伏格列波糖片治疗2型糖尿病的临床疗效及不良反应

目的探讨伏格列波糖片治疗2型糖尿病的临床疗效及不良反应。方法选择我院2011年1月至2012年2月住院治疗的2型糖尿病患者76例分为观察组(n=38)与对照组(n=38),观察组采用伏格列波糖片治疗,对照组采用阿卡波糖片治疗。观察比较两组患者的治疗效果及不良反应。结果两组患者治疗后空腹血糖(FPG)、餐后2h血糖、糖化血红蛋白(HbA1c)均低于治疗前,差异均有统计学意义(P<0.05),观察组FPG、餐后2h血糖、HbA1c降低优于对照组,但两组治疗后比较差异无统计学意义(P>0.05)。观察组不良反应发生率明显低于对照组,差异有统计学意义(P<0.05)。两组均未见其他严重不良反应发生。结论伏格列波糖片治疗2型糖尿病不良反应少,并发症风险能有效降低,临床效果较好,是临床治疗2型糖尿病的首选。     

优泌乐25联合伏格列波糖治疗2型糖尿病的临床观察

目的：探讨优泌乐25联合伏格列波糖治疗2型糖尿病的临床疗效。方法76例2型糖尿病患者随机将其分为对照组（36例）和观察组（40例），对照组患者采取优泌乐25治疗，观察组患者给予优泌乐25联合伏格列波糖治疗，对两组治疗前后血糖水平及不良反应情况进行比较。结果观察组治疗后空腹血糖、餐后2 h血糖及糖化血红蛋白明显低于对照组，差异有统计学意义（P＜0.05）。结论优泌乐25联合伏格列波糖治疗能安全有效控制总体血糖，值得在2型糖尿病治疗中深入研究利用。     

伏格列波糖片对2型糖尿病空腹血糖、餐后2 h血糖、糖化血红蛋白的影响

目的探讨伏格列波糖片对2型糖尿病空腹血糖、餐后2 h血糖、糖化血红蛋白的影响。方法随机从我院2018年1月至2018年12月已收治的患者当中抽取100例2型糖尿病患者,并根据就诊的先后顺序进行平均分组,给予对照组患者阿卡波糖片治疗,给予研究组患者伏格列波糖片治疗。观察并分析两组2型糖尿病患者的临床疗效、血糖水平,以及不良反应发生率。结果研究组患者临床总有效率为96.00%,其临床疗效明显比对照组更加理想,P <0.05;研究组患者空腹血糖为(7.38±1.41)mmol/L,餐后2 h血糖为(10.02±1.13)mmol/L,糖化血红蛋白为(7.21±1.23)%,其血糖水平明显比对照组更加稳定,P <0.05;研究组患者不良反应发生率为4.00%,其不良反应发生情况明显比对照组更少,P <0.05。结论 2型糖尿病患者服用伏格列波糖片不仅能稳定血糖水平,还能降低不良反应的发生概率,具有高效、安全等特点,值得在2型糖尿病治疗中推广和应用。     

α糖苷酶抑制剂与二肽基肽酶-4抑制剂联合治疗2型糖尿病的价值

目的探讨α糖苷酶抑制剂与二肽基肽酶-4抑制剂联合治疗2型糖尿病的价值。方法收集2014年3月至2016年1月我院2型糖尿病患者100例,分为:研究组(口服二肽基肽酶-4抑制剂西格列汀+α糖苷酶抑制剂伏格列波糖)和对照组(口服二肽基肽酶-4抑制剂西格列汀)。对比,①两组治疗前后空腹血糖、餐后2 h血糖、糖化血红蛋白。②两组服用药物期间不良反应。结果①两组治疗前空腹血糖、餐后2 h血糖、糖化血红蛋白比较无差异(P>0.05),两组治疗后空腹血糖、餐后2 h血糖、糖化血红蛋白比较有差异(P<0.05)。②研究组服用药物期间1例发生恶心、1例皮疹;对照组出现2例胃肠胀气,1例便秘,两组不良反应结果比较无差异(P>0.05)。结论α糖苷酶抑制剂与二肽基肽酶-4抑制剂联合使用后可以提高降糖效果,对促进糖化血红蛋白达标有积极意义,同时使用时安全性好。     

