高效液相色谱法测定氨咖黄敏胶囊的含量

目的建立同时测定氨咖黄敏胶囊中对乙酰氨基酚和咖啡因含量的高效液相色谱法。方法色谱柱为Aglient C18柱(250 mm×4.6 mm,5μm),流动相为1%醋酸溶液(用乙二胺调pH至3.7)-甲醇(60:40),流速为1.0 mL/min,检测波长272 nm,柱温30℃。结果对乙酰氨基酚、咖啡因进样量分别在0.122 2～3.055 5μg和0.007 482～0.187 1μg范围内与峰面积呈良好线性关系,r分别为1.000 0和1.000 0(n=6),平均加样回收率分别为99.54%(RSD=0.66%)和100.43%(RSD=0.92%)。结论该方法快速简便、准确可靠,可用于氨咖黄敏胶囊的质量控制。     

HPLC法同时测定氨咖黄敏胶囊中2组份的含量

建立用HPLC法测定氨咖黄敏胶囊中对乙酰氨基酚和咖啡因含量的方法.用Kromasil苯基色谱柱;流动相:乙腈-水-三乙氨(20∶79∶1)(磷酸调pH值3.1),流速:1.0mL·min-1;检测波长:260nm.线性范围,对乙酰氨基酚:15.1320～35.3080μg,r=0.9998;咖啡因:0.9063～2.1147μg,r=1.0000.平均回收率,对乙酰氨基酚99.45%,RSD=0.53%;咖啡因99.96%,RSD=0.32%.本方法简便、快速、准确,适用氨咖黄敏胶囊含量测定和质量控制.     

HPLC法测定氨咖黄敏胶囊中对乙酰氨基酚、咖啡因的含量

目的建立以HPLC法同时测定氨咖黄敏胶囊中对乙酰氨基酚、咖啡因的含量。方法色谱柱C18(250mm),流动相:甲醇-4.2%冰醋酸溶液(3∶7),流速:1.0ml.min-1,检测波长为275nm,进样量为20μl。结果对乙酰氨基酚,咖啡因的线性范围分别为25~200μg.ml-1(r=0.9999)、2~12μg.ml-1(r=0.9998),平均回收率分别为99.8%、100.1%。结论本方法简便、快速、准确、专属性高,可用于氨咖黄敏胶囊中对乙酰氨基酚、咖啡因的含量测定。     

UPLC法测定小儿氨咖黄敏颗粒中对乙酰氨基酚、咖啡因和马来酸氯苯那敏的含量

目的使用超高效液相色谱(UPLC)法建立测定小儿氨咖黄敏颗粒中3种西药成分含量的方法。方法色谱柱为Acquity UPLC~BEH C18柱(7.5cm×0.21cm,1.7μm);柱温为35℃;流动相为0.03mol·L-1磷酸氢二铵溶液-乙腈(88∶12);检测波长为214nm。结果线性范围为:对乙酰氨基酚0.149~1.489μg,r=0.999 8;咖啡因0.010~0.101μg,r=0.999 4;马来酸氯苯那敏0.005~0.082μg,r=0.999 9。平均回收率:对乙酰氨基酚99.3%,RSD=0.42%;咖啡因98.8%,RSD=0.50%;马来酸氯苯那敏99.5%,RSD=0.78%。结论相对于现行药品执行标准中的含量测定方法,UPLC法测定3种西药含量更准确、方便,可较好地控制小儿氨咖黄敏颗粒的质量。     

HPLC法同时测定氨咖黄敏胶囊中三组分的含量

目的建立同时测定氨咖黄敏胶囊中三组分(对乙酰氨基酚、咖啡因、马来酸氯苯那敏)的高效液相色谱法。方法色谱柱为Agilent TC-C18(4.6 mm×150 mm,5μm);流动相为磷酸盐缓冲液(取磷酸二氢铵11.5 g,加水适量使溶解,加磷酸1 mL,用水稀释至1 000 mL)-乙腈(85∶15);流速为1.0 mL·min-1;检测波长为225 nm;柱温为30℃。结果对乙酰氨基酚、咖啡因和马来酸氯苯那敏的进样量分别在2.523～7.569,0.149 6～0.448 8和0.010 08～0.03024μg范围内与峰面积呈良好线性关系,r值分别为0.999 8,0.999 9,0.999 9,平均回收率分别为99.6%,99.5%,99.8%,RSD分别为0.56%,0.60%,0.65%(n=9)。结论本方法简便、快速、准确,可用于氨咖黄敏胶囊的质量控制。     

