Quantification of active ingredients in suppositories by FT‐Raman spectroscopy

An efficient method for the quantitative determination of acetaminophen (AAP) and diclofenac sodium (DS) in commercial suppositories based on partial least squares (PLS) treatment of FT‐Raman spectra is described. The relative standard errors of prediction (RSEP) were calculated for calibration and validation data sets to evaluate the quality of the constructed models. In the case of DS determination, RSEP error values of 1.9 % and 2.3 % for the calibration and validation data sets, respectively, were found. For AAP these errors amounted to 1.6–2.3 % and 1.8–2.8 %, respectively, for the different calibration models. Four commercial preparations containing 5, 12.5, 16.7 and 33.3 % (w/w) AAP and one containing 5 % (w/w) DS were successfully quantified using the developed models. Concentrations derived from the developed models correlated strongly with the declared values and yielded recoveries of 99.4–100.2 % and 99.6 % for AAP and DS, respectively. The proposed procedure can be used as a fast, economic and reliable method for quantification of the active pharmaceutical ingredients in suppositories. Copyright © 2012 John Wiley & Sons, Ltd.     

Natural remedies for non‐steroidal anti‐inflammatory drug‐induced toxicity

The liver is an important organ of the body, which has a vital role in metabolic functions. The non‐steroidal anti‐inflammatory drug (NSAID), diclofenac causes hepato‐renal toxicity and gastric ulcers. NSAIDs are noted to be an agent for the toxicity of body organs. This review has elaborated various scientific perspectives of the toxicity caused by diclofenac and its mechanistic action in affecting the vital organ. This review suggests natural products are better remedies than current clinical drugs against the toxicity caused by NSAIDs. Natural products are known for their minimal side effects, low cost and availability. On the other hand, synthetic drugs pose the danger of adverse effects if used frequently or over a long period. Copyright © 2016 John Wiley & Sons, Ltd.     

双氯芬酸二乙胺凝胶外擦减轻静脉化疗局部疼痛的临床观察

目的观察双氯芬酸二乙胺凝胶减轻静脉化疗局部疼痛的效果。方法选择采用吉西他滨和顺铂联合化疗方案的患者，按单双日静脉化疗分别进行疼痛观察。患者均在相同条件下输入化疗药物。单日输注为观察组，穿刺固定后，在穿刺以上，沿静脉走向长15cm，宽7cm的皮肤，均匀涂擦双氯芬酸二乙胺凝胶并轻轻按摩，在化疗药物的输注过程中每4h涂擦1次，输液结束时再涂擦一次；双日输注为对照组，按常规操作，不使用双氯芬酸二乙胺凝胶涂擦，比较两组患者疼痛程度。结果观察组患者疼痛程度明显较对照组患者轻，差异有极显著意义（x2=122．83，P〈0．01）。结论双氯芬酸二乙胺凝胶局部涂擦能减轻静脉化疗疼痛程度，该方法简单、方便、安全、适用，可在临床推广使用。     

双氯芬酸钠致不良反应的文献分析

目的探讨双氯芬酸钠致药品不良反应（ADR）的一般规律和特点。方法检索《中国期刊全文数据库》（CNKI）1994—2008年双氯芬酸钠所致ADR文献，进行统计、分析。结果ADR涉及泌尿系统、消化系统、血液系统、皮肤及附件、神经系统及其他，在高年龄段发生率较高。结论临床上应重视双氯芬酸钠所致ADR，坚持合理用药。     

荷移光谱法测定双氯芬酸钠含量

目的:建立荷移光谱法测定双氯芬酸钠(DS)的含量。方法:分别以7,7,8,8-四氰基对二次甲基苯醌(TCNQ)在丙酮介质中和氯冉酸(CL)在乙醇介质中为荷移试剂,在350～900nm 波长处扫描吸收光谱。结果:DS 与 TCNQ 形成的络合物在743nm 和842nm 有2个吸收峰,表观摩尔吸光系数分别是2.10×10~4L·mol~(-1)·cm~(-1)和3.07×10~4L·mol~(-1)·cm~(-1);与 CL形成的络合物在530nm 处有吸收峰,表观摩尔吸光系数8.77×10~2L·mol~(-1)·cm~(-1)。药物浓度分别在3～50mg·L~(-1)(TCNQ法)和15～750mg·L~(-1)(CL 法)范围内服从比尔定律,平均回收率分别为97.8%和98.6%,RSD 分别为1.4%,1.0%(n=6)。用摩尔比法和等摩尔连续变化法测得荷移络合物中 DS 与配体的摩尔比均为1:1。结论:本方法操作简便,结果准确可靠,适用于测定 DS 片中的含量。     

双氯芬酸钠泊洛沙姆凝胶体外释放的影响因素研究

目的:以双氯芬酸钠为模型药,研究泊洛沙姆407(P407)制剂体外释放的影响因素。方法:采用无膜释放法考察不同P407浓度、振荡频率、温度、等渗调节剂、附加剂等对凝胶溶蚀和药物释放的影响。结果:随振荡频率的增加及等渗调节剂PBS,NaC l或葡萄糖的添加,凝胶溶蚀和药物释放增加;P407浓度增加及处方中加入羟甲基纤维素钠(CMC-Na)、羟丙甲纤维素(HPMC)、甲基纤维素(MC)、羧甲基壳聚糖(O-CMC)等抑制了凝胶溶蚀和药物释放;温度升高药物释放加快而对凝胶溶蚀没有明显影响。结论:药物释放主要取决于凝胶溶蚀,可通过调节处方中影响凝胶溶蚀及药物扩散的因素来控制药物从407凝胶中的释放。     

