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 invstigate the diagnosis role of VEMP for inferior vestibular neuritis. METHODS 18 patients with inferior vestibular neuritis were studied. Especially, the oVEMP and cVEMP were recorded in all cases. RESULTS All 18 patients with VN (vertigo symptom in 15 cases, and balance disorders in 3 cases) presented normal in PTA, caloric test and Ovemp test. By contrast, the cVEMPs was abnormal in all patients with VN, including flat/no amplitude of cVEMP in 14 cases, and lower amplitude in 4 cases. After three months, 10 patients recovered, with nomal amplitude of cVEMP in 9 cases and lower amplitude in 1 case. And after half-a-year-follow-up, 18 patients went back to normal, with lower amplitude in only 2 cases. CONCLUSION The VEMP examination is valuable in the diagnosis and prognosis of inferior vestibular neuritis.

Objective To evaluate the efficacy of endoscopic thyroidectomy via the breast areola. Methods From August 2004 to May 2008,36 patients with benign thyroid nodules (

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.

Objective To diagnose the first imported case of Plasmodium ovale infection by laboratory detection. Meth?ods The epidemiological data and blood samples of the case were collected,and the samples were detected by the microscopic examination,rapid diagnostic test(RDT)and nested PCR. Results The patient was a construction worker backing from Con?go,Africa. He experienced the symptoms of irregular fever and weakness one month after returning in Lingyang Town,Junxian County. The results of RDT only suggested no?Plasmodium falciparum infection. Under the microscope,it was seen that the in?fected RBC were obviously disfigured and in irregular shape,the ring forms were thick and big,and also thick granulas in big trophozoite stage and schizont stage were found. The results of PCR showed that the size of amplified product was about 800 bp, which was conformed to that of P. ovale. Conclusion Though microscopic examination is the golden standard for malaria diag?nosis,as P. ovale is difficult to be identified under microscope,the microscopic method combined with PCR test can be used for definite diagnosis.

Mesenchymal stem cells (MSCs), which are regarded as the promising option of cell replacement therapy, are able to regulate immune response after tissue damage caused by traumatic brain injury (TBI). Secondary neuroinflammation following the mechanical injury is the essential factor of neural cell necrosis and apoptosis, even after the intracranial pressure has returned to normal. Their immune environments caused by neuroinflammtary response determine the outcome and long-term behavior function of TBI in survivors directly. MSCs modulate macrophage/microglia, drive them to polarize into alternative M2-like cells through releasing soluble cytokines, such as prostaglandin E2 (PGE2), tumor necrosis factor-stimulated gene 6 protein (TSG-6), IL-1 and TGF-β, which limits the progression of inflammation and maintain micro-environment stable. Meanwhile, macrophage/microglia exerts significant effects in MSCs survival, proliferation, differentiation and activation. It provides a novel approach as a practical anti-inflammatory therapy in clinical treatment.

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.