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Development of Orodispersible Tablets of Candesartan Cilexetil- β -cyclodextrin Complex.

Sravya M, Deveswaran R, Bharath S, Basavaraj BV, Madhavan V - J Pharm (Cairo) (2013)

Bottom Line: Drug-excipient compatibility studies showed no interaction, and characterization proved the formation of inclusion complex.The optimized formulation was found to be stable after 6 months and showed no significant change in drug content.This work proved β-cyclodextrins to be effective solubilizing agent in improving the solubility of poorly water soluble drugs.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, M.S. Ramaiah College of Pharmacy, Bangalore 54, India.

ABSTRACT
The aim of this study was to investigate the use of inclusion complexation technique employing β-cyclodextrin in improving the dissolution profile of candesartan cilexetil, a BCS class-II drug, and to formulate the inclusion complex into orodispersible tablets. The inclusion complexes were formed by physical mixing, kneading, coevaporation, and lyophilisation methods. Inclusion complexes were characterized by FTIR, DSC, XRD, NMR, and mass spectral studies. Inclusion complexes prepared using kneading, and lyophilisation techniques in the molar ratio 1 : 5 with β-cyclodextrin were used for formulating orodispersible tablets by direct compression with different superdisintegrants like croscarmellose sodium, crospovidone, sodium starch glycolate, and low substituted hydroxypropyl cellulose in varying concentrations. The directly compressible powder was evaluated for precompression parameters, and the prepared orodispersible tablets were evaluated for postcompression parameters. Drug-excipient compatibility studies showed no interaction, and characterization proved the formation of inclusion complex. In vitro disintegration time was found to be within 3 minutes, and all the formulations showed complete drug release of 100% within 20 minutes. The optimized formulation was found to be stable after 6 months and showed no significant change in drug content. This work proved β-cyclodextrins to be effective solubilizing agent in improving the solubility of poorly water soluble drugs.

No MeSH data available.


Related in: MedlinePlus

NMR spectra. (a) NMR spectra of candesartan cilexetil, (b) NMR spectra of β-cyclodextrin, (c) NMR spectra of candesartan cilexetil-β-cyclodextrin complex prepared by kneading method, and (d) NMR spectra of candesartan cilexetil-β-cyclodextrin complex prepared by lyophilisation method.
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fig6: NMR spectra. (a) NMR spectra of candesartan cilexetil, (b) NMR spectra of β-cyclodextrin, (c) NMR spectra of candesartan cilexetil-β-cyclodextrin complex prepared by kneading method, and (d) NMR spectra of candesartan cilexetil-β-cyclodextrin complex prepared by lyophilisation method.

Mentions: The 1H-NMR chemical shift for each proton of candesartan cilexetil and βCD was evaluated for the formation of inclusion complex between candesartan cilexetil and βCD at molar ratio 1 : 5 of candesartan cilexetil and βCD. The chemical shifts for different protons in candesartan cilexetil (Figure 6(a)) were seen at 1-2, 2.4, 4.5, 5.5, and 6.8–7.6 ppm. The chemical shifts for different protons in β-cyclodextrins (Figure 6(b)) were seen at 2, 3.2, 3.6, 4.4, 4.8, and 5.8 ppm. The chemical shifts for the protons present in both candesartan cilexetil and β-cyclodextrins were found in inclusion complexes prepared by kneading method and lyophilisation technique (Figures 6(c)-6(d)). Since the complexes which were analysed were prepared using 1 : 5 molar ratio, the chemical shift values for protons present in candesartan cilexetil were seen in minimal intensity. These minimal intensity chemical shifts seen in inclusion complexes can also be accounted to the inclusion complexation of candesartan cilexetil into the cavity of β-cyclodextrins.


Development of Orodispersible Tablets of Candesartan Cilexetil- β -cyclodextrin Complex.

Sravya M, Deveswaran R, Bharath S, Basavaraj BV, Madhavan V - J Pharm (Cairo) (2013)

NMR spectra. (a) NMR spectra of candesartan cilexetil, (b) NMR spectra of β-cyclodextrin, (c) NMR spectra of candesartan cilexetil-β-cyclodextrin complex prepared by kneading method, and (d) NMR spectra of candesartan cilexetil-β-cyclodextrin complex prepared by lyophilisation method.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4590806&req=5

fig6: NMR spectra. (a) NMR spectra of candesartan cilexetil, (b) NMR spectra of β-cyclodextrin, (c) NMR spectra of candesartan cilexetil-β-cyclodextrin complex prepared by kneading method, and (d) NMR spectra of candesartan cilexetil-β-cyclodextrin complex prepared by lyophilisation method.
Mentions: The 1H-NMR chemical shift for each proton of candesartan cilexetil and βCD was evaluated for the formation of inclusion complex between candesartan cilexetil and βCD at molar ratio 1 : 5 of candesartan cilexetil and βCD. The chemical shifts for different protons in candesartan cilexetil (Figure 6(a)) were seen at 1-2, 2.4, 4.5, 5.5, and 6.8–7.6 ppm. The chemical shifts for different protons in β-cyclodextrins (Figure 6(b)) were seen at 2, 3.2, 3.6, 4.4, 4.8, and 5.8 ppm. The chemical shifts for the protons present in both candesartan cilexetil and β-cyclodextrins were found in inclusion complexes prepared by kneading method and lyophilisation technique (Figures 6(c)-6(d)). Since the complexes which were analysed were prepared using 1 : 5 molar ratio, the chemical shift values for protons present in candesartan cilexetil were seen in minimal intensity. These minimal intensity chemical shifts seen in inclusion complexes can also be accounted to the inclusion complexation of candesartan cilexetil into the cavity of β-cyclodextrins.

Bottom Line: Drug-excipient compatibility studies showed no interaction, and characterization proved the formation of inclusion complex.The optimized formulation was found to be stable after 6 months and showed no significant change in drug content.This work proved β-cyclodextrins to be effective solubilizing agent in improving the solubility of poorly water soluble drugs.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, M.S. Ramaiah College of Pharmacy, Bangalore 54, India.

ABSTRACT
The aim of this study was to investigate the use of inclusion complexation technique employing β-cyclodextrin in improving the dissolution profile of candesartan cilexetil, a BCS class-II drug, and to formulate the inclusion complex into orodispersible tablets. The inclusion complexes were formed by physical mixing, kneading, coevaporation, and lyophilisation methods. Inclusion complexes were characterized by FTIR, DSC, XRD, NMR, and mass spectral studies. Inclusion complexes prepared using kneading, and lyophilisation techniques in the molar ratio 1 : 5 with β-cyclodextrin were used for formulating orodispersible tablets by direct compression with different superdisintegrants like croscarmellose sodium, crospovidone, sodium starch glycolate, and low substituted hydroxypropyl cellulose in varying concentrations. The directly compressible powder was evaluated for precompression parameters, and the prepared orodispersible tablets were evaluated for postcompression parameters. Drug-excipient compatibility studies showed no interaction, and characterization proved the formation of inclusion complex. In vitro disintegration time was found to be within 3 minutes, and all the formulations showed complete drug release of 100% within 20 minutes. The optimized formulation was found to be stable after 6 months and showed no significant change in drug content. This work proved β-cyclodextrins to be effective solubilizing agent in improving the solubility of poorly water soluble drugs.

No MeSH data available.


Related in: MedlinePlus