Corneal pharmacokinetics of the 2% diacerein eye drops between multiple administration and single administration / 国际眼科杂志(Guoji Yanke Zazhi)

·AIM: To compare the pharmacokinetic differences of the 2% diacerein eye drops between conjunctival sac multiple administration and single administration in the cornea, and to provide the experimental basis for clinicians to use the conjunctival sac multiple administration. · METHODS: Male Kunming mice were randomly divided into the multiple administration group and the single administration group. The multiple administration group were given diacerein eye drop every 2min(3 times in total). The concentrations of the metabolites of diacerein in the cornea were measured by high performance liquid chromatography after given eye drop 5, 15, 30, 60, 120, and 180min. The pharmacokinetic parameters were calculated by pharmacokinetic software (DAS2.1.1). ·RESULTS: The metabolites of diacerein, rhein, was detected in the cornea at each time point. The concentration of the metabolite of diacerein in the cornea was 318.678±40.88,210.02±25.66,188.83±31.74,112.24± 11.70,90.28±22.01 and 57.67±13.71μ g/g after given eye drop 5, 15, 30, 60, 120, and 180min in the multiple administration group. The concentration in the single administration group was 145.17 ± 19.29, 97.95 ± 10.49, 71.18±18.70,39.11±2.44,18.10±2.34 and 9.08±2.04μ g/g respectively. The concentration of rhein in the cornea was the highest at 5min after the administration in the two groups. The concentration of the multiple administration group was higher than that in the single administration group at 5, 15, 30, 60, 120, and 180min (P<0.01). The half-life of the drug was 0.89 ± 0.31h in the single administration group. · CONCLUSION: Compared with the single administration, the conjunctival sac multiple administration has the advantages of high drug concentration and long duration. Therefor the conjunctival sac multiple administration is a more effective method to treat acute infectious corneal diseases.

Clinical observation of Oxycodone Controlled-release Tablets in docetaxel second-line treatment of advanced lung cancer / 上海预防医学

[Objective] To evaluate the efficacy and safety of oxycodone controlled-release tablets in patients with advanced non-small cell lung cancer ( NSCLC ) who suffered from cancer pain and needed the treatment of docetaxel as second-line drug. [Methods] Data from 40 patients with NSCLC who suf-fered from moderate and severe cancer pain and were treated with oxycodone controlled -release tablets and docetaxel 75mg/m2 on d1 every 3 weeks from Feb 2007 to July 2011.The analgesic effects, karnofsky per-formance status scales ( KPS) and adverse effects were observed . [ Results] A group of 40 patients were available for evaluation, of whom the response rate was 27.5%,the disease control rate 60%,and the medi-an survival of all 9.35 months, with one-year survival rate being 37.5%.Compared with the condition be-fore treatment, pain in patients was greatly relieved , and the total pain relief rate was 97.5%,with the NRS score decreased significantly , and KPS score significantly raised , whose differences were statistically signifi-cant (P<0.05).The main side effect was hematologic toxicity and constipation , which could be solved af-ter treatment. [ Conclusion] Oxycodone combined with Docetaxel has satisfactory efficacy for the pa-tients with moderate to severe pain in NSCLC , thus markedly improving the quality of life of the patients .

Mechanism of Shenqi compound recipe anti-earlier diabetic artherosclerosis in GK rats / 中国中药杂志

