Study On The Making Of Helicid Dripping Pills And Pharmacokinetics

Helicid (Helicid, formaldehydephenlyl-O-p-D-pyranosylalloside),is an effective component extracted from fruits of Helicia nilagirica Bedd. It is often used in clinic to treat with neurasthenic syndromes,vascular headache,and trigeminalache with high efficiency and low side effect and toxicity. But now only a common helicid tablet are marketed.In this paper, helicid dripping pills were made, the process of helicid dripping Pills has been optimized; We have studyed the quality standards of the the helicid dropping pills, and the concentration of helicid Dripping Pills has been measured; the method for measuring the plasma concentration of helicid has been constructed, we have studied the pharmacokinetics of helicid in rats in vivo and the relative bioavailability of helicid dropping pills in Beagle dogs.We have achieved good results.The results are as follows.1. We developed a liquid chromatography-electrospray ionization mass spectrometry(LC-MS-MS)method for identification and quantification of helicid in rat plasma. Investigated the Pharmacokinetic processes of of helicid in rats at intragastric administration doses of50,100,300mg/kg, the results show that helicid was in linear dynamic processes in50-300mg/kg.2. Helicid dropping pills have been made. Comprehended the two factors of moldability and mouthfeel, we choose sodium citrate and stevioside as correctant. They impoved the taste of helicid.PEG4000and PEG6000(1:1) were combined as a matrix, dimethicone were used as cooling agent,Gum Acacia were uwede as dispersant. We conducted the four factors and and three levels of L9(34) orthogonal experiment with The ratio of drug and matrix, liquid temperature, the amount of correctant, the temperature of cooling agent.Then we got the best condition of dripping process:Drug:matrix=1:7; liquid temperature of90℃; the correctant of3%; cooling agent temperature of3℃3. The HPLC method for mesauring helicid of helicid pills has been established.We extract it by water ultrasound.The mobile phase was acetonitrile water-acetic acid (10:89:1) at the flow rate of1.0ml/min.The column temperature was kept at30℃.This method has advantages such as convenience,speediness,high selectivity and sensitivity,the recovery of98.9%,high intra-and inter-day precisions. It can be used to control the quality of helicid Dripping Pills.We got the conclusion that the content of helicid dripping pills was13.08%.4. The relative bioavailability study of helicid Dripping Pills compared to conventional tablets.The Tmax of beagle dogs oral administration helicid dripping pills is significantly shorter than that of helicid conventional tablets(0.5,0.92,P<0.05), the relative bioavailability of helicid Dripping Pills in beagle dogs is108%.