HPLC法测定氨咖黄敏胶囊中对乙酰氨基酚、咖啡因、马来酸氯苯那敏的含量

目的:建立HPLC法测定氨咖黄敏胶囊中对乙酰氨基酚、咖啡因和马来酸氯苯那敏的含量;方法:色谱柱:Kromasil苯基柱(250 mm×4.6 mm,5μm);流动相:乙腈-水-三乙氨(20:79:1)(磷酸调pH至3.1),检测波长为260 nm;结果:线性范围:对乙酰氨基酚15.13～35.30μg,r=0.9999;咖啡因0.911～2.11μg,r=1.0000;马来酸氯苯那敏0.06～0.15μg,r= 0.9998;平均回收率:对乙酰氨基酚99.5%,RSD%=0.5%;咖啡因100.0%,RSD%=0.3%;马来酸氯苯那敏99.6%,RSD%=0.9%。结论:本方法简便、准确、灵敏度高、重现性好,可更好地控制本品质量。     

RP-HPLC法测定氨林酚咖胶囊中3组分的含量

目的建立氨林酚咖胶囊中氨基比林、对乙酰氨基酚和咖啡因含量的RP-HPLC测定方法。方法用Kro-masil C18色谱柱(250×4.6mm,5μm),以甲醇-水(60:40)为流动相,流速为1.0ml.min-1,检测波长为260nm。结果氨基比林、对乙酰氨基酚和咖啡因分别在10.0～30.0μg.ml-1(r=0.9992)、8.3～24.8μg.ml-1(r=0.9993)和3.1～9.2μg.ml-1(r=0.9998)范围内呈线性关系,平均回收率分别为99.4%、98.4%、99.2%,RSD=0.7%、0.6%、0.8%(n=9)。结论本法适用于氨林酚咖胶囊中氨基比林、对乙酰氨基酚和咖啡因的含量测定。     

RP-HPLC法同时测定氨咖敏片中3组份的含量

目的:建立用 RP-HPLC 法测定氨咖敏片中氨基比林、咖啡因和马来酸氯苯那敏含量的方法。方法:用 Kromasil C_(18)柱(250 mm×4.6 mm,5μm),以乙腈-0.3%十二烷基硫酸钠溶液-磷酸(60:40:0.02)(用三乙胺调 pH 至3.3)为流动相,流速1.0ml·min~(-1),检测波长215 nm。结果:氨基比林、咖啡因和马来酸氯苯那敏分别在30.2～90.5μg·ml~(-1)(r=0.999 9),2.8～8.4μg·ml~(-1)(r=0.999 6)和10.1～30.2μg·ml~(-1)(r=0.999 9)范围内呈线性关系,平均回收率分别为99.4%,RSD=0.3%(n=9),99.6%,RSD=0.5%(n=9)和99.3%,RSD 0.4%。结论:本法简单、快速和准确,适用于氨咖敏片质量控制。     

HPLC法测定氨咖黄敏胶囊中对乙酰氨基酚和咖啡因的含量

目的:建立高效液相色谱法测定氨咖黄敏胶囊中对乙酰氨基酚和咖啡因的方法。方法:色谱柱为K rom asil C18(250mm×4.6mm,5μm),流动相为甲醇∶水(1∶1),检测波长为245nm,流速为0.6m l.m in-1。结果:对乙酰氨基酚和咖啡因的平均回收率分别为99.92%和99.74%;RSD分别为0.36%和0.43%(n=5)。     

