Development and Evaluation of Praziquantel Solid Dispersions in Sodium Starch Glycolate

被引:26
作者
Chaud, Marco V. [1 ]
Lima, Andrea C. [2 ]
Vila, Marta M. D. C. [1 ]
Paganelli, Maria O. [3 ]
Paula, Fabio C. [4 ]
Pedreiro, Liliane N. [4 ]
Gremiao, Maria P. D. [5 ]
机构
[1] Sorocaba Univ UNISO, Lab Dev & Evaluat Bioact Subst, Sorocaba, SP, Brazil
[2] Univ Metodista Piracicaba, Piracicaba, SP, Brazil
[3] Univ Estadual Campinas, UNICAMP, Campinas, SP, Brazil
[4] Ribeirao Preto Univ UNAERP, Ribeirao Preto, SP, Brazil
[5] Sao Paulo State Univ, UNESP, Araraquara, SP, Brazil
基金
巴西圣保罗研究基金会;
关键词
Praziquantel; Drug bioavailability; Schistosomiasis; Solid dispersion; Co-precipitation; Sodium starch glycolate; INTESTINAL-ABSORPTION; SOLUBILITY;
D O I
10.4314/tjpr.v12i2.5
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Purpose: To develop and characterize solid dispersions of praziquantel (PZQ) with sodium starch glycolate (SSG) for enhanced drug solubility. Methods: PZQ solid dispersion (SD) was prepared using co-precipitation method by solvent evaporation. The ratios of PZQ to SSG were 2:1, 1:1, 1:2, 1:3 (w/w). PZQ solubility was evaluated in purified water, and PZQ dissolution test was carried out in 0.1N HCl. Structural characterization of the dispersions was accomplished by x-ray diffraction (XRD) and infrared spectroscopy (FTIR) while the external morphology of the SDs, SSG and PZQ were studied by scanning electron microscopy (SEM). Mucoadhesion properties of the SD (1:3) and SSG, on mucin disks were examined using texture profile analysis. Results: The highest solubility was obtained with 1:3 solid dispersion, with PZQ solubility of 97.31 %, which is 3.65-fold greater than the solubility of pure PZQ and physical misture (PM, 1:3). XRD results indicate a reduction in PZQ crystallinity while infrared spectra showed that the functional groups of PZQ and SSG were preserved. SEM showed that the physical structure of PZQ was modified from crystalline to amorphous. The amount of PZQ in PM and SD (1:3) that dissolved in 60 min was 70 and 88 %, respectively, and these values increased to 76 and 96 %, respectively. The solid dispersion reduced the mucoadhesive property of the glycolate. Conclusion: Solid dispersion formulation using SSG is a good alternative approach for increasing the dissolution rate of PZQ.
引用
收藏
页码:163 / 168
页数:6
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