Ketorolac tromethamine floating beads for oral application: Characterization and in vitro/in vivo evaluation

The floating beads have been employed to make a sustained release of the drug in the stomach and to decrease the dose of the drug and hence overcome its side effects. The common benefits of the floating beads were it is easy preparation, without the need of a high temperature, and high percentage of the drug entrapment. In the present work, the Ketorolac tromethamine (KT) floating beads were prepared by extrusion congealing method utilizing calcium carbonate as a gas forming agent. The physical characters of the produced beads were investigated such as KT yield, KT loading, and entrapment efficiency of the drug. In addition, floating behavior, swelling, particle size, morphology and KT stability were also evaluated. In vitro drug release study was carried out, and the kinetics of the release was evaluated using the linear regression method. Furthermore, the in vivo analgesic effect of KT after oral administration of the selected formula of floating beads (F10) was carried out using hot plate and tail flick methods. Oral commercial KT tablets and KT solution were used for the comparison. The prepared beads remained floated for more than 8 h. The optimized formulation (F10) exhibited prolonged drug release (more than 8 h) and the drug release follows the Higuchi kinetic model, with a Fickian diffusion mechanism according to Korsmeyer-Peppas (n = 0.466). Moreover, F10 showed a sustained analgesic effect as compared to the commercial tablet.     

酮咯酸氨丁三醇联合吗啡用于老年人术后自控镇痛的临床研究

目的观察酮咯酸氨丁三醇联合吗啡用于老年人术后自控镇痛的疗效及不良反应。方法选择前列腺激光手术男性老年患者72例,随机分为A、B 2组,A组术后静脉维持使用酮咯酸氨丁三醇;B组术后静脉维持使用芬太尼。结果 2组病人镇痛效果(VAS评分)、镇静程度(Ramesay评分)、脉搏氧饱和度、心率和血压组间比较无差异。结论低剂量静脉酮咯酸氨丁三醇和硬膜外吗啡联合镇痛用于老年人可以显著降低阿片类药物不良反应发生率,对合并基础疾病的老年人而言该术后镇痛方式疗效确切且具有很高的安全性。     

酮咯酸氨丁三醇联合曲马多用于下肢骨科手术后静脉自控镇痛的临床研究

目的观察联合酮咯酸氨丁三醇和曲马多用于下肢骨科手术后患者静脉自控镇痛的疗效。方法选择80例ASA(Ⅰ～Ⅱ)级择期在椎管内麻醉行下肢骨科手术的患者,随机分为2组:PCIA:曲马多组(A组)40例;曲马多复合酮咯酸氨丁三醇组(B组)40例。观察术后24h内(6h、12h、18h、24h)VAS评分、PCA按压次数、不良反应情况。结果术后6h、12hB组VAS评分低于A组,2组患者恶心、呕吐、头晕、头痛等不良反应无明显差异,PCA按压次数减少。结论酮咯酸氨丁三醇联合曲马多用于术后镇痛,可增强单用曲马多的镇痛效果,并且减少其用量,静脉自控镇痛效果好,而并不增加恶心、呕吐、头晕、头痛等不良反应发生率。     

关节腔内注射酮咯酸氨丁三醇用于老年患者膝关节镜术后镇痛

目的 观察关节腔内注射酮咯酸氨丁三醇或吗啡复合罗哌卡因对老年患者膝关节镜术后的镇痛效果.方法 48例腰一硬联合阻滞下行膝关节镜手术的老年患者,随机均分为关节腔内注射吗啡复合罗哌卡因组(RM组)、酮咯酸氨丁三醇复合罗哌卡因组(RK组)和生理盐水对照组(C组),记录术后2、4、8、12、24和48 h患者屈膝关节90°状态下的VAS评分、镇痛满意度及术后8 h内按需注射曲马多用量.结果 术后2、4、8、12、24和48 h患者屈膝90°VAS评分RM、RK组均显著低于C组(P<0.01);术后镇痛满意度RM、RK组较C组高,而RK组高于RM组(P<0.05);RM、RK组术后8 h曲马多平均使用量较C组明显减少(P<0.05).结论 关节腔内注射酮咯酸氨丁三醇复合罗哌卡因可有效缓解老年患者膝关节镜术后疼痛,患者满意程度优于吗啡复合罗哌卡因.     

Rapid regression of duodenal inflammatory myofibroblastic tumor after intravenous ketorolac: case report and review of the literature

Inflammatory myofibroblastic tumors are known to sometimes regress spontaneously or in response to treatment with antiinflammatory drugs. We present the case of a 13-year-old boy with an inflammatory myofibroblastic tumor of the proximal duodenum, which regressed rapidly within days of an open surgical biopsy, resulting in perforation of the duodenum. Ketorolac was administered intravenously after the biopsy and is implicated as a potential cause of the rapid regression of the tumor. We discuss the surgical management of this patient and present a review of the literature.     

