不同静脉给药方法对尼莫地平注射液稳定性影响

目的考察尼莫地平注射液在不同静脉给药方法下的稳定性。方法采用高效液相色谱法测定尼莫地平含量。结果尼莫地平注射液在输液泵给药途径下，8h后浓度下降约1％；在常规输液途径下，尼莫地平注射液于玻璃瓶装0．9％氯化钠注射液中比较稳定，8h后浓度下降约10％，但经过PVC输液器之后，浓度迅速下降，8h后仅为初始浓度的45％左右。结论输液泵静脉给药方式是尼莫地平的临床最佳给药途径。     

葛根素在大鼠体内的排泄过程与给药途径的相关性

目的 比较葛根素不同途径给药后的排泄过程.方法 太鼠经静脉或灌胃给予葛根素后,按一定时间段收集尿和粪便,以高效液相色谱荧光光谱法检测尿和粪样中的葛根素.结果 给大鼠灌胃葛根素混悬液后,葛根素由粪便中排泄的累积排泄率为41.56%,其中4～8h由粪便排泄量占由粪便排泄葛根素总量的75.26%,8～12h的排泄量占23.99%;12h内由尿中排泄的葛根素占给药量的0.64%,0～4h、4～8h葛根素由尿的排泄量分别占由尿排泄总量的27.91%和66.28%;24h内经粪便中排泄的葛根素约占排泄总量的98.40%.大鼠经尾静脉注射葛根素注射液24h内,葛根素由尿中排泄的累积排泄率为36.15%,而其中的97.43%是在前4h内排泄的;由粪便中排泄的葛根素占给药量的9.18%.而其中的99.19%是在给药后的8～12h之间排出的;24h内经尿中排泄的葛根素占排泄总量的79.64%.结论 葛根素的排泄与给药途径有关.大鼠灌胃给药后.葛根素主要经肠道排泄,而经静脉给药后,葛根素主要经肾脏排泄.     

Quinacrine不同给药途径对家兔血药浓度的影响

目的　研究 quinacrine经不同途径给药的血药浓度 ,了解 quinacrine经阴道向子宫内给药绝育 (quinacrine女性非外科绝育法 )可能产生的毒副反应。方法　以兔为模拟对象 ,用荧光分析法分别测定宫腔内缓释给药、静脉、口服和输卵管内注射等 4种不同途径给quinacrine的血药浓度变化。结果　血药浓度峰值以静脉给药法最高 ,宫腔内缓释给药法最低。宫腔内缓释给药法的血药浓度水平接近其他给药方法血药浓度水平的残余浓度。血药浓度下降的起点静脉法在给药后立即产生 ,口服法在给药后 8h出现 ,输卵管内注射法见于给药后 4h ,而宫内缓释法则可维持到 7d。结论　从是否产生全身性的毒副反应的角度看 ,quinacrine宫腔内缓释给药法比口服法低 ,用于女性非外科手术绝育是安全的     

尼莫地平2种给药途径治疗蛛网膜下腔出血后脑血管痉挛的疗效观察

目的:观察尼莫地平2种给药途径治疗蛛网膜下腔出血后脑血管痉挛的疗效。方法:68例原发性蛛网膜下腔出血患者,随机分为静脉尼莫地平组和口服尼莫地平组,通过经颅多普勒检测2种给药途径治疗脑血管痉挛后脑血流速度的变化,观察血管痉挛发生率、再出血率及死亡率,评价2种给药途径的疗效。结果:2组患者治疗后21d大脑中动脉血流速度明显改善,同治疗前比较,差异有显著性(P<0.05),治疗后21d神经功能缺损评分有显著性差异(P<0.05),且静脉尼莫地平组神经功能改善最佳,但2组无显著性差异(P>0.05);2组患者脑血管痉挛发生率、死亡率及再出血发生率明显降低,组间比较无显著性差异(P>0.05)。2组不良反应均较轻微。结论:尼莫地平治疗蛛网膜下腔出血疗效确切,口服及静脉给药疗效相当。     

