双苯甲酰沙丁胺醇的合成

目的：合成肺靶向前体药物双苯甲酰沙丁胺醇酯。方法：以氮－苄基保护胺基酮为原料,经氢化、苯甲酰化,还原三步合成双苯甲酰沙丁胺醇酯。结果：所合成的化合物为浅黄色固体,经质谱、核磁、红外光谱等初步鉴定为双苯甲酰沙丁胺醇酯。结论：该合成方法可用于制备双苯甲酰沙丁胺醇酯。     

一种新型醛糖还原酶抑制剂的合成

以5-氨基-1-萘磺酸为原料,用苯甲酰氯酰化,得到5-苯甲酰胺基-1-萘磺酸,再经氯化后,与甘氨酸酰化,合成了一种新型的醛糖还原酶抑制剂——5-苯甲酰胺基-1-萘磺酰甘氨酸。     

对氨基苯甲磺酰吡咯烷的合成

目的合成得到选择性5-HT1B/1D受体激动剂阿莫曲普坦的关键中间体对氨基苯甲磺酰吡咯烷。方法以氯苄为起始原料经过硝化、磺化、氯化、氨解、还原硝基等多步反应得到目标产物。结果与结论实验成功得到目标产物并且新的合成路线操作简便,便于工业化生产。     

镇静药苯甲酰苯巴比妥合成工艺改进

报道了苯甲酰苯巴比妥的合成和苯巴比妥、苯甲酰苯巴比妥、N,N-二苯甲酰苯巴比妥之间的分离方法。     

叶酸的合成

目的：以二亚胺作为中间体合成叶酸。方法：以1，1，3，3－四甲氧基丙醇和N－对氨基苯甲酰－L－谷氨酸为原料生成二亚胺，二亚胺与三氨啶硫酸盐反应生成叶酸。结果与结论：合成了叶酸，总产率可达65．5％，本工艺简单易行。     

镇静药苯甲酰苯巴比妥合成工艺改进

报道了苯甲酰苯巴比妥的合成和苯巴比妥、苯甲酰苯巴比妥、N,N-二苯甲酰苯巴比妥之间的分离方法。     

手性拆分剂D／L-二苯甲酰酒石酸的制备

用D/L-酒石酸和过量的苯甲酰氯反应得D/L-二苯甲酰酒石酸酐,利用原料、产物和副产物在甲苯中的溶解度差异,可得到苯甲酸残留量低于0.1%的D/L-二苯甲酰酒石酸.     

N甲基—N—苯甲酰甲基—α,β—环氧—β—苯基丙酰胺的制备

以苯甲醛为原料经Ｄａｒｚｅｎｓ缩合,酯妥交换及氧 步反应制备Ｎ－甲基－Ｎ－苯甲酰甲基－α、β－环氧－β－苯基丙酰胺的方法,三就总收率为４６．５％,该方法操作简单,较适合于大量制备的要求。     

过氧苯甲酰乳膏稳定性研究

目的：考察过氧苯甲酰乳膏在同存过程中的稳定性。采用经典恒温加速法,利用紫外伤发光的二阶导数光谱法。不经分离直接测定乳膏中过氧苯甲酰的含量。结果：光线对该制剂的稳定性无影响;在4℃放置30日,含量降低了10%。结论：该制剂宜在冰箱中贮存,期限为30日。     

苯甲酰乙基四氢异喹啉类化合物的合成及对心血管的活性

为寻找新的高效、低毒、副作用小的心血管药物,设计合成了12个苯甲酰乙基四氢异喹啉类衍生物。并进行了初步药理实验。     

丹参酮胶囊联合5%过氧苯甲酰凝胶治疗寻常型痤疮的疗效观察

目的:观察丹参酮胶囊联合5%过氧苯甲酰凝胶治疗寻常型痤疮的疗效与安全性。方法:将84例寻常型痤疮患者根据就诊次序随机均分为治疗组和对照组。治疗组口服丹参酮胶囊,每次4粒,tid,同时外用5%过氧苯甲酰凝胶,每日早、晚各1次;对照组仅外用5%过氧苯甲酰凝胶,每日早、晚各1次。2组疗程均为6周。结果:治疗组和对照组有效率分别为92.8%和71.4%,2组比较有显著性差异(P<0.01)。2组不良反应均较轻微,组间比较差异无统计学意义(P>0.05)。结论:丹参酮胶囊联合5%过氧苯甲酰凝胶治疗寻常型痤疮疗效显著,未见明显不良反应。     

