Polymeric ethosomal gel loaded with nimodipine: Optimisation,pharmacokinetic and histopathological analysis

This study was performed with the main objective of formulating and evaluating the potential of ethosomesl gel (Etho gel) to deliver nimodipine (NiM) for cardiovascular disease, a potent water insoluble anti-hypertensive drug via skin to reach the deeper layers of skin. The Box-Behnken design (BBD) was used to optimize the NiM-Eth to determine the impact of the independent and depended variables. The effectiveness of drug entrapment, vesicle size, and cumulative drug release were assessed for the NiM loaded ethosomes and NiM-Eth gel using carbopol 934 as a gelling agent. Fourier transform infrared spectroscopy (FTIR), Differential scanning calorimetry (DSC), Power X-ray diffraction (PXRD), and scanning electron microscopy (SEM) analysis were performed and analysed their physicochemical characters. Rat abdomen skin was used to investigate drug permeability and deposition. As compared to marketed products, NiM-Eth gel produced an improved drug permeability in ex vivo experiments. The mean AUC₀ to AUC_0-∞ of NiM-Eth gel when compared to oral formulation (Nymalize oral preparation) was found to be increased from 4.1 to 5.9 folds which was found to be resulted from first pass effect. Histophatlogical findings revealed that the maximum amount of NiM penetrated the stratum corneum of the skin and create drug depots in the deep layer. In summary, it can be said that NiM might be successfully prepared in NiM-Eth gel for transdermal drug delivery.     

Validated RP-HPLC method for quantification of felodipine in rabbit plasma: Application in a bioequivalence study

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Clinical trial of Nimodipine for single attacks of classic migraine

In a randomized, double-blind cross-over study, 43 patients with classic migraine received 40 mg Nimodipine and placebo as sublingual capsules. There was no significant effect on patients' preference, development of headache, need for escape medicine, duration of headache, severity of headache or headache index. Considerable methodological problems were encountered. Only 54% of the 79 patients selected for the trial could be evaluated. Suggestions for future trials are made.     

奥拉西坦联合尼莫地平治疗重症脑挫裂伤的临床观察

目的观察奥拉西坦联合尼莫地平治疗重症脑挫裂伤的临床疗效。方法选取新疆医科大学第二附属医院2010年11月—2014年10月收治的重症颅脑损伤患者130例,随机分为对照组(68例)和治疗组(62例)。两组患者术后均转入ICU监护并给予等常规治疗,对照组给予尼莫地平注射液4 mg/次,加入到250 m L生理盐水中静脉滴注,1次/d。治疗组在对照组基础上加用注射用奥拉西坦,4 g/次,加入到250 m L生理盐水中缓慢静滴,1次/d。两组均连续治疗14 d。比较两组的临床疗效,同时比较两组治疗前,治疗第3、7、14天神经功能缺损(NIHSS)评分、颅内压、GCS评分、脑电图快慢波比值、大脑中动脉(Mc A)平均血流速度、双侧平均肌力的变化。结果对照组和治疗组总有效率分别为61.76%、80.65%,两组比较差异有统计学意义(P0.05)。对照组NIHSS评分从治疗第7天,治疗组从治疗第3天开始显著下降,同组比较差异有统计学意义(P0.01)。从治疗第3天开始治疗组NIHSS评分显著低于对照组,两组比较差异有统计学意义(P0.05、0.01)。两组颅内压均从治疗第3天开始降低,GCS评分、Mc A平均血流速度、双侧平均肌力从治疗第3天开始升高,同组治疗前后差异有统计学意义(P0.01)。治疗组从治疗第3天开始,GCS评分、Mc A平均血流速度高于对照组,治疗组在治疗第3、7天颅内压低于对照组,在治疗第7天快慢波比值低于对照组,在治疗第3、14天双侧平均肌力高于对照组,两组比较差异有统计学意义(P0.05、0.01)。结论奥拉西坦联和尼莫地平治疗重症脑挫裂伤术后患者具有较好的临床疗效,可促进患者神经功能恢复,提高患者生存质量,为进一步探索和治疗重症脑挫裂伤患者提供明确的思路。     

