复合磷酸酯酶肠溶片治疗肝病患者腹胀的疗效分析

目的评价复合磷酸酯酶肠溶片对乙型病毒性肝炎腹胀患者的疗效,并与复方消化酶进行比较。方法107例慢性乙型病毒性肝炎以腹胀为主要症状的患者,分为复合磷酸酯酶肠溶片14 d组(1组)25例,复合磷酸酯酶肠溶片28 d组(2组)27例;复方消化酶14 d组(3组)28例,复方消化酶28 d组(4组)27例。治疗结束后观察患者腹胀的缓解率和不良反应。采用意向性分析和符合方案分析,进行卡方检验。结果复合磷酸酯酶肠溶片14 d组、复合磷酸酯酶肠溶片28 d组、复方消化酶14 d组、复方消化酶28 d组治疗后腹胀均有所缓解,行意向性分析分别为88.0%、92.6%、89.3%、96.3%,各组比较差异均无统计学意义(P>0.05);行符合方案分析分别为88.0%、96.2%、89.3%、96.0%,各组比较差异均无统计学意义(P>0.05)。结论复合磷酸酯酶肠溶片治疗肝病患者腹胀的效果好,疗效与复方消化酶相当,且无明显的不良反应。     

复合磷酸酯酶肠溶片预防抗结核药物肝损害的临床研究

目的 探讨复合磷酸酯酶肠溶片对初治菌阳肺结核患者抗结核药物肝损害的预防效果.方法 将68例初治菌阳肺结核分为观察组和对照组,均应用"2HRZS(E)/4HR"方案抗结核化疗,观察组加用复合磷酸酯酶肠溶片,对照组加服肝泰乐.结果 观察组药物性肝损害发生率为4.6%;中断抗结核化疗为2.86%;调整化疗方案为2.86%;与对照组的18.2%、12.1%、9.1%比较,均有显著性差异(P<0.01).结论 复合磷酸酯酶肠溶片可显著降低初治菌阳肺结核患者抗结核药物肝损害的发生率,减少因抗结核药所致肝损害而造成的不规则化疗.     

复合磷酸酯酶肠溶片在肝病治疗方面的应用概述

经过多年的临床验证,复合磷酸酯酶肠溶片对各种肝病、硬皮病、再生障碍性贫血、小儿顽固性皮癣、冠心病等多种疾病均有着较好的治疗效果。本文主要针对其在肝脏疾病治疗方面的研究情况进行综述。     

复合磷酸酯酶肠溶片联合水飞蓟宾胶囊治疗70例单纯酒精性肝病的临床观察

目的 探讨复合磷酸酯酶肠溶片联合水飞蓟宾胶囊治疗单纯酒精性肝病的临床疗效.方法 选取70例单纯酒精性肝病随机分成两组,对照组采用肌苷片联合水飞蓟宾胶囊,治疗组在对照组基础上加用复合磷酸酯酶肠溶片,观察两组患者的ALT/AST/TBIL/GGT以及临床症状的改善情况.结果 复合磷酸酯酶肠溶片联合水飞蓟宾胶囊能有效的降低转氨酶,改善症状总有效率为100%,对照组总有效率为57.14%,治疗组临床总有效率明显高于对照组(P<0.05).结论 复合磷酸酯酶肠溶片联合水飞蓟宾胶囊临床治疗效果良好,值得应用.     

复合磷酸酯酶对大鼠高脂血症性脂肪肝的作用

目的研究复合磷酸酯酶对高脂血症性脂肪肝的防治作用.方法连续灌胃脂肪乳剂30天,复制大鼠高脂血症性脂肪肝模型,造模同时给药;测定肝脏中TC、TG、MDA含量及SOD活性,观察大鼠肝组织病理变化.结果与正常对照组相比,模型组大鼠肝脏中TC、TG、MDA显著升高,SOD活性显著降低,肝细胞中出现明显的脂肪变性,而复合磷酸酯酶可以降低模型大鼠肝脏TG、TC、MDA含量,提高SOD活性,改善肝细胞脂肪变性程度.结论复合磷酸酯酶能够抑制高脂血症性脂肪肝大鼠肝脏TC、TG、MDA的异常增加,增强肝脏SOD活性,减少肝脏内脂肪的沉积,对高脂血症性脂肪肝有较好的防治作用.     