伏格列波糖联合二甲双胍治疗初治肥胖2型糖尿病的观察

目的观察伏格列波糖联合二甲双胍治疗初治肥胖2型糖尿病的有效性和安全性。方法选择新诊断肥胖2型糖尿病患者60例,随机分成两组,A组30例,给予二甲双胍片1次0．25--0．5g,1日3次,餐后口服;B组30例,在A组的基础上给予伏格列波糖胶囊1次0．2mg,1日3次,餐时口服,两组均治疗16周。观察用药前后的血糖、糖化血红蛋白、体重指数等变化及不良反应发生情况。结果两组患者血糖、糖化血红蛋白、体重指数均明显下降,且B组下降更明显（P〈0．01）。结论二甲双胍联合伏格列波糖治疗初治的肥胖型2型糖尿病安全、有效、医嘱依从性高,值得临床应用。     

沙格列汀联合伏格列波糖对老年2型糖尿病患者糖脂代谢的影响

目的:观察沙格列汀联合α-葡萄糖苷酶抑制剂(伏格列波糖)对老年2型糖尿病(T2DM)患者糖脂代谢的影响.方法:选取2018-02～ 2019-05我院90例老年T2DM患者,采用随机数字表法分组,各45例.对照组予以伏格列波糖治疗,观察组在对照组基础上予以沙格列汀治疗.对比两组治疗前后血糖指标[空腹血糖(FBG)、餐后2h血糖(2 hPG)、糖化血红蛋白(HbA1c)]、血脂指标[总胆固醇(TC)、低密度脂蛋白胆固醇(LDL-C)]、血管内皮细胞功能[一氧化氮(NO)、内皮素-1(ET-1)]水平.结果:治疗3个月后观察组血清FBG、2 hPG、HbA1c、TC、LDL-C水平低于对照组(P＜0.05);观察组血清NO水平高于对照组,血清ET-1水平低于对照组(P＜0.05).结论:沙格列汀联合伏格列波糖治疗老年T2DM患者,不仅能降低血糖,改善糖脂代谢,还可调节血管内皮细胞功能.     

联合用药治疗2型糖尿病的临床观察

目的探讨比较吡格列酮、二甲双胍二药联用和吡格列酮、二甲双胍、伏格列波糖三药联用治2型糖尿病的疗效及安全性。方法76例对磺脲类+双胍类药物治疗失败后的2型糖尿病患者,随机分为治疗组、对照组各38例,停用磺脲类,治疗组用吡格列酮30 mg/d、伏格列波糖0.6 mg/d、二甲双胍1.5 g/d三药联用,对照组用同样剂量的二甲双胍和吡格列酮,两组均治疗6个月,监测治疗前、后两个时间节点的空腹、餐后2 h血糖、糖化血红蛋白、空腹胰岛素,肝功能、肾功能,计算胰岛素抵抗指数(IR)。结果空腹、餐后2 h血糖、糖化血红蛋白,胰岛素抵抗指数,治疗前两组指标比较差异无统计学意义(P>0.05);治疗后两组指标与治疗前比较差异均有的统计学意义(bP<0.05),治疗组更显著(aP<0.01);治疗后组间指标比较变化差异有统计学意义(cP<0.05)。空腹胰岛素:治疗前后两组指标比较差异无统计学意义(eP>0.05)。没有发现心力衰竭、严重肝肾损害、血尿和骨质疏松等严重不良反应。结论二甲双胍、吡格列酮联用是治疗磺脲类+双胍类药物治疗失败后的2型糖尿病的有效方法,加用伏格列波糖三联合用可取得更好的疗效。     

