| Xiao Er Fu Xie Nuan Qi San（XEFXNQS） is the prescription which comes from Maste Zhu Qiyong’ clinical experience.XEFXNQS can be used to warm spleen and stop coprorrhea,expel cold and alleviate ache and dry phlegmatic hygrosis.It smells fragrance and has several Chinese crude drug,including Fructus Psoraleae,Fructus Evodiae,Flos Caryophylli and someone else. XEFXNQS possesses definitely clinical effectiveness in coprorrhea and abdominal ache especially caused by appetite deficient cold.The prescription has been used in form of paste,but it existes defects in using,saving and so on. In order to be used for adapting the special structure of the umbilicus,we choose some new adjuvants and make it into one kind of new dosage form---plastic patch to stick in umbilicus,which is good at penetrating abdominal skins, carrying more drugs,keeping moist and so on.（1） Homogeneous design was used firstly to study the medical material proportion in prescription,diarrheal model of mouse caused by castor oil was used to evaluate the effectiveness of each prescription.The final outcome showed that the best effectiveness is reached at this proportion,Fructus Psoraleae:Fructus Evodiae:Semen Alpiniae Katsumadai:Cortex Cinnamomi: Flos Caryophylli as 9:3:4.5:4.5:1.（2） Fructus Psoraleae is extracted by ethanol,psoralen and isopsoralen are measured as targets and we apply orthogonal experiment to choose the best craft:10 times of ethanol at the density of 70%,2h per time,thrice;The content of effective compositions and extractum are targets for Fructus Psoraleae’s solution extracted by ethanol,and the optima technology as follows: physic liquor was concentrated to 0.50g/mL,add in the distilled water to 3 times.Volatile oil of Fructus Evodiae was extracted with steam distillation. Under this condition,we could get more alkaloids:10 times of ethanol at the density of 70%,1.5h per time,thrice;Meanwhile:concentrated to 0.25g/mL, add in distilled water to 3 times.Semen Alpiniae Katsumadai,Flos Caryophylli and Cortex Cinnamomi mainly contain Volatile oil,we use orthogonal experiment again to sieve the best technology and gain this result:crashing through 20 mesh,addin distilled water to 6 times,decoction 6h.Finally,we reapplicated orthogonal experiment to optimize the technology of clathrating Volatile oil withβ-CD:Volatile oil:β-CD as 1:8（mL:g）,20%ethanol as dissolvant,ultrasound for 3 h.（3） By evaluating forming,plasticity and stipping of different adjuvants, we obtained the optimal preparing conditions of plasticity patch by taking the measures of single-factor experiment,and the best proportion of the black media is that PVP:AGS:ZnO:Glycerine:water are 0.5:0.8:4:6.3:10.（4） Taking forming,plasticity and transdermal absorption in vitro of the patch as judging indexes,the patach has the best dosage as 30 percents.When we choose 20 percents PEG400 as the recepte media,rat skin of abdomen as skin model,the transdermal absorption in vitro showed excellent result when 1%Azone was used.The preparing techniques of the plasticity umbilicus patch: weigh water,glycerol,PVP-K30 according to the proportion,and then heat until dissolved completely,addin AGS,ZnO and stir uniformly,addin extracta liquida of Fructus Psoraleae,Fructus Evodiae,aqua extract of the compound recipe,composite volatile oil,and 1%Azone until the drug vs blank matrix as 30%,and then stir uniformly,packed into a model made by myself,solidificate in oven at the temperature of 40℃for 3.5h,lastly maintain in adhesive plaster.（5） The estimation of the outside-body quality of the plasticity umbilicus patch is also investigated.We choose methanol as the solvents and extracting 30 min with ultrasound.With this method,we simultaneous determination psoralen and isopsoralen in each patch,and the result as followes:4.20mg and 3.93mg.The evaluation of penetrating the skin property showes that psoralen and isopsoralen can accumulately release to 140.84±0.79μg·cm-2 and 102.60±1.17μg·cm-2 after 24h.Delivery level in vitro is investigated and the results indicated that 90%in the patch can be released within 8h.（6） Darrhea model of mouse induced by castor oil and propulsive gut motility experiment are used to evaluate the effective of the patch,the high dose and media dose can significantly reduce the onset of diarrhea and also show a significant reduction in gastrointestinal motility on charcoal meal test in mice.Acute experiment and toxicity test indicate that XEFXNQS has no toxicity;Irritate test indicates that this preparation has no stimulus to integrity skins,but defective skins not. |
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