Enhancement of Solubility and Dissolution Rate of Lercanidipine Solid Dispersions

DOI:

https://doi.org/10.37285/ijpsn.2019.12.1.8

Authors

  • Ashok Kumar U
  • Suresh Gande

Abstract

Lercanidipine hydrochloride is a BCS class II antihypertensive drug with poor solubility and low bioavailability of about 10%. Solid dispersion preparation through solvent evaporation technique has been proven to enhance the solubility and bioavailability of this drug. In the present study, Kolliwax GMS and Gelucire 44/14 were used in the ratio of 1:3 with SLS and this formula exhibited the highest solubility. Dissolution studies of optimized formulation S20 showed highest drug release of 99.08% at the end of 90 minutes among all formulations. FTIR spectroscopy (FTIR), X-Ray diffraction (XRD) and Scanning electron microscopy (SEM) were used as analytical tools to analyze the optimized formulation. FTIR spectra show that there are few interactions between lercanidipine, Gelucire and Kolliwax GMS. The XRD peaks were absent in final formulation but were present in pure drug. These results suggest the transformation of crystalline drug to amorphous form with increased scope of solubility. Therefore, it is concluded that lercanidipine solid dispersions are one of the promising methods to increase its solubility and bioavailability.  

Downloads

Download data is not yet available.

Metrics

Metrics Loading ...

Keywords:

Lercanidipine, Hypertension, Gelucire, Kolliwax, Solid dispersions

Downloads

Published

2019-01-31

How to Cite

1.
U AK, Gande S. Enhancement of Solubility and Dissolution Rate of Lercanidipine Solid Dispersions . Scopus Indexed [Internet]. 2019 Jan. 31 [cited 2024 Dec. 21];12(1):4412-21. Available from: https://ijpsnonline.com/index.php/ijpsn/article/view/286

Issue

Vol. 12 No. 1 (2019): January-February 2019

Section

Research Articles
Crossref
Scopus
Google Scholar
Europe PMC

References

Barchielli M, Dolfini E, Farina P, Leoni B, Targa G, Vinaccia V and Tajana A (1997). Clinical pharmacokinetics of Lercanidipine. Journal of Cardiovascular Pharmacology 29: 1-5.
Bolla N, Chandra S, Rao GSNK and Devi PU (2013). Improvement of simvastatin solubility using natural polymers by solid dispersion technique. International Journal of Pharmaceutical Research and Biomedical Analysis 2(2): 01-06.
Chaulang G, Patel P, Hardikar S, Kelkar M, Bhosale A and Bhise S (2009). Formulation and Evaluation of Solid Dispersions of Furosemide in Sodium Starch Glycolate. Tropical Journal of Pharmaceutical Research 8(1): 43-51.
Chen S, Zhu J, Ma F, Fang Q and Li Y (2007). Preparation and characterization of solid dispersions of dipyridamole with a carrier "copolyvidonum Plasdone S-630". Drug Dev Ind Pharm. 33(8): 888-99.
Chiou WL and Riegelman S (1971). Pharmaceutical applications of solid dispersion systems. J Pharm Sci. 60(9): 1281-302.
Dhirendra K, Lewis S and Udupa N (2009). Solid Dispersions A Review. Pak. J. Pharm. Sci. 22(2):234-246.
Ford JL (1986). The current status of solid dispersions. Pharm Acta Helv 61(3): 69-88.
Garad SD (2004). How to improve the bioavailability of poorly soluble drugs. Am. Pharm. Rev. 7: 80-85.
Hancock BC and Zografi G (1997). Characteristics and significance of the amorphous state in pharmaceutical system. J. Pharm. Sci 86: 1-12.
Howlader MSL, Kishore CJ and Sadique FK (2012). Enhancing dissolution profile of diazepam using hydrophilic polymers by solid dispersion technique. International Current Pharma-ceutical Journal 1(12): 423-430.
Jatwani S, Rana AC, Singh G and Aggarwal G (2011). Solubility and Dissolution enhancement of simvastatin using synergistic effect of hydrophilic carriers. Der Pharmacia Lettre 3(6): 280-293.
Lakshmi K, Reddy MPK and Kaza R (2012). Dissolution enhancement of Telmisartan by surface solid dispersion technology. International Journal of Innovative Pharmaceutical Research 3(4): 247-251.
Luscher TF and Cosentino F (1998). The classification of calcium antagonists and their selection in the treatment of hypertension. Am. reappraisal Drugs 55: 509-517.
Mandal D, Ojha PK, BC Nandy and LK Ghosh (2010). Effect of Carriers on Solid Dispersions of Simvastatin (Sim) Physico-Chemical Characterizations and Dissolution Studies. Der Pharmacia Lettre 2(4): 47-56.
Patel A, Prajapati P, Boghra R and Shah D (2011). Solubility enhancement of poorly aqueous soluble Furosemide using PEG-4000 by solid dispersion. Asian Journal of Pharmaceutical Sciences and Clinical Research (AJPSCR) 2(1): 1-9.
Poovi G, Uma Maheswari M, Kumar S and Raja Lakshmi AN (2013). Development of Domperidone Solid Dispersion Powders Using Sodium Alginate as Carrier. European Journal of Applied Sciences 5(2): 36-42.
Sawant MS, Biswas MM, Khan MA, Sinha S and Pradhan NSC (2012). Polymorphic form of Lercanidipine hydrochloride and process for the preparation thereof. U.S. Patent US8097729.
Shamma RN and Basha M (2013). Soluplus A novel polymeric solubilizer for optimization of Carvedilol solid dispersions. Formulation design and effect of method of preparation. Powder Technology 237: 406-414.
Yang G, Zhao Y, Feng N, Zhang Y, Liu Y and Dang B (2015). Improved dissolution and bioavailability of Silymarin delivered by a solid dispersion prepared using supercritical fluids. Asian Journal of Pharmaceutical Sciences 10: 194-202.