The Stability And Intragastric Buoyant Sustained-Release System Of Sulforaphane(SF)

Sulforaphane (CH3S(O)CH2CH2CH2CH2N=C=S) is one of a class of chemicals called isothiocyanates, which is produced from hydrolyzing thioglucosinolate. It has been identified to be one kind of best chemopreventive and anticancer natural compounds, especially cancer of esophagus, lung cancer, colon cancer and breast cancer, so there is prospect of a very profitable market. It has been established that the content of cruciferous vegetables, such as broccoli, cabbage and cauliflower, is the highest. At present, the preparation studies of Sulforaphane are very weak, while the most of international studies are medicinal studies of cruciferous vegetables; moreover there are few correlative reporters for the stability and medicament of sulforaphane interiorly and overseas. In this article, a Pre-HPLC method for the isolation and purification of sulforaphane in the content of broccoli seeds meal was reported. The flow rate, sample amount were optimized. This method is simple, reliable, specific. The purification of sulforaphane reached to95%.On the other hand, through a serious of experiments, the stability of sulforaphane and its aqueous solution was observed. The concentrations of sulforaphane was determined by HPLC. The stability of sulforaphane and its solution under heat, pH value and light was studied. The average recovery of the assay was100.45%with the relative standard deviation of1.02%. After being treated with long time heating, high temperature, and alkalescent pH, the content of SF was decreased. Sulforaphane was unstable to heat. Sulforaphane appeared as a stable compound when being exposed to light and in acidic condition with pH3.0.A novel intragastric buoyant sustained-release system of Sulforaphane(SF) is proposed for eradication of Helicobacter pylori in vitro evaluation. The design of the delivery system was based on SF and Hydroxypropyl methylcellulose (HPMC, K15M, K100), which is the major rate-controlling polymer excipient to prolong the gastric retention time of the delivery system. All these properties were optimized and evaluated. Results indicated that the tablets consisting of30mg of SF and90mg of HPMC was the best choice for the desirable accumulative release within the period of12h. good stability of SF in the gastric acid environment has been achived. In this case, the total release fraction reached to95.27%and tablet keeps floating. The floating characteristic extending the gastric retention time of the designed system and maintaining an effective localized concentration of sulforaphane were proved. The in vitro drug release followed the Ritger and Peppas equation. The developed system has potential to increase the efficacy of the therapy and improve patient compliance.