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多西他赛注射液说明书欧阳引擎（2021.01.01）【药品名称】通用名称：多西他赛注射液商品名称：多帕菲英文名称：Docetaxel Injection汉语拼音：Duoxitasai Zhusheye【成份】本品主要成份为多西他赛,其化学名称为:｛2aR-[2aα,4β,4aβ,6β,9α(αR*,βS*),11α,12α,12aα,12bα]｝-β-｛[(1,1-二甲基乙氧基)羰基]氨基｝-α-羟基苯丙酸[12b-乙酰氧-12-苯甲酰氧-2a,3,4,4a,5,6,9,10,11,12,12a,12b-十二氢-4,6,11-三羟基-4a,8,13,13-四甲基-5-氧代-7,11-亚甲基-1H-环癸五烯并[3,4]苯并[1,2-b]氧杂丁环-9-基]酯。
化学结构式：分子式：C43H53NO14分子量：807.88Cas No：114977-28-5分子量：807.88辅料名称：柠檬酸，吐温-80，乙醇【性状】本品为黄色至棕黄色澄明油状液体。
【适应症】1.适用于局部晚期或转移性乳腺癌的治疗。
2.适用于局部晚期或转移性非小细胞肺癌的治疗，即使是在以顺铂为主的化疗失败后。
【规格】20mg【用法用量】多西他赛只能用于静脉滴注。
所有病人在接受多西他赛治疗前均必须口服糖皮质激素类药物，如地塞米松，在多西他赛滴注一天前服用，每天16mg，持续至少3天，以预防过敏反应和体液潴留。
多西他赛的推荐剂量为70-75mg/m2，静脉滴注一小时,每三周一次。
多西他赛注射液及溶剂使用说明：1.制备多西他赛预注射液1）若从冰箱中取出所需数目的多西他赛，需在室温下放置5分钟。
2）用一装有针头的刻度注射器将与多西他赛注射液对应的溶剂吸出。
3）将装药液的瓶子倾斜,将注射器中全部溶剂注入对应的多西他赛注射液瓶中。
4）拔出针管及针头,手工反复倒置混合至少45秒,不能摇动。
5）将混合后的药瓶室温放置5分钟，然后检查溶液是否均匀澄明（由于处方中含吐温-80，放置5分钟后通常还会有泡沫）。
原装道康宁PMX-0345（DC345）环硅氧烷混合物
INCI名称：DC-345环戊硅氧烷和环己硅氧烷
产品性质：
1、令皮肤有柔软丝质感觉
2、解粘性
3、改善涂布性能
4、清爽，非油腻性肤感
技术指标：
外观：无色透明液体
比重：0.957
折光：1.398
沸点：217℃
凝固点：<-50℃
闪点，闭杯：77℃
粘度：6Cs
环四硅氧烷（D4）含量：<1.0%
表面张力，达因：20.8/cm
DC345（PMX-0345）是由多种环状聚有机硅氧烷混合物组成，具有适当挥发性的有机硅聚合物，与许多化妆品组份有着很高的相溶性，
质感轻盈、清爽、不油腻,可改善配方、改善触感，且无长久性残留，是化妆品配方常用的理想原料。
广泛应用：
1、个人护理品的基油成分，铺展性良好，易涂抹，润滑并具有独特的挥发性。
2、止汗剂、去味剂、喷发胶、洗面奶、护肤霜、乳液等护理用品、沐浴油、晒黑剂、剃须用品、彩妆品、指甲油。
3、也可以用作粉类彩妆、香水、科隆香水及剃须膏的添加物。
4、用于条状物产品时，产品具有适宜的铺展性和挥发性。
注意事项：
1.产品应贮存在干净，密闭的容器中，避免接触酸，碱及混入其它杂质，不要接触明火。
2.产品按非危险品贮存运输。
3.产品的有效贮存期办三年，超过贮存期后应复检，合格可使用。
![3-碘-4-氨基吡唑并[3,4-d]嘧啶-安全技术说明书MSDS](https://img.taocdn.com/s1/m/5f90063d77c66137ee06eff9aef8941ea76e4bc7.png)
第一部分化学品及企业标识化学品中文名：3-碘-4-氨基吡唑并[3,4-d]嘧啶化学品英文名：3-Iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine4-Amino-3-iodo-1H-pyrazolo[3,4-d]pyridine CAS号：151266-23-8分子式：C5H4IN5产品推荐及限制用途：工业及科研用途。
第二部分危险性概述紧急情况概述造成皮肤刺激。
造成严重眼刺激。
可引起呼吸道刺激。
GHS危险性类别无危害分类标签要素：象形图：警示词：警告危险性说明：H315 造成皮肤刺激H317 可能导致皮肤过敏反应H319 造成严重眼刺激●预防措施：—— P264 作业后彻底清洗。
—— P280 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
—— P261 避免吸入粉尘/烟/气体/烟雾/蒸气/喷雾。
—— P272 受沾染的工作服不得带出工作场地。
●事故响应：—— P301+P310 如误吞咽：立即呼叫解毒中心/医生—— P330 漱口。
—— P302+P352 如皮肤沾染：用水充分清洗。
—— P332+P313 如发生皮肤刺激：求医/就诊。
—— P362+P364 脱掉沾染的衣服，清洗后方可重新使用—— P305+P351+P338 如进入眼睛：用水小心冲洗几分钟。
如戴隐形眼镜并可方便地取出，取出隐形眼镜。
继续冲洗。
—— P310 立即呼叫解毒中心/医生—— P304+P340 如误吸入：将人转移到空气新鲜处，保持呼吸舒适体位。
—— P312 如感觉不适，呼叫解毒中心/医生●安全储存：—— P403+P233 存放在通风良好的地方。
保持容器密闭。
—— P405 存放处须加锁。
●废弃处置：—— P501 按当地法规处置内装物/容器。
物理和化学危险：无资料。
健康危害：造成皮肤刺激。
可能导致皮肤过敏反应。
造成严重眼刺激。
环境危害：无资料。
第三部分成分/组成信息√物质混合物第四部分急救措施急救：吸入：如果吸入，请将患者移到新鲜空气处。
[药品名称]通用名称：注射用亚胺培南西司他丁钠商品名称：泰能?（TIENAM?）英文名称：Imipenem and Cilastatin Sodium for Injection汉语拼音：Zhusheyong Yaanpeinan Xisitadingna[成份]本品为复方制剂，其组份为亚胺培南500mg和西司他丁钠（以C16H26N2O5S计）500mg。
辅料为碳酸氢钠。
亚胺培南的化学结构式：分子式：C12H17N3O4S?H2O分子量：317.4西司他丁钠的化学结构式：分子式：C16H25N2O5SNa分子量：380.4[性状]本品为白色至类白色粉末。
[适应症]本品（注射用亚胺培南西司他丁钠）为一非常广谱的抗生素，特别适用于多种病原体所致和需氧/厌氧菌引起的混合感染，以及在病原菌未确定前的早期治疗。
本品适用于由敏感细菌所引起的下列感染:腹腔内感染、下呼吸道感染、妇科感染、败血症、泌尿生殖道感染、骨关节感染、皮肤软组织感染、心内膜炎本品适用于治疗由敏感的需氧菌/厌氧菌株所引起的混合感染。
这些混合感染主要与粪便、阴道、皮肤及口腔的菌株污染有关。
脆弱拟杆菌是这些混合感染中最常见的厌氧菌，它们通常对氨基糖甙类、头孢菌素类和青霉素类抗生素耐药，而对本品敏感。
已经证明本品对许多耐头孢菌素类的细菌，包括需氧和厌氧的革兰氏阳性及革兰氏阴性细菌所引起的感染仍具有强效的抗菌活性；这些细菌耐药的头孢菌素类抗生素包括头孢唑啉、头孢哌酮、头孢噻吩、头孢西丁、头孢噻肟、羟羧氧酰胺菌素、头孢孟多、头孢他啶和头孢曲松。
同样，许多由耐氨基糖甙类抗生素（如庆大霉素、阿米卡星、妥布霉素）或青霉素类（氨苄西林、羧苄西林、青霉素、替卡西林、哌拉西林、阿洛西林、美洛西林）的细菌引起的感染，使用本品仍有效。
本品不适用于脑膜炎的治疗。
预防对那些已经污染或具有潜在污染性外科手术的病人或术后感染一旦发生将会特别严重的操作，本品适用于预防这样的术后感染。
Lamivudine （拉米夫定）C 8H 11N 3O 3S229.26 2(1H )-Pyrimidinone, 4-amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-, (2R-cis )-.(–)-1-[(2R,5S )-2-(Hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine [134678-17-4]. » Lamivudine contains not less than 98.0 percent and not more than 102.0 percent of C 8H 11N 3O 3S, calculated on the anhydrous and solvent-free basis.在无水和无溶剂基础上计算，拉米夫定应含 (C 8H 11N 3O 3S)在90%-105%。
Packaging and storage — Preserve in well-closed, light-resistant containers. Store at room temperature.包装和贮存：保存在密闭容器中，和可控制温度处。
USP Reference standards 11—USP Lamivudine RS参考标准：美国药典拉米夫定的标准品 USP Lamivudine Resolution Mixture A RS由美国药典拉米夫定的标准品分离出来的混合物A USP Lamivudine Resolution Mixture B RS .由美国药典拉米夫定的标准品分离出来的混合物BIdentification —鉴别——A: Infrared Absorption 197M . 红外吸收<197m>B: The retention time of the major peak in the chromatogram of the Test solution corresponds to that in the chromatogram of the Resolution solution, as obtained in the test for Limit of lamivudine enantiomer.供试品溶液的主要色谱峰的保留时间与拉米夫定对映体的相对应。
