氢醌脂肪酸单酯的简便合成

氢醌脂肪酸单酯是一类皮肤祛色素剂 ,其作用机理与氢醌相同 ,即抑制皮肤组织中酪氨酸酶的活性 ,从而阻断黑色素形成。与氢醌相比 ,氢醌脂肪酸单酯具有对皮肤刺激性小 ,性质更加稳定 ,且祛色素性能更好等优点[1] 。氢醌脂肪酸单酯的合成方法 ,文献 [2 ,3] 报道较多的是以氢醌与酰氯在 DMAP催化下反应制备。此方法反应复杂 ,所用试剂比较昂贵 ,反应副产物多 ,后处理较困难 ,且产率不高 ,文献[2 ] 收率 58%～ 65% ,文献[3 ] 收率 >70 % ,因此不宜于大规模制备。本文参考文献 [4 ]以氢醌单丙酸酯 (1 )为例 ,采用氢醌二丙酸酯 (2 )为原料 ,在甲…     

氢醌羧酸酯的合成及其除去皮肤色素的性能

以丙酰氯与氢醌合成氢醌单丙酸酯,产率>70%。经药效观察,其除去皮肤色素和抗氧化性能远优于氢醌。     

高效液相色谱法测定复方氢醌霜中氢醌的含量

目的 :建立测定复方氢醌霜中氢醌含量的高效液相色谱方法。方法 :采用KromasilC18 柱 ,以甲醇 -水 (30∶70)为流动相 ,检测波长293nm。结果 :在2 5～60μg/ml范围内 ,氢醌的峰面积与浓度呈现良好线性关系 ;方法平均回收率为99 9 % ,RSD=0 73 %。结论 :本方法可用于测定复方氢醌霜中氢醌的含量。     

甲萘氢醌二磷酸酯钠的制备

目的:合成甲萘氢醌二磷酸酯钠六水合物。方法:以甲萘醌为起始原料,二水合氯化亚锡为还原剂,经还原、酯化、成钙盐、重结晶得到甲萘氢醌二磷酸酯钠六水合物固体。结果:目标化合物经UV法测得含量在98.5%。元素分析、质谱、红外光谱、核磁共振氢谱(1H-NMR)、碳谱(13C-NMR)确证化学结构,总收率为72%。结论:本合成路线简单,生产成本较低,易于工业化生产。     

双波长紫外分光光度法测定复方氢醌乳膏中氢醌的含量

目的:建立复方氢醌乳膏中氢醌的含量测定方法。方法:采用双波长紫外分光光度法测定氢醌的含量。结果:氢醌在4.06~24.36μg/mL范围内线性关系良好(r=0.9998,n=6),平均回收率95.87%,相对标准偏差为0.51%。结论:该含量测定方法简便快速,结果准确。     

氢醌酯的合成及其霜剂的制备

目的　增强氢醌消除皮肤色素的能力和抗氧化性能。方法　以氢醌和醋酐合成氢醌二乙酸酯并制成霜剂。结果　氢醌酯霜比氢醌霜具有更强的抗氧化性能。结论　酯化能提高氢醌制剂的稳定性。     

甲萘氢醌二磷酸酯钠注射液处方和工艺研究

目的研究甲萘氢醌二磷酸酯钠注射液的制备工艺。方法对抗氧剂用量、pH值,灭菌条件进行筛选。用紫外分光光度法测定甲萘氢醌二磷酸酯钠的含量及有关物质。结果加入0．4％抗氧剂,药液pH值调为7．0～8．0,105℃热压灭菌30分钟,制剂质量符合药典有关注射剂的质量标准。结论本品处方工艺合理,质量稳定。     

薄层扫描法测定强痛宁制剂中酯蟾毒配基的含量

目的提供合适的方法,以控制强痛宁制剂中蟾酥的含量。方法双波长薄层扫描法测定强痛宁制剂中酯蟾毒配基的含量,λS=295nm,λR=370nm,在1.102~5.510范围内与吸收面积积分值呈良好的线性关系(r=0.999 4)。结果平均加样回收率为98.88%,RSD值为0.71%(n=5)。结论本法简单、准确,可作为蟾酥质量控制方法。     

高效液相色谱法测定醋酸甲萘氢醌片的含量

目的:建立反相高效液相色谱法测定醋酸甲萘氢醌片的含量.方法:色谱柱为KF-C18柱,以硝酸异山梨酯为内标物,流动相为甲醇-水(65:35),流速为1.0 mL·min-1,检测波长224 nm.结果:醋酸甲萘氢醌在0.02～0.18μg范围内线性关系良好(r=0.999 9).平均加样回收率为99.7%,RSD为0.4%.结论:本法结果准确、可靠,可用于该制剂的质量分析检验.     

