氯吡格雷联合辛伐他汀治疗不稳定型心绞痛临床观察

目的观察氯吡格雷片联合辛伐他汀片治疗不稳定型心绞痛的临床疗效。方法将本院收治的128例不稳定型心绞痛患者按照入院顺序分为对照组64例和观察组64例,对照组患者给予氯吡格雷片,观察组患者给予氯吡格雷片和辛伐他汀片联合治疗,治疗结束后对比两组患者症状后进行综合效果评价。结果两组治疗前总胆固醇(TC)、低密度脂蛋白胆固醇(LDL-C)水平差别不大,差异无统计学意义;观察组治疗后TC、LDL-C水平均低于对照组,差异有统计学意义。观察组治愈率和总有效率均明显高于对照组,差异有统计学意义。结论氯吡格雷片联合辛伐他汀片治疗不稳定型心绞痛患者具有较好的临床疗效。     

中西医结合疗法心痛逐瘀汤联合氯吡格雷片对不稳定型心绞痛患者血小板的影响观察

目的:研究中西医结合疗法心痛逐瘀汤联合氯吡格雷片对不稳定型心绞痛患者血小板的影响。方法:选取我院2012年6月~2015年12月收治的不稳定型心绞痛患者100例为研究对象,根据患者的不同治疗方式将其分为对照组与观察组,对照组采用氯吡格雷片进行治疗,观察组在对照组的基础上采用心痛逐瘀汤进行治疗,对比分析两组治疗效果。结果:观察组患者的血小板聚集率以及血栓素B2下降程度显著优于对照组。结论:中西医结合疗法心痛逐瘀汤联合氯吡格雷片能够有效治疗不稳定型心绞痛,在临床上值得广泛推广。     

氯吡格雷联合辛伐他汀对于不稳定型心绞痛的治疗效果

目的分析对不稳定型心绞痛患者实施氯吡格雷联合辛伐他汀治疗的临床疗效。方法将80例不稳定型心绞痛患者进行随机分组,对对照组和观察组患者分别实施常规的辛伐他汀和辛伐他汀联合氯吡格雷的治疗。结果两组患者均可取得较好治疗效果,但相比对照组,观察组患者在治疗效果上明显更佳,差异有统计学意义(P<0.05)。而两组患者在治疗安全性上的差异无统计学意义(P>0.05)。结论在对不稳定型心绞痛患者治疗时,通过联合氯吡格雷和辛伐他汀治疗可取得更加有效的临床疗效,有着很高的应用价值。     

吲哚布芬联合氯吡格雷治疗不稳定型心绞痛的临床观察

目的探究不稳定型心绞痛患者采用吲哚布芬联合氯吡格雷的治疗效果。方法于2018年5月至2019年5月这一期间,随机选取某院收治的136例不稳定型心绞痛患者,并按照数字表法分为2组,对比组予以阿司匹林联合氯吡格雷治疗,实验组实施吲哚布芬联合氯吡格雷治疗,并对两组患者心绞痛发作次数、持续时间以及不良反应发生率进行对比。结果治疗前两组患者心绞痛发作次数与持续时间的比较差异不明显(P>0.05);治疗后两组患者心绞痛发作次数与持续时间均低于治疗前,并且实验组心绞痛发作次数与持续时间的降低程度优于对比组(P<0.05);实验组患者不良反应发生率4.41%,明显比对比组患者的23.52%低(P<0.05)。结论不稳定型心绞痛患者采用吲哚布芬联合氯吡格雷治疗,可减少心绞痛发作次数与持续时间,降低不良反应发生率。     

阿司匹林联合氯吡格雷治疗不稳定型心绞痛160例疗效分析

目的探究阿司匹林与氯吡格雷联合治疗不稳定型心绞痛临床疗效。方法随机选择我院收治的160例不稳定型心绞痛患者,并随机平均将其恩成实验组和对照组,两组均给予常规抗心绞痛的治疗,对照组在常规治疗的基础上加用阿司匹林,实验组在对照组的基础上加用硫酸氯吡格雷片,比较两组患者治疗后的疗效。结果实验组其有效率明显优于对照组(P<0.05);实验组4周内心绞痛复发,心肌梗死,心源性猝死事件发生情况均明显低于对照组(P<0.05),实验组1周后心绞痛发作频率、持续时间均明显低于对照组(P<0.05);结论阿司匹林联合氯吡格雷治疗不稳定型心绞痛疗效确切,而且安全有效,值得在临床工作中开展应用。     