HPLC法测定氨咖黄敏胶囊中对乙酰氨基酚和咖啡因的含量

目的用HPLC法测定氨咖黄敏胶囊中对乙酰氨基酚和咖啡因的含量。方法Irland Waters C18柱(5μm,4.6mm×150mm);流动相:甲醇-水(40∶60),流速为1.0mL.min-1,检测波长为216nm,进样体积为20μL,柱温为室温。结果对乙酰氨基酚在0.2mg·mL-1~0.9mg.mL-1浓度范围内、咖啡因在12μg·mL-1~54μg·mL-1浓度范围内与峰面积呈良好的线性关系。结论HPLC法能使对乙酰氨基酚和咖啡因更好地分离,提高了检测的专属性和准确性,可用于氨咖黄敏胶囊中对乙酰氨基酚和咖啡因的含量测定。     

Safety assessment of poloxamers 101, 105, 108, 122, 123, 124, 181, 182, 183, 184, 185, 188, 212, 215, 217, 231, 234, 235, 237, 238, 282, 284, 288, 331, 333, 334, 335, 338, 401, 402, 403, and 407, poloxamer 105 benzoate, and poloxamer 182 dibenzoate as used in cosmetics

Poloxamers are polyoxyethlyene, polyoxypropylene block polymers. The impurities of commercial grade Poloxamer 188, as an example, include low-molecular-weight substances (aldehydes and both formic and acetic acids), as well as 1,4-dioxane and residual ethylene oxide and propylene oxide. Most Poloxamers function in cosmetics as surfactants, emulsifying agents, cleansing agents, and/or solubilizing agents, and are used in 141 cosmetic products at concentrations from 0.005% to 20%. Poloxamers injected intravenously in animals are rapidly excreted in the urine, with some accumulation in lung, liver, brain, and kidney tissue. In humans, the plasma concentration of Poloxamer 188 (given intravenously) reached a maximum at 1 h, then reached a steady state. Poloxamers generally were ineffective in wound healing, but were effective in reducing postsurgical adhesions in several test systems. Poloxamers can cause hypercholesterolemia and hypertriglyceridemia in animals, but overall, they are relatively nontoxic to animals, with LD(50) values reported from 5 to 34.6 g/kg. Short-term intravenous doses up to 4 g/kg of Poloxamer 108 produced no change in body weights, but did result in diffuse hepatocellular vacuolization, renal tubular dilation in kidneys, and dose-dependent vacuolization of epithelial cells in the proximal convoluted tubules. A short-term inhalation toxicity study of Poloxamer 101 at 97 mg/m(3) identified slight alveolitis after 2 weeks of exposure, which subsided in the 2-week postexposure observation period. A short-term dermal toxicity study of Poloxamer 184 in rabbits at doses up to 1000 mg/kg produced slight erythema and slight intradermal inflammatory response on histological examination, but no dose-dependent body weight, hematology, blood chemistry, or organ weight changes. A 6-month feeding study in rats and dogs of Poloxamer 188 at exposures up to 5% in the diet produced no adverse effects. Likewise, Poloxamer 331 (tested up to 0.5 g/kg day(-1)), Poloxamer 235 (tested up to 1.0 g/kg day(-1)), and Poloxamer 338 (at 0.2 or 1.0 g/kg day(-1)) produced no adverse effects in dogs. Poloxamer 338 (at 5.0 g/kg day(-1)) produced slight transient diarrhea in dogs. Poloxamer 188 at levels up to 7.5% in diet given to rats in a 2-year feeding study produced diarrhea at 5% and 7.5% levels, a small decrease in growth at the 7.5% level, but no change in survival. Doses up to 0.5 mg/kg day(-1) for 2 years using rats produced yellow discoloration of the serum, high serum alkaline phosphatase activity, and elevated serum glutamicpyruvic transaminase and glutamic-oxalacetic transaminase activities. Poloxamers are minimal ocular irritants, but are not dermal irritants or sensitizers in animals. Data on reproductive and developmental toxicity of Poloxamers were not found. An Ames test did not identify any mutagenic activity of Poloxamer 407, with or without metabolic activation. Several studies have suggested anticarcinogenic effects of Poloxamers. Poloxamers appear to increase the sensitivity to anticancer drugs of multidrug-resistant cancer cells. In clinical testing, Poloxamer 188 increased the hydration of feces when used in combination with a bulk laxative treatment. Compared to controls, one study of angioplasty patients receiving Poloxamer 188 found a reduced myocardial infarct size and a reduced incidence of reinfarction, with no evidence of toxicity, but two other studies found no effect. Poloxamer 188 given to patients suffering from sickle cell disease had decreased pain and decreased hospitilization, compared to controls. Clinical tests of dermal irritation and sensitization were uniformly negative. The Cosmetic Ingredient Review (CIR) Expert Panel stressed that the cosmetic industry should continue to use the necessary purification procedures to keep the levels below established limits for ethylene oxide, propylene oxide, and 1,4-dioxane. The Panel did note the absence of reproductive and developmental toxicity data, but, based on molecular weight and solubility, there should be little skin penetration and any penetration of the skin should be slow. Also, the available data demonstrate that Poloxamers that are introduced into the body via routes other than dermal exposure have a rapid clearance from the body, suggesting that there would be no risk of reproductive and/or developmental toxicity. Overall, the available data do not suggest any concern about carcinogenesis. Although there are gaps in knowledge about product use, the overall information available on the types of products in which these ingredients are used, and at what concentration, indicates a pattern of use. Based on these safety test data and the information that the manufacturing process can be controlled to limit unwanted impurities, the Panel concluded that these Poloxamers are safe as used.     

