小儿氨酚黄那敏片中对乙酰氨基酚含量的HPLC测定

目的：建立高效液相色谱（HPLC）法测定小儿氨酚黄那敏片中对乙酰氨基酚含量。方法：采用安捷伦EclipseXDB-C18色谱柱（150mm×4.6mm，5μm），甲醇-水（80∶20）为流动相，流速为0.8ml/min，柱温为30℃，检测波长为249nm。结果：对乙酰氨基酚在0.2005～2.0048μg范围内呈良好线性关系，r=0.9999，平均回收率为99.82%，RSD为0.23%（n=6）。结论：该法稳定、简便，可用于小儿氨酚黄那敏片的质量控制。     

肌注蒙洛英与度冷丁治疗肾绞痛的止痛疗效比较

目的:研究肌注蒙洛英与度冷丁治疗肾绞痛的止痛疗效比较。方法:300名肾绞痛患者随机分成两组,蒙洛英组(n=150),肌注蒙洛英2ml,度冷丁组(n=150),肌注度冷丁100mg,用药后0h,0.5h,1h,6h分别进行止痛疗效比较。结果:随着时间变化,两种药物对肾绞痛都有效,但疗效无显著差异性。结论:蒙洛英与度冷丁对肾绞痛的止痛疗效相当,但蒙洛英更安全、用药方便。     

Acetaminophen/diphenhydramine overdose in profound hypothermia

Background. There are few reports of acetaminophen overdose in hypothermic patients and even fewer reports describing profound hypothermia. The kinetics, risk of hepatotoxicity, and the possible dose adjustments to N-acetylcysteine (NAC) therapy are not known in this setting. Case report. A 37-year-old female was found unconscious outside in December and was brought by ambulance to a tertiary care Emergency Department (ED) following a presumed overdose of acetaminophen and diphenhydramine. She later confirmed the ingestion and reported the ingestion had occurred approximately 18 hours prior to being found. On arrival, she was profoundly hypothermic, with a core rectal temperature of 17°C. Her initial serum acetaminophen concentration was 232 mcg/mL 19 hours post ingestion of a reported dose of approximately 50 grams of acetaminophen and 2.5 grams of diphenhydramine. Active rewarming was started immediately and IV NAC was initiated using the standard treatment protocol. The patient did not develop serious signs of hepatic injury or NAC toxicity. The patient's AST and ALT peaked 12 hours after admission at 84 IU/L (ref 10–37 U/L) and 104 IU/L (ref 12–78 U/L), respectively. Her INR peaked 2 hours after admission at 1.46 (ref < 1.2). Discussion. Despite the significant ingestion of acetaminophen, delayed presentation, prolonged period of decreased responsiveness, and profound hypothermia, the patient did not develop any signs/symptoms of liver injury. NAC was administered in a standard dose during her rewarming period without apparent toxicity. The patient's absorption and/or metabolism of acetaminophen were likely slowed by her hypothermia and possibly by the anticholinergic coingestant. Initiation of IV NAC at a standard dose was apparently safe and effective in preventing hepatotoxicity as the patient was rewarmed. Conclusions. Profound hypothermia may be protective of hepatic injury in acetaminophen overdose. Delayed absorption from the coingestant, diphenhydramine, may also have played a role. IV NAC was given in a standard dose without apparent toxicity in the setting of profound hypothermia. Lastly, IV NAC, in standard dosing, appeared to be effective in preventing hepatotoxicity during rewarming in a patient with a potentially hepatotoxic concentration of acetaminophen with a coingestion of the anticholinergic agent, diphenhydramine.     

