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Enhanced solubility and dissolution rate of lamotrigine by inclusion complexation and solid dispersion technique.
J Pharm Pharmacol. 2008 Sep; 60(9):1121-9.JP

Abstract

The solid-state properties and dissolution behaviour of lamotrigine in its inclusion complex with beta-cyclodextrin (betaCD) and solid dispersions with polyvinylpyrrolidone K30 (PVP K30) and polyethyleneglycol 6000 were investigated. The phase solubility profile of lamotrigine with betaCD was classified as AL-type, indicating formation of a 1:1 stoichiometry inclusion complex, with a stability constant of 369.96+/-2.26 M(-1). Solvent evaporation and kneading methods were used to prepare solid dispersions and inclusion complexes, respectively. The interaction of lamotrigine with these hydrophilic carriers was evaluated by powder X-ray diffractometry, Fourier transform infrared spectroscopy and differential scanning calorimetry. These studies revealed that the drug was no longer present in crystalline state but was converted to an amorphous form. Among the binary systems tested, PVP K30 (1:5) showed greatest enhancement of the solubility and dissolution of lamotrigine.

Authors+Show Affiliations

Department of Pharmaceutical Chemistry, Government College of Pharmacy, Karad, Maharashtra, 415124, India.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

18718114

Citation

Shinde, Vikram R., et al. "Enhanced Solubility and Dissolution Rate of Lamotrigine By Inclusion Complexation and Solid Dispersion Technique." The Journal of Pharmacy and Pharmacology, vol. 60, no. 9, 2008, pp. 1121-9.
Shinde VR, Shelake MR, Shetty SS, et al. Enhanced solubility and dissolution rate of lamotrigine by inclusion complexation and solid dispersion technique. J Pharm Pharmacol. 2008;60(9):1121-9.
Shinde, V. R., Shelake, M. R., Shetty, S. S., Chavan-Patil, A. B., Pore, Y. V., & Late, S. G. (2008). Enhanced solubility and dissolution rate of lamotrigine by inclusion complexation and solid dispersion technique. The Journal of Pharmacy and Pharmacology, 60(9), 1121-9. https://doi.org/10.1211/jpp.60.9.0002
Shinde VR, et al. Enhanced Solubility and Dissolution Rate of Lamotrigine By Inclusion Complexation and Solid Dispersion Technique. J Pharm Pharmacol. 2008;60(9):1121-9. PubMed PMID: 18718114.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Enhanced solubility and dissolution rate of lamotrigine by inclusion complexation and solid dispersion technique. AU - Shinde,Vikram R, AU - Shelake,Makarand R, AU - Shetty,Sandeep S, AU - Chavan-Patil,Amit B, AU - Pore,Yogesh V, AU - Late,Sameer G, PY - 2008/8/23/pubmed PY - 2008/12/17/medline PY - 2008/8/23/entrez SP - 1121 EP - 9 JF - The Journal of pharmacy and pharmacology JO - J Pharm Pharmacol VL - 60 IS - 9 N2 - The solid-state properties and dissolution behaviour of lamotrigine in its inclusion complex with beta-cyclodextrin (betaCD) and solid dispersions with polyvinylpyrrolidone K30 (PVP K30) and polyethyleneglycol 6000 were investigated. The phase solubility profile of lamotrigine with betaCD was classified as AL-type, indicating formation of a 1:1 stoichiometry inclusion complex, with a stability constant of 369.96+/-2.26 M(-1). Solvent evaporation and kneading methods were used to prepare solid dispersions and inclusion complexes, respectively. The interaction of lamotrigine with these hydrophilic carriers was evaluated by powder X-ray diffractometry, Fourier transform infrared spectroscopy and differential scanning calorimetry. These studies revealed that the drug was no longer present in crystalline state but was converted to an amorphous form. Among the binary systems tested, PVP K30 (1:5) showed greatest enhancement of the solubility and dissolution of lamotrigine. SN - 0022-3573 UR - https://www.unboundmedicine.com/medline/citation/18718114/Enhanced_solubility_and_dissolution_rate_of_lamotrigine_by_inclusion_complexation_and_solid_dispersion_technique_ L2 - https://doi.org/10.1211/jpp.60.9.0002 DB - PRIME DP - Unbound Medicine ER -