ABSTRACT
OBJECTIVE: To study the dermatopharmacokinetics of dexamethasone acetate by administering three different formulation and preparationcreams on skin of nude mouse and discuss the application prospect of the method. METHODS: At 0, 0.25, 0.75, 1.75, 3, 5, 8, 12, 24 h after administered dexamethasone acetate cream about 0.025 g on the back of the nude mice, the excess formulation was gently removed. Then mice were sacrificed at the chosen contact time points. Skin samples were immediately excised from the fixed area of skin and weighed. Both compounds were precipitated from skin homogenate with methanol. The concentrations of dexamethasone acetate in skin were analyzed by using LC-ESI-MS method. The pharmacokinetics parameters were calculated and the percutaneous absorption process in skin of nude mouse was evaluated. RESULTS: This determination method does not interfere with endogenous substances. Calibration curves were linear over the range of 0.052 4-5.24 μg · mL-1. The mean recovery was in the ranges of 89.95%-95.97%. The intra-run relative standard deviations were less than 15%. All the results showed there were no stability related problems during the samples' routine analysis. DMSO can increase the AUC value of dexamethasone acetate, coarse granularity and crystal of cream may decrease the AUC value of dexamethasone acetate. CONCLUSION: This method is fast, sensitive, accurate with good recovery, reproducibility and low detection limited, which can be successfully applied to determine the concentration of dexamethasone acetate in skin and study the dermatopharmacokinetics of nude mouse. This in vivo time-share sampling method can be used in preclinical evaluation and screening the dermatopharmacokinetics of topical drugs.
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The paper aims to study the pharmacokinetic parameters of gastrodin in rats effected by compound compatibilitiy and different doses of Tiangou Jiangya capsule. The extracts from Gastrodiae Rhizoma( equivalent to gastrodin 16.82 mg x kg(-1) and Tiangou jiangya capsule (equivalent to gastrodin 8.410, 16.82, 33.64 mg x kg(-1)) were oral administrated to rats respectively. The plasma were taken at various time points and treated with acetonitrile to measure the contents of gastrodin by HPLC method. The mean plasma concentration-time data were analyzed by 3P97 pharmacokinetic software and the pharmacokinetic parameters between groups were treated by SPSS 16.0. The results showed that gastrodin in rat was fitted to one-compartment model, Cmax and AUC of Tiangou Jiangya capsule were in direct proportion to oral administration, and t1/2Ka had nothing to do with doses, which indicated that gastrodin was fitted first-order rate transfter process in vivo. Morever, comparison with the Gastrodiae Rhizoma extract, isodose gastrodin in Tiangou Jiangya capsule showed a significant decrease for Cmax, Ke and increase for t1/2Ke, V/Fc, this indicated that compound compatibility can delay the absorbtion of gastrodin, prolong the resident time and promote the distribution in vivo, but its bioavailability is not significantly effected.
