To develop estradiol transdermal film-forming spray (TFS), various polymers were screened using solvent appearance, spray ability, film-forming rate and appearance as indices. The influence of polymer type, plasticizer and penetration enhancer on the transdermal flux were investigated by selecting porcine skin as model, and transdermal flux of TFS was compared with commercial patch and gel. The drug existing state in the formed film was investigated by differential scanning calorimetry (DSC). The solvent appearances, spray abilities, film-forming rates and appearances of eudragit E PO, RL PO, hydroxypropyl cellulose EF, polyvinylpyrrolidone K30, Plasdone S630 and Agrimer VA64 were suitable for the preparation of TFS. TFS prepared by Eudragit RL PO had the biggest transdermal flux of estradiol among all the polymers investigated. Triethyl citrate, the plasticizer, decreased the transdermal flux. Azone increased the transdermal flux, while oleic acid, isopropyl myristate and menthol had opposite effects. TFS had a higher transdermal rate and a higher accumulative penetrated estradiol of 24 h than commercial patch and gel. The DSC result showed that estradiol was spread as molecule in the formed film of TFS. It was indicated that TFS could be expected to be an effective transdermal drug delivery system.

0. 05). The treatment group in the improvement of most clinical symptoms were superior to the control group (P

AIM　To predict skin permeability of drugs with theoretical parameters. METHODS　The semiempirical self-consistent field molecular calculation AM1 method is utilized to obtain the structural parameters of drug molecules. Stepwise multiple regression analysis or BP neural network is then utilized to establish the correlation between skin permeability of drugs and their structural parameters. RESULTS　The calculated human skin permeability coefficients (kp) of 22 model drugs in vitro or the R values (R=absorbed/unabsorbed) of 17 drugs in vivo are in good agreement with their observed values. CONCLUSION　Theoretical parameters can be used to predict skin permeability of drugs.

The contents of gallic acid, catechin, albiflorin, paeoniflorin, benzoic acid and paeonol extracted in different growth years, collecting season and of different parts of Paeonia lactiflora were determined. The results showed that the contents of catechin and paeoniflorin in Paeonia lactiflora collected in autumn are the highest, and the contents of benzoic acid was lower than that of those collected at other time. The longer is the age of Paeonia lactiflora, the higher is the contents of catechin and paeoniflorin. The contents of catechin and paeoniflorin in the root of Paeonia lactiflora were higher than those in other parts of the plant. There is a certain content of paeoniflorin in the leaves of Paeonia lactiflora. Judging from the result, paeoniflorin is synthesized in the leaf and then transported to the root. Catechin is not synthesized in the leaf, but mainly in the root. Paeonia lactiflora should be collected in autumn, and immature plant should not be collected.

Objective To establish the quality standards for compound Shatagan Oral Liquid. Methods Chuanxiong Rhizoma was identified by TLC. The content of ferulic acid was determined by HPLC. Separation was performed on a Diamonsil C18 column (4.6 mm × 250 mm, 5μm) with a mobile phase consisting of methanol-1% acetic acid solution in gradient elution (0-5 min, 35% methanol;5-8 min, 35%→23% methanol;8-22 min, 23% methanol) at 30℃;The flow rate was 1.0 mL/min;The injection volume was 5μL;The detection wavelength was 322 nm.Results Ferulic acid showed a good linear relationship in the range of 0.039 4-0.630 0μg (r=0.999 7,n=7). The average recovery was 98.22% and RSD was 2.62% (n=6).Conclusion The method is reliable, sensitive and with repeatability, which can be used as the quality control method for compound Shatagan Oral Liquid.

OBJECTIVETo screen the formulations of cryptotanshinone gel for treatment of topical diseases such as acne.

METHODDifferent cryptotanshinone gels incorporating various penetration enhancers at different concentrations were prepared using carbopol 934L as matrix. The steady transdermal fluxes and drug retention amounts in skin of the gels were investigated on single chamber diffusion cells using excised rat abdomen skin as model and 40% polyethylene glycol-400 saline as releasing media. The optimal formulation would be the gel which had the maximum drug retention amount/ transdermal drug flux ratio.

RESULTThe promotion effects of menthol at different concentrations were as follows: 5% > 3% > 1%, and the effects on drug retention amount in skin were followed as: 5% approximately equal 3% > 1%; The promotion effects of a zone at different concentrations were as follows: 5% approximately equal 3% > 1%, and the effects on drug retention amount in skin were as follows: 5% > 3% approximately equal 1%. Combination of enhancers showed no superior effects compared to single uses. 5% azone had the maximum retention amount/ transdermal flux ratio.

CONCLUSIONThe optimal formulation was the cryptotanshinone gel containing 5% azone.

Administration, Topical ; Animals ; Chemistry, Pharmaceutical ; Gels ; Male ; Permeability ; Phenanthrenes ; administration & dosage ; chemistry ; metabolism ; Rats ; Rats, Sprague-Dawley ; Skin ; metabolism

OBJECTIVETo investigate the relationship of properties and drug release rate of hot melt pressure sensitive adhesive (HMPSA), and to provide a recommendation of preparing and selecting of HMPSA for transdermal use.