HPLC法测定祛痘类化妆品中的过氧化苯甲酰

目的建立高效液相色谱法测定祛痘除螨类化妆品中的过氧化苯甲酰的方法。方法采用ZORBAX C18柱,4．6×250mm．5μm;以甲醇-0．02mol·L^-1的醋酸铵溶液（80：20）为流动相;检测波长为230nm。结果过氧化苯甲酰在0．224μg·mL^-1～44．8μg·mL^-1范围内呈良好线性关系,r=0．9996．过氧化苯甲酰的平均回收率为95．94％．RSD％为2．5％。结论上述建立的方法简便易行、准确、重现性好,可用于祛痘类化妆品中禁用物质过氧化苯甲酰的检测。     

Efficacy and safety of stabilised hydrogen peroxide cream (Crystacide) in mild-to-moderate acne vulgaris: a randomised,controlled trial versus benzoyl peroxide gel

Background: Benzoyl peroxide (BP) is a first-line topical treatment in acne vulgaris (AV). However, its use can cause mild skin irritation and dryness. A new formulation of hydrogen peroxide stabilised (HPS) in monoglycerides cream (Crystacide 1%), indicated in the topical treatment of superficial skin infections, is now available as an alternative treatment.

Study aim: To evaluate efficacy and local tolerability of HPS in mild-to-moderate AV in comparison with BP gel.

Methods and patients: In a randomised, prospective, investigator-masked parallel-group, 8-week trial, 60 patients (24 men, 36 women, mean age 25?±?6 years) with mild-to-moderate AV, affecting mainly the face, were enrolled in the study, after their informed consent. HPS or BP (PanOxyl gel 4%) was applied topically twice daily for 8 weeks.

Study outcomes: The study endpoints were: (1) Reduction in mean inflammatory (IL), non-inflammatory (NIL) and total (TL) acneic lesions in comparison with baseline; (2) Local tolerability assessed evaluating erythema, dryness and burning sensation, using a 0-3 qualitative score (score 0?=?poor tolerability; score 3?=?very good tolerability).

Results: TL, NIL, and IL were assessed by an investigator unaware of treatment allocation at baseline, and week 8. The tolerability score (TS) was assessed at week 4 and 8. At baseline, the two groups were well matched for the main clinical and demographic characteristics. All patients concluded the trial. At week 0, in the HPS group TL, NIL and IL (mean?±?SD) were: 35?±?8, 20?±?6 and 16?±?7. At week 8, HPS reduced TL to 16?±?7; NIL to 9?±?3 and IL to 7?±?3 (p?<?0.001). At baseline, TL, NIL and IL, in the BP group, were 32?±?9, 24?±?8 and 18?±?7, respectively. At week 8, BP reduced TL, NIL and IL to 14?±?9; 7?±?5 and 7?±?3 (p?<?0.001). In comparison with baseline values, the percentage reductions of IL were 58% and 61% for HPS and BP, respectively (p?=?n.s.). At the end of the study the TS was 2.9?±?0.2 in HPS group and 2.4?±?0.8 in BP group (p?<?0.025). Two patients in HPS group (6%) and seven patients (23%) in BP group suffered from mild-to-moderate local erythema.

Conclusions: HPS has shown to be as effective as BP in reducing both inflammatory and noninflammatory AV lesions in patients with mild-to-moderate disease. In comparison with BP 4% gel, HPS cream shows a better local tolerability profile.     

Lupeol, a triterpene, inhibits early responses of tumor promotion induced by benzoyl peroxide in murine skin.

The modulating effect of Lupeol [lup-20(29)-en-3 beta -ol], a triterpene found in many fruits and medicinal plants, on benzoyl peroxide-induced tumor promotion responses or tumor promotion in murine skin is described. Benzoyl peroxide is an effective cutaneous tumor promoter acting through the generation of oxidative stress, the induction of ornithine decarboxylase activity and the enhancement of DNA synthesis. Benzoyl peroxide treatment increases cutaneous microsomal lipid peroxidation and hydrogen peroxide generation. The activity of the cutaneous antioxidant enzymes, namely catalase, glutathione peroxidase, glutathione reductase and glutathione S-transferase, is decreased and levels of cutaneous glutathione are depleted. Benzoyl peroxide treatment also induces ornithine decarboxylase activity and enhances [3H]thymidine uptake in DNA synthesis. Prophylactic treatment of mice with lupeol (0.75 and 1.5 mg per animal) 1 hour before benzoyl peroxide treatment resulted in a diminution of benzoyl peroxide-mediated damage. The susceptibility of cutaneous microsomal membrane to lipid peroxidation and hydrogen peroxide generation was significantly reduced (P< 0.01 and P< 0.01, respectively). In addition, depleted levels of glutathione and inhibited activity of antioxidant enzymes were recovered to a significant level (P< 0.01, P< 0.05 and P< 0.01, respectively). Similarly, the elevated ornithine decarboxylase activity and enhanced thymidine uptake in DNA synthesis were inhibited significantly (P< 0.05) in a dose-dependent manner. The protective effect of lupeol was dose dependent in all parameters. The results suggest that lupeol is an effective skin chemopreventive agent that may suppress benzoyl peroxide-induced cutaneous toxicity.     

