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.
Highlights
Solubility of a drug is an important property that mainly in uences the extent of oral bioavailability
Raloxifene is available in salt form as raloxifene HCl [3]. e drug is poorly absorbed from the gastrointestinal (GI) tract ; it is important to enhance aqueous solubility and dissolution rate which may lead to enhancement of bioavailability from its oral solid dosage forms
E present study was carried out to investigate the inclusion complex of raloxifene HCl and HPββCD in the solid state and the RLX-modi ed guar gum (MGG) Cogrind mixture using Xray diffractometry (XRD) differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), and scanning electron microscopy (SEM). e objective of this study was to enhance solubility and dissolution rate of RLX which may lead to enhancement of bioavailability of this drug [1, 8, 9]
Summary
Solubility of a drug is an important property that mainly in uences the extent of oral bioavailability. Raloxifene (marketed as Evista by Eli Lilly and Company) is an oral second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It is 2-(4-hydroxyphenyl)-3-({4-[2(piperidin-1-yl) ethoxy] phenyl} carbonyl)-1-benzothiophen-6-ol that has estrogenic actions on bone and antiestrogenic actions on the uterus and breast. E drug is poorly absorbed from the gastrointestinal (GI) tract ; it is important to enhance aqueous solubility and dissolution rate which may lead to enhancement of bioavailability from its oral solid dosage forms. In the second approach, Cogrinding of raloxifene HCl with modi ed guar gum was done. E present study was carried out to investigate the inclusion complex of raloxifene HCl and HPββCD in the solid state and the RLX-MGG Cogrind mixture using Xray diffractometry (XRD) differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), and scanning electron microscopy (SEM). e objective of this study was to enhance solubility and dissolution rate of RLX which may lead to enhancement of bioavailability of this drug [1, 8, 9]
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