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Solubility Enhancement of Raloxifene Using Inclusion Complexes and Cogrinding Method.

Patil PH, Belgamwar VS, Patil PR, Surana SJ - J Pharm (Cairo) (2013)

Bottom Line: The objective of the present work was to enhance the solubility and dissolution of practically water-insoluble drug raloxifene HCl (RLX), for the same two approaches that were used.It was concluded that the prepared inclusion complex showed a remarkable increase in solubility and dissolution of poorly water-soluble drug raloxifene.In the cogrinding mixture, a natural modified gum is used as a surfactant and enhances the solubility and dissolution of RLX without requiring addition of organic solvent or high temperature for its preparation; thus, process is less cumbersome and cost effective.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, R. C. Patel Institute of Pharmaceutical Education and Research, Near Karvand Naka, Shirpur, Dhule, Maharashtra 425405, India.

ABSTRACT
The objective of the present work was to enhance the solubility and dissolution of practically water-insoluble drug raloxifene HCl (RLX), for the same two approaches that were used. In the first approach, drug was kneaded with hydroxypropyl-β-cyclodextrin (HPβCD), and in the second one drug was cogrinded with modified guar gum (MGG). The drug-cyclodextrin complex and drug-MGG cogrind mixtures were characterized by differential scanning calorimetry, X-ray diffraction studies, scanning electron microscopy, and Fourier transform infrared spectroscopy. The solubility and dissolution study reveals that solubility and dissolution rate of RLX remarkably increased in both methods. It was concluded that the prepared inclusion complex showed a remarkable increase in solubility and dissolution of poorly water-soluble drug raloxifene. In the cogrinding mixture, a natural modified gum is used as a surfactant and enhances the solubility and dissolution of RLX without requiring addition of organic solvent or high temperature for its preparation; thus, process is less cumbersome and cost effective. But when both methods were compared; HPβCD complexation method showed significant enhancement of drug solubility.

No MeSH data available.


Related in: MedlinePlus

FTIR spectra of (a) raloxifene HCl, (b) HPβCD, (c) modified guar gum, (d) raloxifene-HPβCD inclusion complex and (e) raloxifene-MGG Cogrind mixture.
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fig3: FTIR spectra of (a) raloxifene HCl, (b) HPβCD, (c) modified guar gum, (d) raloxifene-HPβCD inclusion complex and (e) raloxifene-MGG Cogrind mixture.

Mentions: As shown in Figure 3, FT-IR spectra of RLX exhibited characteristic peaks at 1,642.44 (C=O stretching), 1,596.15 (–C–O–C– stretching), 1,466.91 (–S–benzothiofuran), and 905.61 cm−1 (benzene ring). They were well preserved in the RLX-HPβCD complex and RLX-MGG Cogrind mixture. These results indicate that no interaction occurred between drug and excipients.


Solubility Enhancement of Raloxifene Using Inclusion Complexes and Cogrinding Method.

Patil PH, Belgamwar VS, Patil PR, Surana SJ - J Pharm (Cairo) (2013)

FTIR spectra of (a) raloxifene HCl, (b) HPβCD, (c) modified guar gum, (d) raloxifene-HPβCD inclusion complex and (e) raloxifene-MGG Cogrind mixture.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4590818&req=5

fig3: FTIR spectra of (a) raloxifene HCl, (b) HPβCD, (c) modified guar gum, (d) raloxifene-HPβCD inclusion complex and (e) raloxifene-MGG Cogrind mixture.
Mentions: As shown in Figure 3, FT-IR spectra of RLX exhibited characteristic peaks at 1,642.44 (C=O stretching), 1,596.15 (–C–O–C– stretching), 1,466.91 (–S–benzothiofuran), and 905.61 cm−1 (benzene ring). They were well preserved in the RLX-HPβCD complex and RLX-MGG Cogrind mixture. These results indicate that no interaction occurred between drug and excipients.

Bottom Line: The objective of the present work was to enhance the solubility and dissolution of practically water-insoluble drug raloxifene HCl (RLX), for the same two approaches that were used.It was concluded that the prepared inclusion complex showed a remarkable increase in solubility and dissolution of poorly water-soluble drug raloxifene.In the cogrinding mixture, a natural modified gum is used as a surfactant and enhances the solubility and dissolution of RLX without requiring addition of organic solvent or high temperature for its preparation; thus, process is less cumbersome and cost effective.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, R. C. Patel Institute of Pharmaceutical Education and Research, Near Karvand Naka, Shirpur, Dhule, Maharashtra 425405, India.

ABSTRACT
The objective of the present work was to enhance the solubility and dissolution of practically water-insoluble drug raloxifene HCl (RLX), for the same two approaches that were used. In the first approach, drug was kneaded with hydroxypropyl-β-cyclodextrin (HPβCD), and in the second one drug was cogrinded with modified guar gum (MGG). The drug-cyclodextrin complex and drug-MGG cogrind mixtures were characterized by differential scanning calorimetry, X-ray diffraction studies, scanning electron microscopy, and Fourier transform infrared spectroscopy. The solubility and dissolution study reveals that solubility and dissolution rate of RLX remarkably increased in both methods. It was concluded that the prepared inclusion complex showed a remarkable increase in solubility and dissolution of poorly water-soluble drug raloxifene. In the cogrinding mixture, a natural modified gum is used as a surfactant and enhances the solubility and dissolution of RLX without requiring addition of organic solvent or high temperature for its preparation; thus, process is less cumbersome and cost effective. But when both methods were compared; HPβCD complexation method showed significant enhancement of drug solubility.

No MeSH data available.


Related in: MedlinePlus