| Compared with chemical penetration enhancers,Essential Oils,which shows good penetration ability and low toxicity to the skin,exhibits certain advantages as a novel transdermal absorption enhancer with its own certain pharmacological activity.By in vivo and vitro percutaneous absorption test with pharmacodynamic trials,Essential Oils,were studied for suitability of percutaneous administration formulations and its impact as transdermal enhancer on the percutaneous absorption of models(Ibuprofen),to select the appropriate Essential Oils as transdermal absorption enhancers of ibuprofen.Furthermore,determine the applicable form of preparation for Essential oils to function as penetration enhancers and conduct the study on formulation and quality evaluation.Volatile oil were extracted by steam distillation of by measuring the solubility and stability of choosing the right solution in vitro percutaneous absorption was measured ligustilide monomer and oil-water partition coefficient(lgP)in the volatile oil 2.64,and 1.88,respectively indicating that it is suitable percutaneous penetration.Four different formulations prepared Angelica essential oil(volatile oil inclusion complex solution,volatile oil inclusion complex gel,a solution of volatile oil,volatile oil gel),and compare the in vitro percutaneous absorption ligustilide four formulations behavior,found that cyclodextrin inclusion complex is not conducive to volatile oil of Ligusticum percutaneous absorption,is not conducive to Angelica essential oil of transdermal penetration.Four different formulations prepared Angelica essential oil(volatile oil inclusion complex solution,volatile oil inclusion complex gel,a solution of volatile oil,volatile oil gel),and compare the in vitro percutaneous absorption ligustilide four formulations behavior,found that cyclodextrin inclusion complex is not conducive to volatile oil of Ligusticum percutaneous absorption,is not conducive to Angelica essential oil of transdermal penetration.With ibuprofen as a model drug,the use of Franz diffusion cell to SD rat abdominal skin barrier,were volatile oil containing medicine ibuprofen gel in vitro percutaneous absorption test,compare the different Essential Oils of ibuprofen In vitro percutaneous penetration effect.The results show that in the five kinds of traditional Chinese medicine in the volatile oil,volatile oil for ibuprofen in vitro penetration effect best,ER value of 3.58,1.72 times the cumulative penetration rate of penetration enhancers without a control group.On the basis of the establishment of ibuprofen concentration in vivo analysis methods,the study of pharmacokinetics of Ibuprofen in rats after transdermal administration of ibuprofen gel containing five different herbal volatile oils was conducted.The correlations between the results of both in vivo and vitro study of herbal volatile oils as transdermal enhancers of Ibuprofen was evaluated by deconvolution method,combined with the results of in vitro penetration test.It is revealed that,Chuanxiong Oil evaluation of volatile oil on penetration of ibuprofen in vivo relevance of the results.The results show that in the five kinds of traditional Chinese medicine in the volatile oil,volatile oil penetration to ibuprofen peak plasma concentration Cmax reached(45.97 ± 1.54)mg·L-1,2.11 times the penetration enhancers without a control group,and without penetration enhancers of the control group relative bioavailability was 161.87%,in vivo percutaneous absorption effect is good.Essential Oils outer containing ibuprofen gel for transdermal administration in vivo good correlation,correlation coefficients in the 0.976 to 0.999 8 range,suggesting that in vitro percutaneous absorption test can be used to evaluate or predict formulations for transdermal administration in vivo process.By subcutaneous injection of estradiol benzoate oxytocin binding method to establish female mice model of primary dysmenorrhea,to writhing and uterus NO,Ca2+,PGF2αconcentration factors such as an index,a commercially available oral ibuprofen mixed the suspension for the positive control group,choose the best anti-dysmenorrhea,percutaneous absorption in vivo effect of significantly improved volatile oil as a topical treatment of dysmenorrhea ibuprofen formulations penetration enhancers.Inclusion and technology were applied microemulsion technology to improve the stability of topical formulations of traditional Chinese medicine volatile oil.Choose a suitable emulsifier,co-emulsifier,study their different combinations and proportions,drawing pseudo-ternary phase diagrams,to the appearance and size as an index to determine the final microemulsion is:Ibuprofen:volatile oil:Mixed Surfactant(Cremophor RH40:Transcutol P(3:1)):water=1:3:7:25.By adjusting the amount of each formulation excipients to the appearance of uniformity as an indicator to determine the proportion of prescriptions microemulsion gel ointment(by mass)is:Carbomer 940:sodium polyacrylate:Gan hydroxyl aluminum:tartrate:Gelatin:microemulsion:water=1:4:0.07:0.1:6:37.6:128,and to determine the preparation process.Franz diffusion cell method,in vitro percutaneous absorption test,compare microemulsion gel cream,microemulsion gels,drug-containing volatile oil gel,medicated gel containing ibuprofen percutaneous absorption.The results showed that microemulsion gel paste in vitro percutaneous absorption of the best,ER value reached 3.96,indicating microemulsion gel paste significantly improved ibuprofen percutaneous absorption.Determination microemulsion gel paste during storage,ibuprofen content and ligustilide evaluate its stability,and in accordance with the relevant provisions of pharmacopoeia gel slurries under the investigated formulation excipients by HPLC property,including the amount of paste,content uniformity and other indicators.The results showed that volatile oil in the microemulsion made,has significantly improved the stability of microemulsion gel paste.Ibuprofen volatile oil microemulsion gel paste formulations meet the quality inspection General requirements. |
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