复方氢醌乳膏的制备与临床疗效观察

目的:探讨复方氢醌乳膏的制备,含量测定方法并观察其临床疗效。方法:以氢醌和维生素E为主要原料,选择适宜的乳化剂,制成O/W型乳膏,采用双波长紫外分光光度法测定复方氢醌乳膏中氢醌的含量,设对照组进行临床疗效观察。结果:平均回收率98.67%,RSD=0.54%(n=5);治疗老年性角化斑和黄褐斑有效率分别为85%和80%,明显高于对照组。结论:复方氢醌乳膏性质稳定,临床疗效好。     

Oral Bioavailability of Triamcinolone Tablets and a Triamcinolone Diacetate Suspension

Pharmaceutical Research -     

反相高效液相色谱法测定醋酸甲萘氢醌片的含量

目的建立测定醋酸甲萘氢醌片含量的反相高效液相色谱法。方法采用Welch Materials C18色谱柱(150 mm×4.6 mm,5μm),以乙腈-水(65∶35)为流动相,检测波长285 nm,流速1.0 mL/min,进样量20μL。结果醋酸甲萘氢醌质量浓度在4.0～60.0μg/mL范围内与峰面积线性关系良好(r=1.000),平均回收率99.93%,RSD=1.21%(n=9)。结论所用方法简便,重复性好,结果准确可靠,可作为醋酸甲萘氢醌制剂的质量控制方法。     

氯已定醋酸盐的体外杀精效果及抑菌作用的研究

目的 研究一种对性传播性疾病(STD)病原体有抑制和灭活作用的体外杀精药物。方法 选用氯己定醋酸盐，按照国际计划生育基金会(IPPF)认可的杀精子实验方法，对10例大鼠精液、10例人精液进行了体外杀精试验，并观察了氯已定醋酸盐对白色念珠菌、淋病双球菌的抑菌杀菌作用。结果 氯已定醋酸盐与人精液作用最低有效杀精浓度为1．25mg／mL；与大鼠精液作用最低有效杀精浓度为0．5mg／mL、氯已定醋酸盐对白色念珠菌(28株)最低抑菌浓度(MIC)为0.125一0．50mg／mL，最低杀菌浓度(MBC)为0．25—0．50mg／mL；对淋球菌(2株)最低抑菌浓度(MIC)为0．0125—0．50mg／mL。结论 初步认为氯已定醋酸盐可望成为一种有效、安全的阴道杀精剂，值得进一步研究。     

正交试验法优选氟尿苷二乙酸酯固体脂质纳米粒制备工艺

目的:优选氟尿苷二乙酸酯固体脂质纳米粒(FUDRA-SLN)的工艺条件。方法:以大豆磷脂为载体,采用薄膜超声分散法制备FUDRA-SLN,以包封率、形态为考察指标,设计正交试验优选工艺条件。结果:按最优工艺条件制得的FUDRA-SLN均匀圆整,粒径为(215±83)nm,包封率为98·27%,载药量为8·20%。结论:选择优化的薄膜超声分散工艺制备FUDRA-SLN,包封率及载药量高,适合于实验室制备。     

Wound Dressings Based on Chitosans and Hyaluronic Acid for the Release of Chlorhexidine Diacetate in Skin Ulcer Therapy

In the present work wound dressings, based on chitosan hydrochloride (HCS), 5-methyl-pyrrolidinone chitosan (MPC), and their mixtures with an anionic polymer, hyaluronic acid (HA), were prepared by freeze-drying. Chlorhexidine diacetate (CX) was used as an antimicrobic drug. The mechanical properties of the wound dressings were investigated. In particular, the wound dressings were subjected to dynamic hydration measurements to evaluate their capability to absorb wound exudate and to rheological analysis to investigate their resistance to mechanical stresses on hydration. The wound dressings were also characterized for drug release properties. The antioxidant and antimicrobial activities of medicated and non-medicated wound dressings were also investigated. All the wound dressings are characterized by mechanical resistance suitable for skin application. The addition of hyaluronic acid to chitosans leads to a reduction in wound dressing hydration properties and a modulation of drug release. The wound dressing based on MPC is characterized by the highest elastic properties and by the best scavenger activity. Antimicrobial activity against bacteria and C. albicans is shown by the dressing based on chitosan also in absence of chlorhexidine.     

