5—单硝酸异山梨酯治疗劳力型心绞痛

目的：比较鲁南药厂生产的５－单硝酸异山梨酯（鲁南ＩＳ－５－ＭＮ）与圣多纳药厂生产的５－单硝酸异山梨酯（圣多纳ＩＳ－５０ＭＮ）治疗劳力型心绞痛的疗效。方法：劳力型心绞痛５０例（男性３０例，女性２０例；年龄５８±ｓ６ａ）采用鲁南ＩＳ－５－ＭＮ２０￣４０ｍｇ，ｐｏ，ｔｉｄ治疗。另有劳力型心绞痛２０例（男性１２例，女性８例；年龄５９±８ａ）采用圣多纳ＩＳ－５－ＭＮ２０￣４０ｍｇ，ｐｏ，ｔｉｄ治疗。２组疗程     

5─单硝酸异山梨酯治疗劳力型心绞痛

目的：比较鲁南药厂生产的５－单硝酸异山梨酯（鲁南ＩＳ－５－ＭＮ）与圣多纳药厂生产的５－单硝酸异山梨酯（圣多纳ＩＳ－５－ＭＮ）治疗劳力型心绞痛的疗效。方法：劳力型心绞痛５０例（男性３０例，女性２０例；年龄５８±ｓ６ａ）采用鲁南ＩＳ－５－ＭＮ２０～４０ｍｇ，ｐｏ，ｔｉｄ治疗。另有劳力型心绞痛２０例（男性１２例，女性８例；年龄５９±８ａ）采用圣多纳ＩＳ－５－ＭＮ２０～４０ｍｇ，ｐｏ，ｔｉｄ治疗。２组疗程均为１４ｄ。结果：临床症状与心电图改善的总有效率，鲁南ＩＳ－５－ＭＮ组依次为９８％与８０％，圣多纳ＩＳ－５－ＭＮ组依次为１００％与８５％，组间比较Ｐ值均＞０．０５。２药不良反应均轻微。结论：２个药厂生产的ＩＳ－５－ＭＮ疗效相似。     

国产硝酸异山梨酯注射液治疗冠心病心绞痛

应用国产硝酸异山梨酯（２０ｍｇ加入５％葡萄糖液５００ｍｌ中，２．４ｍｇ／ｈ静脉滴注，ｑｄ，连用１４ｄ）治疗冠心病心绞痛病人４１例，临床总有效率为９２．７％，心电图总有效率为６８．３％，与进口硝酸异山梨酯总有效率分别为９０％及６５％基本相近，该药尚有扩张血管，降低血压，减少心肌氧耗，改善左室功能等作用。     

硝酸异山梨酯静脉内输注治疗冠心病心绞痛102例

目的：比较国产与进口糖硝酸异山梨酯注射液治疗冠心病心绞痛的疗效。方法：冠心病心绞痛病人１５２例，其中１０２例（男性６７例，女性３５例，年龄６３±ｓ９ａ）以国产硝酸异山梨酯注射液２０ｍｇ加于５％葡萄糖液５００ｍＬ中静脉滴注，ｑｄ，连用１４ｄ。另外５０例（男性３５例，女性１５例，年龄６４±８ａ）以德国进口硝权异山梨酯注射液２０ｍｇ，加入５％葡萄糖液５００ｍＬ中静脉滴注，ｑｄ连有１４ｄ。结果：国糖液５０     

静脉滴注硝酸异山梨酯治疗不稳定性心绞痛30例

观察ｉｖｇｔｔ硝酸异山梨酯对不稳定性心绞痛患者的疗效和安全性。方法：３０例不稳定性心绞痛患者ｉｖ ｇｔｔＩｓｏ３０－４０ｍｇ（８０－１５０μｇ／ｍｉｎ）,ｑｄ,疗程１０ｄ。对照组ｉｖｇｔｔ硝酸甘油治疗。结果３０例中１５例症状完全缓解,１２例发作次数减少,症状减轻,３例无效。结论：ｉｖ ｇｔｔ Ｉｓｏ对ＵＡＰ有效,疗效优于硝酸甘油。     

5—单硝酸异山梨酯缓释片相对生物利用度及药物动力学

目的：比较５－单耠酸异山梨酯（５－ＩＳＭＮ）缓释片产普通片的相对生物利用度和药物动力学，进行相对生物利用度及药物动力学参数测定。方法：１０名男性健康受试者交叉ｐｏ给药５－ＩＳＭＮ缓释片４０ｍｇ和普通片２０ｍｇ，以硝酸异山梨互为内标，用毛细管气相色谱－电子捕获（ＧＣ－ＥＣＤ）检测法测定人血浆中５－ＩＳＭＮ的浓度。结果：：两种剂型的药－时曲线均符合一室模型，单剂量时缓释片和普通片的ＡＵＣ０－∞分别为（     

