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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

X-ray diffractograms. (a) X-ray diffractogram of candesartan cilexetil, (b) X-ray diffractogram of β-cyclodextrin, (c) X-ray diffractogram of candesartan cilexetil-β-cyclodextrin complex prepared by kneading method, and (d) X-ray diffractogram of candesartan cilexetil-β-cyclodextrin complex prepared by lyophilisation method.
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fig4: X-ray diffractograms. (a) X-ray diffractogram of candesartan cilexetil, (b) X-ray diffractogram of β-cyclodextrin, (c) X-ray diffractogram of candesartan cilexetil-β-cyclodextrin complex prepared by kneading method, and (d) X-ray diffractogram of candesartan cilexetil-β-cyclodextrin complex prepared by lyophilisation method.

Mentions: The XRD results were in good agreement with the thermal analysis data. X-ray diffraction patterns in Figure 4(a) revealed that pure candesartan cilexetil was clearly in crystalline state as it showed sharp distinct peaks notably at 2θ diffraction angles of 9.97°, 17.04°, 18.74°, 19.40°, 21.63°, 23.94°, 25.16°, 27.96°, and 29.28°. X-ray diffraction pattern in Figure 4(b) revealed that pure β-cyclodextrin was in a crystalline state as it showed sharp distinct peaks at 2θ diffraction angles of 12.4° and 19.0° 2θ. X-ray diffraction pattern of inclusion complexes prepared by kneading and lyophilisation techniques (Figures 4(c)-4(d)) showed sharp distinct peaks at 2θ diffraction angles of 12.4°, 19.0°, 17.04°, 18.74°, and 19.40° that are characteristic for both candesartan cilexetil and β-cyclodextrin. The complex formation led to the broadening of the existing peaks, appearance of a few new peaks, and shifting of certain peaks. This could be due to the conversion of crystalline to amorphous form during complexation [17].


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

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

X-ray diffractograms. (a) X-ray diffractogram of candesartan cilexetil, (b) X-ray diffractogram of β-cyclodextrin, (c) X-ray diffractogram of candesartan cilexetil-β-cyclodextrin complex prepared by kneading method, and (d) X-ray diffractogram 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

fig4: X-ray diffractograms. (a) X-ray diffractogram of candesartan cilexetil, (b) X-ray diffractogram of β-cyclodextrin, (c) X-ray diffractogram of candesartan cilexetil-β-cyclodextrin complex prepared by kneading method, and (d) X-ray diffractogram of candesartan cilexetil-β-cyclodextrin complex prepared by lyophilisation method.
Mentions: The XRD results were in good agreement with the thermal analysis data. X-ray diffraction patterns in Figure 4(a) revealed that pure candesartan cilexetil was clearly in crystalline state as it showed sharp distinct peaks notably at 2θ diffraction angles of 9.97°, 17.04°, 18.74°, 19.40°, 21.63°, 23.94°, 25.16°, 27.96°, and 29.28°. X-ray diffraction pattern in Figure 4(b) revealed that pure β-cyclodextrin was in a crystalline state as it showed sharp distinct peaks at 2θ diffraction angles of 12.4° and 19.0° 2θ. X-ray diffraction pattern of inclusion complexes prepared by kneading and lyophilisation techniques (Figures 4(c)-4(d)) showed sharp distinct peaks at 2θ diffraction angles of 12.4°, 19.0°, 17.04°, 18.74°, and 19.40° that are characteristic for both candesartan cilexetil and β-cyclodextrin. The complex formation led to the broadening of the existing peaks, appearance of a few new peaks, and shifting of certain peaks. This could be due to the conversion of crystalline to amorphous form during complexation [17].

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