Study On The New Dosage Form And Pharmacokinetics Of Helicid

Helicid is an effective component extracted from wilding plant Helicid Hilgirica Beed, and its chemical name is p-formylphenyl O-β-D allopyranoside. It has clear pharmacological effects and has been widely used in the treatment of obstructive sleep, anxiety, depression, headache and so on. But now only a common helicid tablets was marketed, and little research about the pharmacokinetics of the helicid. In this paper, two new kinds of helicid tablets named helicid dispersible tablets and helicid fast-disintegrating oral tablets were made. Plasma drug concentration of helicid, and its pharmacokinetics were determinated by HPLC. Pharmacokinetics and bioavailaility of helicid-phospholipid complex in mouse were also investigated. The results are as follows: 1. helicid dispersible tablets and helicid fast-disintegrating oral tablets have been made. Some methods were used to control its quality. These two kinds of tablets are all take easily and taste fine. The disintegrating time of them were within 30 seconds and dissolved much more quickly than that of the commercial tablet. 2. The method for measuring the plasma concentration of helicid has been constructed. Acetonitrile was used to denature plasma proteins. Chromatographic separation of helicid was performed on a C-18 reversed phase column using a mixture of acetonitrile and acetum (1%) (10:90, v/v) as the mobile phase and ultraviolet detection (270 nm). This method has some advantages such as convenience, speediness and sensitivity. The plasma sample has good stability and its recovery was up to 80%. The inter-and intra-day precision and accuracy were all very good. 3. The pharmacokinetics of helicid in rats was studied at high dose (500 mg·kg^-1), the pharmacokinetic parameters were different from these of the medium and low dose (100 and 200 mg·kg^-1). The difference showed that the pharmacokinetics of helicid is nonlinear at the high dose. The relative bioavailability of helicid phytosomes to the powder is 147%, while that to the philipid mixtures is 122%. The increase in relative bioavailability shows that the chemical/physical properties of phytosoems may have been greatly improved.