白血病新药达沙替尼达沙替尼简介：通用名称：达沙替尼片商品名称：施达赛，SPRYCEL英文名称：Dasatinib Capsules汉语拼音：DashatiniPian成分：本品主要成分为达沙替尼，化学名称为：N-（2-氯-6甲基苯基）-2（{6-[4-（2-羟基乙基）哌嗪基-1]-2-甲基嘧啶基-4}氨基）-1,3-噻唑-5-酰胺-水合物。
化学结构式：分子式：C22H26ClN2O2S·H2O分子量：488.01（无水游离基）；506.02（水合物）临床应用：达沙替尼（Dasatinib/Sprycel），用于已经治疗，包括甲磺酸伊马替尼（Imatinibmesylate/Gleevec）耐药或不能耐受的慢性骨髓性白血病所有病期（慢性期、加速期、淋巴系细胞急变期和髓细胞急变期）的成人患者。
同时，FDA也经正常程序批准达沙替尼治疗对其他疗法耐药或不能耐受的费城染色体阳性的急性淋巴细胞性白血病成人患者。
达沙替尼属多酪氨酸激酶抑制剂，此次主要是依据来自总计包括911例患者的4项国际性、多中心Ⅱ期试验的安全性和疗效结果及其他支持性数据而获准用于上述两适应证的。
它在临床研究中最常报告的副反应有体液潴留、胃肠道症状和出血事件等；最常报告的严重副反应是发热、胸膜积液、发热性中性白)用于粒细胞白血病(CML)6月29日，FDA批准了百时美施贵宝的Sprycel(dasatinib)用于成年患者，治疗两种新的适应症：对伊马替尼等一线药物化疗不敏感的各期慢性粒细胞白血病(CML)，以及对其他疗法无效或不能耐受的Ph染色体阳性的急性淋巴细胞白血病(ALL)。
在已批准上市的药物中，Sprycel是第一种能够抑制多种构型酪氨酸蛋白激酶Abl的口服化疗药。
在纳摩尔浓度，该药能抑制Bcr-Abl, SRC 激酶家族(SRC, LCK, YES, FYN), c-KIT, EPHA2, 和PDGFR-B等多种激酶。
通过抑制上述激酶的作用，Sprycel可抑制CML和Ph+ ALL骨髓中白血病细胞的增殖，但正常红细胞、白细胞和血小板仍可继续增殖。
USP34--地塞⽶松磷酸钠注射液和地塞⽶松磷酸钠原料Dexamethasone Sodium Phosphate InjectionDexamethasone Sodium Phosphate Injection is a sterile solution of Dexamethasone Sodium Phosphate in Water for Injection. It contains not less than 90.0 percent and not more than 115.0 percent of the labeled amount of dexamethasone phosphate (C22H30FO8P), present as the disodium salt.Packaging and storage—Preserve in single-dose or multiple-dose containers, preferably of Type I glass, protected from light. USP Reference standards 11—USP Dexamethasone RSUSP Dexamethasone Phosphate RSUSP Endotoxin RSIdentification—Pipet a volume of Injection, equivalent to 10 mg of dexamethasone phosphate, into a 100-mL volumetric flask, add water to volume, and mix. Pipet 5 mL of this solution into a 125-mL separator, and wash with two 10-mL portions of water-washed methylene chloride, discarding the washings. Transfer the solution into a glass-stoppered, 50-mL tube, and add 5 mL of alkaline phosphatase solution, prepared by dissolving 50 mg of alkaline phosphatase enzyme in 50 mL of pH 9 Bufferwith magnesium (prepared as directed in Identification test A under Dexamethasone Sodium Phosphate). Allow to stand at 37 for 45 minutes, and extract with 25 mL of methylene chloride. Evaporate 15 mL of the methylene chloride extract on a steam bath to dryness, and dissolve the residue in 1 mL of methylene chloride. Apply 5 µL of this solution and 5 µL of a solution of USP Dexamethasone RS in methylene chloride containing 300 µg per mL to a 20- × 20-cm, thin-layer chromatographic plate (see Chromatography 621) coated with a 0.25-mm layer of chromatographic silica gel. Allow the spots to dry, and develop the chromatogram in a tank completely lined with a strip of filter paper, using a solvent system consisting of a mixture of 50 parts of chloroform, 50 parts of acetone, and 1 part of water, until the solvent front has moved about three-fourths of the length of the plate. Remove the plate from the developing tank, mark the solvent front, and allow the spots to dry. Spray the plate with dilute sulfuric acid (1 in 2), and heat at 105 until brown or black spots appear: the RF value of the principal spot obtained from the test specimen corresponds to that obtained from the Reference Standard.Bacterial endotoxins 85— It contains not more than 31.3 USP Endotoxin Units per mg of dexamethasone phosphate.pH 791: between 7.0 and 8.5.Other requirements— It meets the requirements under Injections 1.Assay—Mobile phase—Prepare a suitable degassed solution of 0.01 M monobasic potassium phosphate in a mixture of methanol and water (1:1) which, at ambient temperature and at a flow rate of about 1.6 mL per minute, gives a retention time of about 5 minutes for dexamethasone phosphate.Standard preparation— [note—Prepare this solution at the time of use. ] Dissolve an accurately weighed quantity of USP Dexamethasone Phosphate RS in Mobile phase to obtain a solution having a known concentration of about 80 µg per mL. Assay preparation— Transfer an accurately measured volume of Injection, equivalent to about 8 mg of