Purpose The aim of this study was to compare the pharmacokinetic(PK) profile and relative bioavailability of two sustained release tablets containing 10 mg mizolastine in healthy, young Chinese volunteers. Methods A single oral dose of mizolastine was given under fasting conditions to volunteers aged from 21 to 24 years in this open-label, randomized, crossover study. A ten-day washout period was applied between each of the two formulations. Plasma samples were obtained before dosing and at predetermined time points after dosing up to 48 hours and were analyzed for plasma concentration with a high-performance-liquid chromatography-UV method. PK parameters representing the extent and the rate of absorption of mizolastine were obtained. An analysis of variance, 90% confidence intervals, and two one-sided tests were employed for statistical analysis of relative difference between the two formulations. Results According to the pharmacokinetic and statistical analysis, parameters were not statistically different between the two formulations except the peak concentration (cmax). The point estimates of the ratios of AUC0→t, AUC0→∞ of mizolastine were (101.26 + 9.82) % and (102.52 + 8.61)% with 90% confidence intervals (CIs) of 95. 5% - 106. 5% and 97. 7% -106.9% respectively, comprised in the stipulated 80% - 125% range; for cmax values, the ratios was 82.17% - 15.32% with the 90% CIs of 71. 7% - 91.1%, fell in the recommended range of 70% -143%. Conclusions The results indicate that there is no statistically significant difference in PK parameters except cmax between the two sustained release tablets of mizolastine. The 90% CIs of AUC0→t,AUC0→∞ and cmax are within the predefined range. Thus, the two sustained release tablets of mizolastine are considered bioequivalent and generally well tolerated.

Background Bevacizumab and triamcinolone acetonide (TA) has been widely used in the treatment of diabetic macular edema (DME) clinically,but the effectiveness of both treatment has disadvantage.Therefore,some researchers try to combine bevacizumab with TA for the management of DME,but its efficacy is controversial.Objective This study was to evaluate the efficacy and safety of intraovitreal injection of bevacizumab combined with TA versus bevacizumab for DME.Methods The randomized controlled trials (RCTs) of bevacizumab combined with TA versus bevacizumab via intraovitreal injection for DME were searched from Pubmed,EMbase,Cochrane Library,CNKI.The methodological quality of the literature was evaluated according to evidencebased medicine (EBM),and the quality of the RCTs was appraised based on the Cochrane Handbook for Systematic Reviews of Interventions Version 5.0.The outcome indicators including the change values of central macular thickness (CMT) and best-corrected visual acuity (BCVA) as well as the safety indicators including topical and system adverse response of RCTs were analyzed with Cochrane Collaboration' s software RevMan 5.0.Results Nine RCTs were included with 665 eyes.The decrease value of CMT was more remarkable in the bevacizumab combined with TA group than that of the only bevacizumab group 12 weeks and 18 weeks after intravitreal injection (WMD =-44.69,95％ CI:25.27-64.11,P ＜ 0.000 001 ; WMD =-66.86,95％ CI:40.67-93.05,P ＜ 0.000 001).However,no significant differences were found in the change value of CMT in 6 weeks and 6 months after injection between the two groups (WMD =-15.40,95％ CI:-4.04-34.85,P =0.12 ; WMD =-2.57,95％ CI:-19.62-24.75,P =0.82).The improvement value of BCVA (LogMAR) in the bevacizumab combined with TA group was superior to that of the only bevacizumab group 6 weeks after injection (WMD =-0.04,95 ％ CI:-0.08--0.00,P =0.05),but there were no significant differences between the two groups at 12weeks,18 weeks and 6 months after treatment (WMD =-0.04,95％ CI:-0.12-0.05,P=0.36;WMD =-0.04,95％ CI:-0.11-0.03,P=0.28; WMD =0.03,95％ CI:-0.05-0.12,P=0.45).The incidence rate of transient anterior response after injection was not significantly different between the two groups (RR =0.89,95％ CI:0.49-1.60,P =0.70).Secondary ocular hypertension after injection occurred in 30 eyes in the bevacizumab combined with TA group,but no hypertension was seen in the only bevacizumab group.Conclusions Compared with only bevacizumab,intravitreal injection of bevacizumab combined with TA has a better efficacy in improving CMT but no obvious dominant in increasing BCVA for early DME.Intravitreal injection of bevacizumab combined with TA seemingly has a higher risk of inducing controllable ocular hypertension than administration of only bevacizumab.

Objective To investigate the effect of neonatal overfeeding on the expression of lipid metabolic associated enzymes and molecular mechanisms in the livers of rats. Methods Male Sprague-Dawley rats were randomly assigned to litter sizes of three group ( small litters,SL group) or ten ( normal litters,NL group) on postnatal day 3. Body weight,milk intake,liver and fat pad (epididymal and retroperitonea) weight,and hepatic histological anal-ysis were recorded in week 2 and week 3,respectively. The levels of lipids were detected by the automatic biochemical analyzer. The mRNA expressions of acetyl-CoA carboxylase ( ACC) ,lipoprotein lipase ( LPL) ,liver-type fatty acid-binding protein (L-FABP), carnitine palmitoyltransferase 1(CPT1),microsomal triglyceride transfer protein (MTP), sterol regulatory element-binding protein-1c (SREBP-1c) and peroxisome proliferator activated receptorα(PPARα) in liver were determined by real time PCR;the protein expressions of SREBP-1c and PPARα were determined by Western lot. Results As early as week 2,the body weight of rats in SL group began to elevate (t=-5. 997,P<0. 001) and food intake (t=-3. 462,P=0. 002) compared with the rats in NL group,and persistent to weaning (body weight:t=-17. 019,P<0. 001;food intake:t=-2. 276,P=0. 031). By the time of 3 weeks old,SL rats increased visceral fat pad [ret-roperitonea (t=-7. 643,P<0. 001),epididymal (t=5. 997,P=0. 001)],liver weight (t=-7. 812,P<0. 001),hepatosomatic index (t=-3.829,P=0. 003) and serum triglyceride (TG) level (t=-2. 703,P=0. 022) compared with those of NL rats,as well as the level of hepatic ACC mRNA (t=-3. 751,P=0. 007),LPL (t=-2. 721,P=0. 017) and L-FABP mRNA (t=-2. 521,P=0. 026) . While CPT1 mRNA (t=-1. 531,P=0. 155) and MTP mRNA (t=-1. 741,P=0. 098) levels remained unchanged in both groups. Hepatic SREBP-1c mRNA expression increased in SL rats after 2 to 3 weeks (t=-2. 836,P=0. 016),paralleled with ACC and LPL mRNA expression;while the mRNA and protein expression of PPARα re-mained unchanged (t=-0. 854,P=0. 411). Conclusions Postnatal overfeeding can promote higher liver pad and dyslip-idemia at the time of weaning. The process may be regulated by up-regulated expression of ACC, LPL and L-FABP. SREBP-1c may be participated in the regulation of ACC,a rate-limiting enzyme involved in lipogenesis.

