To prepare and study the pharmacokinetics and release bioavailability in olunteers and concentrations in plasma in patients. METHODS: Ethylcellulose was used matrix in phase separation-coacervation for preparation of microencapsulation. The release experiments were performed in a rotating shaker. The isoniazid concentration in plasma was determined by spectrophotometrical method following a single oral dose of sustained-release cupsule and ordinary tablet respectively given to 10 volunteers in a open randomized cross-over test. MCP86 was used to process main pharmacokinetic parameters. RESULTS: The sustained-release of capsule and ordinary teblet in vitro, T50 was 1 h and 0.032 h respectively. The drug in sustained-release capsule was sustained release over 10 h. The main parameters in body: ordinary tablets: cmax=11.12 μgml-1, tmax=1.41 h, K=0.201 h-1; sustained release capsule: cmax=4.99 μgml-1, tmax=1.80 h, K=0.03 h-1. The concentration of blood at 36 h was (0±0)μgml-1 and 1.63 μgml-1 respectively. Except tmax, there was significant difference between the two fomulations (P＜0.01). The concentration of blood in patient at 1.5 h and 36 h. ordinary tablet and sustained-release capsule respectively were (8.24±2.60)μgml-1, (0±0)μgml-1and (3.69±0.86)μgml-1, (2.09±0.56)μgml-1. CONCLUSION: The sustained-release capsule will play an important part in prevention and treatment of tuberculosis as the result of its reasonable formulation and simple technology.

Objective To establish the quality standard of Shenxin Capsules.Methods The contents of ginsenoside Rg1 and ginsenoside Re in Shenxin Capsules were determined by HPLC with the mobile phase consisting of acetonitrile- 0.05 % phosphoric acid water solution (95 ∶ 405) and UV detection wavelength at 203 nm .Qualitative analysis of Radix Ginseng, Cornu Saigae Tataricae and Herba Asari in Shenxin Capsule was carried out by TLC. Results Ginsenoside Rg1 showed a good linearity in the range of 1.032～ 9.288 ? g( r=0.9998, n=5) , the average recovery being 99.76 % and RSD being 2.10 % . Ginsenoside Re showed a good linearity in the range of 0.850～ 7.650 ? g( r=0.9998, n=5) , the average recovery being 96.24 % and RSD being 1.67 % . The chromatographic spots of Radix Ginseng, Cornu Saigae Tataricae and Herba Asari were identified without the interference of negative control .Conclusion The method is accurate , reproducible and can be used for the quality control of Shenxin Capsules.

Objective: To evaluate the value of an 11-gauge stereotactic vacuum-assisted biopsy (SVAB) device for the diagnosis of breast microcalcifications. Methods: The 11-gauge SVAB was performed in 93 patients with microcalcifications in X-ray mammograms. The patients who were diagnosed as having breast cancer, atypical hyperplasia, unclarified breast lesions and imaging-histologic discordance should require surgical excision. The histopathological results of biopsy specimens and postoperative specimens were compared. Results: Of 97 lesions with microcalcifications, 96 (99.0%) calcified tissues were obtained. The pathological results showed that 71 (73.2%) were benign lesions, 19 (19.6%) were malignant lesions, 6 (6.2%) were atypical hyperplasia lesions. Of the 25 patients receiving surgical excision, 2 (2/13, 15.4%) with ductal cancer in situ had a final diagnosis of invasive breast cancer, 1 (1/4, 25.0%) with atypical hyperplasia lesions had a final diagnosis of ductal cancer in situ , 1 with imaging-histologic discordance had a final diagnosis of ductal cancer in situ . Of 71 patiens with a pathological diagnosis of benign lesions, 49 had a median follow-up of 14.5 months, and no obvious abnormalities were observed. The complications of 11-gauge SVAB included vasovagal reactions (1.0%), bleeding (2.1%) and hematoma formation (3.1%). Conclusion: The 11-gauge SVAB is an effective and reliable method with slight side effects for the diagnosis of breast microcalcifications if it is applied appropriately. For the breast lesions diagnosed as having atypical hyperplasia and ductal carcinoma in situ or with imaging-histologic discordance, the surgical biopsy should be performed subsequently. Copyright© 2012 by TUMOR.

