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Enhancement of solubility and dissolution rate of poorly water soluble raloxifene using microwave induced fusion method
Patil, Payal Hasmukhlal; Belgamwar, Veena Sailendra; Patil, Pratibha Ramratan; Surana, Sanjay Javerilal.
Affiliation
  • Patil, Payal Hasmukhlal; R.C. Patel Institute of Pharmaceutical Education and Research. Department of Pharmaceutics. Shirpur. IN
  • Belgamwar, Veena Sailendra; R.C. Patel Institute of Pharmaceutical Education and Research. Department of Pharmaceutics. Shirpur. IN
  • Patil, Pratibha Ramratan; R.C. Patel Institute of Pharmaceutical Education and Research. Department of Pharmaceutics. Shirpur. IN
  • Surana, Sanjay Javerilal; R.C. Patel Institute of Pharmaceutical Education and Research. Department of Pharmaceutics. Shirpur. IN
Braz. j. pharm. sci ; 49(3): 571-578, July-Sept. 2013. ilus, tab
Article de En | LILACS | ID: lil-689911
Bibliothèque responsable: BR1.1
ABSTRACT
The objective of the present work was to enhance the solubility and dissolution rate of the drug raloxifene HCl (RLX), which is poorly soluble in water. The solubility of RLX was observed to increase with increasing concentration of hydroxypropyl methylcellulose (HPMC E5 LV). The optimized ratio for preparing a solid dispersion (SD) of RLX with HPMC E5 LV using the microwave-induced fusion method was 15 w/w. Microwave energy was used to prepare SDs. HPMC E5 LV was used as a hydrophilic carrier to enhance the solubility and dissolution rate of RLX. After microwave treatment, the drug and hydrophilic polymer are fused together, and the drug is converted from the crystalline form into an amorphous form. This was confirmed through scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) studies. These results suggested that the microwave method is a simple and efficient method of preparing SDs. The solubility and dissolution rate of the SDs were increased significantly compared with pure RLX due to the surfactant and wetting properties of HPMC E5 LV and the formation of molecular dispersions of the drug in HPMC E5 LV. It was concluded that the solubility and dissolution rate of RLX are increased significantly when an SD of the drug is prepared using the microwave-induced fusion method.
RESUMO
O objetivo do presente trabalho foi aumentar a solubilidade e taxa de dissolução do cloridrato de raloxifeno (RLX), que é pouco solúvel em água. A solubilidade do RLX aumentou com o aumento da concentração de hidroxipropilmetilcelulose (HPMC E5 LV). A proporção otimizada para a preparação de uma dispersão sólida (DS) de RLX com HPMC E5 LV utilizando o método de fusão induzida por microondas foi de 15 (p/p). A energia do microondas foi usada para preparar DS. O HPMC E5 LV foi utilizado como veículo hidrofílico para aumentar a solubilidade e a taxa de dissolução de RLX. Após o tratamento por microondas, o polímero hidrofílico e o fármaco são fundidos em conjunto, sendo o fármaco convertido da forma cristalina para a amorfa. Confirmou-se por meio de microscopia eletrônica de varredura (MEV), calorimetria exploratória diferencial (DSC) e difração de raios X do (PXRD). Estes resultados sugerem que o método de microondas é simples e eficiente para a preparação de DS. A solubilidade e taxa de dissolução de DS foram aumentadas, significativamente, em comparação com RLX puro devido às propriedades tensoativas e umectantes de HPMC E5 LV e à formação de dispersões moleculares do fármaco em HPMC E5 LV. Concluiu-se que a solubilidade e a taxa de dissolução de RLX foram significativamente aumentadas quando a DS do fármaco é preparada utilizando o método de fusão induzida por microondas.
Sujet(s)
Mots clés

Texte intégral: 1 Indice: LILACS Sujet Principal: Solubilité / Chlorhydrate de raloxifène / Dissolution / Micro-ondes langue: En Texte intégral: Braz. j. pharm. sci Année: 2013 Type: Article

Texte intégral: 1 Indice: LILACS Sujet Principal: Solubilité / Chlorhydrate de raloxifène / Dissolution / Micro-ondes langue: En Texte intégral: Braz. j. pharm. sci Année: 2013 Type: Article