ABSTRACT
The study was carried out to investigate the pharmacokinetics and in vitro/in vivo correlation of ibuprofen with essential oils as penetration enhancers (PE) following transdermal administration. With Azone as the positive control, ibuprofen hydrogels containing Chuanxiong oil, Angelica oil or Cinnamon oil as PE were prepared and administered to the rat abdominal skin. Then the pharmacokinetics of ibuprofen following transdermal administration were investigated and compared. In comparison with negative control (no PE was added), the relative bioavailability values with the addition of Chuanxiong oil, Angelica oil, Cinnamon oil and Azone as PE were determined to be 161.87%, 171.05%, 151.37% and 148.66%, respectively. In vitro/in vivo correlation analysis was performed by deconvolution method and the results demonstrated a good correlation between in vitro and in vivo percutaneous absorption studies. The correlation coefficients were measured to be 0.999 7, 0.995 2 and 0.999 4 for Chuanxiong oil, Angelica oil and Cinnamon oil respectively. In summary, Chuanxiong oil, Angelica oil and Cinnamon oil as PE could significantly enhance the bioavailability of ibuprofen following transdermal administration. A satisfactory in vitro/in vivo correlation could be obtained by using hydrogel as the dosage form.
ABSTRACT
The results of previous studies showed potential correlations between the penetration enhancement effect of essential oils and the drug properties of traditional Chinese medicine based on the data mining method. As chemical composition is the material basis of drug properties of traditional Chinese medicine, this article further analyzed the correlation between the chemical composition of essential oils and the drug properties. Firstly, essential oils were extracted by steam distillation, and then physicochemical parameters of essential oils, such as relative density and refractive index, were measured. The chemical components of 20 essential oils were analyzed by GC-MS, and divided into 12 categories according to skeleton features and functional groups. Finally, Logistic regression analysis was applied to reveal the correlations. The results proved that five flavors, four tastes and channel tropisms showed the correlation with chemical composition of essential oils (P<0.05). In conclusion, there were obvious correlations and regularity between the drug properties of traditional Chinese medicine and the chemical composition of essential oils.
ABSTRACT
To study the association between penetration enhancement effect of essential oils and drug properties of traditional Chinese medicines. Through literature research, 34 kinds of essential oils with the penetration enhancement effect were collected. The methods of frequency analysis and variable crosstab were used for intuitive analysis and association analysis. The association between penetration enhancement effect of essential oils and drug properties (four natures, five flavors, channel tropism) were analyzed by a general linear model. According to the findings, the essential oils with penetration enhancement effect were all sourced from acrid traditional Chinese medicines, because their positive drug nature contributed to the enhancement of the penetration effect of essential oil; five flavors had little effect on penetration enhancement (P = 0.6982), but four natures and channel tropism showed significant effects (P = 0.011, 0.077). In conclusion, there were obvious association and regularity between penetration enhancement effect of essential oils and drug properties of traditional Chinese medicine.