Ketorolac Tromethamine and Hemorrhage in Tonsillectomy: A Prospective,Randomized, Double-Blind Study

Ketorolac tromethamine (KT) is a nonsteroidal, antiinflammatory analgesic. Its nonsedating property makes it an attractive analgesic for sleep apnea patients undergoing uvulopharyngopalatoplasty, but its antiplatelet activity makes the potential for postoperative hemorrhage a concern. A prospective, randomized, double-blind study was designed to evaluate the bleeding risk of KT using adult tonsillectomy patients as the model. Patients were randomized into two groups receiving Meperidine (MP) (controls) or KT for the first post-operative day. Posttonsillectomy bleeding rates of 7% (3/43) in the MP group and 18.9% (7/37) in the KT group were demonstrated, but this difference was not statistically significant. The number of KT doses administered had no effect on the incidence of bleeding or the number of cases requiring return to the operative suite for hemostasis. Although this study did not attain statistical significance, the trend towards increased hemorrhage with KT is worrisome. This study and other reports in the literature support the manufacturer's warning that the use of KT is contraindicated in major surgery.     

HPLC同时测定复方盐酸莫西沙星酮咯酸氨丁三醇滴眼液的含量

摘 要 目的： 建立复方盐酸莫西沙星酮咯酸氨丁三醇滴眼液中药物含量测定的HPLC方法。方法: 采用菲罗门C₁₈色谱柱(250 mm×4.6 mm, 5 μm),以25 mmol·L^-1磷酸二氢钾溶液（磷酸调pH至3.2,0.5%三乙胺） 甲醇（40∶60, v/v）为流动相,流速:1.0 ml·min^-1,检测波长:308 nm,柱温:30℃,进样量:20 μl。结果: 盐酸莫西沙星和酮咯酸(r=0.999 9)氨丁三醇可达到较好分离,盐酸莫西沙星质量浓度在1.0～20.0 mg·L^-1内（r=0.999 9）,酮咯酸氨丁三醇质量浓度在1.0～20.0 mg·L^-1内与峰面积呈良好的线性关系,平均回收率分别为99.9%(RSD=0.81%,n=9)、100.1%(RSD=0.76%, n=9)。结论: 本方法简便、快速、准确,重复性好,可用于复方盐酸莫西沙星酮咯酸氨丁三醇滴眼液中药物含量测定。     

酮咯酸联合解痉药物治疗急性结石性肾绞痛的疗效评估

目的 评估酮咯酸联合解痉药物在急性结石性肾绞痛治疗中的作用.方法 对403例急性结石性肾绞痛患者肌注酮咯酸氨丁三醇及654-2,并静脉滴注诺仕帕,补液500～1000 ml.应用视觉模拟评分法分别评估治疗前后疼痛程度,记录副反应及初次治疗后72 h内疼痛复发的情况.结果 352例(87.3%)显效,27例(6.7%)部分显效,24例(6.0%)无效.8例(2.0%)出现轻微中枢神经系统症状,10例(2.5%)出现轻微胃肠道症状,13例(3.2%)出现轻微迷走神经抑制症状.12例(3.0%)于离院72 h内疼痛再发.结论 酮咯酸联合解痉药物并适当补液,疗效好,副反应少,镇痛效果持久,是治疗急性结石性肾绞痛的有效选择.     

Use of ketorolac is associated with decreased pneumonia following rib fractures

Background

The effectiveness of the nonsteroidal anti-inflammatory drug ketorolac in reducing pulmonary morbidity after rib fractures remains largely unknown.

Methods

A retrospective cohort study was conducted spanning January 2003 to June 2011 assessing pneumonia within 30 days and potential adverse effects of ketorolac among all patients with rib fractures who received ketorolac <4 days after injury compared with a random sample of those who did not.

Results

Among 202 patients who received ketorolac and 417 who did not, ketorolac use was associated with decreased pneumonia (odds ratio, .14; 95% confidence interval, .04 to .46) and increased ventilator-free days (difference, 1.8 days; 95% confidence interval, 1.1 to 2.5) and intensive care unit–free days (difference, 2.1 days; 95% confidence interval, 1.3 to 3.0) within 30 days. The rates of acute kidney injury, gastrointestinal hemorrhage, and fracture nonunion were not different.

Conclusions

Early administration of ketorolac to patients with rib fractures is associated with a decreased likelihood of pneumonia, without apparent risks.     

Comparative analgesic efficacy and tolerability of ketorolac tromethamine and glafenine in patients with post-operative pain

Summary

In a randomized, single-dose, double-blind, parallel comparative trial of analgesic efficacy, 96 adult patients received either 10?mg ketorolac tromethamine or 400?mg glafenine orally the morning after surgery if they requested pain relief medication. Each patient provided a baseline pain assessment and then received the assigned medication. Patients assessed pain intensity and pain relief and reported any adverse events in interviews held 30 minutes after drug administration and then hourly for 6 hours. The demographic characteristics, baseline pain intensity, and surgical categories of the 47 patients who received ketorolac tromethamine and the 49 who received glafenine were similar. Both drugs provided prompt, sustained pain relief throughout the 6-hour observation period, and there were no statistically significant differences between the two groups in any of the efficacy measures analyzed. The global assessment recorded by patients suggested a slight clinical advantage for ketorolac tromethamine (32.6% of ‘excellent’ responses) as compared to glafenine (12.5% ‘excellent’). The differences in overall response were statistically significant (p = 0.017). Fourteen (30%) patients who received ketorolac tromethamine and 17 (35%) who received glafenine reported adverse experiences that began or seemed to worsen after administration of the study drugs. The most prominent were drowsiness and sleeping, both of which are common in post-surgical patients.