Is benzoyl peroxide 3% topical gel effective and safe in the treatment of acne vulgaris in Japanese patients? A multicenter,randomized, double‐blind,vehicle‐controlled,parallel‐group study

Benzoyl peroxide (BPO) as an anti‐acne medication is not yet approved in Japan. This study evaluated the efficacy and safety of a once‐daily topical application of BPO 3% gel versus an inert vehicle gel in Japanese acne patients. Three hundred and sixty patients were randomized to receive BPO 3% or vehicle for 12 weeks. The primary efficacy end‐point was absolute change in number of total lesions (TL) from baseline to week 12 to demonstrate the superiority of BPO 3% versus vehicle. Secondary efficacy end‐points were absolute and percent change in TL, inflammatory lesions (IL), non‐inflammatory lesions (non‐IL) and Investigator's Static Global Assessment (ISGA). Change in TL counts from baseline to week 12 for BPO 3% was superior to vehicle (difference, ?21.0; P < 0.001). Absolute and percent reductions in TL, IL and non‐IL counts were greater for BPO 3% at all study visits. The proportion of patients with improvement in ISGA scores was significantly higher with BPO 3% than with vehicle from week 2. All adverse events were mild or moderate. Adverse drug‐related reactions were higher for BPO 3% (30%) than with vehicle (5%). Local tolerability scores of grade 1 or more (slight to moderate) were more frequent with BPO 3% than vehicle with the most significant differences observed in dryness (56% vs 27% at week 1–4), peeling (19% vs 9% at week 1–2) and burning/stinging (58% vs 15% at week 1–12). These results indicate that BPO 3% is effective while maintaining a favorable safety and tolerability profile in Japanese acne patients.     

Allergic complications from orthopaedic joint implants: the role of delayed hypersensitivity to benzoyl peroxide in bone cement

Background. Orthopaedic implants and osteosynthesis materials are increasingly being used. Complications include mainly physical–mechanical problems and infections. Uncommonly, an allergic reaction towards an alloy metal or a bone cement component has been implicated. Potential bone cement allergens include acrylates, benzoyl peroxide, N,N‐dimethyl‐p‐toluidine, and gentamicin. Typical symptoms are pain, swelling, inflammatory skin reactions, implant loosening, and fistula formation. Objectives. To report on 5 patients with complications from a knee or a shoulder joint implant in whom a relevant sensitization to benzoyl peroxide was shown. Methods. Patch tests were performed with the European baseline series, an extended metal series, and a bone cement series. Patch tests with benzoyl peroxide were performed twice in all patients. A bone cement‐free replacement was chosen in sensitized patients. Results. In 4 patients sensitized to benzoyl peroxide, a bone cement‐free replacement resulted in a considerable decrease or disappearance of pain and swelling, and complete clearing of cutaneous symptoms. Conclusions. Components of bone cement, such as benzoyl peroxide, may rarely cause allergic complications. However, because of the irritant potential of these substances, careful performance, reading and interpretation of the patch tests is required.     

参附汤体内代谢化学成分的初步研究

为了确定口服参附汤后体内吸收成分的化学结构 ,分离并鉴定了参附汤的组成成分之一———黑附片的主要成分 ;通过大鼠整体实验方法研究了参附汤体内代谢情况。结果显示 :口服参附汤后 ,乌头类生物碱卡米查林 (carmichaeline ,Ⅰ )、塔拉胺 (talatisamine ,Ⅱ )、附子灵 (fuziline ,Ⅲ )以原形形式被吸收 ,人参皂苷经肠内细菌代谢后以代谢产物CompoundK形式吸收进入体内     

草乌提取物乌头碱和新乌头碱的透皮速率测定

目的:测定草乌提取物中乌头碱、新乌头碱的透皮速率。方法:用改良Franz扩散池法收集草乌提取物的透皮接受液,用高效液相色谱法测定其中乌头碱、新乌头碱的透皮速率。结果:在促透剂氮酮和丙二醇各为4%的条件下,浓度为600mg/ml的草乌提取物中乌头碱、新乌头碱24h的累积渗透量分别为165.819和487.747μg/cm2;透皮速率常数分别为18.391和78.805μg·cm-2·h-1。结论:草乌提取物中乌头碱、新乌头碱在氮酮和丙二醇的促透作用下能较好地透过大鼠皮肤,透皮吸收过程符合Higuchi方程。     

棓酰苯胺类的合成及其抗心律失常的构效关系

根据作者以往报道的数十个棓酰苯胺衍生物,经药理初筛,提示这些衍生物都具有一定的不同程度的抗心律失常作用,在此基础上分析了构效关系,又设计合成13个新类似物,经用乌头碱诱发健康雄性大鼠室性心律失常模型筛选,并与临床用的利多卡因对照试验,除3个化合物无效外,其他10个化合物的治疗指数均较利多卡因高,毒性也较利多卡因低。     

