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Solvent and emulsion pressure-sensitive patches for compound Nanxing pain paste were prepared respectively in this study. Franz diffusion cell method was adopted to determine in vitro release of eugenol in compound Nanxing pain paste of the two stromata, with microfiltration membranes in place of skins. The results of the experiment demonstrated that solvent pressure-sensitive patches were superior to emulsion pressure-sensitive patches in terms of the accumulated release percentage of eugenol, with both of their release processes in line with Higuchi model and non-Fick diffusion mechanism. In conclusion, emulsion pressure-sensitive stroma was more beneficial to in vitro release of eugenol in compound Nanxing pain paste.

To study the in situ intestinal absorption kinetics of flrubiprofen in rats, the absorption of flurbiprofen in small intestine (duodenum, jejunum and ileum) and colon of rats was investigated using in situ single-pass perfusion method and the drug content was measured by HPLC. The effects of drug concentration on the intestinal absorption were investigated. The K(a) and P(app) values of flurbiprofen in the small intestine and colon had no significant difference (P > 0.05). Drug concentration (4.0, 10.0 and 16.0 mg x L(-1)) had no significant influence on the K(a) values (P > 0.05). However, when concentration was 4.0 mg x L(-1) and 10.0 mg x L(-1), significant effect on the P(app) values (P < 0.05) was found, but significant effect on the P(app) values was not shown between 10.0 mg x L(-1) and 16.0 mg x L(-1) (P > 0.05). The K(a) and P(app) values of flurbiprofen on the perfusion flow rate had significant difference (P < 0.05). Flurbiprofen could be absorbed at all segments of the intestine in rats and had no special absorption window. The absorption of flurbiprofen complies with the facilitated diffusion in the general intestinal segments, and accompany with the cytopsistransport mechanism probably. The perfusion flow rate had significant effect on the K(a) and P(app).

Objective: A sensitive liquid chromatography-tandem mass spectrometric (LC-MS/MS) method has been developed and validated for the determination of brucine and strychnine in rat plasma., Method: Samples were extracted by ethyl acetate-n-butanol (7: 3). Chromatographic separation was operated on ZORBAX XDB-C18 column with gradient elution of acetonitrile-methanol-water (0.05% acetic acid and 10 nmol x L(-1) ammonium formate contained), followed by LC-MS/MS in positive electrospray ionization. Quantification was carried out on multiple reaction monitoring (MRM) of the transition m/z 395.2/324.2, m/z 335.2/184.2 and m/z 199.1/171.1 for brucine, strychnine and tacrine (internal standard), respectively., Result: The method was linear in the range of 0.195-100 and 0.07840 microg x L(-1) for brucine and strychnine, with coefficient correlation 0.994 and 0.996 respectively. The recoveries of extraction were 78.9% - 102.4% for brucine and 95.2% - 106.1% for strychnine. Precision, accuracy, stability and matrix effect of the analytes met the requirement. The method was applied to a pharmacokinetic study of brucine and strychnine after cutaneous administration of Semen Strychni niosome gel. The C(max) were (26.20 +/- 5.81) and (12.50 +/- 3.00) microg x L(-1) while the AUC(0-infinity), were (193.75 +/- 39.43) and (98.25 +/- 28.54) microg x h x L(-1) of the two components., Conclusion: We conclude that the niosomes may reduce the systemic exposures and prolong the local release of brucine and strychnine.

As an important member of metabotropic glutamate receptors (mGluR), metabotropic glutamate receptor 1 (mGluR1) plays an important role in the signal transduction of central nervous system. Selective mGluR1 antagonists can block the signaling pathway activated by mGluR1 and exert a series of physiological actions including analgesia, antianxiety, antidepression, etc. Currently, the discovery and modification of selective mGluR1 antagonists have become a hot research focus. This paper reviews the structural catalogs of selective mGluR1 antagonists and their structure-activity relationships in the last decade.