法舒地尔与尼莫地平不同给药途径预防动脉瘤栓塞术后脑血管痉挛的疗效比较

【目的】探讨法舒地尔与尼莫地平不同给药途径对脑动脉瘤栓塞术后发生脑血管痉挛的防治价值。【方法】收集自2010年1月至2014年1月本院脑动脉瘤栓塞术后患者74例,随机分为两组,每组37例。对照组患者术中使用尼莫地平静脉滴注扩脑血管,观察组患者经动脉微导管推注法舒地尔进行扩血管治疗。比较两组患者脑脊液S100蛋白和血清神经元特异性烯醇化酶（NSE）变化,采用格拉斯哥预后评分评价治疗效果,比较两组患者的不良反应发生情况。【结果】两组患者治疗后脑脊液S100蛋白以及血清NSE均显著高于治疗前（ P ＜0．05）,治疗后尼莫地平组脑脊液S100蛋白以及血清NSE均显著高于法舒地尔组,且两组相比较差异有显著性（ P ＜0．05）。两组均无死亡病例,法舒地尔组总有效率（91．9％）显著高于尼莫地平组（75．7％）（ P ＜0．05）。法舒地尔组不良反应发生率显著低于尼莫地平组（18．9％ vs 43．2％,P＜0．05）。【结论】法舒地尔与尼莫地平都具有缓解脑血管痉挛的效果,能有效减少脑血管痉挛的发生,减少脑损伤,且法舒地尔预防和治疗脑血管痉挛的效果优于尼莫地平。     

偏头痛采用阿司匹林和尼莫地平治疗的临床比较

目的：探讨在治疗偏头痛方面阿司匹林和尼莫地平的效果。方法选取2012年5月—2014年5月来我院治疗的114例偏头痛患者，随机分为2组各57例，命名为试验组和对照组。对照组患者采用尼莫地平治疗，试验组患者采用阿司匹林治疗，记录2组患者的治疗效果、并发症发生情况及半年内的复发情况等，并进行对比分析。结果经过一段时间治疗后，试验组患者的治疗总有效率明显高于对照组（P<0.05），且并发症发生率、半年内复发率明显低于对照组（P<0.05）。结论阿司匹林治疗偏头痛的效果显著，并发症发生率和复发率也都比较低，安全性高，值得在临床上推广使用。     

Complication rate of intraarterial treatment of severe cerebral vasospasm after subarachnoid hemorrhage with nimodipine and percutaneous transluminal balloon angioplasty: Worth the risk?

Background and purpose

Delayed cerebral ischemia (DCI) is a complication of aneurysmal subarachnoid hemorrhage (SAH). Arterial cerebral vasospasm (CVS) is discussed as the main pathomechanism for DCI. Due to positive effects of per os nimodipine, intraarterial nimodipine application is used in patients with DCI. Further, percutaneous transluminal balloon angioplasty (PTA) is applied in focal high-grade spasm of intracranial arteries. However, clinical benefits of those techniques are unconfirmed in randomized trials so far, and complications might occur. We analyzed the occurrence of new infarcts in patients with severe CVS treated intra-arterially to assess benefits and risks of those techniques in a large single-center collective.

依达拉奉联合尼莫地平序贯疗法对脑出血患者神经功能及血清NSE、OPN、BDNF表达的影响

目的探讨依达拉奉联合尼莫地平序贯疗法对脑出血患者神经功能及血清神经元特异性烯醇化酶(NSE)、骨桥蛋白(OPN)、脑源性神经营养因子(BDNF)表达的影响。方法收集我院自2016年1月～2019年2月收治的76例脑出血患者,按随机数字表法分为两组,各38例。两组均给予神经内科常规综合治疗,对照组加用尼莫地平序贯疗法,观察组在对照组基础上联合依达拉奉治疗。比较两组神经功能、血肿与周围水肿体积及疗效,检测两组血清NSE、OPN、BDNF水平变化情况。结果治疗后,观察组NIHSS评分低于对照组(P0.01);观察组总有效率为92.11%,高于对照组的73.68%(P0.05);治疗后,观察组血肿体积与周围水肿体积均小于对照组(P0.05);治疗后,观察组血清NSE、OPN低于对照组,BDNF高于对照组(P0.05)。结论依达拉奉联合尼莫地平序贯疗法治疗脑出血效果确切,可显著缩小血肿及其周围水肿体积,解除血肿占位效应,恢复患者神经功能,改善生化指标。     

尼莫地平注射液联合6-氨基己酸在蛛网膜下腔出血中的应用效果

目的：探讨尼莫地平注射液联合6-氨基己酸在蛛网膜下腔出血中的应用效果。方法选取2012年5月—2014年7月赫章县人民医院收治的蛛网膜下腔出血患者50例，将患者随机分为对照组与治疗组，每组25例。对照组单独使用尼莫地平注射液治疗，治疗组应用尼莫地平注射液联合6-氨基己酸治疗，比较两组临床疗效、格拉斯哥预后量表（GOS）评分与并发症发生情况。结果治疗组总有效率（92.00%）高于对照组（64.00%），再出血发生率（16.0%）低于对照组（32.0%），差异有统计学意义（P ＜0.05）。观察组患者 GOS 评分高于对照组，差异有统计学意义（P ＜0.05）。结论尼莫地平注射液联合6-氨基己酸治疗蛛网膜下腔出血临床效果好，可显著降低再出血发生率，改善患者预后。