吲哚美辛栓质量分析

目的:评价国产吲哚美辛栓的质量现状和问题。方法:按照2010年度国家评价性抽验计划,采用法定检验方法结合探索性研究进行样品检验。结果:本文采用英国药典32版和2005年版中国药典方法,通过专属性实验和各厂家样品杂质含量结果的比较,证实2005年中国药典方法更为简便,而2个主要杂质经质谱分析,证明为工艺杂质,来源于原料。采用美国药典32版溶出度方法检查样品的溶出情况,发现国内产品采用脂溶性基质,国外产品采用水溶性基质,两者溶出情况不一致。结论:目前吲哚美辛栓的产品质量能符合现行标准的要求;探索性研究提示可以以提高吲哚美辛原料质量的方式,提高制剂质量。     

吲哚美辛栓致结肠直肠应激性溃疡1例

患者 ,男 ,3 2岁。因肛旁肿痛 4d ,以肛周脓肿收入院。既往体健 ,入院第 2天在骶麻下行肛周脓肿切开挂线术 ,术后予0 .5%甲硝唑冲洗伤口后 ,五黄软膏纱条换药 ,肛门内塞入吲哚美辛栓 1枚 (10 0mg ,湖北省江陵制药厂生产 ,批号 :990 12 0 ) ,每天 1或 2次 ,15d后 ,肛门伤口已基本愈合。第 16天 ,患者无明显诱因排出约 10 0mL暗红色血便 ,立即予 0 .9%氯化钠注射液10 0mL加阿米卡星 0 .2g ,云南白药 2 .0g保留灌肠。次日仍间断排出大量暗红色或鲜红色血便 50 0～ 60 0mL ,出现头晕、出汗 ,便后晕厥 1次 ,血压 80 50mmHg(1mmHg =0 .13 3kPa…     

吲哚美辛栓诱发全身肌无力合并失语症一例

患者女,35岁,因腰痛、发冷、发热4 d入院.入院前4 d无明显诱因出现腰部持续性胀痛,发冷、发热,体温39.5℃,初诊为"肾盂肾炎",给予抗感染治疗.入院当日19:00患者未经医生许可,将家中自备的吲哚美辛栓50 mg直肠给药.     

直肠应用吲哚美辛栓致过敏性哮喘及急性心肌缺血

1例43岁男性患者因发热给予吲哚美辛栓50mg直肠应用。约20min后患者出现胸闷气短、呼吸困难，颜面、口唇及四肢末端发绀、端坐呼吸，两肺满布哮鸣音。紧急予吸氧，雾化吸入布地奈德，静脉滴注甲泼尼龙及多索茶碱。血气分析提示呼吸性酸中毒，心电图检查提示急性心肌缺血。予气管插管、呼吸机辅助呼吸。经综合抢救4d，患者病情渐平稳。     

HPLC测定复方吲哚美辛栓中的吲哚美辛

目的采用HPLC法测定复方吲哚美辛栓中吲哚美辛的含量。方法采用C18色谱柱,流动相为0.05 mol·L-1乙酸-乙腈(50∶50),测定波长260 nm。结果吲哚美辛25.59～307.13 mg·L-1与峰面积的线性关系良好(r=0.9999),回收率为98.9%(RSD=2.0%,n=6)。结论所用方法准确、可靠,可用于复方吲哚美栓的质量控制。     

吲哚美辛栓致肌无力1例

<正>临床资料:患者,女,40岁。因咳嗽、恶寒、发热4 d收入院。入院查体:T39.3℃、P108次/分、R22次/分、BP120/70mmHg,神志清,精神不振,营养一般,自主体位,血常规示:WBC:10.8×109.L-1,入院诊断:气管感染。入院后即给予NS 100 mL,哌拉西林舒巴坦钠1.25 g静脉滴注,每天两次,复方甘草合剂10 mL口服,每日3次。患者于入院第二天     

吲哚美辛栓的临床应用评价

目的 通过调查吲哚美辛栓的临床应用,进一步评价其疗效和用药安全性.方法 对2008年3月～2010年5月临床使用吲哚美辛栓治疗前列腺电切术后膀胱痉挛、中枢性高热、恶性肿瘤晚期疼痛、发热、痛经、人工流产镇痛和妇科术后镇痛的情况进行调查,了解吲哚关辛栓在临床中的应用范围、药物的疗效和主要的不良反应.结果 吲哚美辛栓治疗的总...     

吲哚美辛缓释栓的实验研究

以明胶为成囊材料制成吲哚美辛微囊,再以聚乙二醇为基质,制成具速释与缓释功能的栓剂,并与其它类型栓剂进行了溶出度比较。     

吲哚美辛栓致不良反应1例

患者,女,58岁,体质消瘦,营养中度,体检发现右肾积水,于2010年8月11日入院,体温（T）36．5℃,心率（P）80次／min,呼吸（R）20次／min,血压（BP）60／90mmHg（1mmHg=0．133kPa）,无发热、尿急、尿痛、尿频、无肉眼血尿。饮食二便正常,既往史一般状况良好,无药物过敏史。     

吲哚美辛栓引起的全身性过敏反应

吲哚美辛栓具有解热、镇痛及非特异性抗炎作用。其最常见的不良反应是胃刺激和头痛。过敏反应较为罕见。吲哚美辛栓可避免胃肠道刺激,使用方便、副作用少。但在我院对症治疗的同时,就2000年7～8月份在妇产科出现吲哚美辛栓致全身性过敏反应的人数达5人以上,其中最为严重的1例现报道如下。     

Determination of indometacin in Compound indometacin suppositories by HPLC

目的 采用HPLC法测定复方吲哚美辛栓中吲哚美辛的含量.方法 采用C18色谱柱,流动相为0.05 mol·L-1乙酸-乙腈(50∶50),测定波长260 nm.结果 吲哚美辛25.59～307.13 mg·L-1与峰面积的线性关系良好(r=0.9999),回收率为98.9％(RSD=2.0％,n=6).结论 所用方法准确、可靠,可用于复方吲哚美栓的质量控制.     

