RESUMEN
This study aimed to investigate the enhancing effect of muscone on the transdermal penetration of traditional Chinese medicine ingredients and explore its possible mechanism of action. The Franz diffusion cells were employed to investigate the effect of muscone on the transdermal permeation of a series of model drugs with a wide range of log P values. The solubilities at saturation and the stratum corneum(SC)/vehicle partition coefficients of model drugs were measured to evaluate the effect of muscone on drug thermodynamic activities and partition of drugs into SC. Attenuated total reflectance-Fourier transform infrared spectroscopy(ATR-FTIR) was employed to explore the effect of muscone on the molecular structure of SC. The results showed that muscone significantly promoted the transdermal penetration of hydrophilic and lipophilic drugs, and the enhancement ratio(ER) increased with the decrease in the log P. Muscone could interact with the SC lipids to increase the disorder and fluidity of lipid bilayer packing, which improved skin permeability and promoted transdermal absorption of drugs. This study provides a scientific basis for the application of muscone in traditional Chinese medicine topical preparations.
Asunto(s)
Animales , Ratas , Administración Cutánea , Cicloparafinas , Medicina Tradicional China , Permeabilidad , Ratas Sprague-Dawley , Piel/metabolismo , Absorción CutáneaRESUMEN
Based on the previous study of compound liquorice microemulsion, this paper aims to prepare the compound liquorice microemulsion gel and investigate its pharmacodynamics of chronic eczema. The type, dosage and adding method of gel matrix, and formula dosage of humectant were optimized by single factor method to obtain the formula and preparation technique of the gel. With glycyrrhizic acid, glycyrrhetin and oxymatrine used as evaluation indexes, the Franz diffusion cell method was adopted to monitor the in vitro release profile of the gel. Eczema model of delayed-type hypersensitivity in mice was chosen to detect the ear swelling rate, degree of inflammatory cell infiltration of ear pieces, and pathological changes of ear pieces, so as to investigate the therapeutic effect of the microemulsion gel. The preparation process of the compound liquorice microemulsion gel was stable. The release of glycyrrhizin and oxymatrine was most consistent with the Hixcon-Crowell kinetic model, while the release of glycyrrhizic acid was most consistent with the Ritger-Peppas kinetic model. The pharmacodynamics studies proved that compound liquorice microemulsion gel could significantly reduce the ear swelling rate in mice, with good anti-inflammatory effect as well as the ability to resist the pathological changes of chronic eczema and inhibit the infiltration of dermal inflammatory cells. Therefore, the preparation process of compound liquorice microemulsion gel is feasible, with stable drug release and a significant therapeutic effect on chronic eczema.
Asunto(s)
Glycyrrhiza , Administración Cutánea , Animales , Liberación de Fármacos , Emulsiones , Geles , Ratones , Absorción CutáneaRESUMEN
To explore the potential of "physical property model" based on the concept of quality by design(QbD),during the application of process analysis technology(PAT) in the concentration process. The Carthami Flos was used as a model drug. Firstly, the total flavonoid retention rate and the hydroxysafflor yellow A(HSYA) retention rate of the concentrated solution were used as indicators to determine the concentration temperature range of the Carthami Flos extract. Then different concentrations were prepared at the optimal concentration temperature, and the corresponding viscosity(η) and electrical conductivity(σ) at different concentrations and temperatures were measured. Data processing software such as Excel, 1 stOpt, SPSS, and MATLAB were used to establish Carthami Flos extract's mathematical model of physical parameters: ρ-C, η-C, η-T, η-C-T, σ-T, σ-C-T. The results showed that the best concentration temperature of the Carthami Flos extract should not exceed 60 â, and the R~2 of the exponential equation and Arrhenius equation established based on physical parameters was all greater than 0.9, indicating that such model had better predictive ability. The mathematical model:η=14.465 1 exp(-0.019 8T+ 0.771 1C-0.058 3C~2), σ=4.061 0 + 0.004 3T +(-1.104 1 +0.950 9T)C-0.556 9TC~2 can be used to reflect the comprehensive effect of concentration and temperature on viscosity or conductance, laying foundation for the establishment of an online monitoring system for the viscosity or conductivity of the extraction liquid in the concentration step, rapid prediction of the concentration status, and control of the concentration endpoint. This study has initially proved the feasibility of using the physical property model as the core of the research idea in application of PAT for intelligent quality control of traditional Chinese medicine concentration links, providing a reference for the online intelligent monitoring of concentration steps of traditional Chinese medicine extracts.
Asunto(s)
Medicamentos Herbarios Chinos , Medicina Tradicional China , Flavonoides , Flores , Modelos TeóricosRESUMEN
<p><b>OBJECTIVE</b>To explore the effect of soy isoflavone on obesity in the light of hypothalamus and peripheral orexigenic gene regulation.</p><p><b>METHODS</b>Fifty-four female rats were randomly assigned to 6 groups: one sham-operated group (SHAM), one ovariectomized (OVX) control group, three OVX groups fed with 400 ppm (L-SI), 1200 ppm (M-SI) and 3600 ppm (H-SI) isoflavone respectively, and one OVX group receiving 0.45 ppm diethylstilbestrol (EC). All rats were allowed to take high-fat diet for 4 weeks. Some neuropeptides were measured by RT-PCR. These neuropeptides included NPY, pro-opiomelanocortin (POMC), cocaine and amphetamine regulated transcript (CART), orexin, melanin-concentrating hormone (MCH), melanin-concentrating hormone precursor (P-MCH), ghrelin, and leptin.</p><p><b>RESULTS</b>Compared with the OVX control group, the body weight and food intake in the H-SI group were reduced significantly and there was a significant dose-dependent manner in the 3 isoflavone groups. The results of RT-PCR showed that the NPY level in the 3 isoflavone groups was significantly increased and the POMC/CART gene expression decreased significantly in rats' hypothalamus compared with that in the OVX control group. However, the expression of orexin, MCH and P-MCH had no change. The peripheral grelin mRNA expression was higher in the 3 isoflavone groups, while leptin gene expression in the fat was not consistent.</p><p><b>CONCLUSIONS</b>This research showed that isoflavone could prevent obesity induced by high-fat diet and ovariectomy through regulating hypothalamus and peripheral orexigenic gene expressions associated with food intake.</p>