贝诺酯片剂的研制及生物利用度研究

通过减小药物粒径,提高贝诺酯片剂的生物利用度。在市售片以A(500mg)基础上研制了新处方片剂B(400mg)。建立贝诺酯片剂体外溶出度试验方法,即以表面活性剂溶液作溶出介质,以浆法进行溶出度测定。用HPLC法测定贝诺酯在体内的水解产物水杨酸和扑热息痛的血药浓度。结果表明药物研磨粉碎前后体外溶出速度常数分别为0.0152min-1及0.0337min^-1(P<0.001)。A及B体外平均溶出时间分别为42.25min及15.77min(P<0.001)。体内研究表明A及B水杨酸的C_max,T_p,AUC之间均无显著性差异(P>0.1)(A,B的服用量分别为4.5g及3.6g),B的相对生物利用度为125.59%。     

The use of sustained low efficiency dialysis (SLED) in massive paracetamol overdose

Context: Massive paracetamol ingestion causing mitochondrial dysfunction is uncommon. Use of sustained low-efficiency dialysis (SLED) to improve acidaemia and enhance paracetamol elimination has not been previously described.

Case details: A 44-year-old male presented to the emergency department 2.5?hours post overdose of 200?g (2.5?g/kg) of paracetamol. Examination revealed a BP 85/60?mmHg, pulse 112 bpm, temperature 33.9?°C and blood glucose of 13.9?mmol/l. Venous blood gas 5.5-hours post-ingestion showed a pH 6.9, pCO₂ 58?mmHg, HCO₃ 13?mmol/l and lactate 14?mmol/l. Fifty-grams of nasogastric activated charcoal and double-strength intravenous acetylcysteine were administered. Paracetamol concentration peaked at 4207 µmol/l six hours post-ingestion. SLED was commenced nine-hours post ingestion and acetylcysteine dose was doubled again during dialysis. Paracetamol extraction ratio was 47–52%. Plasma paracetamol clearance was steady throughout SLED (53–58?ml/min). Hepatotoxicity did not develop and the patient recovered.

Discussions: Intermittent hemodialysis (IHD) is more efficient than SLED or continuous renal replacement therapy for enhancing paracetamol elimination and clearance. IHD plasma clearance is reported to range from 36 to 215?ml/min compared with endogenous clearance of 224?ml/70?kg/min.

Conclusions: SLED improved acidaemia with only moderate overall increase in paracetamol plasma clearance. Lack of development of hepatotoxicity was likely the result of early administration of acetylcysteine rather than any effect of SLED on paracetamol elimination.     

Treatment of fibromyalgia (Fibrositis syndrome): A parallel double blind trial with carisoprodol,paracetamol and caffeïne (Somadril comp®) versus placebo

Summary Forty-three of fifty-eight (74.1%) female patients with fibromyalgia completed an eight-week treatment period testing the combination of carisoprodol, paracetamol (acetaminophen) and caffeine versus placebo. Twenty-three patients received placebo and twenty active medication. In the placebo group 56.5% of the patients used additional analgesics or nonsteroidal anti-inflammatory drugs compared to only 20% in the active treatment group (p=0.015). Forty-three percent of the patients in the placebo group and none of the patients in the active treatment group used tricyclic antidepressants, anxiolytics or sedatives (p=0.0008). Active treatment gave statistically significant improvement after treatment for pain (p<0.01), for sleep quality (p<0.01) and for the general feeling of sickness (p<0.05). In the active treatment group increased pressure pain threshold after eight weeks was found at 70% of the sites measured, while the pressure pain threshold was increased at only 30% of the sites in the placebo group. In the placebo group improvement was found for the pain and sleep quality (p<0.05). This improvement may in part be due to the large amounts of extra medication in this group. Thus, the combination of carisoprodol and paracetamol (acetaminophen) and caffeine are effective in the treatment of fibromyalgia.     

Randomised comparative trial of the efficacy of paracetamol syrup and dispersible tablets for the treatment of fever in children

ObjectiveFever is the most common reason for the presentation of children in the outpatient department. Paracetamol is marketed in different formulations for ease of administration to the paediatric population. These include syrups, dispersible tablets and rectal inserts. Dispersible tablets disintegrate rapidly in liquid and are subsequently taken orally, providing another oral formulation. We determined if there is a difference in the antipyretic efficacy of the syrup and the dispersible formulation of paracetamol, thereby prompting the development of the latter (another oral formulation) for use in children.MethodsA randomised, controlled, double-blind intervention of a single dose of both formulations was given to febrile children, and their temperatures were documented twice in 30-minute intervals. Temperature changes were compared statistically.ResultsThe mean temperatures at recruitment were 38.2 ± 0.5°C and 38.3 ± 0.6°C for the dispersible and syrup group, respectively. There was no significant difference between the temperature changes at T2 (30 minutes) and T3 (60 minutes) between the two study arms. However, the temperature was significantly different at T1 (baseline), T2 and T3 within the dispersible and syrup groups.ConclusionThe decreasing trend in temperature was similar in both groups. Both preparations produced statistically similar antipyretic effects with no reported adverse drug reaction.     

