OBJECTIVETo study the in vitro mucosal permeation properties of paeonol and the factors that affect such permeability.

METHODBullfrog skin was selected as the permeation model, and the modified Franz diffusion cell was adopted to investigate the percutaneous adsorption in vitro. Content of paeonol was quantified by HPLC. Kinds of receiving solution, parts of bullfrog skin and impacts of drug concentration on percutaneous adsorption in vitro were systematically studied.

RESULTPercutaneous permeation of paeonol was to some extent affected by osmotic pressure and pH value of the receiving solution. Abdominal skin, lateral abdominal skin and dorsal skin, with the permeability coefficient form high to low, had great influence on the permeation of paeonol. There existed a good percutaneous permeation of paeonol. And the relationship between the cumulative permeability rate and time was coincided with the first order kenetical process.

CONCLUSIONTake the in vitro abdominal skin of bullfrog as the permeation model, some similarities are revealed between in vitro percutaneous permeation of paeonol and mucosal adsorption.

Acetophenones ; metabolism ; Animals ; Chromatography, High Pressure Liquid ; Hydrogen-Ion Concentration ; In Vitro Techniques ; Mucous Membrane ; metabolism ; Osmotic Pressure ; Permeability ; Rana catesbeiana ; metabolism ; Skin ; metabolism

OBJECTIVETo study the factors that affect mucosal absorption of gardenia extract.

METHODTake vitro frog skin as a model to study the vitro mucosal permeation. The impacts of the osmotic pressure and the pH value of permeation medium on the Papp of the Jasminoidin were studied, and the effect of frog skin on the stability of Jasminoidin was investigated also.

RESULTThe Papp of Jasminoidin were (0.53 +/- 0.01), (0.21 +/- 0.05), (0.44 +/- 0.12), (0.42 +/- 0.13), (0.26 +/- 0.03) cm x min(-1) by using the normal saline (pH 6.88), pure water, 1.8 % NaCl solution, normal saline (pH 4.05) and normal saline (pH 10.05) as permeation medium for each. The accumulated permeation rate was (55.69 +/- 9.81)% by 12 h, using normal saline as permeation medium respectively, and there was no obvious time lag. Jasminoidin began to degrade around 8 h by affectedof frog skin, the constant of degradation rate (K) was 1.999, and the t1/2 was 0.347 h.

CONCLUSIONThe mucosal permeability of gardenia extract by using the vitro model of frog skin is good, and consistent with zero level absorption process. The osmotic pressure and pH value significantly affected the permeation and the isotonic and partial neutral permeation medium are more conducive to the permeation and absorption of Jasminoidin. The degradation effect of frog skin to the Jasminoidin will not affect mucosal permeation research. In vitro model of frog skin is a suitable way to simulate mucosal permeation process of the gardenia extract.

Gardenia ; chemistry ; Hydrogen-Ion Concentration ; Mucous Membrane ; drug effects ; physiology ; Permeability ; drug effects ; Plant Extracts ; chemistry ; pharmacology ; Skin ; drug effects ; Skin Absorption ; drug effects ; physiology ; Solubility

OBJECTIVETo establish a sensitive HPLC method for determining the concentrations of paeonol in rat plasma and to evaluate its pharmacokinetic characteristics.

METHODThe paeonol from eortex Moutan was distilled by the way of water-vapor. A single i.v. dose of 4 mg x kg(-1) paeonol injection was given to 5 health rats. Paeonol was separated on a Diamonsil -C18 column with methanol-water (60: 40)as mobile phase. The plasma concentrations of paeonol were determined and its pharmacokinetic parameters were calculated and evaluated by using kinetica 4.0.

RESULTThe linear range of the method for paeonol was 0.204-20.4 mg x L(-1) and the determination limit was 0.204 mg x L(-1). The main pharmacokinetic parameters, such as AUC, MRT, C(max), Kel, t(1/2kel), after a single dose of paeonol injection were (111.88 +/- 14.44) mg x L(-1) x min(-1), (23.25 +/- 5.86) min, (8.99 +/- 0.84) mg x L(-1), (0.082 +/- 0.015) min(-1) and (8.73 +/- 1.54) min, respectively.

CONCLUSIONThe HPLC method for determining paeonol concentration in plasma is simple, rapid, sensitive and suitable for pharmacokinetic studies.

Acetophenones ; blood ; pharmacokinetics ; Animals ; Chromatography, High Pressure Liquid ; methods ; Male ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo develop a RP-HPLC method for the simultaneous determination of five components including ligustrazine, ferulic acid, butylphthalide, ligustilide and butene-NBP in Rhizoma Chuanxiong, a Chinese herbal medicine.

METHODThe chromatographic analysis was carried out by using a grace smart RP C18 column with the mobile phase consisted of acetonitrile and 0.1% phosphoric acid (volume fraction), which was in gradient elution. A DAD detector was used to detect the components. The peak area was chosen under their maximum absorption wavelength for different components, and quantitated by using the external standard method.

