Development Of YHN Tablet Based On New Oral Preparation

YHN is a new drug with antiviral activity. There is no oral delivery system of YHN in clinical. In this study, we developed YHN tablets, optimized the tablets formula and manufacturing parameters in order to provide a new oral preparation of YHN to patients.First, we developed the research of YHN prescription and methodology. This work provided the basements for the later researches. The solubility of YHN in water is 1.32 mg·ml-1. And with the increasing of pH, the solubility of YHN increased .The solubility of YHN in the same pH phosphate buffer is higher than its solubility in hydrochloric acid solution .This result showed the solubility of YHN is metal ion-dependent. The oil-water distribution coefficient of YHN is about 1.4.Second, the tablets were prepared using the wet granulation tabletting method. We screened the kind and amount of filler, adhesive and disintegrants using single-factor test and orthogonal design. Last, we chose lactose and microcrystalline cellulose as filler; sodium carboxymethyl starch as disintegrants, 80% ethanol as adhesive, and magnesium stearate as lubricant. The results showed that using sodium carboxymethyl starch (about 3%) as disintegrants and magnesium stearate (0.5%) as lubricant, the appearance of tablets is smooth and the dissolution of tablets is qualified.Third, the qualities of YHN tablets were evaluated, The content of YHN tablets was detected by HPLC. The dissolution of YHN tablets was detected by UV spectrophotometry. We chose distilled water as the dissolution medium and 50rpm speed as the condition of detecting YHN dissolution. The time of 90% dissolution is 45min. the results showed that the appearance, weight difference, content and dissolution were up to quality standard.Last, the stability of YHN tablets was investigated by the influencing test, acceleration test and long-term test. The results of influencing factor test showed the appearance, content and dissolution of YHN tablets are no significant changes in high temperature or strong light conditions. However, in 92.5% humidity, the content and dissolution of YHN tablets decreased significantly. In 75% humidity, the content and dissolution of YHN tablets decreased slightly. So YHN tablets shoulder be packaged with moisture-insulation materials. In accelerated tests, The appearance, content and dissolution of YHN tablets in 3 months accelerated testing were not significantly changed, indicating the stability of YHN tablets is excellent. And we gained the same result in 6-month long-term test.