dexamethasone phosphate, to a 100-mL volumetric flask. Dilute with Mobile phase to volume, and mix. Chromatographic system (see Chromatography 621)—The liquid chromatograph is equipped with a 254-nm detector and a 4-mm × 30-cm column that contains packing L1. Chromatograph five replicate injections of the Standard preparation, and record the peak responses as directed under Procedure: the relative standard deviation is not more than 1.5%. Procedure—By means of a suitable sampling valve, separately inject equal volumes (about 20 µL) of the Standard preparation and the Assay preparation into the chromatograph, record the chromatograms, and measure the responses for the major peaks. Calculate the quantity, in mg,of C22H30FO8P in each mL of the Injection taken by the formula:0.1(C / V)(rU / rS)in which C is the concentration, in µg per mL, of USP Dexamethasone Phosphate RS in the Standard preparation, V is the volume, in mL, of Injection taken, and rU and rS are the peak responses at equivalent retention times obtained from the Assay preparation and the Standard preparation, respectively.原料部分USP34Dexamethasone Sodium Phosphate(dex'' a meth' a sone soe' dee um fos' fate).C22H28FNa2O8P 516.41Pregna-1,4-diene-3,20-dione, 9-fluoro-11,17-dihydroxy-16-methyl-21-(phosphonooxy)-, disodium salt, (11,16)-.9-Fluoro-11,17,21-trihydroxy-16-methylpregna-1,4-diene-3,20-dione 21-(dihydrogen phosphate) disodium salt [2392-39-4]. Dexamethasone Sodium Phosphate contains not less than 97.0 percent and not more than 102.0 percent ofC22H28FNa2O8P, calculated on the water-free and alcohol-free basis. Packaging and storage— Preserve in tight containers.USP Reference standards 11—USP Dexamethasone RSUSP Dexamethasone Phosphate RSIdentification—A: pH 9 Buffer with magnesium—Mix 3.1 g of boric acid and 500 mL of water in a 1-L volumetric flask, add 21 mL of 1 N sodium hydroxide and 10 mL of 0.1 M magnesium chloride, dilute with water to volume, and mix.Alkaline phosphatase solution— Transfer 95 ± 5 mg of alkaline phosphatase enzyme to a 50-mL volumetric flask, dissolve by adding pH 9 Buffer with magnesium to volume, and mix. Prepare this solution fresh daily.Standard solution—Weigh 15 mg of USP Dexamethasone RS into a 5-mL volumetric flask. Dissolve in and dilute with ethyl acetate to volume. [note—Sonication may be required to ensure dissolution. ]Test solution— Weigh 20 mg of Dexamethasone Sodium Phosphate into a 15-mL centrifuge tube. Add 5.0 mL of Alkaline phosphatase solution, shake vigorously, and allow to stand for 30 minutes. Add 5.0 mL of ethyl acetate, shake vigorously, centrifuge, and use the upper, ethyl acetate layer. Procedure— Apply 10-µL portions of the Test solution and the Standard solution to a thin-layer chromatographic plate (see Chromatography 621) coated with a 0.25-mm layer of chromatographic silica gel mixture. Develop the chromatogram in a mobile phase consisting of a mixture of chloroform, methanol, and water (180:15:1) to a distance of three-fourths of the length of the plate. Air-dry the plate and observe under short-wavelength UV light: the RF value of the principal spot obtained from the Test solution corresponds to that obtained from the Standard solution.B: The residue from the ignition of it meets the requirements of the tests for Phosphate 191 and for Sodium 191.Specific rotation 781S: between +74 and +82, calculated on the water-free and alcohol-free basis. Test solution: 10 mg per mL, in water.pH 791: between 7.5 and 10.5, in a solution (1 in 100).Water, Method I 921—Determine the water content. The sum of the percentages of water content, and alcohol content, determined as directed in the test for Alcohol, does not exceed 16.0%.Limit of phosphate ions—Standard phosphate solution—Dissolve 143.3 mg of dried monobasic potassium phosphate, KH2PO4, in water to make 1000.0 mL. This solution contains the equivalent of 0.10 mg of phosphate (PO4) in each mL.Phosphate reagent A— Dissolve 5 g of ammonium molybdate in 1 N sulfuric acid to make 100 mL. Phosphate reagent B—Dissolve 350 mg of p-methylaminophenol sulfate in 50 mL of water, add 20 g of sodium bisulfite, mix to dissolve, and