氯吡格雷联合阿司匹林治疗稳定型心绞痛伴糖尿病的疗效及安全性研究

目的探讨氯吡格雷联合阿司匹林治疗稳定型心绞痛伴糖尿病的疗效及安全性。方法 2011年5月至2012年5月我院门诊及住院治疗的糖尿病合并冠状动脉粥样硬化性心脏病、稳定型心绞痛患者98例随机分为2组,每组49例。对照组予以阿司匹林治疗,研究组予以氯吡格雷联合阿司匹林治疗,比较两组的临床疗效。结果治疗后研究组总有效率高于对照组(93.87%vs.83.67%,P<0.05)。两组治疗1周后血小板聚集率均较基线水平明显下降,其中研究组的下降水平明显低于对照组(P<0.01)。治疗后研究组的心绞痛发作次数明显低于对照组(P<0.05)。对照组不良反应发生率为6.12%,研究组为8.16%,两组比较差异无统计学意义(P>0.05)。结论氯吡格雷联合阿司匹林治疗稳定型心绞痛伴糖尿病具有较好的临床的疗效,安全性高,且能有效降低血小板聚集率,避免心脏不良事件的发生。     

阿司匹林联合氯吡格雷双重抗血小板在不稳定性心绞痛中的作用探讨

目的探讨阿司匹林联合氯吡格雷双重抗血小板治疗在不稳定性心绞痛中的临床作用。方法选择50例患者使用阿司匹林联合氯吡格雷的双重抗血小板治疗,并与单纯使用阿司匹林抗血小板治疗的患者比较,两组治疗期间每周心绞痛发展次数以及心绞痛发作时间,并统计治疗期间发生的不良反应。结果治疗后观察组每周心绞痛发生次数显著少于对照组（P〈0.05）,心绞痛发作时间亦显著短于对照组（P〈0.05）,两组总的不良反应发生率差异无统计学意义（P〉0.05）,同时各种不良反应间差异亦无统计学意义（P〉0.05）。结论阿司匹林与氯吡格雷联合治疗不稳定性心绞痛临床效果佳,安全性高,值得临床推广。     

氯吡格雷联合阿司匹林治疗不稳定型心绞痛临床疗效观察

目的研究氯吡格雷联合阿司匹林治疗不稳定型心绞痛的疗效和安全性。方法将80例不稳定型心绞痛患者随机分成2组。对照组40例,给予常规治疗;治疗组40例,在常规治疗基础上应用氯吡格雷治疗。结果与对照组比较,氯吡格雷治疗组心绞痛发作次数减少,持续时间缩短,心电图心肌缺血减轻(P<0.05),无出血、粒细胞减少等并发症发生。两组血小板、白细胞计数、心肌酶、肌钙蛋白Ⅰ等无显著变化(P>0.05)。结论氯吡格雷联合阿司匹林治疗不稳定型心绞痛比单用阿司匹林疗效更好,且安全,副作用少。     

辛伐他汀、低分子肝素联合氯吡格雷治疗不稳定型心绞痛疗效分析

目的分析辛伐他汀、低分子肝素联合氯吡格雷治疗不稳定型心绞痛的疗效。方法将82例不稳定型心绞痛患者随机分为研究组和对照组各41例,两组患者入院后均给予常规内科治疗,研究组在常规内科治疗的基础上同时给予低分子肝素、辛伐他汀、氯吡格雷片,连用4周后比较两组的疗效。结果研究组总有效率明显高于对照组,差异有统计学意义(P<0.05)。两组肝肾功能未见明显异常,均未出现皮肤黏膜及内脏出血。结论辛伐他汀、低分子肝素联合氯吡格雷治疗不稳定型心绞痛可提高疗效,且使用安全、可靠,副反应少,值得广泛推广和应用。     

氯吡格雷治疗老年不稳定型心绞痛的临床观察

目的探讨氯吡格雷治疗老年不稳定型心绞痛的临床疗效。方法选取2013年10月至2016年9月期间我院收治的老年不稳定型心绞痛患者100例,采取国际通用随机字母表法将入组患者分为两组,观察组和对照组均包含50例。两组患者均给予常规不稳定型心绞痛治疗,观察组患者在此基础上给予口服氯吡格雷进行治疗。结果观察组患者的临床治疗总有效率96.0%,显著高于对照组的82.0%,比较差异具有统计学意义P<0.05。两组患者治疗前的心绞痛发作次数、ST变化、血小板计数、纤维蛋白原水平相当,比较差异不具有统计学意义P>0.05;治疗后观察组患者以上各项指标均得到了显著改善,改善程度显著优于对照组,比较差异具有统计学意义P<0.05。结论氯吡格雷治疗老年不稳定型心绞痛可显著提高患者的治疗效果,并对心绞痛发作次数、ST变化、血小板计数、纤维蛋白原水平等指标具有明显的改善效果。     