尼莫地平不同给药途径治疗重型颅脑外伤合并创伤性蛛网膜下腔出血

目的:评价尼莫地平不同给药途径时重型颅脑外伤合并创伤性蛛网膜下腔出血患者脑血流的影响以及治疗效果.方法:68例重型颅脑外伤合并创伤性蛛网膜下腔出血患者随机分为(A)对照组,(B)尼莫地平静脉给药组,(C)尼莫地平术野灌洗组,术中采用TCD探测病变侧颈内动脉血流速度变化,分析尼莫地平对患者脑血流的影响;术后CT评价脑梗死情况,半年后进行COS评分.结果:(1)C组脑血流速度在尼莫地平灌洗后明显下降(P<0.05),A、B组则无明显变化;(2)术后A、B、C 3组患者脑梗死发生率分别20%,13.6%,7.69%,3组比较差异无显著性(P>0.05);(3)3组患者GOS评分比较:B、C 2组比A组预后更佳(P<0.05).结论:尼莫地平术中灌洗安全、有效,可以显著缓解颅内血管痉挛,结合术后静脉榆注,能够降低术后脑梗死发生率.     

米力农在微量泵输注过程中的稳定性研究

目的 考察微量泵持续静脉给药下，米力农在给药后48h内的稳定性。方法 采用ACQUITY UPLC BEH C₁₈(100mm×2.1mm,1.7μm)色谱柱，水-甲醇-硼酸钠缓冲液(725∶250∶25)为流动相，流速0.18mL·min^-1，检测波长269 nm，建立输液中米力农含量测定的HPLC法。将米力农注射液按临床常规剂量加入5%葡萄糖注射液中，在遮光与不遮光的条件下，采用HPLC法测定米力农在输液泵中不同时间点的浓度变化及有关物质，并观察溶液外观性状，测定pH值和渗透压。结果 建立的用于测定输液中米力农浓度的HPLC法具有良好的专属性、线性关系(r=0.999 8)、精密度(RSD=0.23%)和稳定性(RSD=1.04%)。米力农注射液经配制后，在48 h内无论遮光或不遮光，外观性状均澄明，无沉淀及浑浊出现；输液中米力农含量百分比、有关物质、pH值及渗透压均无明显变化，遮光条件下的RSD分别为0.95%、2.17%、0.25%和1.10%，不遮光条件下的RSD分别为0.94%、1.43%、0.32%和0.68%。结论 米力农用5...     

蒙药那如-3不同给药途径对家兔血药浓度的影响

目的:研究那如-3味丸与那如-3巴布剂不同给药途径下家兔血药浓度的变化。方法:采用高效液相色谱法。结果:那如-3味丸家兔口服给药后1h即可测到新乌头碱,血药质量浓度为0.109 6mg.L-1;6h达到峰值为1.061mg.L-1,随后迅速下降,至24h已降至0.175 43mg.L-1。那如-3巴布剂经皮给药后1h,还测不到血中的新乌头碱,3h时血药质量浓度为0.133 2mg.L-1,6h为0.209 8mg.L-1,至18h达到峰值为1.224mg.L-1,随后血药浓度缓慢下降,至48h降至0.172 1mg.L-1。结论:在不同给药途径下,家兔血药浓度差异有显著性。     

重组人血管内皮抑制素在静脉输液中的稳定性研究

目的 考察重组人血管内皮抑制素注射液（恩度）在静脉输液中的稳定性,为临床合理用药提供依据。方法 模拟临床给药剂量和给药时间,采用高效液相色谱法测定重组人血管内皮抑制素注射液在聚氯乙烯（PVC）输液袋、非PVC输液袋及全自动注药泵中不同温度、不同时间点的药物浓度。结果 在25 ℃或37 ℃下,重组人血管内皮抑制素注射液在PVC和非PVC氯化钠输液中至少保持稳定4 h,在全自动注药泵中48 h内保持稳定。结论 在临床实践中,重组人血管内皮抑制素注射液以PVC和非PVC材质的0.9%氯化钠注射液500 mL静脉点滴2 h或全自动注药泵（250 mL）恒速给药24 h,从药品稳定性角度讲是可行的。     

