Pharmaceutical Research And Safety Evaluation Of The Shuangbai Film Spraying Agent

ObjectiveTo screen the extraction technology、the concentration technology and the filming formula of the Shuangbai film spraying agent;to establish the quality evaluation system of the Shuangbai film spraying agent; to investigate the long-term stability tentatively and the skin irritation of the Shuangbai film spraying agent.Methods(1)Using the content detection of these components, such as Aloeemodin, Rhein, Rheum emodin, ChrysopHanol, PHyscion, Berberine, Palmatine chloride, Quercitrin and Gallic acid, as the index, screen the extraction solvent by extracting the all prescription using55%,75%or95%ethanol respectively.(2) Combining the content detection of these components, such as Aloeemodin, Rhein, Rheum emodin, ChrysopHanol, PHyscion, Berberine, Palmatine chloride, Quercitrin and Caffeic acid, and the concentrated volume, temperature, relative density as indexes, screen the concentration technology.(3)Using leachability, filming time, film performance as indexes, do filming experiments with polyvinylpyrrolidone(PVP-K30) and Hydroxypropyl Methyl Cellulose (HPMC) and confirm the dosage and the proportion of them.(4)Establish the quality evaluation system of the Shuangbai film spraying agent including TLC identification, the content detection of index components, characteristic atlas, checking items consist of viscosity, relative density, pH value, filming time, ethanol content, capacity, gushing total, film performance.(5)Investigate the preliminary stability for6months of the Shuangbai film spraying agent through these items of character, odor, identification, gushing amount, the content determination, spray bottle color change.(6)Investigate the skin irritation of the Shuangbai film spraying agent by spraying it to the back of white guinea pigs to observe animals have these phenomenon of erythema, edema or not.Results(1)The contents of Aloeemodin, Rheum emodin, ChrysopHanol, PHyscion, Palmatine chloride and Berberine in the75%ethanol-extraction liquid were all higher than in the55%or95%ethanol-extraction liquid, but Rhein was lower because of the instability itself possibly. Therefore, the extract method of the Shuangbai film spraying agent was that extracting the all prescription three times for1hour each time by using75%ethanol. The dosage of75%ethanol was8times,5times and5times of the all prescription.(2)Respectively concentrating the75%ethanol-extraction liquid from500mL to400mL,300mL,200mL, the concentration of Aloeemodin, Rhein, Rheum emodin, Palmatine chloride and Berberine were all increasing gradually, but ChrysopHanol and PHyscion were increasing at first, and then reducing, for the reason was both of them heated volatile or their solubility brought down as alcohol depression. Ethanol was reducing gradually. Its itethanol content was38.4%when it was concentrated to200mL. When the concentrated density was0.92(50℃), the contents of Aloeemodin, Rhein, Rheum emodin, Berberine were all highest and other contents were not that big of a difference. Synthetically comparing of concentration of the index components and the content of ethanol, it was more reasonable to concentrate the ethanol-extraction liquid in80℃and made the relative density reach0.92under50℃.(3)When the dosage of K30was5%and the dosage of HPMC was0.4%, the Shuangbai film spraying agent had small leachability and its skinning time was3’37". Tt could become film which Edge was smooth, the quality was uniform and dense, components and accessory integrate totally.(4)Identificating Radix et Rhizoma Rheiand, Amur CorKtree BarK, Cacumen Platycladi in TLC in the three equal lots of the Shuangbai film spraying agent, there were the same color spots at the corresponding position of reference substance. or control medicinal materials and the negative was not interferential. The method was good repeatability and strong specificity. Detect the average principal component contents of the three equal lots in HPLC which Aloeemodin were50.98μg·mL-1, Rhein were124.14μg·mL-1, Rheum umodin were89.17μg·mL-1, ChrysopHanol were63.81μg·mL-1, PHyscion were14.94μg·mL-1, Palmatiine chloride were52.31μg·mL-1, Berberine were117.16μg·mL-1, Callic acid were158.25μg·mL-1, Quercitrin were148.39μg·mL-1. the RSD of the relative retention time was less than2%and the peak area was less than5%in the precision, the stability and the repeatability tests of the feature mapping study methodology. The method was good accuracy, repeatability and stability. In the three equal lots of the Shuangbai film spraying agent, the average viscidity was14.8mpa·s, the average relative density was0.9647, the average pH valu was4.4, the average skinning time was3’37", the average content of ethanol was33.67%, the average gushing total was45.74g. They could become film which Edge was smooth, the quality was uniform and dense, components and accessory integrated totally.(5)Preliminary stability test showed that, after the Shuangbai film spraying agent was placed six months at room temperature, the character, identification, the color of the spray bottle had no significant change. The stability of Aloeemodin, Rhein, Rheum emodin, gallic acid, Palmatine hydrochloride, berberine hydrochloride and quercetin was good in the Shuangbai film spraying agent. They were appropriate for the content control indexes of the Shuangbai film spraying agent. But ChrysopHanol and PHyscion were counter to them.(6)There were no erythema, edema and abnormal phenomenon to the white guinea pigs of the complete skin group and the breakage skin group.Conclusion(1) The medicine dosage of the alcohol extraction method is only one seventh of the water extraction method. The alcohol extraction method of Shuangbai powder saves medicinal materials greatly and improves the utilization rate of medicinal materials.(2)The study confirms the dosages of film material combination consisting of polyvinylpyrrolidone and hydroxypropyl methyl cellulose. They can become film which Edge is smooth, the quality is uniform and dense, components and accessory integrate totally. The film time is short.(3)In the study, it can observe the membrane structure by microscope and taking pictures with imaging software. Taking the syncretic situation of membrane materials and components for index, it can screen the varieties and dosages of film materials. This method can be used to screen film materials of film spraying agent.(4)The quality is stability and controllable preliminarily. There is no irritation to skin.