非洛地平缓释片与尼群地平片治疗高血压病的疗效比较

目的：比较非洛地平缓释片与尼群地平片治疗高血压病的疗效。方法：轻、中度高血压病病人１６２例,其中９８例（男性６７例,女性３１例,年龄５１ａ±ｓ６ａ）用非洛地平缓释片５～１０ｍｇ,ｐｏ,ｑｄ×４ｗｋ治疗。另６４例（男性４７例,女性１７例,年龄５０ａ±８ａ）用尼群地平片１０ｍｇ,ｐｏ,ｂｉｄ或ｔｉｄ×４ｗｋ治疗。结果：非洛地平缓释片组总有效率９５％,与尼群地平片组（８１％）相比,差别有非常显著意义（Ｐ＜０．０１）。不良反应发生率非洛地平缓释片组１５％,与尼群地平片组（２０％）比较,差别有显著意义（Ｐ＜０．０５）。结论：非洛地平缓释片对高血压病的疗效显著而又安全,优于尼群地平片。     

The comparative bioavailability of an extended-release niacin and lovastatin fixed dose combination tablet versus extended-release niacin tablet, lovastatin tablet and a combination of extended-release niacin tablet and lovastatin tablet

Lovastatin and extended-release (ER) niacin in a fixed dose combination (Advicor) is approved for the treatment of dyslipidemia. Since both drugs are extensively metabolized, this study investigated the bioavailability and pharmacokinetics of their co-administration following single-dose administration. In a 4-way crossover study 40 subjects received: two 1000/20 Advicor tablets (ADV), two 1000 mg niacin ER tablets (NSP), two 20mg lovastatin tablets (Mevacor; MEV), and two niacin ER 1000 mg tablets with two lovastatin 20mg tablets (NSP+MEV). Plasma was assayed for niacin, nicotinuric acid (NUA), lovastatin, lovastatin acid and HMGCoA reductase inhibition. Urine was assayed for niacin and its metabolites, NUA, N-methylnicotinamide and N-methyl-2pyridone-5-carboxamide. Least square mean ratios and 90% confidence intervals for C(max) and AUC((0-t)) were determined for NSP+MEV versus MEV or NSP, ADV versus MEV or NSP, and ADV versus NSP+MEV. Co-administration of niacin and lovastatin did not significantly influence C(max) and AUC((0-t)) of lovastatin, niacin, NUA and total urinary recovery of niacin and metabolites. A 22 to 25% decrease in lovastatin acid C(max) was observed while lovastatin acid AUC((0-t)) was not affected. The HMGCoA reductase inhibition C(max) and AUC((0-t)) were not affected indicating that the difference in lovastatin acid C(max) was not clinically relevant.     

Vardenafil orodispersible tablet

Vardenafil orodispersible tablet (ODT) is a supralingual formulation of vardenafil that is available for the on-demand treatment of erectile dysfunction. The pharmacokinetics of vardenafil ODT are not equivalent to those of the vardenafil film-coated tablet in that the ODT formulation provides consistently greater vardenafil systemic exposure. Therefore, the two formulations are not interchangeable. The efficacy of on-demand vardenafil ODT 10 mg was established in the POTENT I and II studies, which were 6-week, randomized, double-blind, multinational trials in men with erectile dysfunction of at least 6 months duration. In both trials, vardenafil ODT improved erectile function significantly more than placebo, as indicated by International Index of Erectile Function-Erectile Function subscale scores at week 12 and overall erection success rates during treatment according to responses to questions 2 and 3 of the Sexual Encounter Profile (coprimary endpoints). In a pooled analysis of both trials, vardenafil ODT improved erectile function regardless of age, severity of erectile dysfunction at baseline or the presence or absence of underlying medical conditions. Vardenafil ODT was generally well tolerated in clinical trials, including in men aged ≥65 years, and adverse events were mostly mild or moderate in severity.     

