://doi.org/10.31351/vol29iss1pp76-87.
16. Prajapati ST, Patel MV, Patel CN. Preparation and evaluation of sublingual tablets of zolmitriptan. Int J Pharm Investig. 2014;4(1):27-31. https://doi.org/10.4103/2230-973X.127737.
17. Bhairav BA, Jagtap LR, Saudagar RB. Solubility and dissolution enhancement of Pioglitazone using solid dispersion technique. Int J Curr Pharm Res. 2017;9(5):186-93. https://doi.org/10.22159/ijcpr.2017v9i5.22326.
18. Tian B, Ju X, Yang D, Kong Y, Tang X. Effect of the third component on the aging and crystallization of cinnarizine-soluplus® binary solid dispersion. IJPham. 2020; 580. https://doi.org/10.1016/j.ijpharm.2020.119240.
19. Akram A, Irfan M, Abualsunun WA, Bukhary DM, Alissa M. How to Improve Solubility and Dissolution of Irbesartan by Fabricating Ternary Solid Dispersions: Optimization and In-Vitro Characterization. Pharmaceutics. 2022;14(11):2264. https://doi.org/10.3390/pharmaceutics14112264.
20. Shi X, Xu T, Huang W, Fan B, Sheng X. Stability and bioavailability enhancement of telmisartan ternary solid dispersions: the synergistic effect of polymers and drug-polymer (s) interactions. AAPS pharmscitech. 2019;20:1-3. https://doi.org/10.1208/s12249-019-1358-3.
21. Ali SK, Al-Khedairy EB. Solubility and Dissolution Enhancement of Atorvastatin Calcium using Solid Dispersion Adsorbate Technique. IJPS. 2019;28(2):105-14. https://doi.org/10.31351/vol28iss2pp105-114.
22. Salih OS, Nief RA. Effect of natural and synthetic polymers on the properties of candesartan cilexetil matrix tablet prepared by dry granulation. Asian J Pharm Clin Res. 2016;9(3):161-70. https://doi.org/10.22159/ajpcr.2016.v9s3.14719.
23. Hussien MA, Essa E, El-Gizawy SA. Investigation of the effect of formulation additives on telmisartan dissolution rate: Development of oral disintegrating tablets. Eur. J. Biomed. Pharm. Sci. 2019;6(4):12-20. https://www.ejbps.com/ejbps/abstract_id/5594.
24. Jassim ZE. Formulation and evaluation of furosemide liquisolid compact. Int J Appl Pharm. 2017;9(6):39-48. https://doi.org/10.22159/ijap.2017v9i6.21458.
25. Abed KK, Hussein AA, Ghareeb MM, Abdulrasool AA. Formulation and optimization of orodispersible tablets of diazepam. AAPS Pharm scitech. 2010; 11:356-61. https://doi.org/10.1208/s12249-010-9387-y.
26. Jassim ZE, Rajab NA, Mohammed NH. Study the effect of wet granulation and fusion methods on preparation, characterization, and release of lornoxicam sachet effervescent granules. Drug Invent Today. 2018;10(9):1612-6. https://scholar.google.com/scholar?oi=bibs&hl=en&cluster=6689927614267561003.
27. Hasson KJ, Ghareeb MM. Long Term Stability and In-vitro Release Study of Telmisartan Complex included by Hydroxypropyl-beta-cyclodextrin in Directly Compressed Tablet Using Ion-pair Reversed Phase High-performance Liquid Chromatography. International Journal of Drug Delivery Technology. 2021;11(0):974-979. https://impactfactor.org/PDF/IJDDT/11/IJDDT,Vol11,Issue3,Article54.pdf
28. Jihad HM, Al-Akkam EJ. Formulation and in-vitro Evaluation of Carvedilol Gastroretentive Capsule as (Superporous Hydrogel). IJPS. 2021;30(2):196-207. https://doi.org/10.31351/vol30iss2pp196-207.
29. Nasser SJ, Sameen LH, Ghareeb MM. Preparation and Evaluation of Oral Disintegrating Tablets of Ketoprofen by Direct Compression. IJPS. 2012;21(2):63-8. https://doi.org/10.31351/vol21iss2pp63-68.
30. The United State Pharmacopeia (USP) 37 NF 32. 2014. https://www.uspnf.com/
31. Abduljabbar HH, Abd Alhammid SN.Enhancement of the solubility and the dissolution rate of tamoxifen citrate solid dispersion using Soluplus by solvent evaporation technique. Asian J Pharm Clin Res. 2019;12(1):216-21. https://doi.org/10.22159/ajpcr.2018.v12i1.28933.
32. Hadi, BM, Al-Khedairy, EBH. Preparation and Characterization of Atorvastatin Calcium Trihydrate-cyclodextrin Inclusion Complex. International Journal of Drug Delivery Technology. 2022;12(3):1171-1179. https://doi.org/10.25258/ijddt.12.3.41.
33. Borde S, Paul SK, Chauhan H. Ternary solid dispersions: classification and formulation considerations. Drug Development and Industrial Pharmacy. 2021;47(7):1011-28. https://doi.org/10.1080/03639045.2021.1908342.
34. Ganapuram BR, Alle M, Dadigala R, Kotu GM, Guttena V. Development, evaluation and characterization of surface solid dispersion for solubility and dispersion enhancement of irbesartan. JoPR. 2013;7(6):472-7. https://doi.org/10.1016/j.jopr.2013.06.012.
35. Rajab NA, Hussein AA. Formulation and in-vitro evaluation of darifenacin hydrobromide as buccal films. Iraqi Journal of Pharmaceutical Sciences. 2019;28(2):83-94. https://doi.org/10.31351/vol28iss2pp83-94
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