Subject(s)
Animals , Female , Male , Rats , Administration, Oral , Benzyl Alcohols , Chemistry , Pharmacokinetics , Pharmacology , Blood Pressure , Flavonoids , Chemistry , Pharmacology , Furans , Chemistry , Pharmacology , Gastrodia , Chemistry , Glucosides , Chemistry , Pharmacokinetics , Pharmacology , Lignans , Chemistry , Pharmacology , Rats, Sprague-Dawley , SoftwareABSTRACT
<p><b>OBJECTIVE</b>To study in situ intestinal absorption kinetics of baicalin contained in Tiangou Jiangya capsules, and the effect of different intestinal segments, pH value, drug concentration and P-gp inhibitor on the absorption.</p><p><b>METHOD</b>The in situ intestinal perfusion test was adopted, and HPLC method was used to determine the content of baicalin in samples at different time points. Ultra-violet (UV) spectrophotometry was used to determine the content of phenol red in samples at different time points.</p><p><b>RESULT</b>When pH value was at 5. 0, 6. 5, 7. 4, the absorption of baicalin was not impacted. P-gp inhibitor verapamil could enhance the absorption of baicalin. When the quality concentration of the test solution ranged between 5-20 g L -1 , the linearity of the absorption amount of baicalin increased. The absorption kinetic equation of baicalin was Y = -0. 073 7X +0. 118 7 (r = 0. 994 8) , K. 0. 073 7 h -1 , t1/2 9. 40 h.</p><p><b>CONCLUSION</b>Baicalin is mainly absorbed in colon. The absorption of baicalin shows the first-order kinetics process, with the absorption mechanism of passive diffusion. Baicalin is a substrate for P-gp.</p>
Subject(s)
Animals , Female , Male , Rats , ATP Binding Cassette Transporter, Subfamily B, Member 1 , Benzyl Alcohols , Chemistry , Reference Standards , Flavonoids , Chemistry , Metabolism , Reference Standards , Furans , Chemistry , Reference Standards , Glucosides , Chemistry , Reference Standards , Hydrogen-Ion Concentration , Intestinal Absorption , Kinetics , Lignans , Chemistry , Reference Standards , Quality Control , Rats, Wistar , Verapamil , PharmacologyABSTRACT
Objective To investigate the prevalence of anti-hepatitis E virus (HEV) and genotypes of hepatitis E virus in 8 species of animals including swine, cattle, sheep, horse, donkey, dog, chicken and duck in the suburb of Beijing. Methods Serum samples were collected from the 8 species of animals, and fecal samples of younger swine were collected from 2 stock farms. Anti-HEV was detected by Double Antigen Sandwich Assay. HEV RNA from fecal samples was detected by a reverse transcription nested polymerase chain reaction (RT-nPCR). Parts of the PCR products were cloned and sequenced. The swine HEV sequences were analyzed genetically. Results The positive rates of anti-HEV in serum specimens of swine, cattle, horse, donkey, sheep, dog, duck and chicken were 80.43%(481/598), 15.02%(52/346), 14.29%(40/280) ,0(0/26) ,9.88%(33/334), 0(0/ 21) ,3.03% (7/231) and 2.53%(8/316), respectively. The anti-HEV prevalence of adult swine(≥6 months)and younger swine(≤3 months)were 87.86%(369/420)and 62.92%(112/178)respectively. 74 of 111 (66.67% ) pig faces were positive for HEV RNA. Sequence analysis on these positive samples showed that there were 6 groups of HEV designated as bjsw1, bjsw2, bjsw3, bjsw4, bjsw5 and bjsw6. The 6 strains of HEV shared 94.5%-99.6% sequence identity of partial HEV ORF2 nucleotide with each other. The identities of HEV ORF2 nucleotide sequences between the 6 strains and genotype 1, 2, 3 and 4 were 75.6%-78.6% , 75.6%-76.2%, 77.1%-80.7% and 83.7%-94.5%, respectively. The sequence identity between the 6 strains and human HEV genotype 4d was 90.0%-94.5% . Conclusion HEV infection was seen in swine, cattle, horse, sheep, duck and chicken in the suburbs of Beijing. The anti-HEV positive rate appeared the highest in swine and the lowest in dog and donkey. The six strains of HEV isolated from younger swine belonged to genotype 4d.
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<p><b>OBJECTIVE</b>To study the chemical constituents from roots of Platycodon grandiflorum.</p><p><b>METHOD</b>Column chromatography (silica gel, macroporous resin, sephadex LH - 20 and the preparative RP - HPLC were used to isolate the constituents. Their structures were elucidated by physical and spectral data.</p><p><b>RESULT</b>Eight compounds were isolated and identified as tangeritin (1), 3-O-beta-D-glucopyranosylplatycodigenin methyl ester (2), 3-O-beta-D-glucopyranosylplaticogenic acid A lactone (3), 3-O-beta-D-glucopyranosylplatycodigenin (4), deapio-platyconic acid A lactone (5), deapio-platycodin-D (6), platycoside-G1 (7) and platycoside-E (8).</p><p><b>CONCLUSION</b>Compounds 1,3 and 5 were isolated from this plant for the first time.</p>