The Preparation And Quality Evaluation Of Xiaochuan Gel Ointments

1 objectiveThis research was to develop Xiaochuan compound,a traditional day moxibustion therapy as a kind of safe,effective and convenient Xiaochuan gel Ointments.Through optimizing the extraction technique,preparation technology,and establishing the quality standard,Xiaochuan gel Ointments was prepared.This research can provide experimental basis for clinical medication.And the Experimental methods and technical means can provide new idea and reference for the secondary development of other famous topical formulations.2 Methods2.1 Optimization of the Extraction Technique of Xiaochuan gel Ointments A method used for the determination of Sinapine Thiocyanate was established by HPLC.An orthogonal test method was used to investigate the extraction time,solvent volume,the concentration of alcohol and backflow extract times.The extraction rate of sinapine thiocyanate was considered as the evaluation index to optimize the extraction technique.2.2 The preparation of Xiaochuan gel OintmentsThe influential factors of matrix are screened out on the basis of preliminary test.The orthogonal test method was used and tacking strength,cohesive strength,uniformity,comfort,spread of the paste,and the effect of different penetration enhancers on the transdermal penetration were used as evaluation indexes to optimize the formulation of matrix.2.3 The quality evaluation of Xiaochuan gel OintmentsOn the quality standard requirement of gel Ointments,appearance,ointment content,adhesion,formability,sinapine thiocyanate content,Skin Irritation of Xiaochuan gel Ointments were investigated.3 Results3.1 Optimization of the Extraction Technique of Xiaochuan gel OintmentsWe developed the method of detecting sinapine thiocyanate by HPLC-UV method.Chromatographic column:Dikma platisil ODS(5 ?m,250mm×4.6mm)column;guard column:Phenomenex guard column;mobile phase:acetonitrile-mol · L-1 KH2PO4((14:86);flowing rate:1.0mL · min-1;detecting wavelength:326nm;column temperature:30?.Under the chromatographic condition,sinapine thiocyanate had symmetrical peaks and the retention time of control,sample,control herbs were consistent.The precision and stability could meet the analytical requirements.The method was specific and the negative sample had no interference,which can be used to the quantitative determination of sinapine thiocyanate.The optimized extraction technique was as follows:the medicinal material was extracted for 2 times with six fold amount of 70%alcohol,2hours per time.The optimized technique is reasonable which can provide a good basis for the continuing research of transdermal absorption of this compound prescription.3.2 The preparation of Xiaochuan gel OintmentsThe optimal matrix formulation of Xiaochuan gel Ointments is Viscomate NP-700:NP700:Dihydroxy aluminum aminoacetate:Carbomer;PVP:Glycerol:Tartaric acid:EDTA:=1.5:0.04:15:1.5:8:0.2:0.05.The tacking strength,holding strength and sensory of optimal matrix formulation was good,and the gel Ointments was easy to use.The kinetic parameters of percutaneous absorption,such as permeability amount,penetration rate were evaluated with different enhancers.The results showed that 3%Azone was the best penetration enhancer.3.3 The quality evaluation of Xiaochuan gel OintmentsThree batches of Xiaochuan gel Ointments with optimal matrix formulation were prepared.And the appearance,ointment content,adhesion,formability,transdermal permeation in vitro,skin irritation was investigated.The result shows that they can stick on the 23th steel ball,and cohesive strength time is 35s.The ointment content of Xiaochuan gel Ointments was 23.2765g per gel Ointments.The formability of Xiaochuan gel Ointments meet the requirements of Chinese pharmacopoeia(2010).The sinapine thiocyanate content of Xiaochuan gel Ointments was 76.62mg per gel Ointments.Xiaochuan gel Ointments can observably reduce the skin irritation effect.No irritation was observed in integral skin,but low-grade irritation occurred in injured skin of rabbits.