OBJECTIVETo establish the analytical method for the release kinetic (RK) of Aconitum Brachypodum gel based on the nonlinear mixed effect model (NLMEM), in order to rationally evaluate the drug release process and explain the release mechanism.

METHODThe zero-order kinetic model containing for non-corroded drug system with the random effect was taken as the base model. The fixed effect and random effect factors impacting the drug release were analyzed by PROC NLMIXED of SAS to establish the final typical model. Subsequently, 10 training subsets were randomly extracted from the primary data to respectively their RK models, calculate the corresponding predicted root-mean-square error and average relative error, and evaluate the model stability and prediction accuracy.

RESULTThe burst effect F0 had a very significant effect on the RK model. Among the component factors, carbopol 940 showed an obvious effect on the inherence release speed constant k0 and the concentration gradient change constant a, with different variations on the basis of dosage range. The random effect factors of k0 and a had a significant impact. The final RK model was proved to be stable, effective and reliable in the cross validation.

CONCLUSIONThe drug release kinetic analysis method could be used to rationally evaluate the drug release process and explain the release mechanisms.

Aconitum ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Gels ; Kinetics ; Monte Carlo Method ; Nonlinear Dynamics

Clinical Medicine ; Humans ; Neoplasms ; prevention & control ; Periodicals as Topic ; Research

Coronary Disease ; drug therapy ; Humans ; Hypolipidemic Agents ; administration & dosage ; therapeutic use

Cardiovascular Diseases ; drug therapy ; prevention & control ; Humans ; Hypolipidemic Agents ; administration & dosage ; therapeutic use ; Risk Reduction Behavior

The clinical practice on real patients is more and more difficult in the present condition of the hospitals.Then,the modern medical simulating teaching is the main direction of the development in this field due to its characteristics,based on high- technology,simulating the real clinical circumstance,and being applicable in practice and avoiding the risk of clinical miscarriage. The significance and main development direction of modern medical simulated teaching will be discussed in this article.

Objective To evaluate the relationship between recurrent intussusception and enlarged mesenteric lymph nodes (EMLNs) in children by ultrasound.Methods A total of 35 cases (a total of 75 relapse) with imaging features of recurrent intussusception were retrospectively analysed.The sequence,size,number,morphology and location of EMLNs were recorded.Results Twenty cases of EMLNs were found in 35 cases recurrent intussusception (57.1%,20/35).At least three EMLNs were found in and / or around the mesentery of intussusception.The imaging feature of recurrent intussusception was a " target" appearance on transverse scans and a "sleeve" sign on longitudinal scans .All the EMLNs were smooth and oval-shaped hypoechoic nodule.The largest longitudinal diameter of the EMLNs ranged between 7-20 mm ,the largest transverse diameter of the EMLNs ranged between 3-8 mm with the aspect ratio≥2.0.Conclusion The Enlarged mesenteric lymph node recurrence of intussusception in children is crucial factor.Ultrasound can not only accurately and timely diagnose and treat intussusception while scanning enlarged mesenteric lymph nodes,which can provide an important basis for reducing the recurrence of intussusception.

OBJECTIVETo determine the pseudo-ginsenoside GQ (PGQ) in rat bile, feces and urine, and to study on the excretion of pseudo-ginsenoside GQ.

METHODReverse phase high-performance liquid chromatography (RP-HPLC) method with an evaporative light-scattering detector (ELSD) was performed on Diamonsil C18 column (4.6 mm x 250 mm, 5 microm), and the mobile phase was consisted of methanol-water (24: 7) with flow rate of 1.0 mL x min(-1). ELSD parameters were set as follows: nitrogen gas pressure 3.0 bar, drift tube temperature 50 degrees C.

RESULTThe method fulfilled all the standard requirements of precision, accuracy and linearity. The main way of excretion of PGQ in rat administrated through sublingual vein was at the bile. The bile excretion ratio of PGQ was 41.60%, and feces excretion ratio was 9.97%. Only trace amount of PGQ was excreted in urine.

CONCLUSIONAlmost all unchanged PGQ was excreted in bile, feces and urine.

Animals ; Bile ; metabolism ; Chromatography, High Pressure Liquid ; Feces ; Female ; Ginsenosides ; administration & dosage ; metabolism ; pharmacokinetics ; urine ; Male ; Rats ; Rats, Sprague-Dawley ; Rats, Wistar ; Reverse Transcriptase Polymerase Chain Reaction

AIMTo investigate the effects of omapatrilat (OMA) on endothelin-1-induced proliferation of cardiac fibroblasts (CFs).

