期刊
JOURNAL OF INCLUSION PHENOMENA AND MACROCYCLIC CHEMISTRY
卷 83, 期 3-4, 页码 401-409出版社
SPRINGER
DOI: 10.1007/s10847-015-0569-9
关键词
Altretamine; Cyclodextrin; Matrix tablet; Sustained release
资金
- UGC-BSR
- Department of science and technology (DST-FIST), CCOST/MRP [1926]
- UGC-MRP [42-706/2013 (SR)]
The aim of present study was to prepare sustained release tablets of a poorly soluble anticancer drug using cyclodextrin complexation as a potential approach. Altretamine is an alkylating agent practically insoluble in water and posses poor oral bioavailability. For this, the most suitable binary system of ALT-HP-beta-CD was selected to improve the aqueous solubility and then embedding the complexed drug into a matrix tablet with fusion method. Tablets were prepared using glycerol monostearate (GMS) and polyethylene glycol 4000 (PEG4000). Complexes were prepared at different ratios and mixed with other excipients to achieve tablets with efficient dissolution profile complying with the requirements for sustained delivery of solid dosage forms. Results of Fourier Infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and X-ray diffractometry (XRD) proved that kneading was most efficient technique for preparation of amorphous cyclodextrin inclusion complex with ALT and entrapping this complex into tablet. Dissolution profile of ALT was enhanced significantly in pH 6.8 from the binary system and significant within the limits (t test Student p < 0.05). The release kinetics of the tablets showed that diffusion was responsible for controlling the release from the tablets.
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