Fentanyl buccal tablet

Studies of populations with chronic cancer pain have shown a high prevalence of breakthrough pain (BTP), defined as transitory, severe flares of pain that occur on a background of otherwise controlled, persistent pain. High BTP prevalence rates have also been reported in patients with chronic noncancer pain, although data in these patient populations are more limited. The incidence of BTP appears to be associated with progression of chronic disease, with more than 80% of patients reporting BTP with far-advanced, end-stage cancer and noncancer terminal conditions (1). The most widely accepted therapeutic approach for the management of BTP involves use of short-acting opioids taken as needed in addition to the around-the-clock opioid regimen being used for the continuous component of the persistent pain syndrome. For some patients, an optimal treatment outcome for BTP may be unattainable because of a mismatch between the time course of the BTP episode and the onset of analgesia of short-acting opioids. Breakthrough pain typically reaches peak intensity within a few minutes, whereas the onset of analgesia with traditional, orally administered short-acting opioids is between 30 and 60 minutes (2-7). Consequently, treatment outcomes for BTP are likely to be improved with agents that have a more rapid onset of analgesia. Fentanyl buccal tablet (FBT) is a new formulation of fentanyl indicated for the management of BTP in patients with cancer who are already receiving, and who are tolerant to, opioid therapy for their underlying persistent cancer pain. The FBT formulation uses OraVescent (Cephalon, Inc., Frazer, PA, USA) drug delivery technology to provide rapid absorption of fentanyl through the buccal mucosa. In pharmacokinetic studies in healthy volunteers, FBT demonstrated high, early systemic absorption. In addition, FBT delivered a larger proportion of the fentanyl dose transmucosally and produced a greater early systemic exposure than oral transmucosal fentanyl citrate (OTFC), which is also indicated for the management of BTP in opioid-tolerant cancer patients. A number of short-term studies have evaluated the efficacy, safety and tolerability of FBT in the management of BTP in opioid-tolerant patients with chronic pain. All these studies included an open-label dose-titration phase prior to randomized, placebo-controlled, double-blind treatment. Pain Intensity of a BTP episode was measured using an 11-point scale (0 = no pain, 10 = worst pain), and the primary outcome measure was the Summed Pain Intensity Difference (SPID) at a specified time point. Secondary efficacy measures included Pain Relief, Pain Intensity Differences, and the proportion of BTP episodes demonstrating >or=33% and >or=50% improvement in Pain Intensity scores at each time point postdose, and the proportion of BTP episodes requiring supplemental medication. In a pivotal study of opioid-tolerant patients with cancer-related chronic pain and BTP, the primary outcome measure, SPID at 30 minutes (SPID(30)), significantly favored FBT compared with placebo (mean +/- SE: 3.0 +/- 0.12 vs. 1.8 +/- 0.18, p<0.0001). Better efficacy was also observed with FBT compared with placebo for pain relief, Pain Intensity Differences, and the proportion of episodes showing >or=33% and >or=50% improvement in Pain Intensity Scores. Treatment with FBT was generally well tolerated. Most adverse events were mild to moderate in severity and typical of those associated with opioid use (e.g., nausea, dizziness) (8). Similar results have been observed in studies of opioid-tolerant patients with BTP in association with noncancer-related chronic pain. In a study of patients with chronic low back pain, the primary outcome measure, SPID(60), significantly favored FBT over placebo (mean +/- SE: 8.3 +/- 0.66 vs. 3.6 +/- 0.57, p <0.0001). All secondary efficacy measures were similarly improved, with Pain Intensity Differences and Pain Relief scores showing significant differences versus placebo as early as 10 and 15 minutes, respectively. As in the study of cancer patients, treatment with FBT was well tolerated (9). Across all studies, there was no simple linear relationship between the effective dose of FBT and the dose of the around-the-clock opioid regimen or the previous supplemental opioid, indicating that doses of FBT should be individually titrated to effectiveness rather than calculated as a percentage of existing opioid regimens. This monograph summarizes current data on the clinical pharmacology, efficacy, safety and tolerability of FBT relating to the management of opioid-tolerant patients with BTP in association with chronic pain.     

硝苯地平缓释片与普通片治疗原发性高血压的疗效比较

目的：比较硝苯地平缓释片与普通片治疗原发性高血压的疗效。方法：用单盲、交叉对照法治疗４２例原发性高血压病人（男性２２例，女性２０例，年龄５４±ｓ７ａ）。甲组先用缓释片２０ｍｇ，ｐｏ，ｂｉｄ×１４ｄ，间隔１ｄ，改服普通片１０ｍｇ，ｐｏ，ｔｉｄ×１４ｄ，乙组服药先后次序与甲组相反，剂量相同，疗程均为２９ｄ。结果：缓释片与普通片的降压有效率分别为９８％及６４％，有明显差异（Ｐ＜０．０５），降压幅度缓释片也高于普通片（Ｐ＜０．０１），其影响病人心率加快反应显著小于普通片（Ｐ＜０．０１），其他不良反应的发生率较低，程度也较轻。结论：硝苯地平缓释片（２０ｍｇ，ｂｉｄ）较普通片（１０ｍｇ，ｔｉｄ）更高效而安全。     