注射用乌司他丁与2种常用溶剂在输液泵中的配伍稳定性考察

目的:考察注射用乌司他丁与2种常用溶剂在输液泵中的配伍稳定性。方法:将注射用乌司他丁500 000单位分别与0.9%氯化钠注射液和5%葡萄糖注射液各50 m L配伍后,分别在25℃和37℃下于0、1、2、4、8、12、24 h时观察配伍液的外观变化,测定其pH值和不溶性微粒数,采用高效液相凝胶过滤色谱法测定配伍液中乌司他丁的相对百分含量。结果:在上述条件下,配伍液在24 h内外观和p H值均无明显变化;≥10μm的微粒数<25粒/m L,≥25μm的微粒数<3粒/m L,均符合药典标准;乌司他丁在24 h内各时间点的相对百分含量为99.45%~102.55%。结论:注射用乌司他丁与0.9%氯化钠注射液、5%葡萄糖注射液配伍后,在25℃和37℃条件下,24 h内保持稳定,可在输液泵中持续给药。     

头孢曲松钠与含钙溶液配伍稳定性考察

目的:研究头孢曲松钠与复方氯化钠注射液、乳酸钠林格注射液配伍的稳定性;并模拟体内头孢曲松钠血药峰浓度和静脉推注葡萄糖酸钙注射液离子瞬间高浓度时配伍液的稳定性。方法:采用高效液相色谱法测定配伍液中头孢曲松钠的含量,同时观察室温下配伍液外观、pH值、不溶性微粒变化。结果:头孢曲松钠与复方氯化钠注射液配伍后,0～2h澄清,2h后配伍液有肉眼可见的白色混浊,pH值升高,头孢曲松钠含量下降,不溶性微粒增加;与乳酸钠林格注射液配伍后,头孢曲松钠含量下降;模拟体内浓度进行配伍,外观无变化,头孢曲松钠含量稍有下降。结论:头孢曲松钠与复方氯化钠注射液、乳酸钠林格注射液不能配伍应用;静脉滴注头孢曲松钠达血药峰浓度后,成人是否可以静脉推注葡萄糖酸钙还有待进一步探讨。     

配液泵预调配模式研究和方法论证

目的：研究预调配模式在静脉用药调配中心的应用及方法论证。方法：选择注射用头孢地嗪钠及注射用拉氧头孢钠为研究对象，利用配液泵调配储备液，建立预调配模式，从效率和工作强度方面与手工调配比较。利用高效液相色谱法测定储备液在4℃保存24 h后的含量变化来确定最佳溶解体积，并考察这两种药物的残留量。检测药物储备液在4℃保存24 h后不溶性微粒。结果：注射用头孢地嗪钠及注射用拉氧头孢钠通过泵调配、手工调配得到的储备液残留量没有明显差距。确定预调配最佳溶解体积为4 mL。两种药物储备液中不溶性微粒均符合国家标准。与手工调配相比，预调配模式效率提高25%~45%。结论：利用配液泵建立的预调配模式在静脉用药调配中心有良好的应用前景。     

尼莫地平双层渗透泵片的制备及其体外释放度考察

目的:制备尼莫地平双层渗透泵控释片,并考察其体外释放度。方法:以体外累积释放度作为评价指标,以含药层助悬剂聚氧化乙烯(PEO)200000的用量、促渗剂氯化钠的用量、致孔剂聚乙二醇(PEG)2000的含量及包衣增重为考察因素,采用正交设计优化尼莫地平双层渗透泵控释片的处方;参照《中国药典》释放度测定法第二法测定其体外释放度。结果:最优处方为含药层PEO20000080mg,氯化钠10mg,助推层PEO500000040mg,PEG2000用量8%,包衣增重8%。所制片剂释药速率恒定,12h的体外累积释放度达90%以上。结论:尼莫地平双层渗透泵片工艺稳定,体外释放行为在12h内具有明显的零级释放特征(r=0.9903),达到了控释要求。     

