A rotundine-polyion complex(PIC)release system was prepared first by granulation of rotundine containing chitosan acetate solution and then by complexing with carboxymethyl glucomannan(CMGM)solution on the granular su...A rotundine-polyion complex(PIC)release system was prepared first by granulation of rotundine containing chitosan acetate solution and then by complexing with carboxymethyl glucomannan(CMGM)solution on the granular surface.The granules have an average diameter of 1.38-1.53 mm and the drug content reaches 62.89％.The external release tests showed T_(50) to be 45 rain and the total release time 4 h in an artificial gastric juice,while no more than 60％ of the drug was released in the same period of time in an ar- tificial intestinal fluid.The various factors affecting the external release were examined.展开更多
Aim The aim of the present study was to prepare tablets which can rapidlydisintegrate in saliva, containing active ingredient in high dose (37.5% W/W). Methods Rapidlydisintegrating tablets containing rotundine were p...Aim The aim of the present study was to prepare tablets which can rapidlydisintegrate in saliva, containing active ingredient in high dose (37.5% W/W). Methods Rapidlydisintegrating tablets containing rotundine were prepared by direct compression, wet granulation andmoulding, respectively . Different disintegrants and excipients were decided by single factor test.The typical disintegration time measurement and a new method of wetting time measuring wereintroduced for assessing rapidly disintegrating tablets. Results The tablets (80 mg) prepared bydirect compression have the crushing strength of 4.0 kg ?mm^(-2) and rapidly disintegratewithin 15 s in the saliva of healthy volunteers; the tablets prepared by wet granulation also havesufficient strength, a little longer but acceptable disintegration time (within 25 s in saliva) ;and the tablets obtained by moulding show disintegration within 40 s in saliva but low strength (2kg·mm^(-2)) . Disintegration time profiles of tablets are similar to those of wetting time, and thedisintegration and wetting times in vitro are similar to the disintegration time in vivo, thelatter having higher correlation with that in oral cavity. Conclusion The rapidly disintegratingtablets can be prepared by using these three techniques and excipients. Both in vitro disintegrationtime and wetting time are necessary indexes for judgment of in vitro disintegration profile.展开更多
基金This project was supported by National Natural Science Foundation of China
文摘A rotundine-polyion complex(PIC)release system was prepared first by granulation of rotundine containing chitosan acetate solution and then by complexing with carboxymethyl glucomannan(CMGM)solution on the granular surface.The granules have an average diameter of 1.38-1.53 mm and the drug content reaches 62.89％.The external release tests showed T_(50) to be 45 rain and the total release time 4 h in an artificial gastric juice,while no more than 60％ of the drug was released in the same period of time in an ar- tificial intestinal fluid.The various factors affecting the external release were examined.
文摘Aim The aim of the present study was to prepare tablets which can rapidlydisintegrate in saliva, containing active ingredient in high dose (37.5% W/W). Methods Rapidlydisintegrating tablets containing rotundine were prepared by direct compression, wet granulation andmoulding, respectively . Different disintegrants and excipients were decided by single factor test.The typical disintegration time measurement and a new method of wetting time measuring wereintroduced for assessing rapidly disintegrating tablets. Results The tablets (80 mg) prepared bydirect compression have the crushing strength of 4.0 kg ?mm^(-2) and rapidly disintegratewithin 15 s in the saliva of healthy volunteers; the tablets prepared by wet granulation also havesufficient strength, a little longer but acceptable disintegration time (within 25 s in saliva) ;and the tablets obtained by moulding show disintegration within 40 s in saliva but low strength (2kg·mm^(-2)) . Disintegration time profiles of tablets are similar to those of wetting time, and thedisintegration and wetting times in vitro are similar to the disintegration time in vivo, thelatter having higher correlation with that in oral cavity. Conclusion The rapidly disintegratingtablets can be prepared by using these three techniques and excipients. Both in vitro disintegrationtime and wetting time are necessary indexes for judgment of in vitro disintegration profile.
