Research On Transdermal Characteristic And Preparation Of Sophorae Flavescentis Radix Antipruritic Prescription

Sophorae Flavescentis Radix antipruritic prescription is mainly composed of Sophorae Flavescentis Radix,Cnidii Fructus,Kochiae Fructus,Atractylodis Rhizoma,Menthae Haplocalycis Herba.It is a experience prescription for the treatment of skin pruritus.However,the percutaneous absorption of drugs will be affected by the cuticle barrier,which seriously hinders the percutaneous penetration of drugs and affects their efficacy.In this paper,Sophorae Flavescentis Radix,Cnidii Fructus.Kochiae Fructus,Atractylodis Rhizoma,Menthae Haplocalycis Herba in Sophorae Flavescentis Radix antipruritic prescription were used as research obj ects to investigate their percutaneous penetration effect in vitro,and they were made into O/W microemulsions and ointments with good percutaneous penetration.The main contents of this paper are as follows:Chapter 1 Study on the current situation of transdermal administration of antipruritic traditional Chinese medicineThis paper systematically elaborated the research status of transdermal administration of antipruritic drugs,understood the difficulties faced by transdermal administration of antipruritic drugs and common solutions,and laid a solid foundation for experimental research.Chapter 2 Study on transdermal characteristic of Sophorae Flavescentis Radix antipruritic prescriptionWith the essential oils extracted from traditional Chinese medicines(Menthae Haplocalycis Herba,Atractylodis Rhizoma,Cnidii Fructus)of Sophorae Flavescentis Radix antipruritic prescription as penetration enhancers,with the isolated skin of the SD rats as the transdermal permeation barrier and the average cumulative transmittance of components with anti-pruritus effects as evaluation indicators,the effects of transdermal permeation were investigated.Section 1 Study on transdermal permeation of alkaloids from Sophorae Flavescentis RadixTaking the average cumulative transmittance of six alkaloids as the evaluation index,the experiment showed that different mass fractions of Menthae Haplocalycis Herba oil,Atractylodis Rhizoma oil,Cnidii Fructus oil and mixed extraction oil promoted the transdermal permeation of alkaloids compared with the blank group and the penetration effect with ER as the index was as follows:3%mixed extraction oil>1%Atractylodis Rhizoma oil>1%Cnidii Fructus oil>3%azone?3%Atractylodis Rhizoma oil>5%Atractylodis Rhizoma oil>3%Cnidii Fructus oil?5%Cnidii Fructus oil>3%Menthae Haplocalycis Herba oil>5%Menthae Haplocalycis Herba oil>1%Menthae Haplocalycis Herba oil>blank.Section 2 Study on transdermal permeation of coumarins from Cnidii FructusTaking the average cumulative transmittance of five coumarins as the evaluation index,the experiment showed that different mass fractions of Menthae Haplocalycis Herba oil,Atractylodis Rhizoma oil,Cnidii Fructus oil and mixed extraction oil promoted the transdermal permeation of coumarins compared with the blank group and the penetration effect with ER as the index was as follows:3%Cnidii Fructus oil?5%Cnidii Fructus oil?1%Cnidii Fructus oil?3%mixed extraction oil>1%Atractylodis Rhizoma oil>3%Atractylodis Rhizoma oil>5%Atractylodis Rhizoma oil?3%Menthae Haplocalycis Herba oil?1%Menthae Haplocalycis Herba oil>3%azone>5%Menthae Haplocalycis Herba oil>blank.Section 3 Study on transdermal permeation of saponins from Kochiae FructusTaking the cumulative transmittance of saponin IC as the evaluation index,the experiment showed that different mass fractions of Menthae Haplocalycis Herba oil,Atractylodis Rhizoma oil,Cnidii Fructus oil and mixed extraction oil promoted the transdermal permeation of saponins compared with the blank group and the penetration effect with ER as the index was as follows:3%Menthae Haplocalycis Herba oil?5%Menthae Haplocalycis Herba oil>1%Menthae Haplocalycis Herba oil?1%Atractylodis Rhizoma oil?3%Atractylodis Rhizoma oil ?5%Atractylodis Rhizoma oil?1%Cnidii Fructus oil?3%Cnidii Fructus oil?5%Cnidii Fructus oil?3%mixed extraction oil?3%azone>blank.Section 4 Study on transdermal permeation of lactones from Atractylodis RhizomaTaking the average cumulative transmittance of three lactones as evaluation indexes,the experiment showed that different mass fractions of Menthae Haplocalycis Herba oil,Atractylodis Rhizoma oil,Cnidii Fructus oil and mixed extraction oil promoted the transdermal permeation of lactones compared with the blank group and the penetration effect with ER as the index was as follows:1%Atractylodis Rhizoma oil>3%Atractylodis Rhizoma oil>3%mixed extraction oil>1%Cnidii Fructus oil?5%Atractylodis Rhizoma oil>5%Menthae Haplocalycis Herba oil?3%Cnidii Fructus oil>3%Azone?1%Menthae Haplocalycis Herba oil?5%Cnidii Fructus oil>3%Menthae Haplocalycis Herba oil>blank.Section 5 Study on transdermal permeation of phenolic acids and flavonoids from Menthae Haplocalycis