Gabapentin

加巴喷丁
  • 文章类型: Journal Article
    术后疼痛(POP)是最常见,最重要的疼痛类型之一。
    这项研究的目的是比较先发制人的羟考酮的效果,双氯芬酸,和加巴喷丁对胫骨骨折手术患者术后疼痛(POP)的影响。
    这项双盲三组随机对照试验于2023年进行。参与者是111名在全身麻醉下进行胫骨骨折手术的候选人。他们被随机分配给羟考酮,加巴喷丁,和双氯芬酸组通过区组随机化。基线动脉血氧饱和度,心率,术前记录血压,术后恢复期间和术后2、4、6、12和24h测量POP和镇静状态。术后阿片类镇痛药的使用也有记录。使用SPSS软件分析数据(v。20.0)在小于0.05的显著性水平。
    各组在参与者的基线年龄方面没有显着差异,性别,身体质量指数,动脉血氧饱和度,心率,血压,和手术时间(P>0.05)。此外,不同测量时间点的POP和镇静状态组间差异无统计学意义(P>0.05),除了手术后6小时外,加巴喷丁组的POP平均评分明显低于其他两组(P=0.001).术后使用阿片类镇痛药和药物副作用的组间差异也无统计学意义(P>0.05)。
    先发制人的羟考酮,双氯芬酸,和加巴喷丁显著降低了胫骨骨折手术患者的POP,虽然加巴喷丁可能产生更显著的镇痛作用。这三种药物均可用于先发制人镇痛。当然,最佳的先发制人镇痛剂是根据主治医师的意见确定的。
    UNASSIGNED: Postoperative pain (POP) is one of the most common and most important types of pain.
    UNASSIGNED: The aim of this study was to compare the effects of pre-emptive oxycodone, diclofenac, and gabapentin on postoperative pain (POP) among patients with tibia fracture surgery.
    UNASSIGNED: This double-blind three-group randomised controlled trial was conducted in 2023. Participants were 111 candidates for tibia fracture surgery under general anaesthesia. They were randomly allocated to oxycodone, gabapentin, and diclofenac groups through block randomisation. Baseline arterial oxygen saturation, heart rate, and blood pressure were documented before surgery and POP and sedation status were measured during postoperative recovery and 2, 4, 6, 12, and 24 h after surgery. Postoperative opioid analgesic use was also documented. The data were analysed using the SPSS software (v. 20.0) at a significance level of less than 0.05.
    UNASSIGNED: Groups did not significantly differ from each other respecting participants\' baseline age, gender, body mass index, arterial oxygen saturation, heart rate, blood pressure, and surgery duration (P > 0.05). Moreover, there were no significant differences among the groups respecting POP and sedation status at different measurement time points (P > 0.05), except for six hours after surgery at which the POP mean score in the gabapentin group was significantly less than the other two groups (P = 0.001). Among-group differences respecting postoperative use of opioid analgesics and medication side effects were also insignificant (P > 0.05).
