硝酸异山梨酯(消心痛)皮肤喷雾剂防治心绞痛的效果

硝酸异山梨醋(消心痛)皮肤喷雾剂治疗39例稳定性心绞痛的疗效达79.5%,作HoIler监测减少心肌缺血发作有效率为73.4%,运动耐量在喷药后有改善(占79%)。本药具有使用简便、作用时间持久,副作用小、无皮肤过敏等优点。     

Influence of glyceryl trinitrate on venous and arterial effects of chronic,asymmetric isosorbide dinitrate treatment in patients with ischemic heart disease

Asymmetric dosage regimes have been introduced to circumvent development of nitrate tolerance. This study assessed invasively the hemodynamics during supine rest and exercise before and after 4 weeks treatment with 30 mg isosorbide dinitrate (ISDN) or placebo asymmetrically b.i.d. in 14 randomized patients with stable ischemic heart disease in a double-blinded study. An intravenous infusion of glyceryl trinitrate (GTN) was used to assess possible nitrate tolerance. During the initial, medication-free exercise all patients had increased pulmonary arterial wedge pressure (PAWP) 31.4 ± 5.56 mmHg (mean ± SD), showing impaired left ventricular function, while mean arterial pressures (MAP) rose from 112 ± 16.3 mmHg at rest to 141 ± 15.9 mmHg during exercise. After 4 weeks ISDN treatment, mean exercise PAWP and MAP, 3 h after morning dose, were reduced to 22.4 ± 7.09 mmHg and 127 ± 18.2 mmHg, respectively. Before the ISDN treatment, GTN reduced exercise PAWP to 13.9 ± 5.27 mmHg and MAP to 119 ± 11.2 mmHg, whereas after 4 weeks ISDN treatment, the addition of GTN did not reduce exercise PAWP and MAP to the same low levels. Thus, the applied ISDN regimen improved the hemodynamics, but induced a definite, partial nitrate tolerance.     

Comparison of acute haemodynamic effects of nifedipine and isosorbide dinitrate in patients with heart failure following acute myocardial infarction

The acute haemodynamic effects of nifedipine (10 mg sublingually) and isosorbide dinitrate (5 mg sublingually) were compared in 13 patients with heart failure due to acute myocardial infarction. Nifedipine induced a significant reduction in systolic (from 122 ± 5 to 107 ± 3 mm Hg: mean ± SEM; P < 0.002) and diastolic blood pressure (from 85 ± 3 to 75 ± 2 mm Hg; P < 0.01). Heart rate did not change significantly, nor did mean right atrial pressure. The mean pulmonary arterial pressure was lowered from 31 ± 2 to 27 ± 2 mm Hg (P < 0.005). The left ventricular filling pressure decreased from 24 ± 1 to 19 ± 1 mm Hg (P < 0.0001). A significant increase in cardiac index (from 2.33 ± 0.13 to 2.69 ± 0.15 l/min per m²; P < 0.001) and in stroke volume index (from 24 ± 2 to 28 ± 2 ml/beats per m²; P < 0.005) was registered. Systemic vascular resistance fell from 1742 ± 145 to 1308 ± 85 dynes/sec per cm⁻⁵ (P < 0.00005). After isosorbide dinitrate was administered a significant reduction in mean right atrial pressure (from 9.5 ± 1.6 to 5.1 ± 1.2 mm Hg; P < 0.0001), in mean pulmonary arterial pressure (from 32 ± 1 to 23 ± 1 mm Hg; P < 0.00001) and in left ventricular filling pressure (from 23 ± 1 to 16 ± 1 mm Hg; P < 0.0001) was seen. No significant change in systolic and diastolic blood pressure, heart rate, cardiac index, stroke volume index and systemic vascular resistance was registered. No side-effects were seen after nifedipine and isosorbide dinitrate were administered.     

麝香保心丸治疗老年冠心病130例效果观察

目的探讨麝香保心丸治疗老年冠心病临床效果。方法选择2011年1月—2013年1月海洋石油总医院全科门诊中明确诊断的老年冠心病260例,随机分为治疗组和对照组各130例,对照组口服单硝酸异山梨酯缓释片60 mg,1次/d,同时口服阿司匹林肠溶片100 mg,1次/d,治疗组在对照组治疗的基础上,另外口服麝香保心丸2粒,3次/d,两组均观察半年。比较两组疗效、血脂水平及心电图。计量资料采用t检验,率的比较采用χ2检验,P0.05为差异有统计学意义。结果治疗组总有效率为96.9%高于对照组的47.7%,差异有统计学意义(P0.05)。治疗组总胆固醇、甘油三酯、低密度脂蛋白分别为(5.08±1.16)、(1.01±0.71)、(2.03±0.99)mmol/L平均低于对照组的(6.52±1.17)、(1.73±0.53)、(1.01±0.71)mmol/L,差异均有统计学意义(均P0.05)。治疗组心电图改善总有效率90.0%,对照组心电图改善总有效率42.3%,两组比较差异有统计学意义(P0.05)。结论麝香保心丸具有多方面的作用,能够显著改善患者的生活质量,有效防治意外事件的发生,并且安全、可靠,是老年冠心病的有效治疗药物。     

