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

OBJECTIVETo observe the clinical effects of essential hypertension treated with acupuncture at Siguan [Hegu (LI 4) and Taichong (LR 3)], Quchi (LI 11) and Xingjian (LR 2).

METHODSSixty cases of essential hypertension were randomly divided into an acupuncture group and a medication group, 30 cases in each group. Two groups of acupoint, which were (1) Siguan [Hegu (LI 4) and Taichong (LR 3)] and (2) Quchi (LI 11), Xingjian (LR 2), were selected alternatively in the acupuncture group, once everyday. In the medication group, captopril was prescribed for oral administration 25 mg per time, three times per day. Seven days made one session in both groups and totally three sessions were required.

RESULTS(1) After treatment, the blood pressure were decreased significantly in the two groups (all P < 0.01). Compared with the medication group, the diastolic pressure after 14 days, 21 days of treatment in the acupuncture group was decreased significantly (both P < 0.01). (2) In the terms of TCM syndrome score, the improvement of dizziness, soreness and weakness of waist and knees, palpitations was significant in the acupuncture group compared with that in the medication group(all P < 0.05). (3) The acupuncture group had less adverse reactions compared with the control group (P < 0.05).

CONCLUSIONAcupuncture at Hegu (LI4) and Taichong (LR 3), Quchi (LI 11) and Xingjian (LR 2) can effectively decrease blood pressure; the effect of controlling diastolic pressure is better than captopril. It can also improve the symptoms of dizziness, soreness and weakness of waist and knees, and palpitations.

Acupuncture Points ; Acupuncture Therapy ; Adult ; Aged ; Blood Pressure ; Essential Hypertension ; Female ; Humans ; Hypertension ; physiopathology ; therapy ; Male ; Middle Aged ; Treatment Outcome ; Yin Deficiency ; therapy ; Yin-Yang

Objective To explore the personality characteristics of abused children in order to reduce the incidence of child abuse.Methods Two hundred and ninty five middle school students were investigated with general questionnaire and Eysenck Personality Questionnaire of children. Eighty six students experiencing child abuse (CA) last year as study group and one hundred and ninety six non-abuse children as controls (NCA) were analyzed by means of Eysenck Personality Questionnaire of children.Results The score of neuroticism in CA group was significantly higher than that in the control group (55.62±10.60/52.65±10.98,t=-2.114 P=0.035). The score of lie in CA group was significantly lower than that in control group (42.21±9.87/46.04±9.20,t=3.184 P=0.002). On the impact of different sex, the psychoticism score of male was significantly higher than that in the control group(52.37±11.49/48.04±9.97,t=-2.227 P=0.028), and the lie score was significantly lower than that in control group(41.03±9.18/46.18±8.79,t=3.125 P=0.002).The scores of those in the female were not significant.Conclusions There is a close association between the unstable emotion and child abuse in children, so training emotional self-control and emotional expression of children might be a intervention strategy in the future. In addition, the frequency of lie in children is probably one of factors that determine whether children are abused or not.

Objective To explore the expression of c-Fos protein and character of mossy fiber sprouting(MFS) in hippocampus of rat with febrile seizures(FS).Methods Thirty-six 21-day-old male Sprague-Dawley rats were randomly divided into FS group,febrile control(FG) group and normal control(NG) group.FS was established by hyperthermal bath.Immune histochemistry and(Timm′s) staining were used to examine the expression of c-Fos protein in CA1 region and MFS in CA3 region of hippocampus.Results Excessive expression of c-Fos protein presented in the hippocampal CA1 region of FS group.The surface area percentage of c-Fos protein of FS group[(2.26?0.23)%] was higher than that of FG group[(1.08?0.19)%] and NG group[(0.71?0.14)%],there were significant difference between FS group and the other two groups(?~2=10.48 P

Animals ; Antineoplastic Agents ; toxicity ; Brain ; metabolism ; Cisplatin ; toxicity ; DNA Damage ; drug effects ; Deoxyguanosine ; analogs & derivatives ; analysis ; Female ; Kidney ; metabolism ; Male ; Mice ; Mice, Inbred ICR ; Oxidative Stress ; drug effects

Objective To identify mutations site and clinical characteristics of a familial hypercholesterolemia(FH) proband diagnosed clinically through DNA sequencing and family analysis in the proband and his family members of 3 generations.Methods Blood samples and clinical data of the kindred of total 29 from 3 generations members were collected.Proband had a physical examination electrocar-diogrom and vascular ultrasound.The proband and his family members took routine clinical exams,and genomic DNA was isolated.The promoter region and the 18 exons of low density liporotein receptor(LDLR) gene were screened by Touch down polymerase chain reaction -single strand conformation polymorphism(PCR-SSCP) and DNA sequencing.The result of sequencing were matched gene sequence published in the BLAST database.Results 1.Increased intima-media thickness and plaque were detected in the common carotid artery,right subclavian artery of the proband.Aortic valve regurgitation was found by echocardiography.2.No mutation R3500Q of ApoB100 was observed.3.Two heterozygous mutations in exon 10 and 13 of LDLR gene (W462X and A606T) were identified.The proband and 5 members of paternal relatives showed W462X heterozygosis mutation in exon 10 of LDLR gene which introduced the change from tryptophone to a new stop codon.The proband's mother and grandmother harboured A606T heterozygous mutation in exon 13 of LDLR gene due to a single base pair substitution of G for A in the codon for residue 1 879.Conclusions Disease causing mutations of proband are W462X and A606T compound heterozygosis mutation in exon 10 and 13 of LDLR gene inherited from mother and father.Proband shows homozyous phenotype though the genotype analysis indicates heterozygous mutations.

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

Animals ; Disease Models, Animal ; Hypoglycemia ; chemically induced ; metabolism ; Hypothalamus ; drug effects ; metabolism ; Insulin ; pharmacology ; Intracellular Signaling Peptides and Proteins ; metabolism ; Male ; Neuropeptides ; metabolism ; Orexins ; Rats ; Rats, Sprague-Dawley

Female ; Humans ; Liver Neoplasms ; Middle Aged ; Paraganglioma

OBJECTIVETo discuss arthroscopic technique of single Kirschner wire and suture avoiding epiphyseal line fixation for tibial intercondylar eminence fracture and its clinical results.

METHODSFrom May 2008 to December 2012, 21 patients (13 males, 8 females, ranging in age from 6 to 14 years old) with tibial intercondylar eminence fracture were treated arthroscopically with single Kirschner wire and suture avoiding epiphyseal line fixation technique. According to Meyers and McKeever classification, 7 patients were type II, 10 patients were type III, and 4 patients were type IV. Active rehabilitation began at one week after operation. The patients were followed up for 10 to 30 months. X-ray films were taken to evaluate fracture healing at 1, 3, 6 months after operation; range of motion, the anterior drawer test, the lachman test and the Lysholm knee score were used to evaluate clinical effects.

RESULTSAll fractures were healed without displacement at 6 weeks after operation. Anterior drawer test and the lachman test were both negative in all patients at 3 months after operation. Lysholm knee score was 95.5 ±2.5 at 6 months after operation, and postoperative X-ray film did not find epiphyseal line broadening or narrowing.

CONCLUSIONArthroscopic treatment for tibial eminence intercondylar fracture with single Kirschner wire and 8-shaped suture avoiding epiphyseal line fixation technique has many advantages, such as firm fixation,early mobilization, less invasive, less injury of physis and satisfactory effect.

Adolescent ; Arthroscopy ; Bone Wires ; Child ; Female ; Fracture Fixation, Internal ; Humans ; Male ; Sutures ; Tibial Fractures ; surgery