紫外分光光度法测定氢醌乳膏的含量

以甲醇为溶煤，用紫外分光光度法中的对照品比较法测定氢醌乳膏中的氢醌的含量，辅料无干扰。操作简便、快速、准确。平均回收率为１００．１％，ＲＳＤ为１．８９％（ｎ＝３）。     

鹿蹄草素合成方法的改进

报导以邻甲苯胺为原料经氧化－还原反应合成鹿蹄草素方法的改进。采用Ｆｅ／ＨＣＩ还原方法后，使还原反应收率达到了９６．１％，二步总收率提商到了４８．１％。该工艺具有反应时间短、工艺简单、收率高的优点。经熔点、元素分析、红外、紫外光谱证明了该产品的结构。     

Growth Inhibitory Effect of (E)-2,4-bis(p-hydroxyphenyl)-2-Butenal Diacetate through Induction of Apoptotic Cell Death by Increasing DR3 Expression in Human Lung Cancer Cells

The Maillard Reaction Products (MRPs) are chemical compounds which have been known to be effective in chemoprevention. Death receptors (DR) play a central role in directing apoptosis in several cancer cells. In our previous study, we demonstrated that (E)-2,4-bis(p-hydroxyphenyl)-2-butenal, a MRP product, inhibited human colon cancer cell growth by inducing apoptosis via nuclear factor-κB (NF-κB) inactivation and G₂/M phase cell cycle arrest. In this study, (E)-2,4-bis(p-hydroxyphenyl)-2-butenal diacetate, a new (E)-2,4-bis(p-hydroxyphenyl)-2-butenal derivative, was synthesized to improve their solubility and stability in water and then evaluated against NCI-H460 and A549 human lung cancer cells. (E)-2,4-bis(p-hydroxyphenyl)-2-butenal diacetate reduced the viability in both cell lines in a time and dose-dependent manner. We also found that (E)-2,4-bis(p-hydroxyphenyl)-2-butenal diacetate increased apoptotic cell death through the upregulation of the expression of death receptor (DR)-3 and DR6 in both lung cancer cell lines. In addition to this, the transfection of DR3 siRNA diminished the growth inhibitory and apoptosis inducing effect of (E)-2,4-bis(p-hydroxyphenyl)-2-butenal diacetate on lung cancer cells, however these effects of (E)-2,4-bis(p-hydroxyphenyl)-2-butenal diacetate was not changed by DR6 siRNA. These results indicated that (E)-2,4-bis(p-hydroxyphenyl)-2-butenal diacetate inhibits human lung cancer cell growth via increasing apoptotic cell death by upregulation of the expression of DR3.     

T cell-dependent immune reactions to reactive benzene metabolites in mice

Using the popliteal lymph node (PLN) assay in mice, we studied the sensitizing potential of benzene and its metabolites. Whereas benzene and phenol failed to induce a PLN reaction, catechol and hydroquinone induced a moderate, and p-benzoquinone a vigorous response. Following a single injection of the reactive metabolite p-benzoquinone (100 nmol/mouse), cellularity in the draining PLN was increased >15-fold, and reverted back to normal only after ∼100 days. Although the PLN response was T cell-dependent, flow cytometric analysis revealed that the increased cellularity in the PLN after a single injection of p-benzoquinone was mainly due to an increase in B cells. Mice primed to p-benzoquinone and challenged with a small dose of p-benzoquinone (0.1 nmol/mouse) mounted a secondary PLN reaction, indicating hapten specificity of the reaction; this was confirmed by results obtained in the adoptive transfer PLN assay. An unexpected finding was the secondary PLN response to benzene (1 nmol/mouse) observed in mice primed to p-benzoquinone. This finding suggests that some of the benzene (at least 10%) was locally converted into p-benzoquinone, which then elicited the secondary response observed. In conclusion, the reactive intermediate metabolites hydroquinone and p-benzoquinone can act as haptens and sensitize; their precursors, benzene and phenol, may be considered as prohaptens. Received: 7 December 1998 / Accepted: 9 February 1999     

The pro-apoptotic effect of hydroquinone in human neutrophils and eosinophils

Hydroquinone (HQ) is a benzene metabolite that is involved in hematopoiesis via its accumulation into bone marrow. HQ also acts as a toxic agent that influences various immune responses. Both neutrophils and eosinophils function as important leukocytes in immunological regulation and immune diseases. In this study, we examined the toxic effects of HQ on the apoptosis of human neutrophils and eosinophils isolated from the blood of healthy donors. HQ markedly increased the apoptosis of neutrophils and eosinophils in a concentration- and a time-dependent manner. The pro-apoptotic effect is involved in activation of caspase 9 and caspase 3. Reactive oxygen species (ROS) production was enhanced after HQ treatment in a dose-dependent manner. In addition, HQ upregulated the release of IL-8 and MCP-1 from neutrophils and eosinophils, respectively. Taken together, the results of this study demonstrated that HQ strongly induces the apoptosis of neutrophils and eosinophils through the caspase 9/3-dependent pathway and the increased ROS production. HQ exerts a cytotoxic effect in human neutrophils and eosinophils and may impair the regulation of immune responses.