    UNASSIGNED: Pre-emptive oxycodone, diclofenac, and gabapentin significantly reduce POP among patients with tibia fracture surgery, though gabapentin may produce more significant analgesic effects. All these three medications can be used for pre-emptive analgesia. Of course, the best pre-emptive analgesic agent is determined based on the opinion of the treating physician.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    背景和目的:加巴喷丁有望成为治疗酒精戒断综合征的潜在药物。我们旨在评估加巴喷丁作为苯二氮卓类药物保护剂在大型三级医疗保健系统的所有医院接受酒精戒断治疗的患者中的有效性。材料和方法:回顾了2020年1月1日至2022年8月31日期间住院接受戒酒管理的患者的病历。患者分为两组:仅接受苯二氮卓类药物作为主要药物治疗的苯二氮卓类药物治疗和加巴喷丁辅助治疗,除了苯二氮卓类药物外,还接受加巴喷丁治疗。评估的结果包括治疗期间使用的苯二氮卓类药物的总剂量和住院时间。对统计模型进行校准以考虑各种因素。结果:4364例患者纳入最终分析。其中,79例患者(1.8%)除了苯二氮卓类药物外还接受了加巴喷丁,4285例患者(98.2%)仅接受苯二氮卓类药物治疗。服用加巴喷丁的患者需要显著降低的平均累积苯二氮卓类药物剂量,减少约17.9%,与未接受加巴喷丁的患者相比(中位数2mgvs.4mg劳拉西泮等效剂量(p<0.01))。然而,两组间的结局无显著差异.结论:我们的发现表明,使用加巴喷丁和苯二氮卓类药物与酒精戒断的累积苯二氮卓类药物剂量减少有关。考虑将加巴喷丁作为辅助疗法,对于合并疾病的患者有望从减少苯二氮卓类药物的剂量中受益。这一战略值得进一步调查。
    Background and Objectives: Gabapentin has shown promise as a potential agent for the treatment of alcohol withdrawal syndrome. We aimed to evaluate the effectiveness of gabapentin as a benzodiazepine-sparing agent in patients undergoing alcohol withdrawal treatment in all the hospitals of a large tertiary healthcare system. Materials and Methods: Medical records of patients admitted to the hospital for alcohol withdrawal management between 1 January 2020 and 31 August 2022 were reviewed. Patients were divided into two cohorts: benzodiazepine-only treatment who received benzodiazepines as the primary pharmacotherapy and gabapentin adjunctive treatment who received gabapentin in addition to benzodiazepines. The outcomes assessed included the total benzodiazepine dosage administered during the treatment and the length of hospital stay. The statistical models were calibrated to account for various factors. Results: A total of 4364 patients were included in the final analysis. Among these, 79 patients (1.8%) received gabapentin in addition to benzodiazepines, and 4285 patients (98.2%) received benzodiazepines only. Patients administered gabapentin required significantly lower average cumulative benzodiazepine dosages, approximately 17.9% less, compared to those not receiving gabapentin (median 2 mg vs. 4 mg of lorazepam equivalent dose (p < 0.01)). However, there were no significant differences in outcomes between the two groups. Conclusions: Our findings demonstrate that using gabapentin with benzodiazepine was associated with a reduction in the cumulative benzodiazepine dosage for alcohol withdrawal. Considering gabapentin as an adjunctive therapy holds promise for patients with comorbidities who could benefit from reducing benzodiazepine dose. This strategy warrants further investigation.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    背景:在腰椎椎板切除术和椎间盘切除术后补充加巴喷丁可能具有一定的疼痛控制潜力,本荟萃分析旨在探讨补充加巴喷丁对腰椎椎板切除术和椎间盘切除术术后疼痛管理的影响。
    方法:PubMed,EMBase,WebofScience,EBSCO,系统搜索了Cochrane图书馆数据库,我们纳入了评价加巴喷丁对腰椎椎板切除术和椎间盘切除术疼痛控制效果的随机对照试验.
    结果:5项随机对照试验最终纳入meta分析。总的来说,与腰椎椎板切除术和椎间盘切除术的对照干预相比,补充加巴喷丁与2小时疼痛评分显著降低相关(MD=-2.75;95%CI=-3.09至-2.41;P<.00001),4小时疼痛评分(MD=-2.28;95%CI=-3.36至-1.20;P<0.0001),24小时疼痛评分(MD=-0.70;95%CI=-0.86至-0.55;P<.00001)和与对照干预相比的焦虑评分(MD=-1.32;95%CI=-1.53至-1.11;P<.00001),但对12小时疼痛评分无明显影响(MD=-0.58;95%CI=-1.39~0.22;P=.16)。此外,相对于对照干预措施,补充加巴喷丁可以显着降低呕吐的发生率(OR=0.31;95%CI=0.12-0.81;P=0.02),但他们的恶心发生率相似(OR=0.51;95%CI=0.15-1.73;P=.28).
    结论:补充加巴喷丁有利于腰椎椎板切除术和椎间盘切除术后的疼痛控制。
    BACKGROUND: Gabapentin supplementation may have some potential in pain control after lumbar laminectomy and discectomy, and this meta-analysis aims to explore the impact of gabapentin supplementation on postoperative pain management for lumbar laminectomy and discectomy.
    METHODS: PubMed, EMbase, Web of science, EBSCO, and Cochrane library databases were systematically searched, and we included randomized controlled trials assessing the effect of gabapentin supplementation on the pain control of lumbar laminectomy and discectomy.
