Objective To improve the synthetic procedure of the HIV integrase inhibitor raltegravir. Methods With 2-ami-no-2-methyl-propionitrile hydrochloride as starting material,the target compound raltegravir was synthesized through amino protection by benzyl chloroformate ,amidoxime formation,cyclization induced by michael addition&Claisen rearrangement,N-methylation,N-acylation,hydroxyl protection by trimethylacetyl chloride,hydrogenolysis by the system of Pd/C and formic acid,amidation with the 5-methyl-1,3,4-oxadiazol-formyl chloride,and immediate hydrolysis without more purification. Results The chemical structure of raltegravir and the intermediates were characterized by 1H NMR,13C NMR and MS. The overall yield was about 19.45%. Conclusion Compared with the preceding process,the developed route is easy to operate,safe and suitable for industrialized production in accor-dance with the quality standard of active pharmaceutical ingredient(API).

OBJECTIVE:To improve the detection method for the dissolution of dihydroartemisinin in Dihydroartemisinin and piperaquine phosphate tablets. METHODS:The dissolution experiment adopted paddle method using 0.1 mol/L hydrochloric acid so-lution 500 mL as solvent with rotating speed of 75 r/min and sampling time of 45 min. In sample pre-treatment,the volume of 3.6% sodium hydroxide solution was increased from 5 mL to 20 mL,and that of phosphoric acid was increased from 0.2 mL to 0.7 mL. HPLC was adopted to determine the dissolution of dihydroartemisinin. The determination was performed on YMC-Pack ODS-A column with mobile phase consisted of 0.02 mol/L disodium hydrogen phosphate solution(pH adjusted to 2.4 using phosphoric ac-id)-acetonitrile(65 : 35,V/V)at the flow rate of 1.0 mL/min. The detection wavelength was set at 237 nm,and column temperature was 30 ℃. The sample size was 20 μL. RESULTS:The linear range of dihydroartemisinin were 7.802-117.03 μg/mL(r=0.9999). The limit of quantitation was 2.0 ng,and the limit of detection was 0.6 ng. RSDs of precision and reproducibility tests were all low-er than 1.0%. The recoveries were 99.18%-100.46%(RSD=0.45%,n=9). Average dissolutions of dihydroartemisinin in 3 batch-es of samples were 94.9%,77.9%,89.6%,respectively. CONCLUSIONS:Improved method enhance the accuracy for the limit of sensitivity,dissolution and detection results.

0.05). The targets of Group B were elevated than those of Group A (P0.05). Conclusion HTJQ Capsule can decrease the levels NO and NOS in lung tissues of asthmatic guinea pigs and has preventive therapeutic effect for asthma.

Objective To investigate the association between nucleotide polymorphisms (rs1569723 in CD40 gene) and clinical characteristics in Kawasaki disease (KD) in Han Chinese children. Methods A case-control study was performed,and 179 children with KD and other 197 normal children served as controls were included. The SNP genotypes were detected using PCR-RFLP, and all data were analyzed by SPSS 19.0. Results It was found that the SNP (rs1569723) was associated with KD (P=0.048), and the frequency of A allele in KD group was higher than that in control group (OR=1.505, 95%CI:1.095-2.070, P=0.012). SNP genotypes were associated with rash and lymphadenopathy (P=0.041, 0.047), but not associated with conjunctival hyperemia, hand-foot edema, oral mucosa lesions, and coronary artery lesion (P=0.688,0.758, 0.557, 0.552). Conclusions Genotypes of SNP (rs1569723) were associated with KD susceptibility, and A-allele is a risk allele. The SNP loci might be associated with rash and lymphadenopathy in KD in Han Chinese.

Objective To evaluate the results of modified Ludloff osteotomy for the treatment of severe hallux valgus. Methods Fifty six patients (63 feet) with severe hallux valgus were treated with modified Ludloff osteotomy in combination with other procedures during 1999-2000. There were three males (3 feet) and fifty three females(60 feet); the average age of the patients was 46 years old (range from 16 to 65 years old). The severe hallux valgus patients whose first intermetatarsal angles were larger than 16? were treated with modified Ludloff osteotomy. In addition to modified Ludloff osteotomy, combined Reverdin osteotomies were performed in 4 feet, and Akin osteotomies in another three. All patients were followed up for an average of 10 months (6 to 18 months), and evaluated with Maryland clinical rating systems of AOFAS. Weight bearing X-ray films were taken and measured as well. A comparison study was made between the commonly used osteotomies. The advantages and disadvantages as well, of modified Ludloff osteotomy, were evaluated.Results There was no nonunion, delayed union or infection. Based on hallux metatarsophalangea interphalangeal scale of Maryland rating system, 41 feet (65%) were in the score range from 90-100, 17 feet (27%)80-89, 5 feet (8%) 70-79. The rate of excellent or good was 92%. Conclusion Modified Ludloff osteotomy has the advantages of less shortened metatarsal, rapid healing, ability to correct deformity and earlier weight-bearing. It is a perfect procedure for severe hallux valgus patients whose first intermetatarsal angles are larger than 16?, but their first metatarsophalangeal joints are without signs of osteoarthritis.