尼莫地平对小鼠齿状回诱导型一氧化氮合酶的表达及其活性的影响

目的探讨阻断L型电压门控式Ca2+通道(LVGCC)对成年动物齿状回诱导型一氧化氮合酶(Induciblenitricoxidesynthase,iNOS)的表达及其活性的影响。方法通过阻塞大脑中动脉(MCAO)90min制备局灶性脑缺血动物模型。缺血前15min静脉单次注射尼莫地平(2.0mg·kg-1),24h处死动物,采用RTPCR和Westernblot的方法研究尼莫地平对齿状回iNOS的mRNA和蛋白水平的影响,并测定iNOS酶活性和NO含量的变化。用LPS和TNFα诱导培养的星型胶质细胞表达iNOS,同时给予尼莫地平,培养24h后,检测各组细胞的iNOSmRNA水平和iNOS酶活性。结果与假手术组相比,MCAO后小鼠缺血侧齿状回iNOSmRNA和蛋白水平明显升高,iNOS活性增强,NOx含量增加。给予尼莫地平的动物,缺血侧齿状回无论是iNOSmRNA水平、iNOS蛋白含量,还是iNOS活性及NOx含量,与假手术组相比均显著下降。尼莫地平还可以降低培养的星型胶质细胞的mRAN水平。结论尼莫地平阻断LVGCC,可以明显下调缺血动物的齿状回和培养细胞的iNOS表达,降低iNOS的酶活性。     

Pharmacokinetic study of cefsulodin in children

Cefsulodin (CFS), a cephem antibiotic, was administered to 26 children aged from 11 months to 11 years by intravenous injection or intravenous 1-hour drip infusion in doses of 15 and 50 mg/kg body weight to investigate serum and urinary concentrations. The following results were obtained. Serum concentration The serum concentrations of CFS at 5 minutes after intravenous injection of 15 and 50 mg/kg were 57.1 and 224.2 micrograms/ml, respectively. The biological half-lives (T 1/2 beta) were 1.28 and 1.12 hours. The serum concentration of CFS after intravenous 1-hour drip infusion reached a peak at the end of infusion, i.e. 29.9 micrograms/ml for 15 mg/kg and 121.9 micrograms/ml for 50 mg/kg, and T 1/2 beta were 1.22 hours for 15 mg/kg and 1.27 hours for 50 mg/kg. The AUC was proportional to the doses for both intravenous injection and intravenous drip infusion. The serum clearance was about twice the value in adults and the distribution volume was about 1.5 times as large. Urinary excretion The urinary excretion up to 6 hours after administration was: 69.0% for 15 mg/kg and 61.9% for 50 mg/kg in cases of intravenous injection, and 62.4% for 15 mg/kg and 71.1% for 50 mg/kg in cases of intravenous 1-hour drip infusion. The percent urinary excretion was similar to that in adults.     

The metabolism and kinetics of 125I-labeled human intravenous IgG preparation (C-425) in rats and rabbits. I. Blood clearance, excretion into urine and feces, and brain uptake

The metabolism of intravenous human IgG preparation (C-425) was studied by the use of 125I-C-425 in rats and rabbits after intravenous injection of the compound particularly with regard to changes in the levels of radioactive compound or metabolites in the blood as a function of time as well as levels excreted in urine and feces. Brain uptake index of 125I-C-425 was estimated by a slightly modified Oldendorf's method. 125I-Polyglobin was used as the control compound. The half-life of blood clearance of 125I-C-425 radioactivity after the 2nd day was about 8 days in rats and about 5 days in rabbits, respectively. Within a relatively short period of 1 hour, a rapid decrease of blood concentration of radioactivity was recorded. This was due to the transfer of labelled compound from blood into the extravascular compartment. A high concentration of radioactivity in the blood was maintained for one week after intravenous injection of the labelled compound in both rats and in rabbits. Most of the radioactive compound or metabolites were excreted in the urine and relatively little in feces. Excretion in urine of rats reached about 22% for 125I-C-425 and about 17% for 125I-Polyglobin. The excretion rate slowed down over 24 hours. The total recovery rates in rats were about 40% for 125I-C-425 and 125I-Polyglobin and about 55% in rabbits for both drugs. The permeability through the blood-brain barrier was found to be negligible for both drugs.     

