期刊
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
卷 39, 期 9, 页码 1364-1371出版社
TAYLOR & FRANCIS LTD
DOI: 10.3109/03639045.2012.718784
关键词
Pyridostigmine bromide; taste-masked; orally disintegrating tablets; Solid dispersions; central composite design; bioequivalence
资金
- National Natural Science Foundation of China [30973645]
- Specialized Research Fund for the Doctoral Program of Higher Education [20095503120008]
- Chongqing Natural Science Foundation [CSTC 2012JJB10027]
- Chongqing Education Committee [KJ120321]
The purpose of this study was to evaluate the taste masking potential of novel solid dispersions (SDs) using Eudragit (R) EPO as the excipient when incorporated into the orally disintegrating tablets (ODTs) for delivering a highly soluble drug with an extremely bitter taste. The pyridostigmine bromides (PB) SDs (PBSDs) were prepared by solvent evaporation-deposition method. The physicochemical properties of PBSDs were investigated by means of differential scanning calorimetry and Fourier transformed infrared spectroscopy. The dissolution test showed that only about 8% of PB was released from PBSDs in the simulated salivary fluid in 30 s. Therefore, PBSDs were considered taste-masked and selected for formulation of PBODTs. A central composite design was employed for process optimization. Multiple linear regression analysis for process optimization revealed that the optimal PBODTs were obtained, when the microcrystalline cellulose and crospovidone were 17.16 and 5.55 (%, w/w), respectively, and the average in vivo disintegration time was 25 s. The bitterness threshold of PB was examined by a sensory test, and the threshold value was set as 3 mg in each tablet. Taste evaluation of PBODTs in 18 volunteers revealed considerable taste masking with bitterness below the threshold value. PBODTs also revealed rapid drug release (around 99%, 2 min) in the simulated gastric fluid. The mean PB plasma concentration-time profiles of PBODTs and that of the commercial tablets were comparable, with closely similar pattern. Bioequivalence assessment results demonstrated that PBODTs and the commercial tablets were bioequivalent. In conclusion, PBODTs are prepared successfully, with taste masking and rapid disintegration in the oral cavity.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据