对比伏格列波糖片与阿卡波糖片治疗2型糖尿病的临床效果

目的对比伏格列波糖片与阿卡波糖片对2型糖尿病的临床疗效。方法随机选择2012年1月至2013年12月来我院进行2型DM治疗的患者68例,分为伏格列波糖组与阿卡波糖组各34例。两组患者予以对症治疗,嘱患者控制饮食,适量运动。伏格列波糖组给予伏格列波糖片0.2 mg,日3次口服。用量随病情变化调整,可增至0.3毫克/次。阿卡波糖组给予阿卡波糖片50 mg,日3次,餐前即刻口服。根据患者病情酌情增加用量,最多不超过0.2 g,日3次。观察两组患者8周后的临床疗效以及不良反应发生情况。结果两组患者经过8周治疗,空腹血糖与餐后血糖均比治疗前降低,且具有统计学意义(P<0.05)。但是两组患者治疗后的血糖值无组间差异(P>0.05)。两组患者服药后均有腹胀、肠鸣音亢进、排气增多、一过性低血糖等不良反应出现,但是伏格列波糖组患者的不良反应比阿卡波糖组少,具有组间差异(P<0.05)。结论伏格列波糖片与阿卡波糖片对糖尿病的临床疗效无明显差异,但是伏格列波糖片所引起的不良反应要少于阿卡波糖片。     

二甲双胍与伏格列波糖对2型糖尿病患者胰岛素及炎症因子的疗效比较

目的比较伏格列波糖和二甲双胍对新诊断2型糖尿病患者餐后胰岛素分泌、白细胞(WBC)和C反应蛋白(CRP)的影响。方法采用随机、平行对照、前瞻性研究方法,将24例新诊断2型糖尿病患者随机分为两组,分别口服二甲双胍(二甲双胍组)和伏格列波糖(伏格列波糖组)。服药8周后,观察患者餐后0min、30min、60min、1h、2h血糖,胰岛素分泌、白细胞(WBC)和C反应蛋白(CRP)的变化。结果单剂量二甲双胍和伏格列波糖降低标准餐后血糖的效果相似。与伏格列波糖相比,二甲双胍可显著增加2型糖尿病患者标准餐后30min后胰岛素分泌水平,改善白细胞WBC和CRP水平(P<0.05,P>0.01)。结论二甲双胍在促进餐后胰岛素分泌及改善机体炎症状态方面优于伏格列波糖,这可能与其部分恢复早时相胰岛素分泌有关。     

伏格列波糖联合二甲双胍治疗新诊断2型糖尿病的疗效观察

目的 探讨分析伏格列波糖联合二甲双胍治疗2型糖年病的临床疗效.方法 选取我院内分泌科住院部2015年6月~2016年6月期间收治的新诊断2型糖尿病患者78例,随机分为观察组和对照组各39例,观察组给予伏格列波糖联合二甲双胍的治疗,对照组只给予二甲双胍治疗,比较两组患者血糖情况及不良反应发生率.结果 观察组患者治疗后血糖指标(FPG、2hPG、HbAlc)的改善均优于对照组患者,差异均具有统计学意义(P<0.05),两组患者不良反应发生率无显著性差异(P>0.05).结论 伏格列波糖联合二甲双胍可显著改善2型糖尿病患者的血糖水平,且安全性高,值得在临床上进一步推广应用.     

Susceptibility to erythromycin of anaerobes of the genera Bacteroides, Fusobacterium, Sphaerophorus, Veillonella, Clostridium, Corynebacterium, Peptococcus, Peptostreptococcus

The minimal inhibitory concentrations (MIC) of erythromycin were determined by broth dilution tests for 313 anaerobic strains, most of which were clinical isolates. All the gram-positive anaerobes tested (84 Peptococcaceae, including 21 Peptostreptococcus anaerobius and 15 Peptococcus variabilis; 65 Corynebacterium acnes and 29 Clostridium strains, including 13 C. perfringens) were sensitive (MIC values 0.012 through 3.12 microgram erythromycin/ml); so were 111 cultures of gram-negative anaerobes (52 Bacteroides fragilis, 12 B. thetaiotaomicron, 7 B. vulgatus, 13 B. oralis, 4 B. melaninogenicus, 10 Sphaerophorus necrophorus, 2 Veillonella sp., 11 members of other species). Erythromycin at concentrations of 6.25 through 200.0 microgram/ml was active against 24 strains (1 B. fragilis, 4 Fusobacterium fusiforme, 9 Sph. freundi, 10 Sph. varius). The present results are compared to the limited number of reports existing with regard to the susceptibility of anaerobes to erythromycin.     

