ABSTRACT
Objective To investigate the influence of β-cyclodextrin (β-CD ) inclusion and its cataplasma on the transdermal permeability of volatile oil extracted from Chuanxiong Rhizoma and Asari Radix et Rhizoma by means of percutaneous penetration test of four preparations containing of the volatile oil. Methods Using the modified Franz diffusion pool as equipment,with 40% ethanol solution as absorption solution and SD rat skin coated with the volatile oil,aβ-CD inclusion complex of the volatile oil,a cataplasma of theβ-CD inclusion complex of the volatile oil,and a cataplasma of the mixture of the volatile oil andβ-CD,respectively,as experimental skin,the transdermal penetration test was carried out.The cumulative penetrative amounts of volatile oil in the absorption liquid were measured by GC-MS in order to evaluate the differences in the percutaneous permeability. Results The percutaneous penetration rate constant size order of four preparations containing the volatile oil is as follows:the volatile oil directly coated on the skin > the cataplasma of β-CD inclusion complex of the volatile oil > the β-CD inclusion complex of the volatile oil directly coated on the skin > the cataplasma of the mixture of the volatile oil and β-CD. Conclusion The compositions of the volatile oil retrieved from the β-CD inclusion complex are no significant changes. The percutaneous permeability of the cataplasma of β-CD inclusion complex of the volatile oil is better than that of the cataplasma of the mixture of volatile oil and β-CD.
ABSTRACT
Objective To investigate the process conditions for ?-cyclodextrin-inclusion of volatile oil obtained from Rhizoma Chuanxiong and Radix et Rhizoma Asari in Guanxin Zhitong Cataplasma,which is prescribed by Professor Deng Tietao.Methods The orthogonal design was used for the optimization of inclusion conditions.With the transformation rate of the volatile oil in inclusion complex and with the yield of inclusion complex as the evaluation indexes,the mass ratio of ?-cyclodextrin to oil,the temperature and the inclusion time were used as the main factors of L9(34)orthogonal design.Results The optimal conditions for inclusion were as follows: the mass ratio of ?-cyclodextrin to oil being 8∶1,in a saturated water solution,inclusion temperature at 60 ℃,and stirring for 1h.Conclusion The optimal conditions for ?-cyclodextrin-inclusion of volatile oil from Rhizoma Chuanxiong and Radix et Rhizoma Asari are steady and feasible.
ABSTRACT
OBJECTIVE: To seek for the farnesoid X receptor (FXR) inhibitors from the TCM database using chemoinformatics.METHODS: Three-dimensional structure active fraction of FXR-fexaramine compound (PDB code: 1OSH) was analyzed using Cerius2 4.10 software package developed by Accerlrys company.Ligandfit module was applied for molecular docking.RESULTS: 10 compounds which were predicted to have good interactions with FXR were screened using docking score of original inhibitor (fexaramine) and the receptor as threshold value.CONCLUSION: The study could be helpful for development of new lipid-lowering drug and further study of mechanism of FXR and pharmaceutical molecular.