    RESULTS: Five randomized controlled trials were finally included in the meta-analysis. Overall, compared with control intervention for lumbar laminectomy and discectomy, gabapentin supplementation was associated with significantly lower pain scores at 2 hours (MD = -2.75; 95% CI = -3.09 to -2.41; P < .00001), pain scores at 4 hours (MD = -2.28; 95% CI = -3.36 to -1.20; P < .0001), pain scores at 24 hours (MD = -0.70; 95% CI = -0.86 to -0.55; P < .00001) and anxiety score compared to control intervention (MD = -1.32; 95% CI = -1.53 to -1.11; P < .00001), but showed no obvious impact on pain scores at 12 hours (MD = -0.58; 95% CI = -1.39 to 0.22; P = .16). In addition, gabapentin supplementation could significantly decrease the incidence of vomiting in relative to control intervention (OR = 0.31; 95% CI = 0.12-0.81; P = .02), but they had similar incidence of nausea (OR = 0.51; 95% CI = 0.15-1.73; P = .28).
    CONCLUSIONS: Gabapentin supplementation benefits to pain control after lumbar laminectomy and discectomy.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    加巴喷丁已被用于加强手术后恢复(ERAS)途径,以控制接受动态泌尿外科手术的患者的疼痛;然而,它可能会导致不良的副作用。我们研究了微创手术后加巴喷丁与康复速度和围手术期疼痛管理之间的因果关系。
    我们在2018年至2022年之间确定了2397例≤65岁的患者接受前列腺切除术或肾切除术;131例(5.5%)未接受加巴喷丁。我们测试了加巴喷丁使用对出院时间和围手术期阿片类药物消耗的影响,分别,使用多变量线性回归调整潜在的混杂因素,包括年龄,性别,BMI,美国麻醉医师协会评分,和手术类型。
    关于调整后的分析,我们发现,在接受加巴喷丁治疗和未接受加巴喷丁治疗的患者中,没有发现出院时间有差异的证据(加巴喷丁治疗的校正后差异缩短0.07小时;95%CI-0.17,0.31;P=.6).没有证据表明加巴喷丁服用术中阿片类药物的消耗有差异(调整后差异-1.5吗啡毫克当量;95%CI-4.2,1.1;P=3)或在24小时内处于术后阿片类药物消耗的前四分位数的可能性(调整后差异4.2%;95%CI-4.8%,13%;P=4)。我们认为加巴喷丁收到的混杂因素没有重要差异,这表明因果结论是合理的。
    我们的置信区间不包括加巴喷丁的临床意义益处,当与ERAS协议一起使用时,在住院时间或围手术期阿片类药物使用方面。这些结果支持从ERAS方案中省略加巴喷丁用于微创泌尿肿瘤手术。
    UNASSIGNED: Gabapentin has been used in enhanced recovery after surgery (ERAS) pathways for pain control for patients undergoing ambulatory uro-oncologic surgery; however, it may cause undesirable side effects. We studied the causal association between gabapentin and rapidity of recovery and perioperative pain management after minimally invasive uro-oncologic surgery.
    UNASSIGNED: We identified 2397 patients ≤ 65 years undergoing prostatectomies or nephrectomies between 2018 and 2022; 131 (5.5%) did not receive gabapentin. We tested the effect of gabapentin use on time of discharge and perioperative opioid consumption, respectively, using multivariable linear regression adjusting for potential confounders including age, gender, BMI, American Society of Anesthesiologists score, and surgery type.
    UNASSIGNED: On adjusted analysis, we found no evidence of a difference in discharge time among those who did vs did not receive gabapentin (adjusted difference 0.07 hours shorter on gabapentin; 95% CI -0.17, 0.31; P = .6). There was no evidence of a difference in intraoperative opioid consumption by gabapentin receipt (adjusted difference -1.5 morphine milligram equivalents; 95% CI -4.2, 1.1; P = .3) or probability of being in the top quartile of postoperative opioid consumption within 24 hours (adjusted difference 4.2%; 95% CI -4.8%, 13%; P = .4). We saw no important differences in confounders by gabapentin receipt suggesting causal conclusions are justified.
