15-羟基硬脂酸聚乙二醇酯在参麦注射液中的应用研究

本文研究了助溶剂15-羟基硬脂酸聚乙二醇酯(Kolliphor HS 15)在参麦注射液中达到最佳助溶效果的用量,并与采用聚山梨酯80作为助溶剂的参麦注射液对比研究了灭菌前后产品质量与稳定性。结果表明,当Kolliphor HS 15在参麦注射液中用量为0.2%时,可以达到良好的助溶效果,且对产品的质量和稳定性没有影响。为使用安全性更好、助溶原理相同、且能达到等同助溶效果的助溶剂,替换中药注射液中现有安全性差的聚山梨酯80提供一定参考依据。     

心达康滴丸的成型工艺设计研究

目的确立心达康滴丸的最佳成型工艺。方法采用正交试验法,从基质,冷却剂的种类,提取物与基质的用量配比等方面进行考核。结果聚乙二醇6000,冷却温度15℃时,心达康滴丸质量最好。结论证明此工艺是可行的。     

Pharmacokinetic and pharmacodynamic drug interactions between digoxin and macrogol 4000, a laxative polymer, in healthy volunteers

AIMS: The aim of this study was to examine the bioequivalence between a single oral dose of digoxin administered alone and with a coadministration of macrogol 4000 (a laxative polymer) in 18 healthy volunteers. METHODS: This was an open, randomised, two-way cross-over study, with a single dose oral administration of 0.5 mg digoxin administered alone or in combination with macrogol 4000, 20 g day-1 during 8 days. Pharmacokinetics of digoxin, heart rate and PR ECG interval at rest were assessed. RESULTS: Macrogol 4000 coadministration was associated with a 30% decrease of digoxin AUC and a 40% decrease in its Cmax (P<0.05). Digoxin tmax and t1/2,z were not significantly altered. Heart rate and PR interval did not differ during the two therapeutic sequences, digoxin alone and digoxin in combination. CONCLUSIONS: Macrogol 4000 coadministration interacts with single-dose digoxin pharmacokinetics. This is most likely due to a reduction of the intestinal absorption of digoxin. However, there was no consequence of this interaction on heart rate and AV conduction.     

复方聚乙二醇电解质散与番泻叶在结肠镜检查前肠道准备中的应用

为观察复方聚乙二醇电解质散与番泻叶联合应用在结肠镜检查前肠道准备的临床效果,将复方聚乙二醇电解质散与番泻叶联合应用为观察组和单用复方聚乙二醇电解质散为对照组,观察术前的排便次数和粪便性状、术中的肠道清洁满意度。结果显示．观察组排便结束时间明显短于对照组（P〈0．05）。肠道清洁满意度观察组为80．6％（162／201）,对照组为69．6％（133／191）（P〈0．05）。结果表明,复方聚乙二醇电解质散与番泻叶联合应用在结肠镜检查前肠道准备的效果比单用复方聚乙二醇电解质散效果好。     

Anaphylactic shock after oral intake and contact urticaria due to polyethylene glycols

We reported an anaphylaxis after oral intake and contact urticaria due to polyethylene glycols.     

Enhanced Bioavailability of 6-Mercaptopurine After Rectal Administration in Rats

Pharmaceutical Research -     

聚乙二醇4000联合比沙可啶对帕金森病患者便秘症状及相关生活质量的影响

目的探讨聚乙二醇4000联合比沙可啶对帕金森病患者便秘症状及相关生活质量的影响。方法将98例明确诊断为帕金森病便秘的患者随机分为试验组49例和对照组49例,其中对照组予以聚乙二醇4000口服,治疗组在对照组方案基础上联合比沙可啶肠溶片口服,疗程均为2周,观察比较两组患者的大便频率、形状等便秘相关症状及其相关生活质量的变化。结果完成本研究试验者共87例,其中对照组44例,治疗后排便频率和粪便性状均有明显改善(P<0.05),治疗组43例患者在排便频率、粪便性状及费力程度等相关症状方面均较治疗前显著改善(P<0.05),组间比较:治疗组优于对照组(P<0.05);两组患者治疗后生活质量评分均有降低(P<0.05),且组间比较治疗组明显优于对照组,差异有统计学意义(P<0.05)。结论聚乙二醇4000联合比沙可啶对有效改善帕金森病患者便秘相关症状、提高其生活质量具有重要作用。     

Solid state studies of drug–cyclodextrin inclusion complexes in PEG 6000 prepared by a new method

The melting method was investigated as a possible method for producing drug–cyclodextrin (CD) inclusion compounds in a carrier. Various solid dispersions of -, β- and γ-CD in polyethylene glycol (PEG) 6000 with and without the addition of 5% w/w indomethacin or griseofulvin were prepared using the original components. Characterisations of the samples included X-ray powder diffraction, modulated-temperature differential scanning calorimetry and dissolution tests by the paddle method according to USP XXI standard. Evidence of a complex between indomethacin and β-CD in PEG 6000 was found. An indomethacin–γ-CD complex formed a well defined phase in the PEG carrier, with tetragonal structure and unit cell parameters a=23.885(35) Å and c=23.181(64) Å. No complexation of indomethacin with -CD, or with griseofulvin and β-CD could be detected. It is suggested that competition between PEG and the drug for the binding to different CDs along with varying patterns of water loss from the CDs influence the inclusion reaction. The formation of complexes was accompanied by a decrease in the relative crystallinity of the dispersions. Dissolution tests showed that the CDs have a delaying effect on the release of indomethacin from PEG 6000 in the order -CD<γ-CD≤β-CD.