OBJECTIVE:To establish a RP-HPLC method for the determination of Esculetine in Dinglian tablets.METHODS:The chromatographic column was Hypersil ODS C18(200mm?4.6mm,5?m)at a temperature of 25℃;the mobile phase was methyl-water-glacial acetic acid(40∶60∶0.4)at a flow velocity of 1.0mL?min-1,and the detection wavelength was set at 353nm.RESULTS:The linear concentration range of Esculetine was within 0.045～0.360?g(r=0.999 5).The average recovery rate was 97.72%(RSD=1.87%,n=5).CONCLUSION:This procedure is simple,accurate and reliable,and it can be used for the quality control of Dinglian tablets.

Objective:To select the binding-peptide of the cell surface marker CD133 of cancer stem cells from phage peptide library,and to find a new tool for research on stem cells,tumor therapy and anti-metastasis of cancer.Methods:Biotined mouse CD133 extracellular fraction was used as a target to screen phage 7-peptide library by the high affinity of streptavidin and biotin,and the clones were identified by sandwich ELISA and competitive experiment.Single strand DNA was extracted from these positive clones and was analyzed by single-strand dideoxy-sequencing.Results:After three turn solution panning,five peptides with high affinity shared the same amino acid sequence:APSPMIW and three identical peptides with high affinity shared the same amino acid sequence:LQNAPRS.Conclusion:The peptides that bind with mouse CD133 extracellular fraction with high affinity and specificity were first screened from the phage peptide library for the first time,which initially indicates that the feasibility of screening from phage peptide library with small molecule polypeptide biotined as a target.

Objective To discuss the diagnosis and treatment of ductoscopy for intraductal non-protruding lesions. Methods A retrospective analysis was made on characteristics, morphological features, and curative effects of 165 cases of intraductal non-protruding lesions between December 2002 and October 2005. Results Among the 165 cases, there were 135 cases of plasma cell galactophoritis, 18 cases of cystic mastopathy, and 12 cases of galactophoritis. In 144 cases receiving non-surgical treatment, 82 cases were completely relieved and 62 improved. Other 21 cases of plasma cell galactophoritis were surgically treated. Conclusions Mammary ductoscopy is an important way for the diagnosis of intraductal non-protruding lesions. Furthermore, effective treatment can be achieved under ductoscopy in most of cases, and unnecessary surgery may be avoided.

Objective To explore efficacy of mammary ductoscopy in diagnosis and treatment of nipple discharge.Methods 206 cases of nipple discharge underwent 211 examinations of mammary ductoscopy from May 2001 to October 2006.Results Fifty-eight patients diagnosed as non-protrusion lesions under mammary ductoscopy were treated by irrigation therapy and followed up for 3-18 months(mean,12 months) without recurrence.One hundred and forty-eight cases were diagnosed as protrusion lesions,in which 125 cases received operation.115 cases of single mammary intraductal papilloma,7 cases of papillomatosis,and 3 cases of intraductal carcinoma were diagnosed under mammary ductoscopy,while 112 case of intraductal papilloma,10 cases of papillomatosis and 3 cases of ductal carcinoma were confirmed by postoperative pathology.Of the 125 cases,mammary ducts resection was carried out in 120 cases guided by locating needle,segment mammectomy in 1 case,"mammary gland displacement" in 1 case,quadrant resection with nipple-conserving combined with axillary lymph node dissection in 1 case,quadrant resection without nipple-conserving combined with axillary lymph node dissection in 2 cases.Follow-up for 4 to 20 months(mean,10 months) showed no recurrence.3 cases of ductal carcinoma in situ were followed up for 12-18 months,and survived with tumor-free.Conclusions Mammary ductoscopy examination makes accurate diagnosis of nipple discharge induced by intraductal carcinoma before operation,and has important clinical value to choose procedures.Locating needles to locate lesions in mammary ducts may be taken as a guide during operation.

0.6). And there was high internal consistency in major instruments. The validity was examined by comparing the responses of informants and responses (good standards) of the target person in normal control group. There was also a high validity(r=0.21~0.61).Conclusion: The information reconstructed from the informants has good reliability and validity. It is possible to study suicide with psychological autopsy in China.