    UNASSIGNED: Our confidence intervals did not include clinically meaningful benefits from gabapentin, when used with an ERAS protocol, in terms of length of stay or perioperative opioid use. These results support the omission of gabapentin from ERAS protocols for minimally invasive uro-oncologic surgeries.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    目的:观察背根神经节脉冲射频联合臭氧注射治疗中老年急性带状疱疹神经痛的疗效和安全性。
    方法:将164例中老年急性带状疱疹患者随机分为2组:脉冲射频联合臭氧注射组(A组)和脉冲射频组(B组)。使用数字评定量表(NRS)评分和加巴喷丁的平均剂量(mg/天)评估术前和1天的治疗效果,2周,4周,12周,术后24周。记录两组有临床意义的带状疱疹后遗神经痛(PHN)的发生率和并发症。
    结果:数据显示,与基线值相比,两组治疗后的NRS评分和加巴喷丁剂量均显着降低。与B组相比,A组术后NRS评分和加巴喷丁剂量明显低于B组,4、12、24周PHN发生率明显低于B组。
    结论:背根神经节臭氧注射联合脉冲射频治疗对中老年人急性带状疱疹神经痛的治疗效果更好。它为患者提供更持久的疼痛缓解,减少PHN的发生率和药物剂量,与PRF治疗相比,生活质量有所提高。
    OBJECTIVE: To investigate the efficacy and safety of pulsed radiofrequency of the dorsal root ganglion combined with ozone injection for treating acute herpes zoster (HZ) neuralgia in middle-aged and elderly adults.
    METHODS: A total of 164 middle-aged and elderly patients with acute HZ were randomly assigned to 2 groups: the pulsed radiofrequency combined with ozone injection group (group A) and the pulsed radiofrequency group (group B). The therapeutic effects were evaluated using Numeric Rating Scale (NRS) scores and the average doses of gabapentin (mg/d) preoperatively and 1 day, 2 weeks, 4 weeks, 12 weeks, and 24 weeks postoperatively. The incidence of clinically significant postherpetic neuralgia (PHN) and complications in the 2 groups were recorded.
    RESULTS: The data showed that the NRS scores and the doses of gabapentin after treatment were significantly lower when compared with the baseline values in both groups. Compared with group B, the NRS scores and the doses of postoperative gabapentin were significantly lower in group A. The incidence of PHN was significantly lower at weeks 4, 12, and 24 in group A than in group B. No adverse reactions occurred in either of the 2 groups post-treatment.
    CONCLUSIONS: The results indicated that ozone injection in the dorsal root ganglion combined with pulsed radiofrequency therapy was more effective in treating acute HZ neuralgia in middle-aged and elderly adults. It provides patients with longer-lasting pain relief, decreased incidence of PHN and the doses of medication, and improved quality of life than with Pulsed Radiofrequency treatment.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    神经性疼痛在很大程度上影响患者的健康。抗惊厥药和抗抑郁药,比如普瑞巴林,加巴喷丁,和阿米替林,通常被规定为神经性疼痛的初始治疗。研究样本共有270名符合纳入标准的患者,并进一步分为三个大小相等的组(A,B,andC).A组给予加巴喷丁300mg,B组用普瑞巴林75毫克,和阿米替林10mg给C组。使用ADR报告表记录任何药物不良反应的发生,而患者用药后的疼痛使用数字疼痛评定量表(NPRS)记录。在基线和15天后,通过使用ANOVA检验对所有三组的NPRS评分进行比较,发现三组之间的差异在统计学上无统计学意义(p>0.089)。然而,连续使用一个月后,差异变得略微显著(即,p=0.003)。加巴喷丁,普瑞巴林,和阿米替林在缓解神经性(NeP)疼痛方面表现出相似的效果。该研究得出结论,加巴喷丁优于普瑞巴林和阿米替林,不良反应较少,改善患者长期使用的依从性。