Preparation of bilayer-core osmotic pump tablet by coating the indented core tablet

In this paper, a bilayer-core osmotic pump tablet (OPT) which does not require laser drilling to form the drug delivery orifice is described. The bilayer-core consisted of two layers: (a) push layer and (b) drug layer, and was made with a modified upper tablet punch, which produced an indentation at the center of the drug layer surface. The indented tablets were coated by using a conventional pan-coating process. Although the bottom of the indentation could be coated, the side face of the indentation was scarcely sprayed by the coating solution and this part of the tablet remained at least partly uncoated leaving an aperture from which drug release could occur. Nifedipine was selected as the model drug. Sodium chloride was used as osmotic agent, polyvinylpyrrolidone as suspending agent and croscarmellose sodium as expanding agent. The indented core tablet was coated by ethyl cellulose as semipermeable membrane containing polyethylene glycol 400 for controlling the membrane permeability. The formulation of core tablet was optimized by orthogonal design and the release profiles of various formulations were evaluated by similarity factor (f(2)). It was found that the optimal OPT was able to deliver nifedipine at an approximate zero-order up to 24 h, independent on both release media and agitation rates. The preparation of bilayer-core OPT was simplified by coating the indented core tablet, by which sophisticated technology of the drug layer identification and laser drilling could be eliminated. It might be promising in the field of preparation of bilayer-core OPT.     

罗红霉素分散片人体相对生物利用度研究

采用自身前后交叉对照试验方法以 12例男性健康自愿受试者 ,单剂量口服罗红霉素分散片和罗红霉素片 (对照药品 )进行人体生物利用度比较研究。应用高效液相色谱法 (HPL C)测定服药后 48h内的血清罗红霉素浓度。结果表明罗红霉素分散片和罗红霉素片的主要药动学参数达峰时间 Tmax分别为 1.6 7± 0 .6 0和2 .31± 0 .48h,峰值血药浓度 Cmax为 11.0 9± 1.6 8和 9.35± 1.31mg/L ,T1 / 2β分别为 19.5 9± 8.11和 17.70± 4.2 2 h。药时曲线下面积 AUC分别为 16 9.90± 6 6 .41和 142 .77± 40 .0 9mg.h/L ,经双单侧 t检验两者的 Tmax、T1 / 2β无显著性差异 (P>0 .0 5 )。罗红霉素分散片的 Cmax高于普通片 (P<0 .0 5 ) ,AUC略高于普通片 ,但无明显差异 (P=0 .2 386 )。罗红霉素分散片对罗红霉素片的平均相对生物利用度为 118.89% ,以上说明罗红霉素分散片的生物利用度略优于普通片。     

Relations between tablet properties

With the aid of simple mathematical models the relations between specific crushing strength (i.e. crushing strength divided by the breaking surface), friability and disintegration time of a tablet can be given. The friability is related to the porosity of the tablets and the specific crushing strength, independent of the process conditions. For the disintegration time two models have been used, depending on the disintegration mechanism. In the first one the disintegration time is only dependent on the porosity, in the second on the specific surface by weight of the granules of which the tablets are made. The theoretical relationships were verified for two tablet formulations, made under varying process conditions.     

Performance of tablet disintegrants: impact of storage conditions and relative tablet density

Abstract

Tablet disintegration can be influenced by several parameters, such as storage conditions, type and amount of disintegrant, and relative tablet density. Even though these parameters have been mentioned in the literature, the understanding of the disintegration process is limited. In this study, water uptake and force development of disintegrating tablets are analyzed, as they reveal underlying processes and interactions. Measurements were performed on dibasic calcium phosphate tablets containing seven different disintegrants stored at different relative humidities (5–97%), and on tablets containing disintegrants with different mechanisms of action (swelling and shape recovery), compressed to different relative densities. Disintegration times of tablets containing sodium starch glycolate are affected most by storage conditions, which is displayed in decreased water uptake and force development kinetics. Disintegration times of tablets with a swelling disintegrant are only marginally affected by relative tablet density, whereas the shape recovery disintegrant requires high relative densities for quick disintegration. The influence of relative tablet density on the kinetics of water uptake and force development greatly depends on the mechanism of action. Acquired data allows a detailed analysis of the influence of storage conditions and mechanisms of action on disintegration behavior.