dilute with water to 100 mL.Procedure— Dissolve about 50 mg of Dexamethasone Sodium Phosphate, accurately weighed, in a mixture of 10 mL of water and 5 mL of 2 N sulfuric acid contained in a 25-mL volumetric flask, by warming if necessary. Add 1 mL each of Phosphate reagent A and Phosphate reagent B, dilute with water to 25 mL, mix, and allow to stand at room temperature for 30 minutes. Similarly and concomitantly, prepare a standard solution, using 5.0 mL of Standard phosphate solution instead of the 50 mg of the substance under test. Concomitantly determine the absorbances of both solutions in 1-cm cells at 730 nm, with a suitable spectrophotometer, using water as the blank. The absorbance of the test solution is not more than that of thestandard solution. The limit is 1.0% of phosphate (PO4).Limit of free dexamethasone—Mobile phase— Prepare a solution containing 7.5 mL of triethylamine in 1 L of water. Adjust by the addition of phosphoric acid to a pH of 5.4. Prepare a filtered and degassed mixture of 74 parts of the resulting solution with 26 parts of methanol. Make adjustments if necessary (see System Suitability under Chromatography 621).Standard solution— Dissolve an accurately weighed quantity of USP Dexamethasone Phosphate RS in Mobile phase to obtain a solution containing about 0.5 mg per mL. Prepare a second solution by dissolving an accurately weighed quantity of USP Dexamethasone RS in a mixture of methanol and water (1:1) to obtain a solution containing about 50 µg per mL. Transfer 10.0 mL of the first solution and 1.0 mL of the second solution to a 100-mL volumetric flask. Dilute with Mobile phase to volume, and mix to obtain a solution having known concentrations of 50 µg of USP Dexamethasone Phosphate RS per mL and 0.5 µg of USP Dexamethasone RS per mL.Test solution— Transfer about 50 mg of Dexamethasone Sodium Phosphate, accurately weighed, to a 100-mL volumetric flask, dissolve in and dilute with Mobile phase to volume, and mix. Further dilute 5.0 mL of this solution with Mobile phase to 50.0 mL.System suitability solution— Prepare a solution in Mobile phase containing in each mL 0.05 mg of USP Dexamethasone Phosphate RS and 0.02 mg of USP Dexamethasone RS. Chromatographic system (see Chromatography 621)—The liquid chromatograph is equipped with a 254-nm detector and a 4.5-mm × 25-cm column that contains 5-µm packing L11. The flow rate is about 1.2 mL per minute. Chromatograph the Standard solution and the System suitabilitysolution, record the peak responses as directed for Procedure, and determine the chromatographic characteristics from chromatograms obtained from the System Suitability: the column efficiency determined from the analyte peak is not less than 900 theoretical plates; the tailing factor for the analyte peak is not more than 1.6; the resolution, R, between dexamethasone phosphate and dexamethasone is not less than 1.8; and the relative standard deviation for replicate injections is not more than 1.0%.Procedure— Separately inject equal volumes (about 20 µL) of the Standard solution and the Test solution into the chromatograph, record the chromatograms, and measure the responses for the dexamethasone peaks. Calculate the quantity, in µg, of dexamethasone (C22H29FO5) in the portion of Dexamethasone Sodium Phosphate taken by the formula:1000C(rU / rS)in which C is the concentration, in µg per mL, of USP Dexamethasone RS in the Standard solution; and rU and rS are the peak responses obtained from the Test solution and the Standard solution, respectively: not more than 1.0% is found. Chromatographic purity—Acetate buffer— Dissolve 7 g of ammonium acetate in 1 L of water, adjust with glacial acetic acid to a pH of 4.0, and mix.Solution A—Prepare a filtered and degassed mixture of methanol, water, and Acetate buffer (7:7:6). Make adjustments if necessary (see System Suitability under Chromatography 621). Solution B— Prepare a filtered and degassed mixture of methanol and Acetate buffer (7:3). Make adjustments if necessary (see System Suitability under Chromatography 621). Mobile phase—Use variable mixtures of Solution A and Solution B as directed for