Schisandra Sedative And Hypnotic Separation Of The Active Site And Its Dispersible Tablets

Insomnia is a subjective experience that sleeping time and (or) quality is less than demand. Long insomnia not only damages the thinking activities, but also affects people's immune system. Many patients had been treated insomnia with the long-term use of chemical sedative and hypnotic drugs, but certain drugs have been limited for their side effects and addiction in clinic. On the other hand, recent studies have shown herbal drugs exert good sedative and hypnotic effects with few side effects and little toxicity, such as Fructus Schisandrae, which extensively used as traditional Chinese medicine in clinic with the functions of inducing astringency, replenishing and promotion production of body fluid and tonifying the kidney to relieve mental strain. But there are few reports about its theory basement, and the studies on the chemical composition and the effectiveness between Schisandra chinensis and S. sphenanthera with the different price, have not been researched deeply. The effective extracts of Fructus Schisandrae had been screened on sedative and hypnotic activity, and the pharmacodynamic differences between Schisandra chinensis and Schisandra sphenanthera had been compared. Schisandrae dispersible tablets were prepared and systematically studied from the areas of preparation technics, quality standards, stability, rudiment pharmacodynamics and acute toxicity.1. The effective sedative and hypnotic extract of Fructus Schisandrae has been studied preliminaryly. Through observing the effects on spontaneous activity and coePentobar- bital in mice, investigated the sedative and hypnotic effects of different extracts of Furctus Schisandrae. Studies showed that the effective compound should be found in the Petroleum ether and Ethanol extracts, compared with S. sphenanthera, Schisandra Chinensis showed higher sedative effects, but similar hypnotic effects. Respecting the significant differences in the price, the paper chose S. sphenanthera as the study object; as the water extract also showed a little hypnotic effects, and it has many reported effects such as immunoloregulation, anti-aging and anti-oxidation, the paper adopted the method of alcohol-water extraction to extract S. sphenanthera, consisting of alcohol reflux and water decoction. Optimal alcohol extraction conditions were determined as follows: volume parts of the composition of alcohol-water solvent 75%, ratio of material to liquor 1:12, thrice of extraction at 85℃each for 1h. Optimal water extraction conditions were studied by other member of our subject group and determined as follows: boiling water, ratio of material to liquor 1:10, thrice of extraction each for 2h. At the same time, compared the sedative and hypnotic effects of the alcohol extract and the alcohol-water extract of S. sphenanthera, studied showed that the alcohol-water extract had obviously better sedative and hypnotic effects than the alcohol extract.2. Preparation technique of Schisandrae dispersible tablets has been studied. Taking the extract of S. sphenanthera as the remedium cardinale, disintegration time as the main index, the accessories were selected through mono-factor testing, and uniform design was exploited to optimize the preparation technique. The optimum preparation technique of Schisandrae dispersible tablets was: weight 500mg, the extract 33%, crspolyvinylpyrrolidone(PVPP) 8%, low-substituted hydroxypropyl cellulose(L-HPC) 8%, microcrystallisate cellulose(MCC) 20%, lactose 29%, micronized silica gel 1%, magnesium stearate 1%, and the addition method of disintegrant was one half inside and other half outside. The disintegration time and dispersible uniformity of tablets accorded with demand of Chinese pharmacopeia (2005 edition). The dissolution was determind in vitro, relative accumulative dissolution of schisantherin A and schisandrin A were more than 85% within 30min, and accorded with demand of Chinese pharmacopeia (2005 edition).3. The quality standard of Schisandrae dispersible tablets has been established. The elements were identified by TLC: the silica gel thin layer plate GF₂₅₄ and the developing agent consisting of a mixture of N-hexane-acetic ether (8:3) were used, and detected under uviol lamp (254nm). The content of schisantherin A and schisandrin A were determined by HPLC. A Hypersil ODS2 column and the mobile phase consisting of a mixture of methanol-water (73:27) were used with the wavelength of 254nm and the flow rate of 0.8 mL/min at 35℃. The method was sensitive, reproducible and accurate. The content of schisantherin A and schisandrin A should not be less than 1.2mg and 0.9mg per tablet.4. The preliminary stability of Schisandrae dispersible tablets has been studied with accelerated test. The result indicted that the character, identification, detections and content determination were remain valid. It showed that the quality of Schisandrae dispersible tablets was stable.5. Rudimentery pharmacodynamics and acute toxicity tests have been carried out. Through observing the effects on spontaneous activity and coe-Pentobarbital in mice, compared the sedative and hypnotic effects of Schisandrae dispersible tablets and Schisandrae syrup. Studies showed that Schisandrae dispersible tablets have obvious sedative and hypnotic effects, and were better than Schisandrae syrup under the identical dosage. Acute toxicity test showed that Schisandrae dispersible tablets had no obvious toxic reaction.