HerbaTaking the average cumulative transmittance of four phenolic acids and four flavonoids as evaluation indexes,the experiment showed that different mass fractions of Menthae Haplocalycis Herba oil,Atractylodis Rhizoma oil,Cnidii Fructus oil and mixed extraction oil promoted the transdermal permeation of phenolic acids and flavonoids compared with the blank group and the penetration effect with ER as the index was as follows:5%Menthae Haplocalycis Herba oil?3%Menthae Haplocalycis Herba oil?3%azone>1%Atractylodis Rhizoma oil>5%Cnidii Fructus oil>1%Menthae Haplocalycis Herba oil?5%Atractylodis Rhizoma oil?3%Cnidii Fructus oil>3%Atractylodis Rhizoma oil ?1%Cnidii Fructus oil>3%mixed extraction oil>blank(phenolic acids),1%Atractylodis Rhizoma oil>3%mixed extraction oil>1%Cnidii Fructus oil>3%azone?3%Cnidii Fructus oil>5%Menthae Haplocalycis Herba oil?5%Cnidii Fructus oil>5%Atractylodis Rhizoma oil>3%Menthae Haplocalycis Herba oil>3%Atractylodis Rhizoma oil>1%Menthae Haplocalycis Herba oil>blank(flavonoids).Section 6 Study on transdermal permeation of antipruritic compositions from Sophorae Flavescentis Radix antipruritic prescriptionCompared with the blank group,the transdermal penetration of alkaloids,coumarins,saponins,lactones,phenolic acids and flavonoids in Sophorae Flavescentis Radix antipruritic prescription was promoted by different mass fractions of Menthae Haplocalycis Herba oil,Atractylodis Rhizoma oil,Cnidii Fructus oil and mixed extraction oil.Compared with the single medicine,the effect of essential oils on the transdermal penetration enhancement of various components in Sophorae Flavescentis Radix antipruritic prescription changed in different degrees.Menthae Haplocalycis Herba oil has better penetration promoting effect on coumarins,phenolic acids and flavonoids,while Atractylodis Rhizoma oil has better effect on alkaloids,saponins and lactones among them.Chapter 3 Study on the transdermal drug delivery preparations of Sophorae Flavescentis Radix antipruritic prescriptionOn the basis of ascertaining that the essential oils in Sophorae Flavescentis Radix antipruritic prescription can promote the permeation of other ingredients,the extraction process of prescription was optimized,and O/W microemulsion and ointment were prepared to investigate the percutaneous permeation effect of prescription.Section 1 Study on extraction technology of Sophorae Flavescentis Radix antipruritic prescriptionThe optimum process of extracting essential oils by steam distillation is as follows:adding 10 times of water without immersion and distilling for 8 hours.alcohol precipitation process was used to impurity removal,which can retain the most active ingredients when the alcohol content reaches 70%.extracting residue and the remaining two medicinal materials were extractd by alcohol,using orthogonal design experiment to optimize the optimum extraction scheme:10 times of 70%ethanol,heating reflux extraction for three times,the first two hours,and The latter two times one hour.Section 2 Microemulsion preparation process and its transdermal permeationThe optimum composition of microemulsion was selected by the forming area of pseudo ternary phase diagram drawn by water drop method,using the essential oils contained in Menthae Haplocalycis Herba oil,Atractylodis Rhizoma oil,Cnidii Fructus oil as oil phase,the water extraction of the prescription as water phase.The optimum composition of microemulsion was as follows:0.24 g essential oils,2.14 g ethyl oleate,14.28 g Tween 80,4.76 g PEG-400,drug solution(0.4 g.mL-1 crude drugs)added to 100 g.The prepared microemulsion with good antipruritic effect and no skin irritation is a transparent brown-yellow liquid with diameter of 32 nm and pH value of 6.02.The prepared microemulsion matrix was beneficial to the transdermal permeation of various components,enhanced by essential oils,skin surface and appendices such as hair follicles play a role in the transdermal absorption of drugs.Section 3 Ointment preparation process and its transdermal permeationWith the extracted essential oils and suitable oil supplements as the oil phase and the concentrated liquid and water supplements as water phase,The best formulation of the ointment prepared by emulsification was screened by controlling variable method:0.35 g essential oils,1.20 g glyceride monostearate,13.95 g hard ester alcohol,13.95 g white vaseline,4.65 g liquid paraffin,2.80 g Tween 80,10.00 g glycerol,0.10 g ethylparaben,and the drug solution(0.8 g.mL-1 crude drugs)added to 100 g.The prepared ointment with good antipruritic effect and no skin irritation is brown-yellow semi-solid with pH value of 5.98 and the particle size less than 180?m.The prepared ointment matrix was beneficial to the transdermal permeation of various components,enhanced by essential oils,skin surface and appendices such as hair follicles play a role in the transdermal absorption of drugs.