奥扎格雷钠治疗急性脑梗死的疗

目的：观察奥扎格雷钠对急性脑梗死的疗效。方法：选择诊断明确的急性脑死患者６４例,随机分为２组,治疗组３２例,奥扎格雷钠８０ｍｇ溶于２５０ｍｌ生理盐水中ｉｖ ｇｔｔ,ｂｉｄ,２ｗｋ为一疗程。对照组３２例,低分子右旋糖酐５００ｍｌ,加丹参注射液１６ｍｌ,ｉｖ ｇｔｔ,ｑｄ连用１４ｄ。按临床神经功能缺损程度评分标准于治疗前后１４ｄ进行疗效评判。结果：治疗组总有效率和显效率与对照组有显著性差别（Ｐ〈０．０     

硝酸异山梨酯静脉内输注治疗冠心病心绞痛102例

目的：比较国产与进口硝酸异山梨酯注射液治疗冠心病心绞痛的疗效。方法：冠心病心绞痛病人１５２例，其中１０２例（男性６７例，女性３５例，年龄６３±ｓ９ａ）以国产硝酸异山梨酯注射液２０ｍｇ加于５％葡萄糖液５００ｍＬ中静脉滴注，ｑｄ，连用１４ｄ。另外５０例（男性３５例，女性１５例；年龄６４±８ａ）以德国进口硝酸异山梨酯注射液２０ｍｇ加入５％葡萄糖液５００ｍＬ中静脉滴注，ｑｄ，连用１４ｄ。结果：国产组临床总有效率为９４．１％，心电图总有效率为４８．０％，进口组则依次为９６％与５２％；组间比较，Ｐ值均＞０．０５。该药尚有扩张血管、降低血压、减低心肌氧耗，改善左室功能等作用。结论：本药的疗效和作用与进口硝酸异山梨酯注射液相近。     

口服5—单硝酸异山梨醇酯胶囊和进口片剂在健康志愿者的药代动力 …

目的；研究国产５－单硝酸异山梨醇酯（ＩＳ－５－ＭＮ）胶囊及进口ＩＳ－５－ＭＮ片剂在健康志愿者的药动学特征及其生物等效性。方法：随机双盲实验先后一次口服ＩＳ－５－ＭＮ胶囊和进口ＩＳ－５－ＭＮ参比片剂（２０ｍｇ）后，以市郊和气相色谱法时检测其血药浓度，采用ＣＡＰＰ软件包计算药动学参数，并做生物等效性分析。     

高效液相色谱法测定单硝酸异山梨酯胶囊的含量及含量均匀度

高效液相色谱法测定单硝酸异山梨酯胶囊的含量及含量均匀度河北省药品检验所０５００１１韩学静郭毅郑德海刘庆京杜增辉单硝酸异山梨酯（５－ＩＳＭＮ）为新一代抗心绞痛的硝酸酯类药物，是硝酸异山梨酯在体内的主要活性代谢产物。具有半衰期长，生物利用度高等特点，１９...     

Fate of isosorbide dinitrate and mononitrates in patients with renal failure

Summary Isosorbide dinitrate 10 mg, isosorbide 5-mononitrate 5 mg and isosorbide 2-mononitrate 5 mg were administered orally to subjects with and without renal failure, and the plasma concentrations of isosorbide dinitrate and of both the mononitrates were measured. There was no striking difference in plasma concentration as a function of time between subjects with and without renal failure, except for a somewhat higher isosorbide 5-mononitrate concentration after administration of this metabolite to uraemic patients.     

Pharmacokinetics of isosorbide dinitrate and its mononitrate metabolites after intravenous infusion

Plasma concentrations of isosorbide dinitrate (ISDN) and its two active metabolites 2-isosorbide mononitrate (2-ISMN) and 5-isosorbide mononitrate (5-ISMN) have been measured during and for 6 hr after intravenous infusion at a rate of 2.5mg/hr during 1.75 hr in six cardiac patients, by a capillary gas chromatographic method. Data were analyzed by simultaneous modeling of the observed kinetics of the three compounds. Two or three phases were detected on the postinfusion ISDN concentration-time curves. ISDN concentrations declined with a mean terminal half-life of 2.81 hr±0.7 SD. The mean systemic clearance of ISDN (2.9 L/min ±0.7 SD) and its mean total volume of distribution (259 L +- 48 SD) were relatively high. Plasma 5-ISMN concentrations were 5- to 6-fold greater than those of 2-ISMN during the whole observation period. Maximum levels of 2-ISMN (6.7 ng/ml ± 0.9 SD) and of 5-ISMN (27 ng/ml ± 6 SD) occurred within a few minutes after the end of infusion. The mean half-lives of 2-ISMN (1.59 hr± 0.19 SD) and of 5-ISMN (3.78 hr± 0.79 SD) estimated by the model were smaller than those calculated by a model-independent method (2.95 hr± 0.41 SD and 5.98 hr± 2.22, respectively), but were in good agreement with those reported in the literature following separate administration of both metabolites to man. This study shows how such modeling can distinguish between metabolite formation and elimination processes and allow the determination of metabolite half-lives after administration of the precursor drug.     

