关键词: 卡维地洛, 滴丸, 响应面, 溶出度, 表征

Abstract:

The preparation and characterization of a new dosage forms for improving the dissolution of insoluble drug carvedilol were developed. The carvedilol dropping pills were prepared by solid dispersion technique. The response surface methodology was used to select and verify the optimal preparation process. The dissolution rate in vitro were investigated between self-made dropping pills in four mediums. The drug existing state in dropping pills was identified by DSC，IR spectroscopy，and X-ray diffraction. The results show that the optimal preparation process are as follows: the ratio of drug and matrix is 1∶7, the ratio of PEG6000 and PEG4000 is 1∶3, the drug solution temperature is 75℃, dropping speed is 54min^-1. The dissolution rate in vitro is fastest within 30min in the hydrochloric acid solution of pH1.2, reaching over 90%, followed by pH4.5, pH6.8 and deionized water. The dissolution rate in vitro of three batch dropping pills have similarity（f₂ >85）, which show the stability of the optimal process. The presence state of drugs in dropping pills is mainly amorphous, which can improve the dissolution of insoluble drugs and provide important reference for the development of new oral rapid release dosage forms of carvedilol.

Key words: carvedilol, dropping pill, response surface methodology, dissolution rate, characterization