单硝酸异山梨酯定时脉冲释放片的制备及体外溶出度研究

 目的研制单硝酸异山梨酯(5-ISMN)定时脉冲释放片，并考察体外溶出的影响因素。方法采用压制包衣技术制备5 ISMN定时脉冲释放片，以崩解时间和膨胀率为指标，筛选了崩解剂类型和用量；采用反相高效液相色谱法测定体外溶出度，以释药时滞为指标，经均匀设计实验，筛选优化外包衣层处方组成。结果片芯选用羧甲基淀粉钠为崩解剂，用量20％即能达到设计要求。固定硬度，调整亲疏水性成分的比例，确定了时滞为3，4，5 h的3个基本处方。硬度、亲疏水性物质比、溶出介质黏度对时滞影响显著。结论单硝酸异山梨酯压制包衣片能实现体外定时脉冲释药，并可通过调整处方和工艺因素实现不同时滞的控释效果。     

单硝酸异山梨酯片单用和联合曲美他嗪片治疗慢性心力衰竭的疗效比较

目的 探讨单独应用单硝酸异山梨酯片和单硝酸异山梨酯片联合曲美他嗪片治疗慢性心力衰竭患者疗效。方法选取酒泉市人民医院收治的138例慢性心力衰竭患者作为研究对象,采用双盲法将其分为对照组和观察组,各69例。对照组给予单硝酸异山梨酯片治疗,观察组在此基础上增加曲美他嗪片治疗,两组均连续治疗6个月。治疗6个月后,比较两组临床疗效、心功能、炎症指标、血清组织蛋白酶S(Cat S)、血小板反应蛋白-1(TSP-1)、脑钠肽(BNP)水平,并观察两组不良反应发生情况。结果 观察组临床总有效率(91.30%)高于对照组(81.16%),差异有统计学意义(P<0.05)。观察组心功能指标、炎性细胞因子指标、Cat S、TSP-1及BNP水平治疗前后差值高于对照组(P<0.05)。两组总不良反应发生率比较,差异无统计学意义(χ²=0.122,P=0.727)。结论 单硝酸异山梨酯片联合曲美他嗪片可有效改善慢性心力衰竭患者心功能,减轻其炎症反应,改善血清Cat S、TSP-1及BNP水平,疗效确切,且安全性较高。     

Second trimester abortion using isosorbide mononitrate in addition to gemeprost compared with gemeprost alone: a double-blind randomized, placebo-controlled multicenter trial

OBJECTIVE: We aimed to determine whether second-trimester abortion using isosorbide mononitrate (IMN) in addition to gemeprost is more effective and reduces side effects compared with gemeprost alone. STUDY DESIGN: Eighty women who were age 13 to 23 weeks' gestation were randomly assigned to receive per vaginam either IMN 40 mg (group 1, 40 women) or placebo (group 2, 40 women) in addition to gemeprost 1 mg up to 3 times daily 3 hours apart for 2 days. Analysis of variance, a chi 2 test, and a multivariate analysis were performed. RESULTS: Of the 72 women analyzed, 68% (group 1) and 38% (group 2) underwent abortion within day 1 (P < .05). However, group 1 was associated with more headache (18% of women) 3 hours after induction compared to group 2 (0% of women, P = .038). CONCLUSION: IMN in addition to gemeprost is effective for second-trimester abortion, but is associated with more headache compared with gemeprost alone.     

5—单硝酸异山梨醇酯与硝酸异山梨醇酯对冠心病心绞痛的疗效比较

目的：比较5－单硝酸异山梨醇酯与硝酸异山梨醇酯对冠心病心绞痛的疗效,方法：对80例冠心病心绞痛病人随机分为两组,分别给予5－单硝酸异山梨醇酯和硝酸异山梨醇酯治疗,结果：5－单硝酸异山梨醇酯总有效率为92．5％,硝酸异山梨醇酯为72．5％（P＜0．05）,对心电图的疗效前者为62．5％,后者为55％（P＞0．05）,两组血压,心率变化无显著性差异,结论：5－单硝酸异山梨醇酯对冠心病心绞痛的疗效优于硝酸异山梨醇酯。     

强心汤联合鲁南欣康治疗阳虚水泛型冠心病慢性心衰的疗效及心肌保护作用

目的 观察强心汤联合鲁南欣康对阳虚水泛型冠心病慢性心力衰竭患者的疗效及心肌保护作用.方法 纳入阳虚水泛型冠心病慢性心力衰竭患者80例,随机分为两组各40例,均接受常规治疗,对照组同时应用鲁南欣康,观察组在对照组基础上应用强心汤,持续8周.对比2组心功能NYHA分级、Lee氏心衰积分及中医证候改善情况,观察2组超声心动图指标、血浆心肌纤维化指标及神经内分泌因子变化.结果 治疗后观察组Lee氏心衰积分、中医证候积分、左室射血分数(LVEF)、左心室舒张末内径(LVEDD)、二尖瓣舒张早期血流峰值速度/二尖瓣舒张晚期血流峰值速度(E/A)均明显优于对照组(P<0.01);治疗后观察组血浆Ⅲ型胶原前肽(PⅢP)、层粘连蛋白(LN)、醛固酮(ALD),均明显低于对照组,差异有统计学意义(P<0.05或P<0.01).结论 强心汤联合鲁南欣康有助于提升阳虚水泛型冠心病慢性心衰疗效,其机制与抑制血浆Ⅲ型胶原前肽、层粘连蛋白、醛固酮水平有关.     