Sex-related difference in the metabolism of isosorbide dinitrate following incubation in human blood

Isosorbide dinitrate (ISDN) (at a concentration of 100 ng/ml) was incubated aerobically at 37° in whole blood from five male and five female normal volunteers. Following incubation of the blood samples for 0, 30, 60, 120, 240 and 360 min, the samples were centrifuged and the plasma was assayed for ISDN. A linear relationship was observed between the logarithm of the concentration of ISDN remaining and incubation time, and there was a significant difference between the $\text{T}{}_{\mathrm{<mtext>1</mtext><mtext>2</mtext>}}$ of ISDN in blood from males (90.6 min) and females (161.4 min). Very little ISDN metabolism was observed when ISDN was incubated with plasma rather than whole blood. When erythrocytes, resuspended in saline, were incubated with ISDN, there was a time-dependent loss of ISDN from the saline incubation medium. Investigation of the soluble fraction obtained after hemolysis of these erythrocytes also showed a time-dependent loss of ISDN. The saline incubation medium contained sufficient concentrations of the two major ISDN metabolites (isosorbide 2- and 5-mononitrate) to account for the observed disappearance of ISDN. The results indicate that ISDN is metabolized in the cellular compartment of blood and that the metabolic rate in males is greater than that in females.     

Isosorbide dinitrate in plasma and dialysate during haemodialysis

Summary In 10 patients with end stage renal disease on regular haemodialysis the plasma concentrations and dialyzer clearance of isosorbide dinitrate (ISDN) were determined after an oral dose of a retarded release formulation of 60 mg ISDN. The maximal plasma concentration of ISDN 2–7 h after oral administration was higher (14 ng/ml) than has been reported in healthy volunteers. The haemodialyzer clearance of ISDN was 92.4 ml/min at a blood flow of 200 ml/min and dialysate flow of 500 ml/min. During a 5-h haemodialysis an average of 0.3 mg ISDN was removed from the patient's circulation, representing about 0.5% of the administered dose and about 3% of the available drug in the circulation. No influence of haemodialysis on the plasma level of ISDN was found.     

HPLC法测定复方单硝酸异山梨酯缓释片中单硝酸异山梨酯和阿司匹林的含量

目的　采用高效液相色谱法测定复方单硝酸异山梨酯缓释片中单硝酸异山梨酯和阿司匹林的含量。方法　色谱柱为LUNAODSC18(4 6mm× 2 5 0mm ,5 μm) ;流动相为 1%醋酸溶液 (含 0 1%三乙胺 ,pH 3 0 ) -甲醇 (5 5∶4 5 ) ;检测波长 :2 3 0nm ;流速 :1 0ml·min-1。结果　单硝酸异山梨酯进样量在 0 3 93 2～ 6 2 912 μg ;阿司匹林在 0 2 4 72～ 3 95 5 2 μg范围内与峰面积呈良好的线性关系 ,相关系数依次为 0 9999、0 9999,平均回收率依次为 99 4 %、10 0 0 % ,RSD依次为 1 1%、0 8%。结论　本法简便 ,灵敏 ,准确     

单硝酸异山梨醇酯对比格犬心肌缺血再灌注损伤的保护作用

目的观察单硝酸异山梨醇酯(ISMN)对比格犬心肌缺血再灌注损伤(MIRI)的保护作用,探讨其可能的作用机制。方法 30只比格犬随机分为6组:假手术组,缺血再灌注(I/R)组,维拉帕米(VP)0.15mg·kg-1组,ISMN3,6和12mg·kg-1组。采用结扎冠状动脉左前降支90min,再灌90min的方法建立比格犬I/R模型,各组动物分别于缺血前10min股静脉注射生理盐水及相应剂量药物。手术前后不同时间点记录心电图;TTC染色法测定心肌梗死面积;比色法检测血清肌酸激酶(CK)、乳酸脱氢酶(LDH)、超氧化物歧化酶(SOD)活性及丙二醛(MDA)含量;ELISA法测定不同时间点血清中C反应蛋白(CRP)表达。结果与假手术组相比,I/R组缺血90min心电图T波和S-T段明显抬高;再灌90min,出现大面积心肌梗死;血清中CK和LDH活性明显升高,SOD活性明显降低(P<0.01),MDA和CRP含量明显升高(P<0.01)。与I/R模型组比较,VP组和ISMN各剂量组在缺血90min时心电图的T波和S-T段抬高幅度有所降低;再灌注90min后,各给药组心肌梗死面积百分比明显减小(P<0.01);血清中CK和LDH活性明显降低(P<0.05,P<0.01),SOD活性明显升高(P<0.05,P<0.01),MDA和CRP含量明显降低(P<0.05,P<0.01)。ISMN3和6mg·kg-1组对MIRI的治疗效果明显不如VP(P<0.05,P<0.01),ISMN12mg·kg-1的治疗效果与VP基本相当。结论 ISMN对MIRI具有保护作用;其作用机制可能与抗脂质过氧化物产生、提高SOD活力及抗炎有关。     

