OBJECTIVE:To study the in vitro-in vivo correlation of sustained-release naftopidil capsule,review the rationality of the designed dissolution conditions METHODS:Artificial gastric juice was selected as the dissolution medium,the dissolution rate of the two naftopidil sustained-release capsules were studied;the 3p97 pharmacokinetic program was used to characterize the in vivo course of the sustained-release capsules after giving dogs a oral single dose of 200mg,after this,the percentage absorbed at different time were calculated The input functions were obtained by using deconvolution technique Then the correlation coefficients of the calibration graph by plotting the dissolution rate to the percentage absorbed or the input functions were calculated The in vitro-in vivo correlations of sustained-release naftopidil capsules were studied by comparing the correlation coefficients calculated to the critical correlation coefficients RESULTS:The correlation coefficients calculated by the two methods were both more than the critical coefficients,the in vitro-in vivo correlations of the two sustained-release naftopidil capsules were good CONCLUSION:The two methods mentioned in this paper to study the in vitro-in vivo correlation were simple and reliable,the results of this study were very useful in the rapid formulation screening,the designing of rational dissolution rate conditions,and the providing theory basic of evaluation of the naftopidil sustained-release capsules

Objectives: Inquirying the ability of the earlier diagnosis and studying the surgical management of intra and extra middle skull base tumors. Methods: A retrospective study has been made on 43 cases of malignant skull base tumor extended into cavernouse sinus. CT and MRI evaluation were made for all patients. Different approaches have been utilized to remove tumors. Results: In early period there was no obviously clinical sign. 5 year survival rate was 35.1%. Seven cases of no removing totally tumors in cavernous sinus had been alive for 7 months. Conclusions: The symptoms of skull base carcinoma is less, which often leads to false diagnosis and management. Total resection via different approaches may improve clinical results.

AIM　To prepare naftopidil bioadhesive sustained-release capsule and study their pharmacokinetics and relative bioavailability in the dog. METHODS　Bioadhesive polymers such as hydroxypropyl methylcellulse (HPMC) and Carbopol 934 (CP 934) were used in capsule prescriptions. Naftopidil capsule and two formulations of bioadhesive sustained-release capsules (I and II) were given to five healthy male dogs in a cross-over test. The naftopidil concentrations in plasma were determined by a newly developed HPLC method and the pharmacokinetic parameters as well as the relative bioavailability were measured. RESULTS　The C0→∞, Cmax and Tmax of naftopidil capsule was (3728±573) h*ng*mL-1, (697±94) ng*mL-1 and (1.2±0.5) h. These parameters of bioadhesive sustained-release capsule I and II, respectively, were (5518±391) h*ng*mL-1 and (5636±427) h*ng*mL-1; (468±61) ng*mL-1 and (512±72) ng*mL-1; both (4.0±0.7) h. Results from statistics showed that there were significant difference between bioadhesive formulations and the non-bioadhesive one in C0→∞, Cmax and Tmax. The bioadhesive formulations and the non-bioadhesive one were not bioequivalent, the relative bioavailability of the two bioadhesive sustained-release capsules were respectively 150%±14% and 154%±23% when compared with the non-bioadhesive capsule. CONCLUSION　It is much improving bioavailability of naftopidil by using bioadhesion.

OBJECTIVE:To screen the formulations of bioadhesive danazol suppository,and to study its drug release in vitro.METHODS:Hydroxypropyl methylcellulse(HPMC),polyethylene glycol(PEG)6000and PEG600were employed in the bioadhesive sustained-release formulation.Suppositories were prepared and the correlation between drug release rate from suppositories and the ratio of HPMC to PEGs used in the formulae was studied.RESULTS:HPMC retarded drug release,and drug gradually released in the12-hours period when the ratio of HPMC to PEGs was1∶6.5;the law of drug release was conformed to weibull models and mono-exponential models.CONCLUSION:HPMC,PEG6000and PEG600were suitable to the formulation of bioadhesive danazol suppositories,and HPMC could slow down the drug release from the this preparation;the best ratio of HPMC to PEGs was1∶6.5.

Objective To evaluate the practical value of procaleitonin(PCT)in diagnosis of pneumonia in patients after kidney transplantation.Method A total of 102 patients with pneumonia after kidney transplantation were reviewed.According to the diagnostic criteria of pathogens of pneumonia,32 patients were enrolled in bacterial group and 70 patients in non-bacterial group.The data of the PCT level and the C-reactive protein (CRP) level of the two groups were determined and compared with each other.Results There was significant difference in PCT level between bacterial pneumonia patients after kidney transplantation and non-bacterial pneumonia patients group (P<0.01).The difference in CRP level between bacterial pneumonia patients after kidney transplantation and non-bacterial pneumonia patients group was not significant (P>0.05).The changes of PCT level and the CRP level in 32 patients with bacterial pneumonia after kidney transplantation were not significant (P>0.05),and they were not associated with each other.Conclusions Monitoring the PCT level in patients with bacterial pneumonia after kidney transplantation would have an obviously clinical significance in diagnostic value.