脑心通胶囊治疗老年冠心病效果观察

目的观察脑心通胶囊治疗老年冠心病的临床效果。方法选择自2009年8月—2011年8月明确诊断的老年冠心病患者202例,随机分为治疗组和对照组,各101例。对照组采用常规治疗,口服单硝酸异山梨酯缓释片60 mg,每日1次;阿司匹林肠溶片100 mg,每日1次,如有高血压、糖尿病、高脂血症,另给予合理的降压、降糖、降脂(他汀类降脂药)药物治疗。治疗组在对照组治疗的基础上,加服脑心通胶囊4粒,每日3次。两组均治疗半年。治疗期间所有患者均每月随访1次,观察症状的改善情况、血压值的变化、血脂水平的变化、心电图表现、对睡眠的影响以及有无心血管意外事件的发生。计量资料比较采用t检验,计数资料比较采用χ2检验,P0.05为差异有统计学意义。结果对照组临床总有效率为46.5%,治疗组94.1%,两组比较差异有统计学意义(P0.05)。治疗后治疗组血脂水平、血压与对照组相比,差异均有统计学意义(均P0.05)。治疗组心电图、睡眠质量改善情况均优于对照组(均P0.05)。结论脑心通胶囊治疗老年冠心病能够有效缓解症状,改善心电图表现,促进患者康复,效果满意,且安全可靠。     

冠心方治疗心绞痛80例

[目的]观察冠心方治疗冠心病心绞痛疗效。[方法]将80例冠心病心绞痛患者随机分成治疗组41例和对照组39例,治疗组给予冠心方水煎服治疗,每日1剂,连用8周;对照组给予5单硝酸异山梨酯片治疗,每次50mg,每日1次,疗程同治疗组。[结果]治疗组临床疗效总有效率、治疗前后心电图总有效率均优于对照组(P<0.05)。[结论]冠心方治疗冠心病心绞痛有较好疗效,值得临床推广。     

振源胶囊联合胰岛素治疗2型糖尿病性冠心病心绞痛32例

[目的]观察振源胶囊联合西药治疗糖尿病性冠心病心绞痛疗效。[方法]将60例随机分为两组,均给予皮下胰岛素治疗。对照组28例拜阿司匹林、单硝酸异山梨醇酯口服。治疗组32例西药治疗同对照组。口服振源胶囊0.5g/次,3次/1d。治疗1疗程(28d)进行疗效判定。[结果]心绞痛发作次数减少、心电图改善情况治疗组均优于对照组(P<0.01);两组治疗前后空腹血糖(FBG)、餐后2h血糖及糖化血红蛋白均有明显改善(P<0.01),组间无明显差异(P>0.05)。[结论]振源胶囊对于糖尿病性冠心病心绞痛在改善症状及心电图方面具有明显的疗效。     

血府逐瘀汤加减配合西药治疗冠心病静息型心绞痛58例

[目的]观察血府逐瘀汤加减配合西药治疗冠心病静息型心绞痛疗效。[方法]随机将110例冠心病静息型心绞痛患者分为两组。对照组52例西药单硝酸异山梨酯、硝酸甘油等常规治疗,治疗组58例在对照组基础上予以血府逐瘀汤加减。连续治疗14d进行疗效判定。[结果]综合疗效治疗组总有效率优于对照组(P<0.05),治疗后硝酸甘油用量变化、血脂变化治疗组均明显优于对照组(P<0.05,P<0.01)。[结论]血府逐瘀汤加减配合西药治疗冠心病静息型心绞痛安全、有效,优于单纯西药治疗。     

Study on dissolution and absorption of four dosage forms of isosorbide mononitrate: Level A in vitro–in vivo correlation

The objective of the present study was to develop a novel in vitro system to simulate the process of dissolution and permeation of oral solid dosage forms in vivo, and to establish a correlation between in vitro permeation and in vivo absorption that could predict the bioavailability (BA) and bioequivalence (BE) of congeneric products. The in vitro dissolution and absorption kinetics of four dosage forms of isosorbide mononitrate (ISMN) were evaluated by the USP basket/paddle system and drug dissolution/absorption simulating system (DDASS). The corresponding pharmacokinetic study was performed in beagle dogs. A comparative study was carried out between the classical and the novel method to estimate the effectiveness of the modified DDASS in simulating the course of dissolution and absorption in vivo. Indeed, the correlation coefficients of in vitro dissolution and in vivo absorption obtained from DDASS and dogs were higher. Moreover, a higher level A in vitro–in vivo correlation (IVIVC) between DDASS permeation and dog absorption was established, with correlation coefficients of 0.9968, 0.9872, 0.9921, and 0.9728. The DDASS method was more accurate at modeling the process of dissolution and absorption in vivo for both immediate-release (IR) and sustained-release (SR) dosage forms of ISMN.