广地龙中促进子宫收缩的成分

本文研究了自广地龙中提出来的一种引湿性、淡黄色針状結晶(含量約0.2%)对平滑肌器官(特别是对子宮)的作用。介紹了該結晶的提取方法。該結晶0.1毫克加入25毫升Locke液中,能使已孕和未孕大鼠或豚鼠离体子宮角紧张度明显升高,0.3毫克可使之呈痙攣收縮状态。按1毫克/公斤給已孕和未孕麻醉家兔靜脉注射后15—30分钟,在位子宮紧张度升高,作用維持1.5—3小时。按8—10毫克/公斤注射,子宮紧张度立卽升高和血压急剧下降到零而死亡。9只慢性子宫瘻家兔靜脉注射(3—6毫克/公斤)或灌胃給药(10—20毫克/公斤)后15—45分钟,子宮收縮明显增强,作用維持1.5—3小时(注射給药)和7小时以上(灌胃給药)。多数实驗家兔在子宮兴奋同时有排便現象。該結晶对家兔在位腸管和大鼠后肢血管均有强烈兴奋作用,但对豚鼠支气管肌作用极弱。当給小鼠靜脉注射时,LD₅₀为38.7毫克/公斤。     

A novel pharmacokinetic method for analysis of placental transfer of latamoxef in humans

A novel pharmacokinetic method was developed for analysing the behaviour of a drug in tissues. The absolute transfer ratio of a drug to a tissue was defined using the pharmacokinetic parameters obtained by this method. Composite data of latamoxef (moxalactam) concentration in maternal blood, umbilical cord blood and amniotic fluid following a 2g intravenous injection to pregnant women at delivery were analysed by this method to study the drug behaviour in pregnant women, fetuses and amniotic fluid. Latamoxef kinetics in pregnant women at full term were generally similar to that in previously reported healthy subjects. The concentration of latamoxef in umbilical cord blood peaked about 2 hours after dosing then decreased in parallel with the maternal blood concentration. The amniotic fluid concentration peaked about 7 hours after administration, then decreased slowly. The absolute transfer ratios to fetus and amniotic fluid were calculated to be about 2.5 and 0.37% respectively.     

多西他赛注射液与不同溶媒配伍的稳定性考察

目的:考察多西他赛注射液分别与0.9%氯化钠注射液、5%葡萄糖注射液及长链脂肪乳注射液配伍后的稳定性。方法:考察室温下0,1,2,4,6,8,10,12,16,20,24 h时配伍液的外观、不溶微粒分布及粒径大小、pH值,采用高效液相色谱法测定多西他赛的含量。结果:24 h内,药物与0.9%氯化钠注射液、5%葡萄糖注射液的配伍液外观与pH值均无明显改变,但多西他赛的含量在配置后8 h均有明显下降(RSD>2%);24 h内,药物与长链脂肪乳注射液的配伍液外观与pH值均无明显改变,但多西他赛的含量在配置后20 h有明显下降(RSD>2%)。结论:室温条件下,多西他赛注射液与长链脂肪乳注射液配伍的稳定性明显优于0.9%氯化钠注射液及5%葡萄糖注射液。     

The renal clearance of disopyramide after bolus intravenous injection

Following bolus intravenous injection of disopyramide in eight normal volunteers the renal clearance of the drug appeared to fall with time. In the first two hours after injection renal clearance had a mean value of 89.0 ml min-1 and fell to 29.4 ml min-1 between 48 and 72 h. In a separate study disopyramide was given by continuous intravenous (i.v.) infusion for 8 h following a loading dose of the drug. Renal clearance of disopyramide was thus estimated hourly over three narrow serum concentration ranges in a single volunteer. The estimate of renal clearance of the drug over the first hour following the start of these infusions was considerably in excess of values obtained later in the experiments. The change in disopyramide renal clearance following bolus injection is partially time-dependent. There are, however, fallacies in calculating short-term clearance values after bolus drug injection from the venous concentration-time curve and these may partially explain the change in renal clearance of disopyramide with time.