Safety assessment of poloxamers 101, 105, 108, 122, 123, 124, 181, 182, 183, 184, 185, 188, 212, 215, 217, 231, 234, 235, 237, 238, 282, 284, 288, 331, 333, 334, 335, 338, 401, 402, 403, and 407, poloxamer 105 benzoate, and poloxamer 182 dibenzoate as used in cosmetics

Poloxamers are polyoxyethlyene, polyoxypropylene block polymers. The impurities of commercial grade Poloxamer 188, as an example, include low-molecular-weight substances (aldehydes and both formic and acetic acids), as well as 1,4-dioxane and residual ethylene oxide and propylene oxide. Most Poloxamers function in cosmetics as surfactants, emulsifying agents, cleansing agents, and/or solubilizing agents, and are used in 141 cosmetic products at concentrations from 0.005% to 20%. Poloxamers injected intravenously in animals are rapidly excreted in the urine, with some accumulation in lung, liver, brain, and kidney tissue. In humans, the plasma concentration of Poloxamer 188 (given intravenously) reached a maximum at 1 h, then reached a steady state. Poloxamers generally were ineffective in wound healing, but were effective in reducing postsurgical adhesions in several test systems. Poloxamers can cause hypercholesterolemia and hypertriglyceridemia in animals, but overall, they are relatively nontoxic to animals, with LD(50) values reported from 5 to 34.6 g/kg. Short-term intravenous doses up to 4 g/kg of Poloxamer 108 produced no change in body weights, but did result in diffuse hepatocellular vacuolization, renal tubular dilation in kidneys, and dose-dependent vacuolization of epithelial cells in the proximal convoluted tubules. A short-term inhalation toxicity study of Poloxamer 101 at 97 mg/m(3) identified slight alveolitis after 2 weeks of exposure, which subsided in the 2-week postexposure observation period. A short-term dermal toxicity study of Poloxamer 184 in rabbits at doses up to 1000 mg/kg produced slight erythema and slight intradermal inflammatory response on histological examination, but no dose-dependent body weight, hematology, blood chemistry, or organ weight changes. A 6-month feeding study in rats and dogs of Poloxamer 188 at exposures up to 5% in the diet produced no adverse effects. Likewise, Poloxamer 331 (tested up to 0.5 g/kg day(-1)), Poloxamer 235 (tested up to 1.0 g/kg day(-1)), and Poloxamer 338 (at 0.2 or 1.0 g/kg day(-1)) produced no adverse effects in dogs. Poloxamer 338 (at 5.0 g/kg day(-1)) produced slight transient diarrhea in dogs. Poloxamer 188 at levels up to 7.5% in diet given to rats in a 2-year feeding study produced diarrhea at 5% and 7.5% levels, a small decrease in growth at the 7.5% level, but no change in survival. Doses up to 0.5 mg/kg day(-1) for 2 years using rats produced yellow discoloration of the serum, high serum alkaline phosphatase activity, and elevated serum glutamicpyruvic transaminase and glutamic-oxalacetic transaminase activities. Poloxamers are minimal ocular irritants, but are not dermal irritants or sensitizers in animals. Data on reproductive and developmental toxicity of Poloxamers were not found. An Ames test did not identify any mutagenic activity of Poloxamer 407, with or without metabolic activation. Several studies have suggested anticarcinogenic effects of Poloxamers. Poloxamers appear to increase the sensitivity to anticancer drugs of multidrug-resistant cancer cells. In clinical testing, Poloxamer 188 increased the hydration of feces when used in combination with a bulk laxative treatment. Compared to controls, one study of angioplasty patients receiving Poloxamer 188 found a reduced myocardial infarct size and a reduced incidence of reinfarction, with no evidence of toxicity, but two other studies found no effect. Poloxamer 188 given to patients suffering from sickle cell disease had decreased pain and decreased hospitilization, compared to controls. Clinical tests of dermal irritation and sensitization were uniformly negative. The Cosmetic Ingredient Review (CIR) Expert Panel stressed that the cosmetic industry should continue to use the necessary purification procedures to keep the levels below established limits for ethylene oxide, propylene oxide, and 1,4-dioxane. The Panel did note the absence of reproductive and developmental toxicity data, but, based on molecular weight and solubility, there should be little skin penetration and any penetration of the skin should be slow. Also, the available data demonstrate that Poloxamers that are introduced into the body via routes other than dermal exposure have a rapid clearance from the body, suggesting that there would be no risk of reproductive and/or developmental toxicity. Overall, the available data do not suggest any concern about carcinogenesis. Although there are gaps in knowledge about product use, the overall information available on the types of products in which these ingredients are used, and at what concentration, indicates a pattern of use. Based on these safety test data and the information that the manufacturing process can be controlled to limit unwanted impurities, the Panel concluded that these Poloxamers are safe as used.     

