The Pharmaceutical Study On Wuhuo Antihypertensive Dropping Pill

Objective By studying the preparation for Wuhuo Antihypertensive Dropping Pill, the quality standards, the vitro dissolutions and the pharmacokinetics of active ingredients in Rats, this thesis aims to select the best preparation, set up the appropriate quality standards, calculate the cumulative dissolutions, and then provide experimental basis for the pill s pharmaceutical assessment.Methods 1.Preparation:With dissolution time, weight coefficient of variation and appearance as comprehensive evaluation index sign, orthogonal design was applied to select the best process.2. The quality standards:Select the active ingredients, icariin evodiamine and rutaecarpin, in pills as the indexes, to set up differentiation method by TLC and determine the contents of HPLC.3. Vitro dissolution:The dissolution rates of Evodiamine were determined by HPLC; and the quantity of Icariin release and the dissolution rates of Icariin were calculated by UV.4. Pharmacokinetics:to study on the Pharmacokinetics, test the consistency of Icariin in Rats plasma after Epimedium extract ig at different sampling time by way of HPLC.Results 1. the best technological parameters of WuHuo Antihypertensive Dropping Pill were as follows:Poloxamer-188 as matrix, proportion of drug and matrix(1:4), temperature of drug fluids of 90℃, proportion of dimethicone and Liquid paraffin (3:1) as refrigerant, temperature of refrigerant was 10℃, the diameter of dropper was 2.5mm, 20 dropping per minute, drop distance was 4cm.2. The differentiation method by TLC and content determination by HPLC could effectively control the pills quality.3. the T0.5 of Pills with PEG4000,PEG4000,Poloxamer-188 as matrixes were 5.38min,6.33min,7.82min; the Td of Pills with PEG4000,PEG4000,Poloxamer-188 as matrixes were 8.29min, 9.76min,10.50min; the Evodiamine stripping capacity of pills with PEG4000,PEG4000,Poloxamer-188 as matrixes were 95.2%,93.6%, 99.1%. the Td of Dropping Pills was 6.68min, and the Td of tablets was 42.51min; The quantity of Icariin release of dropping pills was 99.0%, and that of the tablets was 94.0%.4. the concentration-time profiles of icariin in rats after ig Epimedium extract were shown to fit a two-compartment open model.Conclusion This preparation of pills is simple, practical, stable, and reproducible; the quality standard is highly sensitive, accurate and fast, and could effectively control the pills quality; The total dissolution of the Evodiamine in dropping pills with Poloxamer-188 as matrixes were higher than the dropping pills with PEG. The quantity of Icariin release and the releasing rate of it in dropping pills is larger and faster than the tablets, so the dropping pills are the better medicament form; the distribution, absorption and elimination of icariin in rats could significantly increase and improve by Poloxamer-188.