基于网络药理学的肝力保胶囊保肝作用机制研究

目的 对肝力保胶囊进行网络药理学研究,探讨肝力保胶囊保肝的作用机制。方法 选取肝力保胶囊化学物质组成中的活性成分,采用反向药效团匹配的方法预测活性成分的作用靶点;在此基础上,采用Cytoscape软件和String数据库分别构建肝力保胶囊"活性成分-作用靶点"的分子调控网络及蛋白-蛋白相互作用网络,最后采用DAVID数据库对靶点进行基因功能和信号通路分析。结果 筛选得到活性化合物19个,涉及作用靶点88个。网络分析结果表明,肝力保胶囊主要通过代谢过程、调节细胞死亡和对脂质的应答等生物过程,以及调节肿瘤坏死因子（TNF）、FoxO、Ras、ErbB、低氧诱导因子-1（HIF-1）和Toll样受体（TLR）信号通路来发挥保肝作用。结论 肝力保胶囊保肝作用具有多成分、多靶点、多通路的特点,其可能通过调节细胞死亡、TNF、FoxO、Ras等相关通路发挥作用。     

五味子保肝作用的研究进展

五味子是常用的传统滋补类中药,具有宁心安神的功效,主治心神失养之虚烦心悸,失眠多梦等症状。近年来,国内外关于五味子在保肝方面的药理作用进行了大量的研究,本文对五味子在此方面的研究进行了总结阐述,为临床研究开发保肝新药提供了理论参考。     

西藏胡黄连保肝利胆作用的研究

目的：通过动物实验研究玄参科植物西藏胡黄连的保肝利胆作用。方法：测定西藏胡黄连的根茎提取物对模型动物及正常动物多种生化指标的影响。结果；（1）西藏胡苋连能明显降低四氯化碳（CCl4)、对乙酰氨基酚（APAP）和硫代乙酰胺（TAA）所引起的急性肝损伤小鼠血清ATL、AST的升高。（2）对CCl4所致的亚急性肝损伤大鼠血清ALT，AST升高有明显抑制作用，同时可升高总蛋白的含量。（3）增加正常大鼠胆汁流量。结论：西藏胡黄连根茎醇提物具有明显的保肝利胆作用。     

水飞蓟宾胶囊保肝作用的药学研究进展

水飞蓟宾胶囊是一种从水飞蓟素中提取主要成分水飞蓟宾制成的保肝药物。本文就近年来国内外关于水飞蓟宾胶囊的药学特性和药品质量研究进行综述,主要从药品的药理作用机制、临床应用、药物动力学、安全性及质量标准等多个维度对水飞蓟宾胶囊进行药学部分的讨论,为临床合理用药提供参考。     

乾坤宁保肝作用的实验研究

用四氯化碳（ＣＣｌ_４）诱导大鼠肝脏损伤，同时用乾坤宁灌喂以保护肝脏损伤，实验结束取动物血测定ＡＬＴ、ＡＳＴ、羟脯氨酸等生化指标，并对肝脏作组织病理学观察。实验各组的ＡＬＴ、ＡＳＴ均显著低于单用ＣＣｌ４组（Ｐ＜０．０１）；羟脯氨酸也低于单用ＣＣｌ_４组（０．０５＜Ｐ＜０．１）；组织病理观察发现，实验各组肝脏病理改变均轻于单用ＣＣｌ_４组，结果表明，乾坤宁对ＣＣｌ_４所致大鼠肝脏形态和功能损伤有明显的保护作用，对肝纤维化有一定预防作用。     

小剂量阿司匹林肠溶片致全血细胞减少

患者女,67岁。因患风心病,联合瓣膜改变,心脏扩大,心律失常,于2004年起口服阿司匹林肠溶片100mg,1次/d;半年左右减为75mg,1次/d;3个月后又减为25mg,1次/d,至2005年11月5日。同时服用的药物有螺内酯20mg,2次/d,苯那普利2.5mg,1次/d。2005年10月全身出现散在皮疹、瘀斑伴瘙痒,门诊血常规检查WBC3.01×109/L。11月5日患者自行停用阿司匹林。停用之后皮疹逐渐减少,瘙痒减轻。11月11日以风心病、联合瓣膜改变、心律失常、心功能不全、粒细胞减少症收住院。入院查T36.8℃,P66次/min,R20次/min,BP105/70mm Hg(1mm Hg=0.133kPa)。全身皮肤黏膜…     

Development of a multiple-unit tablet containing enteric-coated pellets

Film coating of pellets is a common way to design modified-release systems. The aim of this study was to produce a multiple-unit tablet compressed from enteric-coated pellets. The dosage form should comply with Pharmacopoeial demands, especially regarding dissolution, but preferably also all other parameters, including sufficient hardness for packaging procedures. Various approaches, such as using different cushioning excipients, using different enteric coating polymers, changing the tablet shape, and application of an additional protective coating, were employed to develop the dosage form. The final formulation released 9.0?±?1.8% of the drug in an acidic medium and was compliant regarding uniformity of mass, content, and friability, and had a hardness of 59 N. An optimal coating was obtained by mixing two acrylic polymers: relatively brittle Eudragit® L30 D-55 with more flexible Eudragit® FS 30 D. A mixture of Avicel® PH 101 as filler and Kollidon^® VA 64 as dry binder was found to be optimal as a cushioning excipient. It was found that tablet shape and an additional protective pellet coating of Kollidon^® VA 64 were the key elements for this development. A biconvex tablet shape was found to approximately halve the release in an acidic medium compared to a round flat-faced tablet.     