HPLC法测定抗妇炎胶囊中木兰花碱、黄柏碱、药根碱、巴马汀、小檗碱、槐果碱、苦参碱、氧化槐果碱、槐定碱和氧化苦参碱

目的 采用高效液相色谱（HPLC）法同时测定抗妇炎胶囊中木兰花碱、黄柏碱、药根碱、巴马汀、小檗碱、槐果碱、苦参碱、氧化槐果碱、槐定碱和氧化苦参碱10种活性成分。方法 采用InerSustain AQ-C₁₈色谱柱（250 mm×4.6 mm,5 μm）,流动相A：乙腈–无水乙醇（80∶20）,流动相B：0.1%磷酸溶液,梯度洗脱,检测波长220 nm,体积流量1.0 mL/min,柱温30℃,进样量10 μL。结果 木兰花碱、黄柏碱、药根碱、巴马汀、小檗碱、槐果碱、苦参碱、氧化槐果碱、槐定碱和氧化苦参碱分别在2.69～134.50、1.95～97.50、0.63～31.50、0.86～43.00、11.95～597.50、0.59～29.50、6.08～304.00、4.85～242.50、1.66～83.00、19.79～989.50 μg/mL线性关系良好（r≥0.999 3）;平均回收率分别为99.11%、98.23%、96.95%、97.78%、100.02%、97.21%、99.66%、99.52%、98.81%、100.08%,RSD值分别为1.04%、1.23%、1.37%、1.65%、0.70%、1.28%、0.65%、0.81%、1.11%、0.63%。结论 建立的HPLC法可用于抗妇炎胶囊中10种活性成分的测定,作为抗妇炎胶囊质量控制方法。     

Simultaneous measurement of bupivacaine, etidocaine, lidocaine, meperidine, mepivacaine, and methadone

A gas-liquid chromatographic method for the simultaneous measurement of bupivacaine, etidocaine, lidocaine, meperidine, mepivacaine, and methadone in serum is described. The drugs and the internal standard, prilocaine, are extracted from 1 ml of serum. The procedure involves a two-step extraction and injection of the extract into a gas chromatograph equipped with a 10-ft OV-11 glass column and a nitrogen-phosphorus detector. The temperature gradient program results in a run time of 16 min and retention times for meperidine, prilocaine (internal standard), lidocaine, etidocaine, mepivacaine, methadone, and bupivacaine of 3.8, 5.4, 6.0, 8.7, 11.0, 11.7, and 14.8 min, respectively. Standard curves for all drugs were linear over the 80 to 2,000-ng/ml range and recovery of all components averaged 97 +/- 2% with the lowest detection limit of 10 ng/ml for all drugs except meperidine and methadone, which were 20 ng/ml. The within-day coefficients of variation ranged from 12 to 8% at 500 ng/ml. The day-to-day coefficients of variation of the slope and intercept values ranged from 2 to 0% and 130 to 3%, respectively. Response factors of the nitrogen-specific collector varied with the drug analyzed and resulted in peak area variation at constant offset and attenuation of 30%. This method is intended and adequate for therapeutic monitoring of chronically treated pain patients who are being given various combinations of local anesthetic and/or narcotic agents.     