Objective:To investigate the clinical application value of argon-helium knife cryoablation combined with radioactive seed implantation in the treatment of non-small cell lung cancer(NSCLC).Methods:A total of 117 patients with NSCLC admitted to Oncology Department of Fifth Affiliated Hospital of Zhengzhou University from January 2015 to January 2017 were included in our study.And they were divided into the combination group(n=63)treated with CT guided argon-helium knife cryoablation combined with radioactive 125I seeds implantation and the control group(n=54)treated only with argon-helium knife ablation.The changes of blood routine indexes, tumor markers, tumor ablation target volume and CT value were observed before and 1, 3, 6 months after treatment.Adverse reactions during treatment and the evaluation results of efficacy were compared between the two groups.Patients were followed up for 24 months to observe the recurrence and survival rates between the two groups. Results:In the combination group, seeds of(12.49±4.91)were implanted, and the X-ray exposure was(123.16±42.75)Gy.There was no significant difference in general clinical data between the two groups before treatment( P>0.05). At 1, 3 and 6 months after treatment, as compared with control group the combination group showed the significantly decreased platelet count( t=3.154, 3.586, 2.233, P=0.027、0.019、0.034), while, there was no significant difference in white blood cell count, red blood cell count and hemoglobin level between the two groups(all P>0.05). The levels of carcinoembryonic antigen(CEA), neuron-specific enolase(NSE)and tumor volume were significantly lower in combination group than in control group at 3 and 6 months after treatment( t3=3.142, 2.926 and 4.281, t6=4.094, 5.382 and 4.535, all P<0.05), showing significant improvements of illness.While, the above levels showed no significant differences at 1 month after treatment between two groups( t=1.065, 1.037, P=0.197, 0.255). At each monitoring time, the CT value of tumor target area showed a steady downward trend( P<0.05). During the treatment, the incidence of thrombocytopenia was higher in the combination group than in the control group(47.6% or 30/63 vs.24.1% or 13/54, χ2=6.935, P=0.008), while there were no significant differences in the incidence of postoperative fever, pneumothorax, myoglobinuria, pain, bleeding and nausea and vomiting between the two groups(all P>0.05). After 6 months of treatment, the remission rate was higher in the combination group(73.0% or 46/63)than in the control group(48.1% or 26/54). The survival time and relapse-free time of the combination group were longer than those of the control group[(21.81±4.31)months vs.(18.93±5.94)months, (20.48±5.76)months vs.(16.93±7.14)months, Log Rank χ2=8.229 and 9.656, P=0.004 and 0.002)]. Conclusions:Argon-helium knife Cryoablation combined with radioactive seed implantation can effectively control the local progression of NSCLC, reduce the risk of tumor recurrence, and has high safety.

The preliminary metabolic profile of total diterpene acid (TDA) isolated from Pseudolarix kaempferi was investigated by using in vivo and in vitro tests. Pseudolaric acid C2 (PC2) was identified as the predominant metabolite in plasma, urine, bile and feces after both oral and intravenous administrations to rats using HPLC-UV and HPLC-ESI/MS(n), and demethoxydeacetoxypseudolaric acid B (DDPB), a metabolite proposed to be the glucoside of PC2 (PC2G), as well as pseudolaric acid C (PC), pseudolaric acid A (PA), pseudolaric acid A O-beta-D glucopyranoside (PAG), pseudolaric acid B O-beta-D glucopyranoside (PBG) and deacetylpseudolaric acid A (DPA) originated from TDA could also be detected. It was demonstrated by tests that the metabolism of TDA is independent of intestinal microflora, and neither of pepsin and trypsin is in charge of metabolism of TDA, TDA is also stable in both pH environments of gastric tract and intestinal tract. The metabolites of TDA in whole blood in vitro incubation were found to be PC2, DDPB and PC2G, which demonstrated that the metabolic reaction of TDA in vivo is mainly occurred in blood and contributed to be the hydrolysis of plasma esterase to ester bond, as well as the glucosylation reaction. These results clarified the metabolic pathway of TDA for the first time, which is of great significance to the in vivo active form and acting mechanism research of P. kaempferi.

The metabolic profile of pseudolaric acid B (PB) was investigated by using in vivo and in vitro tests. Pseudolaric acid C2 (PC2) was identified as the specific metabolite of PB in plasma, urine, bile and feces using HPLC and HPLC-ESI/MS(n) after both oral and intravenous administration to rats, and almost no prototype was detected in all kinds of samples. The metabolic behaviors of PB orally administered in rats treated with antibiotics to eliminate intestinal microflora were identical with those in untreated rats, demonstrating that the metabolism of PB is independent of intestinal microflora. PB was stable in 48 h respective incubation with artificial gastric juice and artificial intestinal juice, suggesting that neither pepsin nor trypsin is in charge of metabolism of PB, and also demonstrating that PB is stable in both pH environments of gastric tract and intestinal tract. In vitro research on metabolism of PB in rat liver microsomes incubation revealed that little PB was metabolized and that the proposed metabolites were the demethoxy and demethoxydecarboxy products of the prototype. The amount of metabolites was extremely low compared with the prototype, indicating that liver microsomes are not responsible for the metabolism of PB either. PB was gradually metabolized into PC2 during 1 h in whole blood incubation in vitro, and the metabolic process showed dynamically dependent manner with incubation time. Once absorbed into blood, PB was quickly metabolized into PC2, accordingly, little prototype was detected in all kinds of samples. The metabolism was attributed to the rapid hydrolysis of C-19 ester bond by plasma esterase. These results clarified the metabolic pathway of PB for the first time, which was of great significance to identify the in vivo active form and interpret acting mechanism of the active compounds of P. kaempferi.

