The Investigation Of Ubenimex Orally Disintegrating Tablets

Ubenimex is a compound which has two peptides.It was mainly used to assist treatments of the tumor chemotherapy,bone marrow hyperplasia and pure red cell agensis in clinic. It has below good qualities: precise curative effects,low side effects. But the route dosage form of Ubenimex brought some problems for taking medicine and absorption, The emerging of orally disintegrating tablet solved the difficult matter effectually, which improved compliance of treatment. Orally disintegrating tablet could disintegrate or dissolve without water. The type was applicable to child, old men and patients who swallowed difficultly. Orally disintegrating tablets did not only disintegrate rapidly, but also carried large medicine and had good eating. After disintegration, tablets did not have gravel feeling, and the medicine in the mouth cavity remained fairly little. The type was not sensitive to high heat, Preparation and packing were simple, Building price was cheap. Combining the characteristics of Ubenimex and orally disintegrating tablet, The thesis made Ubenimex into orally disintegrating tablet, and investigated a series of indexes. This offered basis for solving the problem of the cancer sufferers who put medicine diffcultly.Passed to investigate the performance of accessories, the thesis ensured the kinds of accessories: L-HPC,MCC,PVPP,CMC-Na were disintegrators, Ste was edulcorator, Man was diluent; According to the single factor experiments and orthogonal experiment, the thesis ensured the ratio of L-HPC:MCC was 1:9,the proportion of CMC-Na was 3%,the proportion of starch paste was 10%,the proportion of Man was 10%,the proportion of magnesium stearate was 5%; The influence sequence of each factor one by one in order was: Man>L-HPC:MCC>CMC-Na. The study ensured the best prescription: 50% Man,L-HPC:MCC=1:9,3% CMC-Na,proper Ste and magnesium stearate. In this basis, the text determined the prescription of Ubenimex orally disintegrating tablets. The joining way of the collapses adopted inside addition, Preparing Ubenimex orally disintegrating tablets accorded to wet granulation performing, and carring on a quality evaluation to the orally disintegrating tablets. The results of angle of repose and compression degree indicated powder body liquidity was good; The hardness of orally disintegrating tablets was in the extents of 29.4N–39.2N, The disintegration limits were in 30s, met the requests; Slice heavy difference and the content even degree were both within the scope of limit, The sign was also up to standard.The article first established the standard of Ubenimex orally disintegrating tablets, examined dissolution,content and related substance of Ubenimex orally disintegrating tablets making use of RP-HPLC. The result displayed dissolution,content and related substance were all met the medical dictionary; The technology result revealed the method had high sensitivity and degree of confidence. Then the article undertook a research on the stability of Ubenimex orally disintegrating tablets. Impact factor experiments(high temperature: the samples were placed 10 days in the terms of 40,60,80℃to examine various index signs; illumination: the samples were put down the 40W sunlight for 10 days, examining various index signs in the first,the third,fifth,tenth day; high humidity: under the conditions of relative humidity 75% and 92.5%, the samples were placed for 3 days under 25℃, examining various index signs every day) illustrated orally disintegrating tablets were not sensitive to high temperature and illumination; Under the high humidity condition, only the external appearance of orally disintegrating tablets took place slight changes, the rest index signs were normal; Accelerated test (40±2℃, RH90%±5%) certificated the related index signs of orally disintegrating tablets did not take place vatiety at 0,1,2,3months, But in the sixth month, the external appearance of orally disintegrating tablets took place slight changes, the rest signs did not. Long test run(20±2℃, RH60%±10%)certificated the related index signs of orally disintegrating tablets did not take place vatiety at 0,3,6,9months, But in the twelfth month, the external appearance of orally disintegrating tablets took place slight changes, the rest signs did not.The thesis studied the pharmacokinetics of Ubenimex orally disintegrating tablets initially and built up RP-HPLC method to examine Ubenimex contents of animal blood plasma. The technology experiment results manifested the method had high accuracy and good reproducibility. The thesis made use of separate room model to compare the pharmacokinetics parameters of self-made orally disintegrating tablets to Ubenimex capsules. The results showed that Cmax of orally disintegrating tablets was higher than capsules, Tmax of orally disintegrating tablets was faster than capsules; The both average bioavailabilities were 115.2%,106.2%. Applying the square differs and the t examine to analyze the main parameters, the parameters showed the two medicines had not significant differences (P>0.05), AUC and Cmax isoeffect examination results of two medicines indicated, Ubenimex orally disintegrating tablets and Ubenimex capsules had bioequiavailability.