Strength of drug habits: For heroin,morphine, methadone,alcohol, barbiturates,pentobarbital, benzedrine,cocaine, and marijuana

The drug habits for 78 confirmed opiate addicts were studied on eight scales from the Process Association Test of Addiction (PATA) for many drug names. Through cluster analysis eight stages of addiction were defined: “to be clean”, “to learn about drugs”, “to hustle”, “to chip” (also “to be high”), to be psychologically dependent or “to need a shot”, “to be hooked”, “to kick a habit” and “to be in treatment”. Associations stimulated by the words heroin and morphine were very similar over the eight stages of addiction in opiate addicts. The subjects were especially inclined to associate morphine and heroin with the most severe level of addiction, “to be hooked”. Associations to both methadone and cocaine were elevated at the “hooked” stage, but in other respects associations to these drugs were opposite. Thus, associations to cocaine were focused on the stage of psychological dependence and the lower intermediate stage of addiction, “to chip” and “to be high”, whereas associations to methadone suggested a turning away from addiction as indicated by avoidance associations (“to come down” and “to kick a habit”) as well as associations to “treatment” and “to be clean”. Marijuana, Benzedrine, “goofball” (barbiturates) and alcohol habits were prominent at an intermediate stage of addiction (“to chip” and “to be high”). Avoidance associations were common for Benzedrine and “goofballs” (also pentobarbital) but not for marijuana or alcohol. “Hustling” associations were frequent for marijuana but not for alcohol.     

Disposition of fluvastatin, an inhibitor of HMG-COA reductase, in mouse, rat, dog, and monkey

The physiological disposition of fluvastatin, a potent inhibitor of hydroxymethylglutaryl-CoA reductase and thus cholesterol synthesis, has been studied in the mouse, rat, dog, and monkey using 14C- or 3H-labeled drug. Oral doses of fluvastatin were absorbed at a moderate to rapid rate. The extent of absorption was dose-independent and was essentially complete in all four species studied. However, the drug was subject to extensive presystemic hepatic extraction followed by direct excretion via the bile, thus minimizing the systemic burden and yielding high liver/peripheral tissue concentration gradients for fluvastatin and its metabolites. Only at high doses far exceeding the intended human daily dose of ca 0.6 mg kg-1 did fluvastatin bioavailability approach unity, apparently due to saturation of the first-pass effect. Dose-normalized blood levels of fluvastatin and total radioactivity were higher in the dog than in the other species, suggesting a smaller distribution volume in the former. Fluvastatin was partially metabolized before excretion, the extent of metabolism being smallest in the dog and greatest in the mouse. The half-life of intact fluvastatin ranged from 1-2h in the monkey to 4-7h in the dog. Regardless of the dose or dose route, the administered radioactivity was recovered predominantly in feces, with the renal route accounting for less than 8 per cent of the dose. No tissue retention of radioactivity was observed, and material balance was essentially achieved within 96h after dosing.     

New antiretroviral drugs: a review of the efficacy,safety, pharmacokinetics,and resistance profile of tipranavir,darunavir, etravirine,rilpivirine, maraviroc,and raltegravir

Background: The introduction and approval of new antiretroviral agents in the US and Canada bring new opportunities and new challenges. Arguably, for the first time ever, clinicians have the drugs necessary to achieve the goal of suppressing HIV RNA to levels less than 50 copies/mL in even the most treatment-experienced patients and in those with extensive drug-limiting resistance mutations. However, the use of these new agents is complicated by many drug–drug interactions and – to some extent – pre-existing mutations. To derive maximum durability from the use of these newer drugs, a thorough understanding of their indications and limitations is critical. Objective: To thoroughly review the six most recently approved or soon-to-be-approved antiretroviral drugs in the US and Canada: tipranavir, darunavir, etravirine, rilpivirine, maraviroc, and raltegravir. Methods: Discussion of the indications for, and pharmacokinetics, resistance profile, activity, toxicity, and clinical trials results of, the six new agents. Results/conclusions: These six new agents have resulted in marked progress towards the goal of being able to provide HIV-infected individuals with the drugs necessary to achieve decades of durable suppression of HIV without substantial toxicity.