Objective To explore the diagnosis, treatment strategies and clinical outcomes of spontaneous subarachnoid hemorrhage in elderly patients. Methods A total of 68 patients aged over 60 years presenting with spontaneous subarachnoid hemorrhage underwent cerebral angiography. And 72 intracranial aneurysms were detected in 60 patients, among whom 47 patients with 59 aneurysms underwent endovascular coil embolization, 6 aneurysms in 6 patients were clipped in microneurosurgery operation, and 7 patients chose conservative treatment. Results A total of 57 aneurysms (96.6%) were embolized successfully, among which 40 aneurysms (70.2%) reached dense occlusion and 17 aneurysms (29.8%) reached incomplete occlusion. Among 47 patients undergoing endovascular treatment, 39 patients (83.0%) were evaluated as good, 7 patients (14.9%) were moderately to seriously disabled according to Glasgow Outcome Scale when they were discharged, and one patient died. Conclusions Active treatment such as endovascular coil embolization can acquire good outcome in elderly patients with spontaneous subarachnoid hemorrhage, especially in elderly patients detected with aneurysms.

Objective:To investigate the application value of magnetic resonance T2mapping in the diagnosis of knee osteoarthritis (KOA).Methods:The MRI data of the knees of 148 patients with KOA who underwent diagnosis and treatment between January 2017 and December 2020 in Benxi Central Hospital (KOA group) and 30 healthy volunteers (control group) were retrospectively analyzed. T2 values of cartilage in each sub-region of the knee were measured, grouped, and statistically analyzed.Results:There was no significant difference in the T2 value of cartilage in each sub-region of the knee between male and female patients in mild and severe KOA groups (all P > 0.05). T2 values in the medial anterior, middle, and posterior areas of the tibia, lateral anterior, middle and posterior areas of the tibia, medial middle, posterior and lateral areas of the femur, and lateral posterior area of the femur were (44.47 ± 2.35) ms, (46.52 ± 3.12) ms, (45.47 ± 2.40) ms, (43.68 ± 2.12) ms, (46.33 ± 3.36) ms, (43.92 ± 3.42) ms, (43.58 ± 2.40) ms, (45.53 ± 3.91) ms, (44.36 ± 3.15) ms, (46.41 ± 3.04) ms, respectively in the control group. They were (49.56 ± 2.05) ms, (51.67 ± 2.38) ms, (50.47 ± 2.53) ms, (48.68 ± 3.05) ms, (51.33 ± 4.62) ms, (48.92 ± 2.53) ms, (48.58 ± 3.15) ms, (50.53 ± 3.72) ms, (48.36 ± 2.41) ms, and (51.41 ± 3.64) ms, respectively in the mild KOA group, and (53.47 ± 2.46) ms, (56.52 ± 3.57) ms, (54.85 ± 2.89) ms, (52.68 ± 3.57) ms, (56.33 ± 3.91) ms, (52.92 ± 3.04) ms, (53.58 ± 3.36) ms, (55.53 ± 3.42) ms, (52.36 ± 4.13) ms, and (56.41 ± 3.56) ms, respectively in the severe KOA group. There were significant differences in abovementioned indices among the three groups ( F = 38.768, 39.412, 38.981, 40.432, 38.416, 38.635, 38.347, 40.712, 38.158, 39.418, all P < 0.05). Conclusion:The T2 value of knee cartilage in patients with KOA is unrelated to gender and related to the severity of the disease. Magnetic resonance T2 mapping can help diagnose KOA, and provide information about the changes in cartilage components of patients with early KOA.

OBJECTIVETo study the chemical constituents of the flavonoids from Sophora tonkinensis.

METHODThe compounds were isolated by chromatography on silica gel, Sephadex LH-20 column and identified by spectroscopic analysis.

RESULTEight compounds were isolated and their structures were identified as tonkinochromane I (1), glabrol (3), lupinifolin (2), tonkinensisol (4), 8-C-prenylkaempferol (5), 7,2'-dihydroxy-4'-methoxy-isoflavanol (6), formononetin (7), and genistein (8), respectively.

CONCLUSIONCompound 1 was a new compound. And compound 6 was firstly isolated from the genus Sophora. Compounds 2, 3 and 5 were isolated from S. tonkinensis for the first time.

Chromatography, High Pressure Liquid ; Flavonoids ; analysis ; chemistry ; Genistein ; analysis ; Isoflavones ; analysis ; Rhizome ; chemistry ; Sophora ; chemistry