复方醋酸棉酚片治疗绝经过渡期功血的临床观察

目的：探讨复方醋酸棉酚片治疗绝经过渡期功血的临床效果。方法：将绝经过渡期功血患者98例随机分成两组,研究组50例,每天口服复方醋酸棉酚片;对照组48例,每天口服甲羟孕酮,连服3个月。随访至停药后3个月,对两组的治疗效果进行对比。结果：用药3个月研究组血清雌二醇、孕酮有不同程度下降（t分别为2.512、2.500,P均〈0.05）,促卵泡激素、黄体生成素明显上升（t分别为-3.045、-3.628,P均〈0.01）;停药3个月研究组发生闭经20例,月经量明显减少23例,月经正常5例;对照组有效治疗的31例患者中,无一例闭经,经量明显减少7例,月经正常9例,15例因月经再次紊乱增多改用其他治疗方法。研究组有9例患者用药1周内出现轻微恶心症状。结论：复方醋酸棉酚片治疗绝经过渡期功血的效果满意,副作用小,临床可推广使用。     

Quantitative determination of benzoyl peroxide by high-performance liquid chromatography and comparison to the iodometric method

A selective high-performance liquid chromatographic (HPLC) procedure for the quantitative determination of benzoyl peroxide in pharmaceutical dosage forms is described. Benzoyl peroxide was dissolved or extracted in the presence of an internal standard, acenaphthylene. The specificity of the stability-indicating HPLC and iodometric procedures are presented for benzoyl peroxide.     

毛细管气相色谱法测定氯高铁血红素原料药中的冰醋酸残留量

目的：测定氯高铁血红素原料药中的冰醋酸残留量。方法：采用毛细管气相色谱法。色谱柱为PEG-20M的石英毛细管柱,柱温为160℃,氢火焰离子化检测器,温度为250℃,载气为氮气,助燃气为氢气和空气,以蒸馏水为溶剂制备溶液直接进样,进样量为1.0μL。结果：冰醋酸检测浓度线性范围为0.00638～0.12751mg·mL-1（r=1.0000）;低、中、高浓度平均回收率（n=9）分别为98.98%、97.76%、98.86%,RSD分别为3.19%、2.06%、1.98%;最低检测限为0.00076mg·mL-1。结论：该法可用于氯高铁血红素原料药中冰醋酸残留量的检测。     

顶空毛细管气相色谱法测定盐酸莫西沙星中残留溶剂的含量

目的：建立盐酸莫西沙星中醋酸、乙酸乙酯、甲醇、乙醇、乙腈5种残留溶剂含量的测定方法。方法：顶空毛细管气相色谱法,氢火焰离子化检测器,醋酸以二甲基亚砜为溶剂,色谱柱为DB-FFAP（0．25mm×30m,0．25μm）;乙酸乙酯、甲醇、乙醇、乙腈以水为溶剂,异丙醇为内标,色谱柱为HP-INNOWax（0．32mm×30m,0．5μm）。结果：5种残留溶剂在对应于限度的20％～200％浓度范围内有良好的线性关系,平均回收率为97．3％～108．4％。结论：所建方法简单,准确,重现性好,可用于盐酸莫西沙星残留溶剂的含量控制。     

VE醋酸酯微乳凝胶的质量评价及初步稳定性研究

目的:对VE醋酸酯微乳凝胶进行质量评价及初步稳定性考察。方法:考察3批样品的性状、pH值、黏度、失水百分率和含量及其在高温、高湿、强光照射、高速离心和室温下的初步稳定性。结果:3批样品外观均呈均匀、细腻、黏稠适宜的乳白色半固体凝胶,pH值约为6.5,黏度约为16mPa·s,失水百分率<20%,主药含量约为10mg·g-1(占标示量95%～100%),均符合相关规定;稳定性试验中除强光下含量略有下降外,其余指标均无明显变化。结论:VE醋酸酯微乳凝胶质量可控、初步稳定性良好,建议避光贮存。     

正交试验法优选过氧苯甲酰凝胶处方

目的 优选过氧苯甲酰凝胶的处方。方法 以正交试验设计，通过不同条件的实验观察、比较，筛选稳定的处方组成，用硫代硫酸钠滴定法测定过氧苯甲酰的含量。结果 最优组方为甘油12.5 g，乙醇18.75 mL，EDTA 2Na0.012 5 g，水杨酸甲酯0.125 g。所得凝胶呈白色乳状粘稠体，稳定性好，且含量测定简单易行。结论 该凝胶剂配方合理，制剂性质稳定，质量易控，适宜痤疮的治疗。