HPLC法测定抗妇炎胶囊中木兰花碱、黄柏碱、药根碱、巴马汀、小檗碱、槐果碱、苦参碱、氧化槐果碱、槐定碱和氧化苦参碱

目的 采用高效液相色谱（HPLC）法同时测定抗妇炎胶囊中木兰花碱、黄柏碱、药根碱、巴马汀、小檗碱、槐果碱、苦参碱、氧化槐果碱、槐定碱和氧化苦参碱10种活性成分。方法 采用InerSustain AQ-C₁₈色谱柱（250 mm×4.6 mm,5 μm）,流动相A：乙腈–无水乙醇（80∶20）,流动相B：0.1%磷酸溶液,梯度洗脱,检测波长220 nm,体积流量1.0 mL/min,柱温30℃,进样量10 μL。结果 木兰花碱、黄柏碱、药根碱、巴马汀、小檗碱、槐果碱、苦参碱、氧化槐果碱、槐定碱和氧化苦参碱分别在2.69～134.50、1.95～97.50、0.63～31.50、0.86～43.00、11.95～597.50、0.59～29.50、6.08～304.00、4.85～242.50、1.66～83.00、19.79～989.50 μg/mL线性关系良好（r≥0.999 3）;平均回收率分别为99.11%、98.23%、96.95%、97.78%、100.02%、97.21%、99.66%、99.52%、98.81%、100.08%,RSD值分别为1.04%、1.23%、1.37%、1.65%、0.70%、1.28%、0.65%、0.81%、1.11%、0.63%。结论 建立的HPLC法可用于抗妇炎胶囊中10种活性成分的测定,作为抗妇炎胶囊质量控制方法。     

Arformoterol: (R,R)-eformoterol, (R,R)-formoterol, arformoterol tartrate, eformoterol-sepracor, formoterol-sepracor, R,R-eformoterol, R,R-formoterol

