Solubility Enhancement of Telmisartan as Solid Dispersion by Different Methods
Keywords:
Poloxamer, Polyethylene glycol, solid dispersion, soluplus,TelmisartanAbstract
Background Telmisartanis an antihypertensive angiotensin II receptor antagonist drug commonly used to treat hypertension. It’s a BCS Class II poorly soluble drug in the Biopharmaceutical Classification System (BCS). Objective To increase the solubility and rate of dissolution of Telmisartan utilizing a solid dispersion method. Methods Two methods were obtained to prepare solid dispersion ofTelmisartan: solvent evaporation and kneading method. Each method used different polymersusing soluplus, poloxamer (188,407), and polyethylene glycol (4000,6000) as hydrophiliccarriersin different ratiosof 1%, 2%, and 3%. Results It was observed that the solid dispersion showsan increase in solubility in comparison to its pure drug. The best formula was obtained withthe formula (Telmisartan, soluplus at a 1:3 ratio) Conclusion By preparingTelmisartanas asolid dispersion via the solvent evaporation method, its solubility, and dissolution have been improved. Using a 1:3 ratio of hydrophilic carriers (drug: carrier). Its enhanced wettability and decreased crystallinity result in enhanced drug solubility and dissolution
Downloads
References
Ali SK, Al-Khedairy EB. Solubility and Dissolution Enhancement of
Atorvastatin Calcium using Solid Dispersion Adsorbate Technique.Iraqi
Journal of Pharmaceutical Sciences. 2019;28(2):105-14.
Savjani KT, Gajjar AK, Savjani JK. Drug solubility: importance and
enhancement techniques. International Scholarly Research Notices.
Abdulqader AA, Al-Khedairy EB. Formulation and evaluation of fast
dissolving tablets of taste-masked ondansetron hydrochloride by solid
/dispersion. Iraqi Journal of Pharmaceutical Sciences. 2017;26(l):50-60.
Ismail MY, Ghareeb MM. Enhancement of the solubility and dissolution rate
of rebamipide by using solid dispersion technique (Part I). Iraqi Journal
of Pharmaceutical Sciences. 2018:55-65.
37.Sabri LA, Hussien AA. Formulation and In-Vitro Characterization of
Solidified Nebivolol Self-Nanoemulsion using Liquisolid Technique.
Systematic Reviews in Pharmacy. 2020;11(3)
Ahmed KK, Al-Jumaili AA, Mutlak SH, Hadi MK. Determinants of national
drug products acceptance across patients, pharmacists, and
manufacturers: A mixed method study. Journal of Generic Medicines.
;17(3):139-153.
Alkufi HK, Kassab HJ. Formulation and evaluation of sustained release
sumatriptanmucoadhesive intranasal in-situ gel. Iraqi J Pharm Sci.
;28(2):95-104.
Yas LS. Effects of hypertension with and without smoking on salivary
electrolytes concentration. Journal of the Faculty of Medicine Baghdad.
;65(l).
Destro M, Cagnoni F, Dognini GP, Galimberti V, Taietti C, Cavalieri C, Galli
E.Telmisartan: just an antihypertensive agent? A literature review. Expert
opinion on pharmacotherapy. 2011;12(17):2719-35.
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. Journal of human hypertension.
;23(5):339-49.
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.
;12(l):216-21.
SwatiS, Jyothi N.,Manjusha P.,Prasanthi N. L., Thireesha B. Formulation and
Evaluation of Immediate Release Telmisartan Tablets using Hydrophilic
Polymers. Asian Journal of Pharmaceutics (AJP). 2017;11(01).
Prajapati ST, Modh SI, Patel CN. FORMULATION AND OPTIMIZATION
OF SUBLINGUAL TABLETS OF TELMISARTAN. World Journal of
Pharmaceutical Research.2015;4(5): 2378-2391.
Jihad HM, Al-Akkam EJ. Formulation and in-vitro Evaluation of
CarvedilolGastroretentive Capsule as (Superporous Hydrogel). Iraqi
Journal of Pharmaceutical Sciences. 2021;30(2):196-207.
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 Highperformance Liquid Chromatography. International Journal of Drug
Delivery Technology. 2021;11(0):974-979.
Powar DR, Desai AV, Rohile VY, Bhosale MV, Inamdar NR. Design
Development and Optimization of Telmisartan’s Ternary Solid
Dispersion with Its Formulation. International Research Journal of
Pharmacy and Medical Sciences(IRJPMS).2O22; 6(1): 21-31.
The United State Pharmacopeia (USP) 37 NF 32. 2014.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.
;12(l):216-21.
Chaudhary A, Sangra M, Kumar S. Formulation design and optimization of
mouth dissolving tablets of telmisartan using solid dispersion technique.
World J Pharm Res. 2014; 3(5):1318-33.
Shrimal P, Jadeja G, Naik J, Patel S. Continuous microchannel precipitation
to enhance the solubility of telmisartan with poloxamer 407 using BoxBehnken design approach. Journal of Drug Delivery Science and
Technology. 2019; 53:101225.
JOSHI R, AKRAM W, Garud N, Dubey A, Bhadkariya S. Development and
optimization of orodispersible tablets using solid dispersion of
Telmisartan. Journal of Drug Delivery and Therapeutics. 2018;8(6):171-
Dubey A, Kharia AA, Chatterjee DP. Enhancement of aqueous solubility and
dissolution of telmisartan using solid dispersion technique. International
Journal of Pharmaceutical Sciences and Research. 2014;5(10):4478-85.
AlKhalidi MM, Jawad FJ. Enhancement of Aqueous Solubility and
Dissolution Rate of Etoricoxib by Solid Dispersion Technique. Iraqi
Journal of Pharmaceutical Sciences. 2020;29(l):76-87.
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.
;10(9):1612-6.
Downloads
Published
Issue
Section
License
You are free to:
- Share — copy and redistribute the material in any medium or format for any purpose, even commercially.
- Adapt — remix, transform, and build upon the material for any purpose, even commercially.
- The licensor cannot revoke these freedoms as long as you follow the license terms.
Under the following terms:
- Attribution — You must give appropriate credit , provide a link to the license, and indicate if changes were made . You may do so in any reasonable manner, but not in any way that suggests the licensor endorses you or your use.
- No additional restrictions — You may not apply legal terms or technological measures that legally restrict others from doing anything the license permits.
Notices:
You do not have to comply with the license for elements of the material in the public domain or where your use is permitted by an applicable exception or limitation .
No warranties are given. The license may not give you all of the permissions necessary for your intended use. For example, other rights such as publicity, privacy, or moral rights may limit how you use the material.