索利那新联合吲哚美辛栓预防前列腺电切术后膀胱痉挛的临床疗效分析

目的评价索利那新联合吲哚美辛栓预防前列腺电切术（TURP）后膀胱痉挛的效果。方法将70例TURP后患者,随机分为对照组35例：给予吲哚美辛栓纳肛（1次100mg,2次／d）。试验组35例：在吲哚美辛栓纳肛的基础上,口服索利那新治疗（5mg,1次／d）。结果试验组在术后72h内出现膀胱痉挛次数、持续时间、疼痛程度及膀胱持续冲洗天数均少于对照组（P〈0．01）。口于、视物模糊等药物不良反应少,且与对照组相比差异无统计学意义。结论索利那新联合吲哚美辛栓预防TURP后膀胱痉挛安全有效,值得推广。     

复方吲哚美辛栓直肠给药对产科手术切口的止痛作用

目的：观察复方吲哚美辛栓治疗分娩术后切口痛的疗效。方法：对４５例会阴切开术和４０例剖宫产的分娩产妇，前者在产后次日直肠给复方吲哚美辛栓１枚（每枚含吲哚美辛７０ｍｇ和沙丁胺醇１．２ｍｇ），ｑｄ×３ｄ；后者在术日麻醉效果消失后给药，用法同前，共４次。对照组６７例，其中３５例是会阴切开术，在分娩次日给安乃近１片（０．５ｇ／片）ｐｏ，ｑｄ×３ｄ，３２例剖宫产，在术日麻醉效果消失后给丁丙诺啡１支（１００ｍｇ／支）ｉｍ，ｑｄ×３ｄ。结果：止痛作用达优、良的有效率，复方吲哚美辛组各为１００％和９５％，对照组各为５４％和４１％。２相关组疗效相比Ｐ皆＜０．０１。结论：复方吲哚美辛栓对产科术后镇痛的效果良好。     

Rectal absorption of insulin suppositories in rabbits

When insulin solutions (100 U kg^?1) at various pH values were placed in the rectum of rabbits, a large decrease in blood glucose concentration was observed except at the pH close to the iso-electric point of insulin. The effect of surface-active agents on the rectal absorption of insulin was examined by measuring the blood glucose concentration after the administration of 2 or 5 U kg^?1. Non-ionic ether type, anionic, cationic and amphoteric surfactants as well as bile acids increased the absorption. The optimal effect with suppositories was reached with the addition of 1% polyoxyethylene (9) lauryl alcohol ether. Insulin suppositories containing agents enhancing rectal absorption were compared with the insulin for intravenous, intramuscular and subcutaneous injection. The changes of blood glucose and plasma immuno-reactive insulin concentration after rectal administration of insulin were similar to those after intravenous injection.     

Rectal absorption of omeprazole from suppositories in rabbits

Rectal absorption of omeprazole, a proton pump inhibitor, from suppositories was studied in rabbits. The suppositories were prepared by the conventional melting method with two types of bases, water-soluble polyethylene glycol (PEG) 4000 and oil-soluble Witepsol H15 bases, and administered intrarectally (ir) to rabbits at a dose of 10 mg omeprazole/kg. The plasma omeprazole concentration-time profiles of the two suppositories were compared with those following intravenous (iv) administration of the same dose. There were no significant differences between the two suppositories in bioavailabilities and peak plasma concentrations (C_max). Bioavailabilities and C_max of PEG- and Witepsol suppositories were 30.3 and 33.9%, and 7.0 and 5.6 μg/ml, respectively. However, PEG suppository showed significantly (P<0.05) shorter time to reach peak plasma concentration (T_max), mean absorption time (MAT) and mean residence time in the plasma (MRT) than Witepsol suppository. The T_max MRT and MAT were 25.0, 83.0 and 38.5 min for PEG suppository, but were 90.0, 122.5 and 78.0 min for Witepsol suppository, respectively. These differences between the two suppositories could be explained by the difference in the in vitro dissolution rates between the suppositories. The dissolution of omeprazole from PEG suppository was reportedly much faster than that from Witepsol suppository. It suggests that plasma profiles of omeprazole, especially C_max, MAT and MRT, could be controlled by modifying thein vitro dissolution rate of the drug from the suppositories. Above results suggest that rectal suppository is worth developing as an alternative dosage form of omeprazole to the conventional oral preparations which need sophisticated treatments, such as enteric coating, to prevent acid degradation of the drug in the stomach fluid.     

Rectal absorption of metronidazol from polyethylene glycol suppositories

The rectal absorption of metronidazol from an aqueous suspension, a fatty suppository and three different polyethylene glycol suppositories was studied in healthy volunteers and compared with absorption from an oral solution. Rectal absorption was found to be rather slow for all suppositories. Of all rectal dosage forms, the polyethylene glycol suppositories gave the highest peak plasma levels and the highest relative bioavailability. Compared with oral administration, a relative bioavailability of 80% could be obtained.     

Rectal absorption of morphine from controlled release suppositories

The absorption profiles and bioavailability of morphine in human volunteers (n = 13) were described after oral administration of MS Contin tablets and rectal administration of a newly developed controlled release suppository. By manipulating the viscosity of fatty suppository base an entirely identical cumulative morphine input could be obtained compared with oral dosing.