    Neuropathic pain largely influences the well-being of patients. Anticonvulsant and antidepressant medications, such as Pregabalin, Gabapentin, and Amitriptyline, are routinely prescribed as initial treatments for neuropathic pain. The study sample has a total of 270 patients who meet the inclusion criteria and are further distributed into three equally sized groups (A, B, and C). Group A was administered with Gabapentine 300mg, Group B with Pregabalin 75 mg, and Amitriptyline 10 mg to Group C. The occurrence of any adverse drug response was documented using the ADR reporting form, while the pain of the patient\'s post-medication was recorded using a numerical pain rating scale (NPRS). The comparison of the NPRS scores of all three groups \"by using ANOVA test\" both at baseline and after 15 days reveal that the differences between the three groups are statistically insignificant (p > 0.089). However, after one month of continuous use, the difference becomes slightly significant (I.e., p = 0.003). Gabapentin, pregabalin, and amitriptyline demonstrate similar effectiveness in alleviating neuropathic (NeP) pain. The study concludes that gabapentin is superior to both pregabalin and amitriptyline with fewer adverse effects, leading to improved patient adherence for long-term use.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    背景:甲基汞(MeHg),水生病的病原体,损害颅神经系统并引起特定的感觉障碍,尤其是感觉减退,在四肢。然而,最近的报道表明,慢性水晶病患者相反会在下肢发生神经性疼痛。对我们建立的水晶病模型大鼠的研究表明,MeHg介导的神经变性可能会随着时间的推移,通过脊髓背角的小胶质细胞激活,诱导体感皮层中神经元激活的重新布线,从而引起神经性疼痛。
    方法:在本研究中,加巴喷丁的作用,一种治疗神经性疼痛的潜在有效方法,使用该水晶病模型大鼠进行评价。为了进一步阐明其药效机制,对水峰病模型大鼠的神经系统进行了组织化学和生化分析。
    结果:加巴喷丁治疗恢复了由甲基汞暴露引起的大鼠疼痛阈值的降低。组织化学和生化分析表明,加巴喷丁对MeHg引起的整个神经系统的神经变性和脊髓背角的小胶质细胞活化没有影响。然而,研究表明,加巴喷丁可以通过其对体感皮层钙通道α2-δ-1亚基的拮抗作用来减少过度的突触发生。
    结论:这些结果表明加巴喷丁可以减轻甲基汞中毒的神经性疼痛,以水生病为代表,通过可逆地调节体感皮层的突触重新布线。
    BACKGROUND: Methylmercury (MeHg), the causative agent of Minamata disease, damages the cranial nervous system and causes specific sensory disturbances, especially hypoesthesia, in the extremities. However, recent reports demonstrate that patients with chronic Minamata disease conversely develop neuropathic pain in the lower extremities. Studies on our established Minamata disease model rats showed that MeHg-mediated neurodegeneration might induce neuropathic pain by over time through inducing rewiring with neuronal activation in the somatosensory cortex via microglial activation in the spinal dorsal horn.
    METHODS: In this study, the effects of gabapentin, a potentially effective treatment for neuropathic pain, was evaluated using this Minamata disease model rats. To further elucidate the mechanism of its medicinal effects, histochemical and biochemical analyses of the nervous system of Minamata disease model rats were conducted.
    RESULTS: Gabapentin treatment restored the reduction in the pain threshold caused by MeHg exposure in rats. Histochemical and biochemical analyses revealed that gabapentin showed no effect on MeHg-induced neurodegeneration in entire nervous system and microglial activation in the spinal dorsal horn. However, it was shown that gabapentin may reduce excessive synaptogenesis through its antagonist action on the alpha2-delta-1 subunit of calcium channels in the somatosensory cortex.