柳氮磺吡啶肠溶片人体生物等效性研究

目的柳氮磺吡啶肠溶片（sulfasalazine enteric—coated tablet,SECT）属于口服不易吸收的药物,其人体药动学和相对生物利用度研究存在一定难度。本研究通过评价不同厂家生产的两种制剂的生物等效性,建立SECT的研究方法。方法对24名健康男性志愿者按随机交叉自身对照的方法,给予单剂量口服500mg SECT受试制剂和参比制剂,两次试验间隔为1周,分别测定血浆柳氮磺吡啶（sulfasalazine,SS）、磺胺吡啶（sulfapyridine,SP）、5－氨基水杨酸（5－aminosalicylic acid,5-ASA）浓度。结果血浆中SS、SP、5-ASA的药动学参数如下：以AUC0→t计算,受试制剂SECT中SS相对生物利用度为（108．8±24．1）％;SP相对生物利用度为（105．0±25．0）％;5-ASA相对生物利用度为（94．1±22．0）％。以AUC0→∞算,受试制剂SECT中SS相对生物利用度为（106．9±23．4）％;SP相对生物利用度为（104．1±25．0）％;5-ASA相对生物利用度为（93．6±22．2）％。受试制剂与参比制剂的血药浓度．时间曲线基本一致,受试制剂与参比制剂主要药动学参数无显著性差异（P〉0．05）。结论两家厂家生产的SECT,受试制剂与参比制剂在健康中国人体内具有生物等效性。     

Comparative bioavailability of two enteric-coated tablet preparations of diclofenac sodium

In a random cross-over study, eight healthy volunteers received single 25 mg doses of enteric-coated diclofenac sodium tablets (as either Voltaren 25, Ciba-Geigy or Anfenax 25, Istituto Biochimico Italiano) after an overnight fast. The bioavailability of these two preparations of diclofenac sodium did not differ significantly as judged by absorption lag time, peak plasma concentration, time to peak plasma concentrations or area under the plasma concentration-time curve. Diclofenac was found to have a plasma clearance of 2.85 +/- 1.03 (s.d.) and 3.39 +/- 1.43 ml min-1 kg-1, a plasma terminal half-life of elimination of 0.61 +/- 0.25 and 0.71 +/- 0.39 h, and an apparent volume of distribution of 0.15 +/- 0.10 and 0.21 +/- 0.13 l kg-1 (the values obtained with the Ciba-Geigy preparation being shown before the Istituto Biochimico Italiano preparation in each case).     

Review of the immunosuppressant enteric-coated mycophenolate sodium

Enteric-coated mycophenolate sodium (EC-MPS; myfortic^®, Novartis Pharma AG) is an advanced formulation delivering mycophenolic acid (MPA). EC-MPS was designed to improve MPA-related upper gastrointestinal adverse events by delaying the release of MPA until reaching the small intestine. At a dose of 720 mg, EC-MPS exhibits equivalent MPA exposure (area under the concentration curve [AUC]) and maximal MPA concentration (C_max) to mycophenolate mofetil (MMF; CellCept^®, Roche AG) 1000 mg. The time to maximal MPA concentration (T_max) for EC-MPS is delayed relative to that for MMF, consistent with a functioning enteric coating. EC-MPS 720 mg b.i.d. has demonstrated therapeutic equivalence to MMF 1000 mg b.i.d. in renal transplant patients. Recent clinical trials have demonstrated that EC-MPS is as effective and safe as MMF in both de novo and maintenance renal transplant patients. Furthermore, studies have confirmed that maintenance patients can be safely converted from MMF to EC-MPS with no compromise of efficacy or safety. EC-MPS therefore presents physicians and patients with a valid alternative MPA therapy with a comparable efficacy and safety profile to MMF.     