METHODHMPSA with different properties were prepared using styrene-isoprene-styrene triblock copolymer as main material, and the tacks, adhesions and cohesions were determined. Drug-in-adhesive type patches were prepared using alpha-asarone as model drug, and the drug release rates were investigated on single chamber diffusion cells using 60% ethanol solution as release media.

RESULTThe prepared HMPSAs had different tacks, adhesions and cohesions. The drug release rates of HMPSA patches were related to the cohesions. The release rate decreased when the cohesion increased.

CONCLUSIONThe HMPSA with appropriate cohesion should be selected when preparing patches to balance the drug release rate and patch property.

Adhesives ; Anisoles ; chemistry ; pharmacokinetics ; Diffusion ; Pharmacokinetics

OBJECTIVEWe studied the licorice provenance rule under the manual simulative water stress conditions, discussed geographical variation pattern and the ecology mechanism and laid the theoretical basis for the licorice seed regionalization and the seed allocation.

METHODOn the spot we investigated and collected seed materials. Setting up water potential gradient by PEG, we observed the seed germination characteristic through the experiment of indoor germination.

RESULTThe sensitivity of various provenance seed germinative energy show quite remarkable difference for water potential reducing. Along with geographic longitude increasing, the seed germinates variation sensitivity increasing gradually to the water stress. The results of climatic factors' correlation analysis indicated that provenance seed germinate energy to the water stress is sensitive, in which the annual average temperature is low and annual precipitation is abundant. But it is insensitive in which the annual precipitation is little, the annual average temperature, average temperature in July and the annual average ground temperature is high.

CONCLUSIONUnder the water stress condition the licorice provenance seed germination characteristic exists remarkable geographical variation. Geographical variation is the result of natural selection.

China ; Dehydration ; Ecosystem ; Geography ; Germination ; Glycyrrhiza uralensis ; physiology ; Seeds ; physiology

OBJECTIVETo study on the effect of different processing methods on the contents of seven major constituents in wild and cultivated Paeonia lactiflora, gallic acid, catechin, albiflorin, paeoniflorin, pentagalloylglucose, benzoic acid and paeonol, in order to provide reference basis for different efficacy and formation mechanism of Paeonia Radix Rubra and Paeonia Radix Alba.

METHODWild and cultivated P. lactiflora were dealt with by four processing methods, direct drying, drying after boiling, drying after decorticating and boiling, and drying after boiling and decorticating. HPLC was use to simultaneously determine the contents of seven chemical constituents.

RESULTWild P. lactiflora showed notable higher content of paeoniflorin and catechin than cultivated P. lactiflora, whereas cultivated P. lactiflora showed higher content of albiflorin than wild P. lactiflora. Both of them were less affected by process methods in above three constituents. Drying after boiling, drying after decorticating and boiling, and drying after boiling and decorticating methods reduced the content of benzoic acid and paeonol to trace in both wild and cultivated P. lactiflora. Clustering analysis results showed that all processing methods assembled wild and cultivated P. lactiflora in 2 groups.

CONCLUSIONThe content differences of Paeonia Radix Rubra and Paeonia Radix Alba are mainly caused by their own differences and less affected by processing methods.

Acetophenones ; chemistry ; Benzoic Acid ; chemistry ; Chromatography, High Pressure Liquid ; Cluster Analysis ; Medicine, Chinese Traditional ; methods ; Paeonia ; chemistry

OBJECTIVEThe main aim of the research was to evaluate genetic variability and interrelationships of mainly quantitative traits in 2-year population, and provide a basis for high-yield breeding of Glycyrrhiza uralensis.

METHODFour genotype G. uralensis population were transplanting in four different environment using complete randomized block design with three replication, and the 10 quantitative traits, including plant height (PH), stem diameter (SD), tiller number (TN), taproot length (TRL), root length (RL), root diameter (RD), diameter of 20 cm below the root head (D20), taperingness (TR), lateral root number (LRN) and root fresh weight (RFW) were measured in field.

RESULTThe difference among population for all evaluated traits were significant (P<0.05) through Duncan's multiple range tests, and the coefficient of variation of RFW and LRN were above 25%. The analysis of variance was used to evaluate the traits of four populations across to four different environment Genotype, environment and their interaction effect were significant (P<0.05) or highly significant (P<0.01) for mainly evaluated traits. Simple correlation between traits showed that PH, SD, LRN, RL, RD and D20 had highly significant (P<0.01) and positive correlation with RFW. Results of the path coefficient analyses showed that D20 had the greatest positive direct effect on RFW, followed by the traits of PH and RL.

CONCLUSIONSelection for increased D20, RL and PH would be the best indirect selection traits for increasing root yield. Meanwhile, ample genetic variability exists in the G. uralensis 2-year population, it could be used for breeding improvement of root yield.

Breeding ; methods ; Environment ; Genes, Modifier ; Glycyrrhiza uralensis ; genetics ; growth & development ; metabolism ; Phenotype ; Plant Roots ; genetics ; metabolism ; Plant Stems ; genetics ; metabolism ; Plants, Medicinal ; chemistry ; Quantitative Trait Loci ; genetics ; Quantitative Trait, Heritable