RESULTThe calibration curves were linear within the range of 0.008 35-0.668, 0.020 6-1.648, 0.012 2-0.976 , 0.050 75-4.06, 0.015 7-1.256 microg for ligustrazine, ferulic acid, butylphthalide, ligustilide and butene-NBP, respectively. The average recoveries of the five components were 101.98%, 99.91%, 96.94%, 100.85% and 99.04%, respectively.

CONCLUSIONThis method is simple, quick, reproducible, with high recovery, and has been successfully applied to the simultaneous determination of the five components in Rhizoma Chuanxiong. This method can be used to control the quality of Rhizoma Chuanxiong and its preparations.

4-Butyrolactone ; analogs & derivatives ; analysis ; Benzofurans ; analysis ; Calibration ; Chromatography, High Pressure Liquid ; methods ; Coumaric Acids ; analysis ; Drugs, Chinese Herbal ; analysis ; Pyrazines ; analysis

OBJECTIVETo develop an HPLC method for the determination of plasma concentration of jasminoidin and study the pharmacokinetics of jasminoidin in rabbits administered Xingnaojing naristillae by nasal medication.

METHODAfter sampling blood from the left arteria carotis of rabbits which were administered Xingnaojing naristillae medication by nasal by 12 mg x kg(-1) (counted by gardenia extract) at 1, 3, 5, 10, 20, 30, 45, 60, 90, 120, 240 min, the plasma samples were dealt with acetonitrile precipitation and HPLC was used to determine the plasma concentration of jasminoidin. The pharmacokinetic parameters were computed by Kinetica software.

RESULTThe calibration curve was linear (r = 0.999 6) within the range of 0.136 5-2.73 mg x L(-1) for jasminoidin in plasma. The average recovery was (97.14 +/- 3.78)%, (95.06 +/- 2.95)%, (91.50 +/- 1.82)%. The within-day and between-day precision met the requirements, because the RSD were both less than 4%. Jasminoidin was fitted to a two-compartment open pharmacokinetic model in rabbits. The mainly pharmacokinetic parameters were: C(max) = (2.013 +/- 0.563) mg x L(-1), T(max) = (6.405 +/- 1.764) min, K(e) = (0.032 5 +/- 0.013 3) min(-1), CL = (0.059 3 +/- 0.0246) L x min(-1) x kg(-1), AUC = (116.89 +/- 50.19) mg x min(-1) x L(-1), MRT = (84.447 +/- 19.420) min.

CONCLUSIONThe method can be used to determine the concentration and to investigate the pharmacokinetics of jasminoidin in rabbits. Jasminoidin was absorbed rapidly by nasal medication and has a good perspective.

Administration, Intranasal ; Animals ; Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; administration & dosage ; pharmacokinetics ; Iridoids ; administration & dosage ; blood ; pharmacokinetics ; Male ; Rabbits

OBJECTIVETo observe the influence of natural borneol and synthetic borneol on mucosal permeability of Gardenia extract.

METHODTaken frog skin as a vitro model to study the vitro mucosal permeation the impacts of the natural borneols and synthetic borneols on the P(app) of the Jasminoidin were studied, and the effect of different borneols on the stability of Jasminoidin were investigated. Compared the 10 h accumulated infiltration rate of each group the effects of influence factors,such as C(Ge), C(B) and rotation speed on P(app) were investigated by using response surface method.

RESULTThe P(app) of Jasminoidin of natural borneol and synthetic borneol group were 1.44 fold and 1.77 fold of control group (P < 0.01). For two borneol groups, the results also showed a significant difference too (P < 0.05). Jasminoidin began to degrade about 8 h after the effect of frog skin for control group and synthetic borneol group, but was stable within 12 h for natural borneol group. The accumulated permeation rate of 10 h was same for different borneol groups. It was about 1.3 fold of control group. The C(Ge) had a salinence influence on the P(app) (P < 0.01) and C(B) had a salience influence on time-lag (P < 0.01).

CONCLUSIONBoth the natural borneol and synthetic borneol can accelerate the permeation of Jasminoidin and the synthetic borneol has stronger effect on the P(app). Both two different borneol can reduce the degradation effect of frog skin to Jasminoidin, but the natural borneol has a better protect effect on it. By using more natural borneol, the mucosal permeability of Gardenia extract can be increased, the time-lag can be reduced, and Jasminoidin has better stability.

Administration, Cutaneous ; Bornanes ; chemical synthesis ; pharmacokinetics ; Dosage Forms ; Drugs, Chinese Herbal ; chemistry ; Gardenia ; chemistry ; Iridoids ; pharmacology ; Mucous Membrane ; metabolism ; Nasal Mucosa ; metabolism ; Permeability ; Skin ; metabolism ; Skin Absorption