Chromatographic system.Test solution— Transfer about 25 mg of Dexamethasone Sodium Phosphate, accurately weighed, to a 25-mL volumetic flask, dissolve in and dilute with Solution A to volume, and mix. Chromatographic system (see Chromatography 621)—The liquid chromatograph is equipped witha 254-nm detector and a 4.6-mm × 25-cm column that contains packing L7. The flow rate is about1 mL per minute. The column temperature is maintained at 40. The chromatograph is programmed as follows.Time(minutes) Solution A(%) Solution B(%) Elution0 90 10 equilibration0–3.5 90 10 isocratic3.5–23.5 90?60 10?40 linear gradient23.5–34.5 60?5 40?95 linear gradient34.5–59.5 5 95 isocratic59.5–60 5?90 95?10 linear gradientChromatograph the Test solution, and record the peak responses as directed for Procedure: the resolution between the major peak and the nearest impurity is not less than 1.0; and the relative standard deviation for replicate injections is not more than 4.0%.Procedure—Separately inject equal volumes (about 15 µL) of the Test solution into thechromatograph, record the chromatogram, and measure the peak responses. Calculate the percentage of each impurity in the portion of Dexamethasone Sodium Phosphate taken by the formula:100(ri / rs)in which ri is the peak response for each impurity; and rs is the sum of the responses of all peaks: not more than 1.0% of any individual impurity is found, and not more than 2.0% of total impurities is found.Alcohol content, Method II 611—Proceed as directed in the chapter except to use column packing S8 and to use the following modifications.Internal standard solution— Pipet 1 mL of isopropyl alcohol into a 100-mL volumetric flask, add water to volume, and mix.Standard stock solution— Prepare a solution of alcohol in water (1 in 50). Determine the specific gravity at 25 (see Specific 841), and obtain the percentage of C2H5OH by reference to the Alcoholometric Table in the section Reference Tables.Standard solution— Into a 10-mL volumetric flask pipet 4 mL of Standard stock solution and 5 mL of Internal standard solution, add water to volume, and mix. Inject 2 µL of this solution into the gas chromatograph.Test solution— Transfer about 500 mg of Dexamethasone Sodium Phosphate, accurately weighed, into a 10-mL volumetric flask. Pipet 5 mL of Internal standard solution into the flask, and mix to dissolve. Add water to volume, and mix. Inject 2 µL of this solution into the gas chromatograph. Calculation—Calculate the percentage of alcohol in the Dexamethasone Sodium Phosphate taken by the formula:4(S / W)(Z / Y)in which S is the percentage of alcohol in the Standard stock solution; W is the weight, in g, of Dexamethasone Sodium Phosphate used in the Test solution; and Y and Z are the ratios of the alcohol peak heights to the internal standard peak heights for the Standard solution and the Test solution, respectively. The content of C2H5OH is not more than 8.0%.Assay—Buffer solution— Dissolve 7.0 g of ammonium acetate in 1 L of water, adjust with glacial acetic acid to a pH of 4.00 ± 0.05, and mix.Solution A—Prepare a filtered and degassed mixture of methanol, water, and Buffer solution (350:350:300).Solution B— Prepare a filtered and degassed mixture of methanol and Buffer solution (700:300). Mobile phase—Use variable mixtures of Solution A and Solution B as directed for Chromatographic system. Make adjustments if necessary (see System Suitability under Chromatography 621).Standard preparation—Dissolve an accurately weighed quantity of USP Dexamethasone Phosphate RS in Solution A to obtain a solution having a known concentration of about 0.92 mg per mL.Assay preparation—Dissolve an accurately weighed quantity of Dexamethasone Sodium Phosphate in Solution A, and mix to obtain a solution having a concentration of about 1.0 mg per mL.Chromatographic system (see Chromatography 621)—The liquid chromatograph is equipped with a 254-nm detector and a 4.6-mm × 25-cm column that contains packing L7. The columntemperature is maintained at about 40. The flow rate is about 1.0 mL per minute. The chromatograph is programmed as follows.Time(minutes) Solution A(%) Solution