Objective To explore the protective effect of L-carnitine on neonates with myocardial injury caused by as?phyxia. Methods Forty-four neonates with myocardial injury caused by asphyxia were randomly divided into L-carnitine treatment group (21 cases) and control group (23 cases). Patients in control group were received routine treatment and pa?tients in treatment group were given L-carnitine 0. 1 g/(kg · d) on the basis of routine treatment for 7 days. Symptoms and physical signs were observed before therapy and during the treatment in two groups. Before and after the treatment, plasma levels of free L-carnitine and cardiac troponin I (cTnI) were detected with the method of colorimetric assay and chemilumi?nescent, respectively. Results The clinical effective rate was significantly higher in treatment group than that of control group (90.48%vs 60.87%, P<0. 05). Compared with the control group, there was a significantly higher plasma concentra?tion of free L-carnitine in treatment group after treatment [(27.00±5.69)μmol/L vs (13.20±3.04)μmol/L, P<0.05]. In treat?ment group, plasma concentration of free L-carnitine was significantly higher after treatment than that of pre-therapy [(14.87 ± 3.95)μmol/L,P<0.05]. Compared with the control group, there was a significantly lower plasma concentration of cTnI after treatment in treatment group [(0.025±0.006)μg/L vs (0.046±0.010)μg/L, P<0.05]. In the treatment group, there was a significant correlation between decreased plasma concentration of cTnI and increased plasma concentration of free L-carnitine (r=0.899, P<0.05). Conclusion Administration of L-carnitine can effectively decrease the abnormal plasma lev?el of cTnI in neonates with myocardial injury caused by asphyxia, and thereby protect the myocardium.

Objective To determine the value of ischemia modified albumin,heart-type fatty acid-binding protein,B-type natri-uretic peptide and homocysteine in the risk stratification of patients with unstable angina pectoris;thus to provide an assessment for the condition of patients in clinic.Methods 135 patients with unstable angina were included in the disease group and subjected to risk stratification according to GRACE risk score software,70 cases of low-risk group,60 cases in the middle-risk group and 5 cases in the high-risk group.Another 145 healthy people were in the control group.The levels of ischemia modified albumin,heart-type fatty acid-binding protein,B-type natriuretic peptide and homocysteine were detected and compared.Results Between the control group and the disease group,significant difference of heart-type fatty acid-binding protein,B-type natriuretic peptide and homocys-teine was found (P <0.05),but the difference of ischemia modified albumin was not statistically significant(P >0.05).In the dis-ease group,the levels of ischemia modified albumin,heart-type fatty acid-binding protein and homocysteine in each risk stratification showed no significant difference(P >0.05).The level of B-type natriuretic peptide in high-risk group was higher than that in the low-risk group and in the middle-risk group and the difference was statistically significant (P <0.05),while there was no statisti-cally significant difference between the low-risk group and the middle-risk group(P >0.05 ).Conclusion The detection of heart-type fatty acid-binding protein,B-type natriuretic peptide and homocysteine possesses certain meaning in diagnosing unstable angi-na,and the level of B-type natriuretic peptide indicates the risk degree of the disease.

Objective To observe the expression of cysteine rich-protein 61 (Cyr61) on renal tubular cells,to explore its effects against hypoxic induced kidney injury and the underlying mechanisms.Methods A stably Cyr61 expressed tubular cell line Cyr61-HK2 was established based on HK2 cells and recombinant Cyr61-lentivirus.BrdU incorporation assay was used for cell proliferation.The apoptosis of cells was analyzed by flow cytometry with Annexin V and propidiumiodide staining.Western bloting was used to detect the protein expression of BAD,Akt and ERK.Results (1) Cyr61-HK2 cells displayed more proliferation ability than HK2 cells.(2) Under hypoxia condition,the apoptosis of both HK2 and Cyr61-HK2 cells increased,but the apoptosis of Cyr61-HK2 cells was lesser than HK2 cells.(3) The expression of Cyr61 led to the phosphorylation of BAD,Akt and ERK on 0 h,0.5 h,1 h (all P ＜ 0.05).Conclusion The expression of Cyr61 can promote cell proliferation and dampen cell apoptosis induced by hypoxia,which may be involved in the Akt/ERK signal pathway.