METHODSIsolated and cultured CFs from neonatal Sprague-Dawley rats (SD) were randomly divided into 7 groups: (1) Control, (2) ET-1, (3) OMA, (4) ET-1 + OMA 10(-9) mol/L, (5) ET-1 + OMA 10(-8) mol/L, (6) ET-1 + OMA 10(-7) mol/L and (7) ET-1 + OMA 10(-6) mol/L. CFs were counted by MTT assay. Cell cycle distribution was determined with a flow cytometer (FCM). [3H]-Proline incorporation was evaluated by scintillation counting. Nitric oxide (NO) was measured by colorimetry.

RESULTS10(-7) mol/L ET-1 significantly increased A490 value and [3H]-Pro incorporation and decreased NO secretion compared with the control group (P < 0.01). 10(-9)-10(-6) mol/L OMA inhibited the effects of ET-1 on CFs in a concentration-dependent manner (P < 0.01 vs. ET-1). In the ET-1 group, the percentage of cells in the S phase was higher than control, which was inhibited by l0(-6) mol/L OMA (P < 0.01 vs. ET-1 and control).

CONCLUSIONOMA can restrain the proliferation and collagen synthesis of cardiac fibroblasts induced by endothelin-1, and this effect may be partially mediated by NO.

Animals ; Cell Proliferation ; drug effects ; Cells, Cultured ; Collagen ; biosynthesis ; Endothelin-1 ; pharmacology ; Fibroblasts ; cytology ; drug effects ; Myocytes, Cardiac ; cytology ; drug effects ; Nitric Oxide ; metabolism ; Pyridines ; pharmacology ; Rats ; Rats, Sprague-Dawley ; Thiazepines ; pharmacology

OBJECTIVETo evaluate the morphological characteristics of alveolar bone defects of the patients with chronic periodontitis using cone-beam CT (CBCT).

METHODSSixty patients with chronic periodontitis were included in this study. CBCT was used to scan the alveolar bone and NNT software to measure the alveolar bone defects and bone loss types in different regions.

RESULTSSeventy-five percent (45/60) of the alveolar bone defect was the generalized type, 25% (15/60) was the localized type. In incisor and canine area, the defect of the mandibular alveolar bone was more severe than in the same sites of maxilla. There was less bone loss in the premolar area of mandible than in the same site of maxilla. In the mesial and buccal sites of mandibular molars and in the lingual site of maxillary molars, the most severe alveolar bone loss was found.

CONCLUSIONSThe obvious alveolar bone defect areas in chronic periodontitis were the palatal side of maxillary molars and the lingual side of mandibular incisors. CBCT can clearly demonstrate the degree of alveolar bone defects in different regions of chronic periodontitis.

Adult ; Alveolar Bone Loss ; diagnostic imaging ; Chronic Periodontitis ; diagnostic imaging ; Cone-Beam Computed Tomography ; Female ; Humans ; Male ; Middle Aged

Rutaecarpine (Rut) is a type of indole quinazoline alkaloid exracted from Ruticarpum. Studies showed that Rut has a wide range of pharmacological effects, such as anti-hypertension, anticancer, anti-inflammation, anti-thrombus formation. Currently, many scholars are committed to developing it into a new antihypertensive and anti-inflammatory drug with all new mechanisms. But studies found that Rut is a highly fat-soluble drug with low water and oil solubility. Its high insolubility is the main obstacle in its oral absorption and application, which greatly reduced its bioavailability. Therefore, hydroxypropyl-beta-cyclodextrin (HP-beta-CD) was used as the inclusion material to prepare Rut-HP-beta-CD inclusion complex in this experiment, in order to increase its water solubility and bioavailability. In this experiment, the inclusion complex was prepared by the stirring-freeze-dry method. The preparation process was optimized by the orthogonal test, with the inclusion rate as the index, and molar ratio between host and guest molecules, inclusion temperature, time and stirring speed as the impacting factors. Moreover, the inclusion complex was verified by detecting the apparent solubility, thin layer chromatography, microscopic identification, melting point detection and dissolution study. The results showed that under the conditions of the molar ratio between Rut and HP-beta-CD of 1: 1, temperature at 60 degrees C, inclusion time of 4h and stirring speed at 600 r x min(-1), the inclusion rate of Rut-HP-beta-CD reached 91.04%. Therefore, the preparation process of Rut-HP-beta-CD inclusion under the optimum conditions is simple and feasible, with a highest inclusion rate and reproducibility, and could significantly improve Rut's solubility and bioavailability, and provide a reliable experimental basis for its clinical application.
2-Hydroxypropyl-beta-cyclodextrin ; Alkaloids ; chemistry ; Chemistry, Pharmaceutical ; methods ; Drug Carriers ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Rutaceae ; chemistry ; Solubility ; beta-Cyclodextrins ; chemistry