Review of the immunosuppressant enteric-coated mycophenolate sodium

Enteric-coated mycophenolate sodium (EC-MPS; myfortic, Novartis Pharma AG) is an advanced formulation delivering mycophenolic acid (MPA). EC-MPS was designed to improve MPA-related upper gastrointestinal adverse events by delaying the release of MPA until reaching the small intestine. At a dose of 720 mg, EC-MPS exhibits equivalent MPA exposure (area under the concentration curve [AUC]) and maximal MPA concentration (C(max)) to mycophenolate mofetil (MMF; CellCept, Roche AG) 1000 mg. The time to maximal MPA concentration (T(max)) for EC-MPS is delayed relative to that for MMF, consistent with a functioning enteric coating. EC-MPS 720 mg b.i.d. has demonstrated therapeutic equivalence to MMF 1000 mg b.i.d. in renal transplant patients. Recent clinical trials have demonstrated that EC-MPS is as effective and safe as MMF in both de novo and maintenance renal transplant patients. Furthermore, studies have confirmed that maintenance patients can be safely converted from MMF to EC-MPS with no compromise of efficacy or safety. EC-MPS therefore presents physicians and patients with a valid alternative MPA therapy with a comparable efficacy and safety profile to MMF.     

莫达非尼肠溶片体外释放度的研究

莫达非尼（modafinil）是一种新型非苯丙胺类中枢神经系统兴奋药，化学名称2-（二苯甲基亚硫酰）乙酰胺，该药略溶于甲醇，在乙醇或乙酸乙酯中做溶，几乎不溶于水，它具有良好的中枢兴奋作用，能改善因长期睡眠剥夺（sleep deprivation，SD）导致人体疲劳困倦程度增加．以及由认知能力下降产生的不良影响。临床用于治疗发作性睡病。改善病人白天嗜睡症状，维持正常工作，却不会出现异常兴奋。有研究认为合理使刖该药是提高部队战斗力和持续作战能力，     

Gastrointestinal transit of an enteric-coated delayed-release 5-aminosalicylic acid tablet

Gastrointestinal transit of an enteric-coated, delayed-release 5-aminosalicylic acid tablet radiolabelled with indium-111 has been monitored in a preliminary study with eight healthy subjects using gamma scintigraphy. Gastric emptying of the tablet was delayed by the presence of food in the stomach. Disintegration occurred about 5 hours after the tablet left the stomach. There was close agreement between the tablet disintegration times and the initial detection of drug in the blood. The site of disintegration could be established in most instances; approximately 80% of the doses resulted in drug dispersion within the ascending colon. The coated tablets provide an effective means of drug delivery to the proximal colon.     

肠溶包衣胰岛素-壳聚糖复合物纳米粒的制备及体内外性质

目的制备肠溶包衣的胰岛素壳聚糖复合物纳米粒,并对其理化性质、体外释药以及在糖尿病模型大鼠体内的降血糖效果进行研究。方法采用离子交联法制备胰岛素壳聚糖复合物纳米粒,使用羟丙基甲基纤维素酞酸酯(HP55)对其进行肠溶包衣;通过扫描电子显微镜观察其表观形态,用激光粒度测定仪测定其粒径大小,用Zeta电势测定仪测定其Zeta电势,使用HPLC法测定离心上清夜中胰岛素浓度,计算包封率。结果制备得到的纳米粒均匀、圆整,包衣前后粒径分别为(281±10)nm和(328±13)nm,Zeta电势分别为(30.4±6.97)mV和(33.7±6.69)mV,包封率分别为78.5%和74.3%;肠溶包衣纳米粒在人工胃液和肠液中的释药速率均明显低于未包衣纳米粒,突释效应显著减小;未包衣复合物纳米粒能够显著降低糖尿病模型大鼠的血糖浓度,其降糖效果能持续20 h以上,肠溶包衣后,降糖效果明显增强;肠溶包衣前后在模型大鼠体内24 h相对生物利用度分别为11.12%和16.29%。结论肠溶包衣胰岛素壳聚糖复合物纳米粒可以有效抑制胰岛素的突释,促进其吸收,显著降低模型大鼠的血糖浓度,能够作为胰岛素口服给药的有效载体。     

The effect of food and tablet formulation on plasma prednisolone levels following administration of enteric-coated tablets.

1 Plasma prednisolone levels have been compared following the administration of enteric-coated prednisolone to fasted and non-fasted subjects. The effect on plasma levels of altering the formulation of the enteric-coating has also been studied. 2 The presence of food in the stomach at the time of administration does not affect the absorption of enteric-coated prednisolone tablets. 3 There was considerable inter-subject variation in plasma prednisolone levels after administration of shellac based enteric-coated tablets. However, plasma levels were more consistent when a preparation whose formulation was based upon cellulose acetate phthalate (CAP) was given. 4 It is concluded that the pattern of absorption and plasma prednisolone levels depend on the formulation of the enteric coating. The bioavailability of the CAP based preparation is similar to that of plain prednisolone.