曲美他嗪与硝酸异山梨酯治疗稳定性劳力型心绞痛的比较

目的 :比较曲美他嗪与硝酸异山梨酯治疗稳定性劳力型心绞痛的疗效。方法 :选择 62例稳定性劳力型心绞痛的病人分为 2组 ,曲美他嗪组 32例[男性 2 0例 ,女性 12例 ,年龄 (61±s 15 )a]用曲美他嗪 2 0mg ,po ,tid× 8wk。硝酸异山梨酯组 30例[男性 19例 ,女性 11例 ,年龄 (61± 14)a]用硝酸异山梨酯 10mg ,po ,tid× 8wk。结果 :曲美他嗪组心绞痛及心电图改善分别为 94 %和 66% ,硝酸异山梨酯组依次为 93%和 67%。组间比较差异无显著意义 (P >0 .0 5 )。结论 :曲美他嗪和硝酸异山梨酯治疗稳定性劳力型心绞痛的疗效相近 ,安全有效     

硝酸酯类药物不同途径给药后的药动学比较

目的 :评价 5 单硝酸异山梨酯 (5 ISMN)片剂和注射剂及硝酸异山梨酯 (ISDN)注射剂在中国健康受试者中的药动学特征。方法 :18名男性健康受试者采用自身对照交叉给药的方式 ,单剂量口服5 ISMN片剂 2 0mg或静脉滴注 (静滴 ) 5 ISMN注射剂 (5mg·h- 1,维持 4h)或ISDN注射剂 (5mg·h- 1,维持 4h) ,采用气相色谱法测定血药浓度。结果 :18名受试者口服 5 ISMN片剂和静滴 5 ISMN注射剂后的药动学参数为 :Tmax 分别为 (0 .7±s 0 .6 ) ,(4 .1± 0 .7)h ;Cmax分别为 (389± 86 ) ,(2 83± 5 9) μg·L- 1;AUC0 ∞ 分别为 (32 6 6± 6 2 4 ) ,(3179± 76 9) μg·h·L- 1。静滴ISDN注射剂后IS DN ,2 单硝酸异山梨酯 (2 ISMN )和 5 ISMN的Cmax分别为 (18± 7) ,(5 9± 4 ) ,(2 0 9± 5 0 ) μg·L- 1;AUC0 t分别为 (85± 2 8) ,(380± 5 9) ,(1384± 4 2 7)μg·h·L- 1;T1/2 分别为 (1.0 0± 0 .2 0 ) ,(2 .6±0 .8) ,(6 .1± 0 .9)h。结论 :5 ISMN片剂与注射剂相比 ,两者的AUC等效 ,但片剂的达峰时间明显快于注射剂。ISDN注射剂给药后能较快达到稳态浓度 ,而且迅速代谢成活性代谢产物。     

甲氧氯普胺与心痛定治疗肾绞痛的疗效比较

目的:观察甲氧氯普胺治疗肾绞痛的疗效。方法:对43例肾绞痛患者应用甲氧氯普胺0.4mg/kg,肌内注射。对照组41例用心痛定10mg,嚼碎含化。结果:甲氧氯普胺治疗肾绞痛的总有效率(86.0％)明显高于心痛定(75.6％)。结论:甲氧氯普胺治疗肾绞痛有效、安全。     

静滴硝酸异山梨酯与硝酸甘油治疗急性心肌梗死的比较

硝酸异山梨酯(Iso)组30例(男性24例,女性6例;年龄69±16a)采用Iso 20mg+5％葡萄糖液500mL持续静脉滴注72h,按35-40μg/min滴速治疗。硝酸甘油(Nit)组16例(男性12例,女性4例;年龄65±11a)采用Nit 20mg+5％葡萄糖液500mL,方法同上。结果:2组疗效相似,但Iso对血压影响小,对心率可略减慢,更适用于血压偏低和(或)伴有心功能不全者。