乌头碱中毒所致心律失常20例抢救体会

本文报道了我院于1966年11月～1983年4月共抢救乌头碱中毒所致各种心律失常20例,全部治愈,无1例死亡,抢救方法如下: 1.立即洗胃,导泻及大量静脉输液,以加速毒物从体内排泄。2.在无特殊拮抗剂的情况下,乌头碱中毒所引起的各种缓慢型心律失常,主要为迷走神经强烈兴奋所致,应选用阿托品,以阻断迷走神经对窦房结及房室结兴奋性的抑制。对于窦房结功能低下而出现的室性心律失常,应用阿托品亦可使其消失。3.患者若出现呼吸抑制,休克或心脏停搏者,均提示中毒严重,应紧急治疗。4.室性心律失常,应立即静脉注射利多卡因。5.乌头碱中毒在体内无蓄积作用,如用阿托品治疗,心律失常消失后,即可停用,以免发生中毒。     

HPLC法同时测定四逆汤中3 种有效成分的含量

 目的建立同时测定四逆汤中乌头碱、新乌头碱和次乌头碱含量的HPLC 法。方法采用HPLC 色谱法,Eclipse XDB-
C18 色谱柱（4.6 mm*150 mm,5 μm）,流动相甲醇-0.1%三乙胺（65:35）,流速为1.0 mL·min-1,柱温为30益,检测波长为240 nm。
结果乌头碱、新乌头碱、次乌头碱分别在0.120 4～6.02 μg（ =0.9997）、0.041 2～2.06 μg（ =0.999 5）、0.080 8～4.04 μg（ =
0.999 9）范围内与峰面积呈良好的线性关系;平均回收率分别为100.74%（RSD=1.88%）、99.9%（RSD=2.98%）、102.9%（RSD=
1.32%）。结论该方法简便可行、重现性好、可作为四逆汤的质量控制方法。     

高效液相色谱法测定草乌叶中新乌头碱、乌头碱和次乌头碱

目的 建立以高效液相色谱法同时测定蒙药草鸟叶中新乌头碱、乌头碱、次乌头碱的方法.方法 Extend-C18柱(250 mm×4.6 mm,5μm),流动相为甲醇-0.3 mol/L三乙胺(65:35),体积流量为0.8 mL/min,检测波长为235 nm,柱温为35℃.结果 经过方法学考察,本测定方法具有一定的专属性、准确性、重现性和可行性,新乌头碱、乌头碱、次乌头碱分别在1～5、0.35～1.75、0.5～2.5 μg呈良好的线性关系,平均加样回收率分别为98.43%、98.98%、98.82%,RSD分别为1.38%、0.89%、1.03%.结论 本方法简便、准确、分离效果好、线性范围宽、灵敏度高,可用于本品的质量控制.     

复方雪莲胶囊的质量标准研究

目的:建立复方雪莲胶囊(雪莲,延胡索,制川乌等)的质量标准,以便更有效地控制产品质量.方法:鉴别项、检查项采用薄层色谱法(TLC).含量项采用高效液相色谱法(HPLC)测定制剂中的延胡索乙素.高效液相色谱条件:Kroma-sil ODS-1 C18柱,流动相:甲醇-磷酸盐缓冲液(65:35).结果:TLC具有专属性.HPLC准确可靠,回收率为100.7%,RSD为1.6%.结论:该标准可用于复方雪莲胶囊的质量控制.     

基于外翻肠囊模型的黄芪-附子配伍对附子6种生物碱肠吸收的影响研究

目的研究黄芪-附子药对配伍对附子3种单酯型生物碱(苯甲酰次乌头原碱、苯甲酰新乌头原碱、苯甲酰乌头原碱)和3种双酯型生物碱(次乌头碱、新乌头碱、乌头碱)肠吸收的影响。方法运用大鼠外翻肠囊模型,选择十二指肠、空肠、回肠为研究肠段,以表观渗透系数(P_(app))为评价指标,考察黄芪对附子6种生物碱P_(app)的影响。结果当附子-黄芪3∶1时,黄芪在十二指肠和回肠能显著降低双酯型生物碱的P_(app),在3种肠段均能降低单酯型生物碱的P_(app);当附子-黄芪1∶1时,除次乌头碱在回肠外,黄芪能显著降低双酯型生物碱的P_(app);当附子-黄芪1∶3时,黄芪能显著降低单酯型生物碱(除回肠外)的P_(app),在各肠段均能显著降低3种双酯型生物碱的P_(app)。结论黄芪可抑制附子生物碱的吸收,且其抑制作用因配伍比例、生物碱的种类和肠段不同而不同。