| Fructus Forsythia is the dry fruit of the plant of Forsythia suspense (Thunb.)Vahl. It is bitter, non-toxic and charactered as slightly cold. Forsythia suspense (Thunb.) Vahl. can clear away heat and toxic, and commonly used in Chinese medicine. It can be usually classified into unripe Fructus Forsythia and ripe Fructus Forsythia due to its different harvest seasons. The shell part of Forsythia is usually used in traditional medicine use, and the seeds are abandoned or only used as a fuel by the local farmers. According to the literature, the seeds weight accounted from 35 percent to 40 percent of the Forsythia fruit, while the volatile is more than 4 percent. After the herbal plant research of the name, medicinal parts, and the original site of the forsythia, it was founded that The root, stem and seed can be medicinal.The present research includes the following sections:(1)The volatil oil was extracted from the seeds of Forsythia suspense (Thunb.) Vahl. with steam distillation method in three different areas of Chian, such as Shangluo in Shaanxi, Luoyang in Henan, and Rizhao in Shandong province. By comparison, the highest average oil yield is in Shandong Rizhao, arriving at 3.18 percent. The essential oil of Forsythia suspense (Thunb.) Vahl., which was extracted in industrial methods in the three different areas, was analyzed and compared by GC-MS technique. The result is that 57,39,37,30 components were respectively separated and identified by their mass spectrogram compared with the standard mass spectrogram, among which the terpenoid was account for more then 70 percent. However, the content and species of the chemical composition were different. For example, Shandong origin had the highest content ofβ-Pinene, accounting for 49.97 percent, and had the special material——Sabinene; Shaanxi and Henan origin had the highest content of Terpineol, especially the total content of 4-Terpineol and alpha.-Terpineol reaching 17.72 percent in Henan origin; the content ofβ-Phellandrene from industrial extraction accounting for 14.91% was more than other three areas, which had only a little even no content in Shandong origin.(2)The crushed level of forsythia seeds, amount of water, and extraction time were investigated to know the impact on essential oil yield of Forsythia suspense (Thunb.).It was adpoted three factors and three level orthogonal experiments. And it was determined of the extraction process of essential oil from Forsythia seeds, which is the medicinal herbs crushed 30 mesh,8 times with water, extraction time 6 hours. In these conditions, essential oil yield of Forsythia seed was 4.59%.(3)The GC method ofβ-pinene in volatile oil of Forsythia seeds was established. Chromatographic condition:Column:HP-5 FFAP(30m X 0.32mm X 0.25um); Column temperature:the temperature program involved in this study consisted of an initial temperature of 40℃,ramped up to 50℃at a rate of 1℃/min followed by a hold at 40℃for 1 min,and continuely ramped up to 70℃at a rate of 5℃/min followed by a hold at 70℃for 1 min,and finally ramped up to 205℃at a rate of 20℃/min followed by a hold at 205℃for 3 min; Injection temperature:250℃; Detector temperature:280℃; FID detector; Carrier gas:N2.Injection volume:luL. Different batches ofβ-pinene in Forsythia seeds'volatile oil was determined,and the mean was 522.8mg/g.(4)A oxford cup assay was used to assess the antimicrobial activity of volatile oil from Forsythia seeds.Eleven bacterial indicator, three common fungi, and three grape pathogenic fungi were used.The results indicated that eleven bacterium were susceptible to volatile oil from Forsythia seeds.There was also antimicrobial activity on three fungi, Penicillium, Rhizopus,and Grey mould.(5)Surveied the bacteriostasis of volatile oil of Forsythiae seeds by transmission electron microscope and SDS-PAGE, supposed the mechanism of bacteriostasis of the volatile oil from Forsythiae seeds that mainly destroied the cell membrane of three indicator bacteria i.e Escherichia coli, Staphylococcus aureus and Saccharomyces cerevisia, induce outleakage of cell content, and to cause apoptosis. Otherwise probably because that it breakdown the protein synthetase of process of growth of the three indicator bacteria, to lead to blocking of cell growth cycle and cell death.(6)The antioxidant activities were assayed through scavenging effects to DPPH and superoxide anion free radical. The result found that essential oil from seeds of Forsythia suspense(Thunb.) Vahl. showed much high antioxidant activity and the clear rate was more than 90 percent, which Has the potential as a natural antioxidant.(7)According to the nature of essential oil from seeds of Forsythia suspense(Thunb.) Vahl., the oil non-ionic surfactant and co-surfactant were screened for the best formula through solubility experiment, orthogonal screen and drawing phase diagram, taking the emulsifying degree, equilibrium time and effective diameter as index. In order to investigate self-emulsifying ability, the micro emulsion of morphology, particle size, dissolution, zeta potential, the rat of self-emulsifyinand the stability in vitro were determined. The result showed that the best formulation of self-emulsifying drug delivery system was made up of the Essential oil of Forsythia suspense (Thunb.) Vahl., Tween-80, ethanol (45:41:14). After being emulsified, the morphology of micro emulsion was homogeneous small spherical drops observed under the electro-microscopy. The particle size was 90.9nm and the selected formulation could completely emulsify in 5 min. The quality of essential oil of Forsythia suspense (Thunb.)Vahl. self-emulsified formulation was stable after strong light exposure, low temperature, thermal-cold cycling for 10 days and constant temperature for 3 months. The self-emulsifying drug delivery system of essential oil of Forsythia suspense (Thunb.) Vahl. is significantly increased in self-emulsified system and the formulation is stable and easy to prepare. The study could provide theoretical foundation for further studying and developing of the essential oil from seeds of Forsythia suspense(Thunb.) Vahl.(8)Through animal acute toxicity test, it was assessed the toxicity of seed oil of Fructus Forsythiae and its SEDDS, their LD50 was 4.111mL/kg and 6.619mL/kg.Respectively. The results indicated that SEDDS can depress the stimulation of drug to stomach and intestine, reduce the toxicity of drug. Simultaneously, the MTT method was adopted, it assaied inhibitory action of seed oil of Fructus Forsythiae and its SEDDS to CaCo-2 cell, also it can be founded that the toxicity of its SEDDS was lower than that of the seed oil itself.(9)It was established the treatment method ofβ-pinene blood plasma sample through the endosomatic pharmacokinetics experiment in rats.The essential oil of Forsythiae Suspensae seeds and it's SEDDS preparations were used. Based on Oral Drug Administration, the drug age curves of seeds essential oil and its suspension was drawn. Combining the compartment model as 1 room, the relative bioavailability of seeds essential oil was evaluated. The results indicated that SEDDS could improve the relative bioavailability of essential oil from Forsythia suspense seeds, so as to become an ideal drug transmission system.(10)In the three samples SEDDS of essential oil from Forsythiae Suspensae seeds,the content ofβ-pinene were evaluated by GC method.they averaged to 236.7mg/g.It provided evidences for the institution of quality standard of Forsythiae Suspensae essential oil's SEDDS.
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