Objective: To investigate the enhancing effect of volatile oils of Rhizoma Zingiberis (RZ), Flos Magnoliae (FM), Fructus Litseae (FL), Azone and pairwise combinations on the permeation of Rotundine in vitro., Methods: To screen out the volatile oils with the best percutaneous enhancing effect on Rotundine, a test of penetration through rats skin was conducted by using an improved Franz diffusion cell. The accumulative penetration amount of Rotundine was determined by UV and HPLC., Results: All of the 3 volatile oils had enhancing effect on Rotundine permeation. The average accumulative doses of Rotundine for 8 hours (Q8, mg/cm2) of 5% volatile oil of FL, 5% volatile oil of, RZ, 2.5% FL + 2.5% Azone were 6.0758, 6.1148, 6.5487, the enhancement ratios of 4 hours were 1.01, 1.00, 1.13 respectively., Conclusion: 2.5% FL + 2.5% Azone had the best effect of percutaneous enhancing on Rotundine.

The paper is to report the establishment of a population pharmacokinetic model for flurbiprofen (FP), an active metabolite of flurbiprofen axetil (FA). 246 FP serum concentration and clinical data were perspectively collected from 23 general anaesthesia patients receiving FA intravenously before operation in Dentofacial Surgery and Otorhinolaryngology Department of the First Affiliated Hospital of Fujian Medical University. Population pharmacokinetic data analysis was performed using NONMEM software. The measure of Bootstrap was applied for internal validation, while Visual Predictive check was adopted for external validation. The data of FP correspond with two-compartment model. The body weight (WT) had conspicuous effect on clearance and volume of central compartment, while sex, age and daily dose of administration had no marked effect on pharmacokinetic parameter of FP. The basic model was described as follows: CL (L x h(-1)) = 1.28x EXP(ETA(1)), V1 (L) = 5.03x EXP(ETA(2)), Q (L x h(-1)) = 8.5 x EXP(ETA(3)), V2 (L) = 4.39 x EXP(ETA(4)). The final model was described as follows: CL (L x h(-1)) = 1.32 x (WT/60) x EXP(ETA(1)), V1 (L) = 5.23 x (WT/60) x EXP(ETA(2)), Q (L x h(-1)) = 8.45 x EXP(ETA(3)), V2 (L) = 4.37 x EXP(ETA(4)). The population typical value of CL, V1, Q and V2 were: 1.32 L x h(-1), 5.23 L, 8.45 L x h(-1) and 4.37 L, respectively. Bootstrap and visual predictive check show that the final model of FP is stable, effective and predictable. A novel population pharmacokinetic model is developed to estimate the individual pharmacokinetic parameter for patients intravenous injecting FA in terms of patients' characteristics and dosing history, and to design a prior dosage regimen.

Objective: To investigate the pharmacokinetics of tetrahydropalmatine monomer and extractive of corydalis and corydalis processed with vinegar in rats., Methods: The plasma concentrations of tetrahydropalmatine were determined by a reversed phase high performance liquid chromatographic. The plasma concentrations-time data were calculated with 3p97 program., Results: The main pharmacokinetic parameters of tetrahydropalmatine monomer and extractive of corydalis and corydalis processesd with vinegar as follows: T(1/2) was (5.66 +/- 1.92), (4.24 +/- l1.54), (4.35 +/- 1.34) h, Tmax was (1.5 +/- 0.5), (1.0 +/- 0.55), (0.5 +/- 0.68) h, Cmax was (0.71 +/- 0.29), (0.37 +/- 0.11), (0.67 +/- 0.35) microg/ml,AUC(o-t), was (2.58 +/- 0.85), (1.96 +/- 0.69), (2.95 +/- 1.61) microg/ml., Conclusion: The T(1/2) of corydalis and corydalis processesd with vinegar is more shorter than tetrahydropalmatine monome, the effect of preventing pain is promoted in rats.

According to the relationship between dosage and effect, the time course of analgesic was determined after oral administration of Xiaohuoluo Pills to mice. Based on this experiment, contrasting the commercial pills with the reference preparation, the bioavailability of Xiaohuoluo Pills was studied. It was shown that the bioavailability of different batches of product from the same factory was different. This method was good for the study of compound preparations of Chinese materia medica.