B(%) Elution0 90 10 equilibration0–3.5 90 10 isocratic3.5–24 90?60 10?40 linear gradient24–35 60?5 40?95 linear gradient35–60 5 95 isocratic60–60.1 5?90 95?10 linear gradient60.1–65 90 10 isocraticChromatograph the Standard preparation, and record the peak responses as directed for Procedure: the relative standard deviation is not more than 2.0%. Chromatograph the Assay preparation, and record the peak responses as directed for Procedure: the resolution, R, between dexamethasone phosphate and the nearest impurity eluting after it is not less than 1.0. Procedure— Separately inject equal volumes (about 15 µL) of the Standard preparation and the Assay preparation into the chromatograph, record the chromatograms, and measure the areas for the major peaks. Calculate the quantity, in mg, ofC22H28FNa2O8P in the portion of Dexamethasone Sodium Phosphate taken by the formula:(516.41 / 472.45)C(rU / rS)in which 516.41 and 472.45 are the molecular weights of dexamethasone sodium phosphate and dexamethasone phosphate, respectively; C is the concentration, in mg per mL, of USP Dexamethasone Phosphate RS in the Standard preparation; and rU and rS are the peak responses obtained from the Assay preparation and the Standard preparation, respectively.。
甲苯磺酸索拉非尼片中文说明书【药品名称】通用名称：甲苯磺酸索拉非尼片商品名称：多吉美英文名称：Sorafenib Tosylate Tablets汉语拼音：Jiabenhuangsuan Suolafeini Pian【性状】多吉美主要成分为甲苯磺酸索拉非尼，是一种多激酶抑制剂。
化学名称为4—(4—｛3—［4-氯—3-(三氟甲基)苯基]脲基}苯氧基)—N2-甲基吡啶-2—羧酰胺—4—甲苯磺酸盐，化学结构式为：多吉美是白色至淡黄色或浅棕色固体,分子式为C21H16ClF3N4O3 x C7H8O3S,分子量为637。
多吉美几乎不溶于水介质，微溶于乙醇（酒精)，溶于聚乙二醇400。
每片有色薄膜包衣药片包含甲苯磺酸索拉非尼(274mg）,相当于200mg的索拉非尼和以下非活性成分：交联羧甲基纤维素钠，羟丙基甲基纤维素，硬脂酸镁，微晶纤维素，聚乙二醇，十二烷基硫酸钠,二氧化钛和氧化铁红。
【临床药理】作用机理索拉非尼是多种激酶抑制剂，抑制肿瘤细胞的靶部位（CRAF、BRAF、mutantBRAF）和肿瘤血管靶部位（KIT、FLT-3、RET、VEGFR—1、VEGFR—2、VEGFR-3、PDGFR—β）。
这些激酶作用于肿瘤细胞信号通路、血管生成和凋亡。
药物代谢动力学索拉非尼的半衰期约为25-48小时。
与单剂量给药相比，重复给药可导致药物蓄积。
给药7天后，索拉非尼血药浓度达到稳态，平均血药浓度峰谷比小于2。
与口服溶液相比，服用索拉非尼片剂平均相对生物利用度为38% — 49％.吸收与分布索拉非尼口服后约3小时达到最高血药浓度。
饮食可导致索拉非尼的生物利用率下降，建议用药时禁止饮食。
代谢与清除索拉非尼主要通过肝脏代谢。
血药浓度达到稳态时，索拉非尼在血浆中约占全部血液分析物70％-85%的比例。
索拉非尼有8个已知代谢产物，其中5个在血浆中被检出。
索拉非尼在血浆中的主要循环代谢产物为吡啶类-N-氧化物.体外试验表明，该物质的效能与索拉非尼相似，它包含了稳态血浆中约9% — 16％的血液分析物。
2632Doxapram / Official Monographs USP 34Add 5mL of 2.5N sodium hydroxide, and extract with three15-mL portions of chloroform. Pass each extract through a Doxazosin Mesylatepledget of glass wool, combine the filtrates in a 50-mL volu-metric flask, dilute with chloroform to volume, and mix. Evapo-rate to dryness about 5mL of this solution. Dissolve the residuein 0.01N sulfuric acid, dilute with the same solvent to 100mL,and mix: the UV absorption spectrum of the solution so ob-tained exhibits maxima and minima at the same wavelengths asa solution similarly prepared, about 50mg of USP DoxapramHydrochloride RS, instead of Doxapram Hydrochloride Injection,C23H25N5O5·CH4O3S 547.58being used.Piperazine, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-[(2,3-Bacterial endotoxins 〈85〉—It contains not more than 3.3dihydro-1,4-benzodioxin-2-yl)carbonyl]-,USP Endotoxin Units per mg of doxapram hydrochloride.monomethanesulfonate.pH 〈791〉:between 3.5 and 5.0.1-(4-Amino-6,7-dimethoxy-2-quinazolinyl)-4-(1,4-benzodioxan-Other requirements—It meets the requirements under Injec-2-ylcarbonyl)piperazine monomethanesulfonate[77883-43-tions 〈1〉.3].Assay—» Doxazosin Mesylate contains not less than 98.0 Mobile phase—Dissolve 2.8g of monobasic potassium phos-percent and not more than 102.0 percent of phate in 1 L of water, adjust with 50% phosphoric acid or 1NC23H25N5O5·CH4O3S, calculated on the dried potassium hydroxide to a pH of 3.0±0.1, and filter through a0.5-µm or finer porosity filter. Prepare a suitable mixture of this basis.solution and acetonitrile (65:35). Make adjustments if neces-Packaging and storage—Preserve in well-closed containers, sary (see System Suitability under Chromatography 〈621〉).and store below 30°.Internal standard solution—Prepare a solution of diphenhy-dramine hydrochloride in water containing about 1.5mg per USP Reference standards 〈11〉—P Doxazosin Mesylate RSStandard preparation—Dissolve an accurately weighed quan-USP Doxazosin Related Compound A RStity of USP Doxapram Hydrochloride RS in