Al-dulaimi, E., Alfahad, M., Qazzaz, M. (2023). Scanning Sildenafil Citrate Solubility in Hydrotropic Solutions. Alustath, 20(2), 79-82. doi: 10.33899/iphr.2023.140337.1045
Ebtissam Ameer Al-dulaimi; Mohanad Alfahad; Mohannad Emad Qazzaz. "Scanning Sildenafil Citrate Solubility in Hydrotropic Solutions". Alustath, 20, 2, 2023, 79-82. doi: 10.33899/iphr.2023.140337.1045
Al-dulaimi, E., Alfahad, M., Qazzaz, M. (2023). 'Scanning Sildenafil Citrate Solubility in Hydrotropic Solutions', Alustath, 20(2), pp. 79-82. doi: 10.33899/iphr.2023.140337.1045
Al-dulaimi, E., Alfahad, M., Qazzaz, M. Scanning Sildenafil Citrate Solubility in Hydrotropic Solutions. Alustath, 2023; 20(2): 79-82. doi: 10.33899/iphr.2023.140337.1045

Scanning Sildenafil Citrate Solubility in Hydrotropic Solutions

Iraqi Journal of Pharmacy
Volume 20, Issue 2, December 2023, Pages 79-82    PDF (717.59 K)
Document Type: Research Paper
DOI: 10.33899/iphr.2023.140337.1045
Authors
Ebtissam Ameer Al-dulaimi1; Mohanad Alfahad* 1; Mohannad Emad Qazzaz2
1Department of pharmaceutics, College of Pharmacy, University of Mosul, Mosul, Iraq
2Department of Pharmacognosy and Medicinal Plants, College of Pharmacy, University of Mosul, Mosul, Iraq
Abstract
Background: Sildenafil citrate (SC) is a selective phosphodiesterase-5 inhibitor with low aqueous solubility (4.1 mg/mL in water), resulting in only 40% bioavailability after oral administration. SC is classified as class II by the Biopharmaceutical Drug Classification System. Hydrotropic agents are ionisable organic salts that provide a simple, safe and effective technique for enhancing the solubility of poorly water-soluble drugs. Method: Solubility study of SC was conducted in water (as a reference) and in various hydrotropic solutions separately (including sodium benzoate, sodium acetate, Urea and mannitol). The concentrations of the hydrotropic solutions were at 10, 20 and 30 % solution concentration, as well as in the solution of 30 % concentration of mixed hydrotropic agents at a 1:1 ratio. Results: The results show marked enhancement of SC solubility in solution of urea at different concentrations while the solubility was enhanced only in 30% solution of sodium benzoate and slightly enhanced in 30% mannitol solution and mannitol-urea solution. The solubility enhancement in urea shows a positive relationship with solution concentration. In addition, the SC solubility was reduced in the solution of sodium acetate at all concentrations and in the solution of sodium benzoate at concentrations of both 10 and 20 % as well as in all mixed hydrotropic solution containing these two agents. Conclusion: Urea shows promising data as a potential additive with SC to achieve higher solubility and bioavailability of the compound.

The results show marked enhancement of SC solubility in solution of urea at different concentrations while the solubility was enhanced only in 30% solution of sodium benzoate and slightly enhanced in 30% mannitol solution and mannitol-urea solution. The solubility enhancement in urea shows a positive relationship with solution concentration.

In addition, the SC was reduced in the solution of sodium acetate at all concentrations and in the solution of sodium benzoate at concentrations of both 10 and 20 % as well as in all mixed hydrotropic solution containing these two agents. In conclusion, urea shows promising data as a potential additive with SC to achieve higher solubility and bioavailability of the compound.
Keywords
Sildenafil citrate; Hydrotropic agents; Solubility; Mixed hydrotropy
References
  1. Al Omari MM, Zughul MB, Davies JED, Badwan AA. Sildenafil/cyclodextrin complexation: Stability constants, thermodynamics, and guest-host interactions probed by 1H NMR and molecular modeling studies. Journal of Pharmaceutical and Biomedical Analysis. 2006;41(3):857–65.
  2. Maheshwari RK, Jagwani Y. Mixed hydrotropy: Novel science of solubility enhancement. Indian journal of pharmaceutical sciences. 2011;73(2):179.
  3. Amidon GL, Lennernäs H, Shah VP, Crison JR. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharmaceutical research. 1995;12:413–20.
  4. Bhalani D V, Nutan B, Kumar A, Singh Chandel AK. Bioavailability Enhancement Techniques for Poorly Aqueous Soluble Drugs and Therapeutics. Biomedicines. 2022;10(9):2055.
  5. Patil MR, Ganorkar SB, Patil AS, Shirkhedkar AA, Surana SJ. Hydrotropic solubilization in pharmaceutical analysis: Origin, evolution, cumulative trend and precise applications. Critical reviews in analytical chemistry. 2021;51(3):278–88.
  6. Khan AD, Tabish M, Kaushik R, Saxena V, Kesharwani P, Gupta S, et al. Hydrotropy : Recent Advancements in Enhancement of Drug Solubility and Formulation Development. 2021;
  7. Maheshwari RK, Goyal S, Adhav R, Vaswani P. Solid as Solvent”-Novel Spectrophotometric Analysis of Piroxicam Tablets Using Solids (Eutectic Liquid of Phenol and Metformin Hydrochloride) As Solubilizing Agents (Mixed Solvency Concept). 2016;
  8. Patidar M, Maheshwari RK, Agrawal S. Solubility Enhancement Of Indomethacin By Forming Solid Dispersion Using Mixed Hydrotropy. Certified Journal │ Patidar et al World Journal of Pharmaceutical Research. 2022;11(1).
  9. Deore PD, Katti SA, Bhamare VG, Gandhi M, Gandhi M. Application Of Mixed Hydrotropy For The Solubility. 2021;10(3):1163–76.
  10. Madan JR, Kamate VJ, Dua K, Awasthi R. Improving the solubility of nevirapine using a hydrotropy and mixed hydrotropy based solid dispersion approach. Polymers in Medicine. 2017;47(2):83–90.
  11. Madan JR, Pawar KT, Dua K. Solubility enhancement studies on lurasidone hydrochloride using mixed hydrotropy. International journal of pharmaceutical investigation. 2015;5(2):114.
  12. Majeed A, Raza SN, Khan  NA. Hydrotrophy: Novel Solubility Enhancement Technique: A Review. International Journal of Pharmaceutical Sciences and Research. 2019;10(3):1025–36.
  13. Dhapte V, Mehta P. Advances in hydrotropic solutions: An updated review. St Petersburg Polytechnical University Journal: Physics and Mathematics. 2015;1(4):424–35.
Statistics
Article View: 196
PDF Download: 170


Journal Management System. Powered by ejournalplus.com