酚氨咖敏颗粒质量标准研究

目的完善酚氨咖敏颗粒的质量标准。方法采用薄层色谱(TLC)法对乙酰氨基酚、氨基比林、咖啡因及马来酸氯苯那敏进行定性鉴别。采用气相色谱(GC)法同时测定4种成分的含量,色谱柱为TR-1弹性石英毛细管柱(30 m×0. 32 mm,0. 25μm),程序升温(起始温度为180℃,保持1 min,再以8℃/min的速率升至240℃,保持2 min),氢火焰离子化检测器温度为260℃。结果 TLC法可同时鉴别酚氨咖敏颗粒中4种成分。对乙酰氨基酚、氨基比林、咖啡因及马来酸氯苯那敏质量浓度线性范围分别为186. 3~5 960μg/m L(r=0. 999 9),124. 9~3 996μg/m L(r=0. 999 9),38. 24~1 224μg/m L(r=1. 000 0)和2. 525~80. 80μg/m L(r=0. 999 9);平均加样回收率分别为98. 69%,99. 45%,99. 52%,101. 40%,RSD分别为1. 36%,1. 62%,1. 20%,1. 25%(n=9)。结论该方法简便快速、准确可靠,适用于酚氨咖敏颗粒中4种成分的定性、定量分析,可更全面地控制该制剂的质量。     

The effect of intravenous paracetamol for the prevention of rocuronium injection pain

Rocuronium is a nondepolarizing neuromuscular blocking agent used in anesthesia induction and is associated with considerable discomfort and burning pain during injection, which is reported to occur in 50–80% of patients. This study was carried out to investigate the effectiveness of intravenous paracetamol pretreatment compared with lidocaine and normal saline to prevent rocuronium injection pain. The study included 150 ASA I–II patients undergoing elective orthopedic, gastrointestinal, and gynecological procedures under general anesthesia. They were allocated into three groups according to pretreatment drugs: lidocaine (40 mg) (n = 50), paracetamol (n = 50), and normal saline group (n = 50). Before anesthesia induction with propofol, all patients were pretreated with rocuronium. The pain caused by the injection was evaluated. Local signs were assessed on the arm at the end of the injection, as well as 24 hours after recovery from anesthesia. There were no patients with blurred speech or vision and there was no respiratory depression in any group after pretreatment with the study drug. The level of pain on injection was statistically lower in those who had received paracetamol compared to normal saline (p = 0.009). There were more patients in the saline group with severe pain (p < 0.001). Paracetamol relieved the rocuronium injection pain better than normal saline but lidocaine was the best of the three drugs (p < 0.001).     

Evaluation of hepatoprotective activity of alcoholic and aqueous extracts of Selaginella lepidophylla

ObjectiveTo screen Selaginella lepidophylla (S. lepidophylla) that are used in traditional medicine for their claimed hepatoprotective properties.MethodsAlcoholic and aqueous extracts of S. lepidophylla were evaluated for their hepatoprotective activity using CCl₄ and paracetamol induced acute hepatic injury model.ResultsTreatment with CCl₄ and paracetamol significantly increased liver weight and volume compared to the normal group. Pretreatment with silymarin alcoholic and aqueous extracts significantly prevent increase in liver weight and volume.ConclusionsFrom the present experimental study it can be concluded that alcoholic and aqueous extract of S. lepidophylla exhibited significant hepatoprotective activity against CCl₄ and paracetamol induced hepatotoxicity in rats, as result showed in physical, biochemical and histopathological parameters.