<p><b>OBJECTIVE</b>To explore the mechanism of Shenqi compound recipe (SQCR) anti-earlier diabetic artherosclerosis in GK rats.</p><p><b>METHOD</b>Four-month specefic pathogen free (SPF) GK rats were divided randomly according to blood glucose level into four groups: model group (5 mL x kg(-1) x d(-1) sterile water), ramipril group (positive control, 1 mg x kg(-1) x d(-1)), SQCR low dosage (0.72 g x kg(-1) x d(-1)) and SQCR high dosage group (2.88 g x kg(-1) x d(-1)) and Wistar rats as normal control group(5 mL x kg(-1) x d(-1) sterile water). GK rats took high-fat diet freely and meanwile were injected N-omega-nitro-L-arginine methyl ester (L-N-AME) intra-peritoneally with the dose of 10 mg x kg(-1) x d(-1) in order to induce earlier diabetic artherosclerosis, while normal control group took regular diet and were injected normal saline intra-peritoneally. In the experiment periods, each group was administrated correspondent substance respectively for 32 d. At the end, sampling blood by abdominal aorta and picking aorta on ice. Determined monocyte chemoattractant protein-1 (MCP-1) concentration by ELISA, messenger ribonucleic acid (mRNA) expression of MCP-1 and peroxisome proliferator-activated receptor gamma (PPARgamma) in aorta by reverse transcriptase PCR (RT-PCR).</p><p><b>RESULT</b>Concentrations of MCP-1 in serum in SQCR low and high dosage groups and the mRNA expression of MCP-1 in SQCR high dosage group were all decreased significantly compared with model group (P < 0.05). The mRNA expression of PPARgamma in SQCR low and high dosage groups all increased compared with model group (P < 0.05 or P < 0.01).</p><p><b>CONCLUSION</b>Inhibiting the mRNA and protein expression of MCP-1 and upregulating the mRNA expression of PPARgamma in aorta might be contribute to SQCR anti-earlier diabetic artherosclerosis in GK rats partly.</p>

Effects of soy isoflavone on levels of low-grade inflammatory peptides in rats with insulin resistance / 南方医科大学学报

<p><b>OBJECTIVE</b>To explore the effects of soy isoflavone (SIF) on low-grade inflammation in rats with high-fat diet-induced insulin resistance (IR) and explore the mechanisms of SIF in improving insulin sensitivity.</p><p><b>METHODS</b>The rats with high-fat diet-induced IR were randomly divided into one model control group and 3 SIF groups gavaged with SIF water solutions at the doses of 50, 150, and 450 mg/kg, respectively. One month after the treatment, fasting blood glucose (FBG), fasting insulin (FINS), interleukin-6 (IL-6), tumor necrosis factor-alpha (TNF-alpha), C-reactive protein (CRP), resistin and adiponectin in the serum were detected by enzymatic method, radioimmunoassay, or enzyme-linked immunosorbent assay.</p><p><b>RESULTS</b>In the 150 and 450 mg/kg SIF groups, fasting body-weights, visceral adipose tissue deposition, FINS, resistin, TNF-alpha in serum, and IR index were lowered in comparison with the model control group, and in 450 mg/kg SIF group, serum IL-6 level was obviously lowered, and adiponectin increased. No differences were found in serum C-reactive protein levels between the 3 SIF groups.</p><p><b>CONCLUSION</b>Soy isoflavone may ameliorate insulin sensitivity by decreasing visceral adipose deposition and adjusting low-grade inflammatory molecules derived from white adipose tissue.</p>

Effects of soy isoflavone on low-grade inflammation in obese rats / 中南大学学报(医学版)

OBJECTIVE@#To explore the effects of soy isoflavone (SIF) on low-grade inflammation in obese rats induced by high-fat diet, and to elucidate mechanisms of SIF in improving insulin sensitivity.@*METHODS@#Obese rats were randomly divided into 4 groups: One model control group and 3 SIF groups that were given water solutions with SIF at 0 mg/(kg x d), 50 mg/(kg x d), 150 mg/(kg x d), and 450 mg/(kg x d), respectively. After one month, fasting glucose, fasting insulin, interleukin-6, tumor necrosis factor-alpha, C-reactive protein, resistin, and adiponectin in serum were detected by enzymic method, radioimmunoassay, and enzyme linked immunosorbent assay, respectively.@*RESULTS@#In the 150 mg/(kg x d) group and 450 mg/(kg x d) group, fasting body-weights, viscera fatty deposition, and contents of insulin, interleukin-6, and tumor necrosis factor-alpha in serum were significantly lower; serum adiponectin levels were significantly higher; and serum resistin levels were significantly lower in the 450 mg/(kg d) group than those of the model control group. There was no difference in serum C-reactive protein levels among the 3 SIF groups.@*CONCLUSION@#Soy isoflavone may improve the insulin sensitivity by decreasing viscera fatty deposition and adjusting low-grade inflammatory molecules derived from white adipose tissues.