Formulation, Development, Characterization and Solubility Enhancement of Amisulpride

DOI:

https://doi.org/10.37285/ijpsn.2024.17.4.4

Authors

  • S.D Mankar Department of Pharmaceutics, Pravara Rural College of Pharmacy, Loni
  • M. H. Markad Department of Quality Assurance Technique, Pravara Rural College of Pharmacy, Loni
  • S.S. Siddheshwar Department of Pharmaceutics, Pravara Rural College of Pharmacy, Loni
  • A.P Patel Department of Pharmacognosy, Pravara Rural College of Pharmacy, Loni

Abstract

Background: Amisulpride (AMP) is a drug that is poorly water-soluble and is typically characterized by high molecular weights, significant log P values, and low bioavailability. Poor water solubility of a drug is caused by strong intermolecular interaction and a drug's affinity for a lipid environment (lipophilicity). 

Objective: The current study aims to improve Amisulpride's (AMP) oral bioavailability and solubility by developing a complex with 2-hydroxypropyl                             β-cyclodextrin (HP-β-CDT). 

Method: This study describes solubility of AMP with β-CDT and HP-β-CDT. Prepared inclusion complex of AMP and HP-β-CDT by different techniques like physical mixture, kneading and lyophilization. 

Result: A notable improvement in AMP's solubility was obtained with an optimized inclusion complex. The result of FT-IR, DSC and XRD confirms the complex between AMP and HP-β-CDT. The physical mixture, kneading and lyophilization technique, the kneading method is most successful in producing an inclusion complex.

Conclusion: The 1.3 ratio gives the best drug content and dissolution profile.

Downloads

Download data is not yet available.

Metrics

Metrics Loading ...

Keywords:

Amisulpride (AMP), Inclusion complex, HP-β-CDT, solubility enhancement, bioavailability

Published

2024-08-15

How to Cite

1.
Mankar S, Markad MH, Siddheshwar S, Patel A. Formulation, Development, Characterization and Solubility Enhancement of Amisulpride. Scopus Indexed [Internet]. 2024 Aug. 15 [cited 2024 Dec. 13];17(4):7467-74. Available from: https://ijpsnonline.com/index.php/ijpsn/article/view/4291

Issue

Section

Research Articles

References

Boyer P, Lecrubier Y, Puech A. J, Dewailly J, Aubin F. Treatment of negative symptoms in schizophrenia with amisulpride. Br. J. Psychiatry 1995;166:68-72.

Gerold M. Complexation and Cyclodextrins. In: Encyclopedia of Pharmaceutical Technology by Marcel Dekkar. 2002; 531-558.

Duchene D, Wouessidjew D. Pharmaceutical uses of Cyclodextrins and derivative. Drug Dev. Ind. Pharm 990;6(17):2487-2499. [http://dx.doi.org/10.3109/03639049009058543]

Suihko E, Korhonen O, Jarvinen T, Ketolainen J, Jarho P, Laine E, Paronen P. Complexation with tolbutamide modifies the physicochemical and tableting properties of hydroxypropyl-beta-cyclodextrin. Int. J. Pharm 2001:215(1-2): 137-145.

Background review for cyclodextrins used as excipients EMA/CHMP/333892/2013

Tirucherai G.S, Mitra A.K. Effect of hydroxypropyl beta cyclodextrin complexation on aqueous solubility, stability, and corneal permeation of acyl ester prodrugs of ganciclovir. AAPS Pharm- SciTech 2003; 4(3):E45

Higuchi T, Connors K.A. Phase-Solubility techniques. Advance Analytical Chemistry Instrumental 1965 4: 117-212.

Loftsson T, Brewster M.E. Pharmaceutical applications of cyclodextrins. Drug solubilization and stabilization. J. Pharm. Sci. 1996, 85(10), 1017-1025.

Krenn, M.; Gamcsik, M.P.; Vogelsang, G.B.; Colvin, O.M.; Leong, K.W. Improvements in solubility and stability of thalidomide upon complexation with hydroxypropyl-beta-cyclodextrin. J. Pharm.Sci. 1992; 81(7): 685-689.

Jambhekar S, Casella R, Maher T. The physicochemical characteristics and bioavailability of indomethacin from s-cyclodextrin, hydroxy-ethyl s -cyclodextrin and hydroxypropyl- s-cyclodextrin complexes. International Journal of Pharmaceutics. 2004; 270:L:149-166.

Onyeji C O, Omoruyi S I, Oladimeji F A, Soyinka J O. Physicochemical characterization and dissolution properties of binary systems of pyrimethamine and 2- hydroxypropyl β–cyclodextrin. Afr J Biotechnol. 2009; 8: 1651-659.

Mankar SD, Tupe A. Solubility enhancement and evaluation of Cilnidipine using solid Dispersion techniques. Int. J. Exp. Res. Rev. 2023;32:347-57.