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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

DSC thermogram 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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fig1: DSC thermogram 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 1, the thermograms of the RLX, HPβCD, and MGG showed respective endothermic peaks at 266.44°C, 97.46°C and 64.95°C corresponding to their melting points. In the thermogram of RLX-HPβCD complex, the peak of drug disappeared indicating the complexation of RLX with cyclodextrin, whereas in DSC spectra of RLX-MGG Cogrind mixture, the peak of drug was observed, but the intensity was reduced suggesting the conversion of raloxifene hydrochloride from crystalline form to amorphous form.


Solubility Enhancement of Raloxifene Using Inclusion Complexes and Cogrinding Method.

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

DSC thermogram 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

fig1: DSC thermogram 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 1, the thermograms of the RLX, HPβCD, and MGG showed respective endothermic peaks at 266.44°C, 97.46°C and 64.95°C corresponding to their melting points. In the thermogram of RLX-HPβCD complex, the peak of drug disappeared indicating the complexation of RLX with cyclodextrin, whereas in DSC spectra of RLX-MGG Cogrind mixture, the peak of drug was observed, but the intensity was reduced suggesting the conversion of raloxifene hydrochloride from crystalline form to amorphous form.

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