A systematic study of the dissolution and relative bioavailability of four ginsenosides in the form of ultrafine granular powder, common powder and traditional pieces of Panax quinquefolius L, in vitro and in beagles.

ETHNOPHARMACOLOGICAL RELEVANCE: Panax quinquefolius L (PQ), also known as American ginseng, has been used as a medicinal herb for thousands of years in the Far East, which was wildly used actively in healing the cardiovascular, endocrine and immune systems, in supporting chemoprevention of cancer. MATERIALS AND METHODS: An integrated, rapid, sensitive and reliable UHPLC-ESI-QQQ MS/MS method was validated and successfully applied in a pharmacokinetics study in which four representative ginsenosides were measured in beagle plasma following oral administration of Panax quinquefolius L (PQ) in the form of ultrafine granular powder, standard powder and an extract. RESULTS: Two paired ions ([M+Na](+) in the positive MS process, and two characteristic ions [Q3](+) in the positive MS/MS process) of the target compounds were optimized and selected for improved qualitative and quantitative analysis of ginsenosides in beagle plasma. The relative bioavailability of the target ginsenosides in these three formulations was measured by the pharmacokinetic parameters, including Cmax, Tmax, AUC0-∞ and so on. The ultrafine granular powder had the highest bioavailability, as well as the greatest extent of and fastest dissolution in vitro. CONCLUSION: Our results show that improved formulations of PQ could facilitate the dissolution and promote absorption of the important compounds it contains.

Dissolution difference of ginsenosides from ultrafine granular powder and common powder traditional pieces of Panacis Quinquefolii Radix in vitro.

The dissolution of Panacis Quinquefolii Radix ultrafine granular powder and common powder, traditional pieces in water and simulated gastric juice in vitro was compared, and the effect of particles size of Panacis Quinquefolii Radix on the dissolution was studied. HPLC method was used for determination of five ginsenosides including Rg1, Re, Rb1, Rc and Rd from ultrafine granular powder and common powder, traditional pieces of Panacis Quinquefolii Radix at different points in time, furthermore, the dissolution curves of Panacis Quinquefolii Radix ultrafine granular powder and common powder, traditional pieces were obtained. The dissolution characteristics of the three Panacis Quinquefolii Radix forms were also compared in this study. According to the results, the dissolution rates of ginsenosides from ultrafine granular powder exceeded 90% of the total content with 5 min, significantly higher than that of the other two forms in water in vitro. At the same time, the dissolved amount of the ultrafine granular powder was fourteen percent higher than that of the traditional pieces and eight percent higher than that of the common powder. Under the condition of simulated gastric juice in vitro, the dissolution rates of ginsenosides from ultrafine granular powder were little lower than that of the other two, but the maximum dissolved amount of the former was fourteen percent higher than that of the common powder and five percent higher than that of the extracts. Therefore the conclusion is that micronization of Panacis Quinquefolii Radix contributed to dissolution of effective components.