water to obtain a N-1,4-Benzodioxane-2-carbonyl piperazine.solution having a known concentration of about 2mg per mL.C13H16N2O3248.28Transfer 5.0mL of this solution and 5.0mL of Internal standard USP Doxazosin Related Compound B RSsolution to a 50-mL volumetric flask, dilute with water to vol-6,7-Dimethoxyquinazoline-2,4-dione.ume, and mix.C10H10N2O4222.20Assay preparation—Transfer an accurately measured volume USP Doxazosin Related Compound C RSof Injection, equivalent to about 100mg of doxapram hydro-2-Chloro-4-amino-6,7-dimethoxyquinazoline.chloride monohydrate, to a 50-mL volumetric flask, dilute with C10H10ClN3O2239.66water to volume, and mix. Transfer 5.0mL of this solution and USP Doxazosin Related Compound D RS5.0mL of Internal standard solution to a 50-mL volumetric flask,1,4-Benzodioxane-2-carboxylic acid.dilute with water to volume, and mix.C9H8O5196.16USP Doxazosin Related Compound E RS Chromatographic system (see Chromatography 〈621〉)—The2,4-Dichloro-6,7-dimethoxyquinazoline.liquid chromatograph is equipped with a 225-nm detector andC10H8Cl2N2O2259.09a 4.6-mm × 15-cm column containing 5-µm packing L10, andUSP Doxazosin Related Compound F RSis maintained at 40°. The flow rate is about 1.5mL per minute.N,N′-Bis(1,4-benzodioxane-2-carbonyl)piperazine. Chromatograph the Standard preparation, and record the re-C22H22N2O6410.42sponses as directed under Procedure: the relative retention timesUSP Terazosin Related Compound A RSare about 1.0 for doxapram and 1.2 for diphenhydramine, the1-(4-Amino-6,7-dimethoxy-2-quinazolinyl)piperazine, resolution, R, between the doxapram and diphenhydraminedihydrochloride.peaks is not less than 3.0; the tailing factor for the peaks is notC14H19N5O2·2HCl362.25more than 2.0, and the relative standard deviation for replicateUSP Terazosin Related Compound C RSinjections is not more than 2.0%.1,4-Bis(4-amino-6,7-dimethoxy-2-quinazolinyl)piperazine, Procedure—Separately inject equal volumes (about 5 µL) ofdihydrochloride.the Standard preparation and the Assay preparation into theC24H28N8O4·2HCl565.45chromatograph, record the chromatograms, and measure theIdentification—responses for the major peaks. Calculate the quantity, in mg, ofdoxapram hydrochloride hydrate (C24H30N2O2·HCl·H2O) in A:Infrared Absorption 〈197K〉.each mL of the Injection taken by the formula:B:The retention time of the major peak in the chromato-gram of the Assay preparation corresponds to that in the chro-(432.98/414.98)(500C/V)(R U/R S)matogram of the Standard preparation, as obtained in the Assay.Loss on drying 〈731〉—Dry it in vacuum at 105° for 4 hours: it in which 432.98 and 414.98 are the molecular weights of dox-loses not more than 2.0% of its weight.apram hydrochloride monohydrate and anhydrous doxapramResidue on ignition 〈281〉:not more than 0.1%. hydrochloride, respectively, C is the concentration, in mg permL, of USP Doxapram Hydrochloride RS in the Standard prepa-Heavy metals, Method II 〈231〉:20µg per g.ration, V is the volume, in mL, of Injection taken to prepare the Related compounds—Assay preparation, and R U and R S are the ratios of the peak re-Solvent A, Solvent D, Mobile phase, System suitability solution, sponses of doxapram and diphenhydramine obtained from the and Chromatographic system—Proceed as directed in the Assay. Assay preparation and the Standard preparation, respectively.Solvent B—Use acetonitrile.Solvent C—Use water.Mobile phase—Use variable mixtures of Solvent A, Solvent B,and Solvent C as directed for Chromatographic system in theAssay. Make adjustments if necessary (see System Suitabilityunder Chromatography 〈621〉).USP 34Official Monographs / Doxazosin2633Standard solution—Dissolve accurately weighed quantities of of the related compounds. The final ratio of Solvent C to Solvent USP Doxazosin Mesylate RS, USP Doxazosin Related Compound D is maintained at 9:1. Sonicate briefly to dissolve completely.A RS, USP Doxazosin Related CompoundB RS, USP Doxazosin Standard preparation—Dissolve an accurately weighed quan-Related CompoundC RS, USP Doxazosin Related CompoundD tity of USP Doxazosin Mesylate RS in approximately 2mL of RS, USP Doxazosin Related