Add Gatifloxacin And The Ribavirin Soft Capsule And The Capsule Shell

Soft gelatin capsules is a dosageform that can seal the oil, solution, suspension and even the solid or semisolid into the gelatin shell. Currently there are many problems for this dosageform. Most researches focus on the preparation, especially for the TCM soft gelatin capsules. The studies on the preparation of hydrophilic drug are not comnon. There are few researches about the stability and the pharmacokinetics of the soft gelatin capsules. To solve these problems, much researches were carried out here.In order to find the effect of the formulation factor on the dissolution rate of gelatin shell, UV method was set up here to determine the release of carmine red from the gelatin shell. The effects of some additions on the dissolution rate of gelatin shell were studied here. The results showed that the dissolution rate changed irregularly wthe the increase of the ratio of the gelatin to glycerine. The cane sugar, acid, sodium chloride and peg 400 can raise the solubility of the gelatin shell. And the plasticizer, CMS-Na, SDS and PVPP have little effect on the dissolution rate.With the vegetable oil as the diluents bases, hydrophobic drug (gatiflocaxin) and hydrophilic drug (ribavirin) soft gelatin capsules were prepared.During the content determination, the whole soft gelatin capsules were dissolved completely in the water, which can assure the accuracy of the determination. Stress tests, accelerated tests and long-term tests were carried out here, the results proved the good stability of the two soft capsules.With three crossover design,the pharmacokinetics of gatiflocaxin soft gelatin capsules and dispersed tablets in beagles dogs was studied comparing with the reference tablet. The t_1/2, T_max, C_(?)ax and AUC of gatiflocaxin soft gelatin capsules , dispersed tablets and reference tablets were: (9.01±2.19) hrs, (9.20±1.14) hrs and (9.50 ±1.24)hrs; (1.583 ± 1.021) hrs, (1.500 ± 0.316) hrsand (2.000 ± 0.316) hrs; (10.61±1.63) μg·ml^-1, (10.85±1.51)μg·ml^-1 and (11.11 ± 1.09) μg·ml^-1; (141.81 ±33.88)μg·h·ml^-1,(144.61 ±28.93)μg·h·ml^-1 and (143.84±33.96)μg·h·ml^-1.The relative bioavailability of gatifloxacin soft capsules and dispersed tablets were (104.19 ± 33.57)% and (104.27 ± 23.45)%.The results of variance analysis showed that there is no significant difference among these dosageform. The two one-sided test results of single oral administration demostrated that these three dosage forms were bioequivalent.