Aim To investigate the effect of SM-1 on seven main cytochrome P450(CYP450)in human liver microsomes.Methods Substrate or SM-1 was incubated with human liver microsomes for 30 min in vitro,and divided into control group and experimental group.The effects of SM-1 on the main phase I metabolic enzymes in human liver microsomes was detected by HPLC.Phenacetin,bupropion,paclitaxel,tolbutamide,omeprazole,dextromethorphan,testosterone were investigated as probe drugs.Results Inhibition rate of SM-1 on the classical substrate of human liver microsomal CYP was 0.05％,3.37％,0.08％,2.07％,4.20％,-0.15％and 10.84％,respectively.Conclusions SM-1 may have inhibitory effect on CYP3A4.Attention should be paid to the interaction of clinical drug induced by CYP enzyme inhibition.

Aim To study absorption characteristics of SM-1 , a novel anti-tumor agent , to provide a research basis for the druggability evaluation of SM-1 and formu-lation design. Methods Caco-2 cell monolayer model and in situ single-pass intestinal perfusion rat model were used to study the absorption characteristics of SM-1 , and the absorption of SM-1 in vivo was evaluated through absolute bioavailability study in rats. Results The results of cell monolayer model showed that cu-mulative absorption and efflux of SM-1 increased line-arly with concentration ( 10 ~40 mg · L-1 ) . There were no significant differences in Papp with different concentrations ( P>0. 05 ) . SM-1 was absorbed mainly through passive diffusion. The intestinal perfusion re-sults showed that Ka and Pef of SM-1 had no significant differences ( P > 0. 05 ) , when the concentrations ranged from 25 to 100 mg · L-1 . SM-1 entered the systemic circulation mainly via on passive diffusion, indicating it is a compound with high permeability. The absorption of SM-1 in duodenum was superior to other intestinal segments ( P <0. 05 ) , there were no significant differences in the jejunum, ileum and colon ( P >0. 05 ) . The absolute bioavailability of SM-1 in rats was 29. 3%. Conclusion The membrane perme-ability of SM-1 is high and it can be absorbed by intes-tine well. The absorption mechanism of SM-1 is pas-sive diffusion, and it possibly escapes from the efflux transporter protein. The absolute bioavailability of SM-1 in rats is low.

We studied the correlation of sustained-release tablet of naftopidil between the in vitro release and the in vivo absorption in the dog. The release rate (X) of naftopidil sustained-release tablet in artificial gastric fluid was determined and the naftopidil concentration in plasma was determined after a single oral dose of 100 mg naftopidil (tablet or sustained-release tablet) in the dog. The absorbed fraction(F) and in vivo absorption rate (A) of the NAF sustained-release tablet in the dog at different time were calculated by W-N method and deconvolution method, respectively. Then the regression equations between F or A and X of the corresponding time point were obtained: F=2. 1533X - 27. 636(r = 0.9927) and A=2.3452X - 25.474(r= 0.9938). W-N method and deconvolution method both indicated that the correlation between the in vitro release and the in vivo absorption in the dog of the NAF sustained-release tablet was good.
Animals ; Biological Availability ; Delayed-Action Preparations ; Dogs ; Naphthalenes ; chemistry ; pharmacokinetics ; Piperazines ; chemistry ; pharmacokinetics ; Solubility ; Tablets

Objective To analyze the causes for the failures after posterior pedicle screw instrumentation for thoracolumbar fractures.Methods From June 2003 to December 2014,182 patients with thoracolumbar fracture were treated by fixation through the posterior approach using pedicle screws and fully followed up in our institute.We analyzed the cases of postoperative infection,recovery of neural symptoms,breakage and loosening of pedicle screws and connecting rod,non-union of the fractured vertebra,and correction loss of kyphosis in associations with the AO classification and Loading Sharing Classification of Spine Fracture (LSCSF) system,osteoporosis,intervertebral disc injury and methods of internal fixation.Results In this series,altogether 27 cases failed(14.8％).The rate of postoperative infection was 1.1％ (2/182).The rate of breakage of pedicle screw or connecting rod was 7.7％ (14/182).The implant breakage rates for fractures of AO types A1,A2 and A3.1 were significantly lower than for other types (P ＜ 0.05).The implant breakage rate for the patients with ≤6 LSCSF points was significantly lower than for those with ≥7 LSCSF points (P ＜ 0.05).The implant breakage occurred in 3 cases of those who underwent fixation of one normal vertebra respectively below and above the two contiguous segments but not in those who underwent additional fixation of the injured vertebrae.The rate of screw loosening was 2.2％ (4/182).The non-union rate of the injured vertebra was 2.7％ (5/182).The rate of kyphosis recurrence was 1.1％ (2/182).Conclusions To prevent the failure of posterior pedicle screw fixation,surgeons should pay more attention to the following key points before operation:the type and evaluation of spinal fractures,a proper approach and method of internal fixation,and the weight bearing capability of the anterior column.

Abstract A new method was established to determine the free inorganic cadmium ion ( Cd2+) in marine bivalves using high performance liquid chromatography and inductively coupled plasma mass spectrometry ( HPLC-ICP-MS) . The free Cd2+ in shellfish was ultrasonic extracted for 40 min by 10 mmol/L Tris buffer solution ( with 0. 1 mol/L NaCl, pH=7. 5), and the separation of Cd2+ was achieved using an IonPac CS5A analytical column with an IonPac CG5A guard column. The mobile phase consisted of 50 mmol/L C2 H2 O4 and 95 mmol/L LiOH. The new method had a good linear relationship with the correlation coefficient of 0. 999 and the standard recoveries of Cd2+ were all above 84. 6%. The free Cd2+ content in several kinds of marine bivalves was determined using the method and the results showed that the percentage of free inorganic Cd2+ to the total Cd content in samples with high Cd content was higher than those with low Cd content.