单硝酸异山梨酯渗透泵控释片的研制

目的制备单硝酸异山梨酯渗透泵控释片。方法建立体外评价方法，采用正交设计筛选出最佳处方。结果优化处方为20％聚乙二醇1500（PEG1500）、80mg氯化钠、4％包衣增重。结论按优化处方制备的渗透泵片符合零级释放特征。     

低分子肝素联合硝酸异山梨酯治疗慢性肺心病心力衰竭疗效分析

目的研究低分子肝素联合硝酸异山梨酯治疗慢性肺心病心力衰竭的疗效。方法将60例慢性肺心病心力衰竭患者随机分为治疗组和对照组,30例患者在常规治疗基础上加用低分子肝素和硝酸异山梨酯作为观察组,30例仅用常规治疗作对照组,均治疗10d。观察心肺功能恢复情况,检查血气分析和肺动脉压力。结果观察组有效率92.8%,对照组有效率为61.1%,2组比较差异有统计学意义（P〈0.05）。结论低分子肝素联合硝酸异山梨酯治疗慢性肺心病心力衰竭疗效满意。     

Electron beam irradiation: a novel technology for the development of transdermal system of isosorbide dinitrate

The development of a transdermal delivery system for isosorbide dinitrate (ISDN) using electron beam irradiation was studied. The solid state stability of the drug to irradiation was assessed. The drug was dissolved in 2-ethylhexylacrylate (EHA)-acrylic acid (AA) system and this solution was directly irradiated on a backing membrane (Scotchpak^®1006) at different doses to get transdermal patches. The developed systems were evaluated for residual monomer content, equilibrium weight swelling ratios (EWSR), differential scanning calorimetry (DSC), weight uniformity, thickness uniformity, drug content and content uniformity, peel strength, in vitro release, skin permeation kinetics and skin irritation potential. The developed system possessed excellent adhesive properties. Increase in the irradiation doses did not have a significant effect on the peel strength values. The systems exhibited promising skin permeation kinetics and no skin irritating potential, both of which are important properties for transdermal drug delivery. The ISDN-EHA-AA system developed at an irradiation dose of 50 kGy showed a higher skin permeation profile as compared to an internationally marketed transdermal matrix system of ISDN.     

5-单硝酸异山梨醇酯缓释胶囊在中国健康男青年的药物动力学(英文)

目的:比较国产和进口5-单硝酸异山梨醇酯缓释胶囊在健康人体内的药动学。方法:20名志愿者交叉随机分两组,口服50mg,GC-ECD测血药浓度,一室模型拟合或梯形法求药动学参数。结果:多剂量组连续5天服国产或进口胶囊,药动学参数C_(max)分别为(677±103)和(702±76)μg·L~(-1);T_(max)分别为(5.1±2.0)和(5.6±1.3)h;MRT分别为(11.5±0.5)和(11.4±0.7)h;AUC_(0-∞)分别为 (12121±1346)和(12352±988)μg·h·L~(-1),两者差异无显著性(P>0.05)。两种胶囊在服药16h后,血药浓度降至产生耐受性的阈值浓度以下(<300μg·L~(-1))。两种胶囊体内吸收分数和其体外相应时间的溶出率均呈显著正相关(P<0.05),单剂量和多剂量下国产对进口胶囊的相对生物利用度分别为96％±11％和98％±10％。结论:两种胶囊药动学特点相似。     

Development of a membrane-controlled transdermal therapeutic system containing isosorbide dinitrate

The formulation of a transdermal delivery system for isosorbide dinitrate (ISDN) was examined. It was found that the target release rate should be 4.01 mg/h per 20 cm² for optimal dosing. In order to reach such this zero order release rate, a membrane permeation controlled transdermal therapeutic system (TTS) formulation was developed, with ethylene vinyl acetate copolymer (EVAC) and polyethylene (PE) membranes as rate controlling membranes; a carbomer gel was used as the drug reservoir. The release of ISDN from this drug delivery device was studied in vitro using FDA recommended method. PIB adhesive on the EVAC or PE membrane caused a decreased flux of ISDN; the release kinetics fitted Higuchi matrix kinetics. TTS with EVAC membrane release ISDN at a rate much lower than the calculated target release rate, but with PE membranes, the release rate was very close to the target. Release rate studies have revealed that, as the VA content in EVAC membrane increased, the flux of ISDN increased. All these results were compared with the commercial product Frandol^® Tape S from Japan. It was found that the release rate of Frandol was close to target release rate and fitted matrix kinetics. These results suggested that TTS that contain PE membrane as rate controlling membrane, polyisobutylene (PIB) adhesive and carbomer gel as a reservoir can be applicable as a TTS for ISDN.     

复方丹参滴丸和硝酸异山梨酯治疗冠心病147例报告

目的：探讨联用复方丹参滴丸与硝酸异山梨酯治疗冠状粥样硬化性心脏病、心绞痛的临床疗效及对心功能的影响。方法：根据，临床症状、体表、心电图、血液流变性和运动、耐力试验等，观察单用上述两种药物或二者合用对心功能的影响。结果及结论：复方丹参滴丸对冠心病、心绞痛有较好的疗效，与硝酸异山梨酯合用更适合血容量不足，及扩血管药物敏感的心绞痛的老年患者。