Analgesia for shock wave lithotripsy

PURPOSE: We evaluated the effectiveness of and patient preference for analgesia used during shock wave lithotripsy by comparing diclofenac alone with a combination of diclofenac and patient controlled analgesia, that is alfentanil. MATERIALS AND METHODS: A total of 64 patients were treated using a Lithotriptor S (Dornier Medical Systems, Marietta, Georgia) and randomized to receive diclofenac alone or combined with an alfentanil patient controlled analgesia pump. If treated twice, they crossed over to the alternative form of analgesia. A record was maintained of the site and size of the stone, maximum power achieved, number of shocks, amount of alfentanil used and need for additional analgesia. After treatment patients scored on a visual analog scale the maximum level of pain and satisfaction with analgesia. RESULTS: There was no difference in the mean size of the stone treated (8.6 and 7.5 mm.), energy level (71% and 71% or approximately 17 kV.) or number of shocks (3,000 and 2,900, respectively) in the groups. Only 2 patients in the diclofenac group required additional analgesia and there were no significant side effects from either treatment. The mean pain scores were not significantly different in the diclofenac and patient controlled analgesia groups (3.54 and 2.93, respectively, (p = 0.34), although those on patient controlled analgesia were more satisfied (7.72 versus 9.14, p = 0.04). Of the 38 patients who presented twice 58% preferred diclofenac alone. CONCLUSIONS: This study suggests that there is no significant difference in the level of pain experienced with diclofenac alone or when combined with an alfentanil patient controlled analgesia pump during shock wave lithotripsy. However, patients are more satisfied with treatment when a patient controlled analgesia pump is available.     

Preemptive diclofenac reduces morphine use after remifentanil-based anaesthesia for tonsillectomy

BACKGROUND: We investigated the effect of preincisional rectal diclofenac on pain scores and postoperative morphine requirements of children undergoing tonsillectomy after remifentanil-propofol anaesthesia in a randomized clinical trial. METHODS: Induction and maintenance of anaesthesia were with remifentanil and propofol. Forty children were randomly assigned into two groups before incision. The diclofenac group (n=20) received diclofenac suppositories (approximately 1 mg x kg(-1)) and the control group (n=20) received no treatment. Following discontinuation of remifentanil, patient-controlled analgesia (PCA) with morphine (a loading dose 50 micro g x kg(-1), a background infusion 4 micro g x kg(-1) x h(-1) and a demand dose 20 micro g x kg(-1) with 5-min intervals) was started. We assessed pain score [verbal analogue scales (VAS), 0-10] and sedation level at 5-min intervals and recorded the total morphine consumption of the first hour in the PACU. Patients were discharged to the ward with a new PCA morphine programme (a demand dose 20 micro g.kg-1 with a lockout time of 30 min, for 4 h), and total morphine consumption was recorded. RESULTS: The mean VAS score of the diclofenac group was significantly lower than the control group on arrival in the PACU (2.85 +/- 0.77, 7.60 +/- 0.83, respectively, P < 0.01) and it remained significantly lower in the PACU stay of the children. The mean total morphine consumption of the diclofenac group was less than the control group in the PACU (130.33 +/- 11.26 and 169.92 +/- 9.22, respectively, P=0.012) and the ward (50.80 +/- 11.38 and 87.77 +/- 10.55, respectively, P=0.021). CONCLUSIONS: Preemptive diclofenac given rectally reduced pain intensity and morphine requirements of children anaesthetized with remifentanil for tonsillectomy.     

Effect of diclofenac on cerebral blood flow velocity in patients with supratentorial tumours

Background. The aim of this investigation was to determine theeffects of diclofenac on cerebral blood flow. Middle cerebralartery blood flow velocity was measured in nine patients withsupratentorial tumours. Methods. Using a transcranial Doppler ultrasound, we measuredthe baseline mean and systolic cerebral blood flow velocity.Measurements were repeated following administration of diclofenac75 mg i.v. Results. There was no significant change in cerebral blood flowvelocity. All other physiological variables remained constant. Conclusion. Diclofenac does not cause a significant change incerebral blood flow velocity in patients with supratentorialtumours. Br J Anaesth 2002; 89: 762–4     

双氯芬酸钠含片的药效学及黏膜刺激性

目的研究双氯芬酸钠低剂量低浓度局部应用的抗炎镇痛作用及黏膜刺激作用。方法观察双氯芬酸钠低剂量低浓度腹腔给药对醋酸致小鼠扭体作用及毛细血管通透性增加的影响，局部给药对大鼠棉球肉芽形成的影响，局部长时间接触对的刺激作用。结果双氯芬酸钠低剂量低浓度给药可明显抑制醋酸致小鼠扭体反应，减轻醋酸致毛细血管通透性的增加，抑制棉球肉芽肿的形成，对黏膜无明显刺激作用。结论双氯芬酸钠低剂量低浓度局部应用具有较强的抗炎镇痛效应，无明显黏膜刺激作用。口含片用于口腔小手术后抗炎镇痛将既可保证具有较好的疗效，又能降低传统给药剂量时出现的不良反应。