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Enhancement of carvedilol solubility by solid dispersion technique using cyclodextrins, water soluble polymers and hydroxyl acid.
J Pharm Biomed Anal. 2014 Aug 05; 96:10-20.JP

Abstract

Aim of the present work is to enhance aqueous solubility of carvedilol (CV) by solid dispersion technique using wide variety of carriers such as: β-cyclodextrin (βCD), hydroxypropyl-β-cyclodextrin (HPβCD), tartaric acid (TA), polyvinyl pyrrolidone K-30 (PVP K-30) and poloxamer-407 (PLX-407). Various products of 'CV-solid dispersion' had been studied extensively in various pH conditions to check enhancement of solubility and dissolution characteristics of carvedilol. Any physical change upon interaction between CV and carriers was confirmed by instrumental analysis: XRD, DSC, FTIR and SEM. Negative change of Gibb's free energy and complexation constants (Kc, 75-240M(-1), for cyclodextrins and 1111-20,365M(-1), for PVP K-30 and PLX-407) were the evidence of stable nature of the binding between CV and carriers. 'Solubility enhancement factor' of ionized-CV was found high enough (340 times) with HPβCD in presence of TA. TA increases the binding efficiency of cyclodextrin and changing the pH of microenvironment in dissolution medium. In addition, ionization process was used to increase the apparent intrinsic solubility of drug. In vitro, dissolution time of CV was remarkably reduced in the solid dispersion system compared to that of pure drug. This may be attributed to increased wettability, dispersing ability and transformation of crystalline state of drug to amorphous one.

Authors+Show Affiliations

Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, West Bengal, India. Electronic address: yuvaju@gmail.com.Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, West Bengal, India.

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

24705456

Citation

Yuvaraja, K, and Jasmina Khanam. "Enhancement of Carvedilol Solubility By Solid Dispersion Technique Using Cyclodextrins, Water Soluble Polymers and Hydroxyl Acid." Journal of Pharmaceutical and Biomedical Analysis, vol. 96, 2014, pp. 10-20.
Yuvaraja K, Khanam J. Enhancement of carvedilol solubility by solid dispersion technique using cyclodextrins, water soluble polymers and hydroxyl acid. J Pharm Biomed Anal. 2014;96:10-20.
Yuvaraja, K., & Khanam, J. (2014). Enhancement of carvedilol solubility by solid dispersion technique using cyclodextrins, water soluble polymers and hydroxyl acid. Journal of Pharmaceutical and Biomedical Analysis, 96, 10-20. https://doi.org/10.1016/j.jpba.2014.03.019
Yuvaraja K, Khanam J. Enhancement of Carvedilol Solubility By Solid Dispersion Technique Using Cyclodextrins, Water Soluble Polymers and Hydroxyl Acid. J Pharm Biomed Anal. 2014 Aug 5;96:10-20. PubMed PMID: 24705456.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Enhancement of carvedilol solubility by solid dispersion technique using cyclodextrins, water soluble polymers and hydroxyl acid. AU - Yuvaraja,K, AU - Khanam,Jasmina, Y1 - 2014/03/21/ PY - 2014/01/06/received PY - 2014/03/08/revised PY - 2014/03/11/accepted PY - 2014/4/8/entrez PY - 2014/4/8/pubmed PY - 2015/1/13/medline KW - Carvedilol KW - Cyclodextrin KW - Dissolution enhancement KW - Ionization process KW - Tartaric acid KW - Water soluble polymer SP - 10 EP - 20 JF - Journal of pharmaceutical and biomedical analysis JO - J Pharm Biomed Anal VL - 96 N2 - Aim of the present work is to enhance aqueous solubility of carvedilol (CV) by solid dispersion technique using wide variety of carriers such as: β-cyclodextrin (βCD), hydroxypropyl-β-cyclodextrin (HPβCD), tartaric acid (TA), polyvinyl pyrrolidone K-30 (PVP K-30) and poloxamer-407 (PLX-407). Various products of 'CV-solid dispersion' had been studied extensively in various pH conditions to check enhancement of solubility and dissolution characteristics of carvedilol. Any physical change upon interaction between CV and carriers was confirmed by instrumental analysis: XRD, DSC, FTIR and SEM. Negative change of Gibb's free energy and complexation constants (Kc, 75-240M(-1), for cyclodextrins and 1111-20,365M(-1), for PVP K-30 and PLX-407) were the evidence of stable nature of the binding between CV and carriers. 'Solubility enhancement factor' of ionized-CV was found high enough (340 times) with HPβCD in presence of TA. TA increases the binding efficiency of cyclodextrin and changing the pH of microenvironment in dissolution medium. In addition, ionization process was used to increase the apparent intrinsic solubility of drug. In vitro, dissolution time of CV was remarkably reduced in the solid dispersion system compared to that of pure drug. This may be attributed to increased wettability, dispersing ability and transformation of crystalline state of drug to amorphous one. SN - 1873-264X UR - https://www.unboundmedicine.com/medline/citation/24705456/Enhancement_of_carvedilol_solubility_by_solid_dispersion_technique_using_cyclodextrins_water_soluble_polymers_and_hydroxyl_acid_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0731-7085(14)00146-0 DB - PRIME DP - Unbound Medicine ER -