Sepracor in the US is developing arformoterol [R,R-formoterol], a single isomer form of the beta(2)-adrenoceptor agonist formoterol [eformoterol]. This isomer contains two chiral centres and is being developed as an inhaled preparation for the treatment of respiratory disorders. Sepracor believes that arformoterol has the potential to be a once-daily therapy with a rapid onset of action and a duration of effect exceeding 12 hours. In 1995, Sepracor acquired New England Pharmaceuticals, a manufacturer of metered-dose and dry powder inhalers, for the purpose of preparing formulations of levosalbutamol and arformoterol. Phase II dose-ranging clinical studies of arformoterol as a longer-acting, complementary bronchodilator were completed successfully in the fourth quarter of 2000. Phase III trials of arformoterol began in September 2001. The indications for the drug appeared to be asthma and chronic obstructive pulmonary disease (COPD). However, an update of the pharmaceutical product information on the Sepracor website in September 2003 listed COPD maintenance therapy as the only indication for arformoterol. In October 2002, Sepracor stated that two pivotal phase III studies were ongoing in 1600 patients. Sepracor estimates that its NDA submission for arformoterol, which is projected for the first half of 2004, will include approximately 3000 adult subjects. Sepracor stated in July 2003 that it had completed more than 100 preclinical studies and initiated or completed 15 clinical studies for arformoterol inhalation solution for the treatment of bronchospasm in patients with COPD. In addition, Sepracor stated that the two pivotal phase III studies in 1600 patients were still progressing. In 1995, European patents were granted to Sepracor for the use of arformoterol in the treatment of asthma, and the US patent application was pending.     

欧洲刺柏（Juniper）

活性成分与药理作用欧洲刺柏药用部位是其浆果，具有促水排泄、防腐、抗胃肠胀气和抗风湿作用，还可改善胃功能。用作促水排泄药可增加尿量（水丢失），但不增加钠排泄。成分萜品烯-4-醇可增加肾小球滤过率，但刺激肾。欧洲刺柏浆果对单纯疱疹病毒体外显示抗病毒活性，并具抗真菌活性。动物实验显示，欧洲刺柏浆果提取物具有堕胎、抗生育、抗炎、抗胚胎植入、降血压、升血压和降血糖作用。欧洲刺柏浆果油具有兴奋子宫的活性，以及利尿、胃肠道抗菌和刺激作用，该油对平滑肌有阻止解痉作用。     

Oral Presentations (LDD, LPES, LNM, LPAT, LNT, LPPT, LPM)

Probiotic microorganisms have been shown to provide specific health benefits when consumed as food supplements or as food components. The main problem of such products is the poor survival of the probiotic bacteria in the low pH of gastric fluid. However the use of synthetic excipients for enteric coating to prevent the exposure of microorganisms to gastric fluid is limited in food supplementary industry. Therefore the aim of this study was to develop an enteric coating formulation containing shellac as a natural polymer. Shellac possesses good resistance to gastric juice; the major disadvantage of this polymer is its low solubility in the intestinal fluid [1, 2]. Thus films containing different ratios of shellac and water-soluble polymers (sodium alginate, hydroxypropyl methylcellulose (HPMC) and polyvinylpyrrolidon (PVP)) or plasticizers (glycerol and glyceryl triacetate (GTA)) were prepared in order to analyse the films’ melting temperatures (T_m), the changes in enthalpy (ΔH), their capability of taking up water, and their solubility in different media. The release characteristics of the films were studied by loading pellets with Enterococcus faecium M74 and coating them with formulations containing different amounts of shellac and polymer or plasticized shellac. Using dissolution tests, performed according to USP XXXI paddle method, the resistance of the coatings to simulated gastric fluid (SGF, pH 1.2) and the release of cells in simulated intestinal fluid (SIF, pH 6.8) was investigated.The trials showed that an increasing amount of plasticizer results in a decrease of T_m and ΔH of the films whereat glycerol had a superior plasticization effect to GTA. The compatibility of films made of water-soluble polymers and shellac was also concentration dependent. HPMC and PVP showed superior compatibility with shellac compared to sodium alginate, since films containing shellac and more than 10% [w/w] sodium alginate tended to separate into two phases. In the end five formulations containing shellac and either 5% [w/w] glycerol, 10% [w/w] PVP, 20% [w/w] PVP, 10% [w/w] HPMC, or 5% [w/w] sodium alginate emerged as feasible for enteric coating purposes.