    CONCLUSIONS: These results indicate that gabapentin may alleviated neuropathic pain in MeHg poisoning, as typified by Minamata disease, by reversibly modulation synaptic rewiring in the somatosensory cortex.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    睡眠剥夺是危重病人普遍存在的问题,导致恢复延迟和谵妄。慢波睡眠(SWS)对能量恢复至关重要,组织修复,和免疫系统的加强。本研究旨在探讨加巴喷丁对危重患者SWS的影响。我们进行了一项前瞻性开放标签随机对照研究,以比较SWS和加巴喷丁与对照干预在24小时内入住重症监护病房(ICU)的危重成人患者的临床结果。记录患者的特征和睡眠相关结果。与睡眠相关的结果,即,双谱分析(BIS),理查兹-坎贝尔睡眠问卷(RCSQ),和胰岛素样生长因子-1(IGF-1)水平,进行了评估。此外,评估了临床结局和安全性.348例患者中的60例符合随机化条件。在研究的第三天,加巴喷丁组患者的SWS显着增加(66.79vs.0.00分钟;p<0.001),总睡眠时间(TST)(331.39vs.46.16分钟;p=0.001),RCSQ得分(55.05±20.18vs.32.80±15.31;p<0.001),和IGF-1浓度(84.33±12.40vs.44.00±10.20ng/mL,p<0.001)与对照组相比。临床结果的改善,比如谵妄,无ICU天数,和无机械呼吸机的日子,被观察到;然而,这些差异没有达到统计学意义.加巴喷丁在睡前增加了SWS,TST,重症患者的IGF-1浓度。该方案可能有利于改善危重病人的睡眠质量。
    Sleep deprivation is a prevalent problem in critically ill patients, which leads to delayed recovery and delirium. Slow-wave sleep (SWS) is essential to energy restoration, tissue repair, and immune system strengthening. This study aimed to investigate the effects of gabapentin on SWS in critically ill patients. We performed a prospective open-label randomized controlled study to compare SWS and the clinical outcomes of gabapentin versus a control intervention in critically ill adult patients admitted to the intensive care unit (ICU) within 24 h. The patients\' characteristics and sleep-related outcomes were recorded. The sleep-related outcomes, namely, bispectral analysis (BIS), the Richards-Campbell Sleep Questionnaire (RCSQ), and insulin-like growth factor-1 (IGF-1) levels, were evaluated. Furthermore, clinical outcomes and safety were assessed. Sixty patients from 348 cases were eligible for randomization. On day 3 of the study, patients in the gabapentin group had significantly increased SWS (66.79 vs. 0.00 min; p < 0.001), total sleep time (TST) (331.39 vs. 46.16 min; p = 0.001), RCSQ score (55.05 ± 20.18 vs. 32.80 ± 15.31; p < 0.001), and IGF-1 concentrations (84.33 ± 12.40 vs. 44.00 ± 10.20 ng/mL, p < 0.001) compared with the control group. Improvements in clinical outcomes, such as delirium, ICU-free days, and mechanical ventilator-free days, were observed; however, these differences did not reach statistically significant. Gabapentin at bedtime increased SWS, TST, and IGF-1 concentrations in critically ill patients. This regimen might be beneficial to critically ill patients for improving their sleep quality.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    “设计质量”(QbD)是一种新颖的产品开发方法,涉及了解产品和工艺,以及关键质量属性(CQA)和关键工艺参数(CPP)之间的关系。本研究旨在使用QbD方法优化加巴喷丁负载的固体脂质纳米颗粒制剂(GP-SLN),并评估体外和离体性能。
    GP-SLN制剂使用微乳液方法通过组合Gelucire48/16、Tween80和PluroolOleiqueCC497来产生。采用Box-Behnken实验设计研究了独立因素对依赖因素的影响。GP-SLN配方基于粒度和分布进行评估,zeta电位,形态学,截留效率,释放动力学,渗透参数,稳定性,和鼻毒性。
    纳米颗粒具有立方体形状,粒径为185.3±45.6nm,zeta电位为-24±3.53mV,包封率为82.57±4.02%。GP-SLN的粒径和ζ电位在3个月内保持一致,并遵循Weibull动力学,其离体渗透性明显高于加巴喷丁溶液(GP-SOL)(1.7倍)。组织病理学研究表明,鼻内施用GP-SLN制剂没有有害作用。
    当前研究报告了使用QbD成功开发GP-SLN制剂。实现了GP的持续释放并增加了其鼻渗透性。具有最佳粒径和高包封效率的固体脂质纳米颗粒可能为药物的鼻内递送提供有希望的方法。
    UNASSIGNED: \"Quality by Design\" (QbD) is a novel approach to product development that involves understanding the product and process, as well as the relationship between critical quality attributes (CQA) and critical process parameters (CPP). This study aimed to optimize the gabapentin-loaded solid lipid nanoparticle formulation (GP-SLN) using a QbD approach and evaluate in vitro and ex vivo performance.
    UNASSIGNED: The GP-SLN formulation was created using the microemulsion method by combining Gelucire 48/16, Tween 80, and Plurol Oleique CC 497. The Box-Behnken experimental design was adopted to investigate the effects of independent factors on dependent factors. The GP-SLN formulation was assessed based on particle size and distribution, zeta potential, morphology, entrapment efficiency, release kinetics, permeation parameters, stability, and nasal toxicity.
    UNASSIGNED: The nanoparticles had a cubical shape with a particle size of 185.3±45.6 nm, a zeta potential of -24±3.53 mV, and an entrapment efficiency of 82.57±4.02%. The particle size and zeta potential of the GP-SLNs remained consistent for 3 months and followed Weibull kinetics with a significantly higher ex vivo permeability (1.7 fold) than a gabapentin solution (GP-SOL). Histopathology studies showed that intranasal administration of the GP-SLN formulation had no harmful effects.
    UNASSIGNED: The current study reports the successful development of a GP-SLN formulation using QbD. A sustained release of GP was achieved and its nasal permeability was increased. Solid lipid nanoparticles with optimum particle size and high entrapment efficiency may offer a promising approach for the intranasal delivery of drugs.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

  • 文章类型: Journal Article
    加巴喷丁(GBP)最初被开发为γ-氨基丁酸(GABA)受体的潜在激动剂,旨在抑制疼痛信号神经元的激活。与最初的期望相反,它不与GABA受体结合。相反,它表现出几种不同的药理活性,包括:(1)与中枢神经系统电压门控钙通道的α-2-δ蛋白亚基结合,从而阻断钙的兴奋性流入;(2)通过调节ERK1/2磷酸化降低CaMKII的表达和磷酸化;(3)抑制谷氨酸的释放并干扰NMDA受体的活化;(4)增强GABA的合成;(5)增加细胞表面δGABA_A受体的表达,有助于其抗伤害性,抗惊厥药,和抗焦虑作用.此外,GBP显示(6)抑制NF-kB激活和随后的炎性细胞因子的产生,和(7)刺激嘌呤能腺苷A1受体,支持其抗炎和伤口愈合特性。最初被批准用于治疗癫痫发作和带状疱疹后神经痛,英镑现在广泛用于各种条件,包括精神疾病,急性和慢性神经性疼痛,和睡眠障碍。最近,作为眼药水配方,它也被探索作为眼表不适的治疗选择,如干眼,神经营养性角膜炎,角膜溃疡,和神经性眼痛。这篇综述旨在总结支持GBP分子效应的证据,特别强调其在眼表疾病中的应用。
    Gabapentin (GBP) was originally developed as a potential agonist for Gamma-Amino-Butyric-Acid (GABA) receptors, aiming to inhibit the activation of pain-signaling neurons. Contrary to initial expectations, it does not bind to GABA receptors. Instead, it exhibits several distinct pharmacological activities, including: (1) binding to the alpha-2-delta protein subunit of voltage-gated calcium channels in the central nervous system, thereby blocking the excitatory influx of calcium; (2) reducing the expression and phosphorylation of CaMKII via modulation of ERK1/2 phosphorylation; (3) inhibiting glutamate release and interfering with the activation of NMDA receptors; (4) enhancing GABA synthesis; (5) increasing cell-surface expression of δGABA_A receptors, contributing to its antinociceptive, anticonvulsant, and anxiolytic-like effects. Additionally, GBP displays (6) inhibition of NF-kB activation and subsequent production of inflammatory cytokines, and (7) stimulation of the purinergic adenosine A1 receptor, which supports its anti-inflammatory and wound-healing properties. Initially approved for treating seizures and postherpetic neuralgia, GBP is now broadly used for various conditions, including psychiatric disorders, acute and chronic neuropathic pain, and sleep disturbances. Recently, as an eye drop formulation, it has also been explored as a therapeutic option for ocular surface discomfort in conditions such as dry eye, neurotrophic keratitis, corneal ulcers, and neuropathic ocular pain. This review aims to summarize the evidence supporting the molecular effects of GBP, with a special emphasis on its applications in ocular surface diseases.
    导出

    更多引用

    收藏

    翻译标题摘要

    我要上传

       PDF(Pubmed)

公众号