CompoundE RS, USP Doxazosin Solvent D, and dilute with Solvent C and Solvent D to obtain a Related CompoundF RS, USP Terazosin Related Compound A solution having a known concentration of 0.6mg per mL. The RS, and USP Terazosin Related Compound C RS in approxi-final ratio of Solvent C to Solvent D is maintained at 9:1. Soni-mately 2mL of Solvent D; and dilute quantitatively, and step-cate briefly to dissolve completely.wise if necessary, with Solvent C and Solvent D to obtain a solu-Assay preparation—Dissolve an accurately weighed quantity tion having a known concentration of 0.0015mg per mL of of Doxazosin Mesylate in approximately 2mL of Solvent D, each of the Reference Standards. The final ratio of Solvent C to and dilute with Solvent C and Solvent D to obtain a solution Solvent D is maintained at 9:1. Sonicate briefly to dissolve having a concentration of 0.6mg per mL, based on the labeled completely.quantity of doxazosin mesylate. The final ratio of Solvent C to Test solution—Dissolve an accurately weighed quantity of Solvent D is maintained at 9:1. Sonicate briefly to dissolve Doxazosin Mesylate in approximately 2mL of Solvent D, and completely.dilute with Solvent C and Solvent D to obtain a solution having Chromatographic system (see Chromatography 〈621〉)—Thea known concentration of 0.6mg per mL. The final ratio of liquid chromatograph is equipped with a 210-nm detector and Solvent C to Solvent D is maintained at 9:1. Sonicate briefly to a 4-mm × 25-cm column that contains 5-µm packing L1. The dissolve completely.flow rate is about 0.8mL per minute, and the column tempera-Procedure—Separately inject equal volumes (about 10 µL) of ture is maintained at 35°. The chromatograph is pro-the Standard solution and the Test solution into the chromato-grammed as follows.graph, record the chromatograms, and measure the responsesfor all the peaks. Calculate the percentage of each impurity inthe portion of Doxazosin Mesylate taken by the formula:SolventTime A Solvent B Solvent C100(C S/C T)(r i/r S)(min)(%)(%)(%)Elution0–102010→2270→58linear gradientin which C S is the concentration, in mg per mL, of each Refer-10–352022→5058→30linear gradient ence Standard in the Standard solution; C T is the concentration,35–40205030equilibrationin mg per mL, of Doxazosin Mesylate in the Test solution; r i isthe peak response for each individual impurity obtained from[NOTE—Between sample injections, the system is re-equilibratedthe Test solution; and r S is the peak response for each individual for at least 7 minutes, or until a stable baseline is obtained,impurity obtained from the Standard solution: not more than representing the starting composition.]0.3% of terazosin related compound A is found; not more thanChromatograph the System suitability solution, and record the 0.25% of any other identified individual impurity is found; notpeak responses as directed for Procedure: the resolution, R, be-more than 0.10% of any other unidentified impurity is found;tween doxazosin related compound A and doxazosin related and not more than 1.0% of total impurities is found. Calculatecompound B is not less than 4.the percentages of doxazosin related compound G and dox-Procedure—Separately inject equal volumes (about 10 µL) of azosin related compound H [NOTE—The doxazosin related com-the Standard preparation and the Assay preparation into the pound G is the mesylate salt and has the same retention timechromatograph, record the chromatograms, and measure the as that of the terazosin related compound A. The doxazosinresponses for the doxazosin mesylate peaks. Calculate the per-related compound H is the mesylate salt and has the same re-centage of C23H25N5O5·CH4O3S in the portion of Doxazosin tention time as that of the doxazosin related compound C.] inMesylate taken by the formula:the portion of Doxazosin Mesylate taken by the formula:100(C S/C T)(r U/r S)(100/F)(C S/C T)(r i/r S)in which C S is the concentration, in mg per mL, of USP Dox-in which the response factor, F, is 0.735 for doxazosin relatedazosin Mesylate RS in the Standard preparation; C T is the con-compound G and 0.769 for doxazosin related compound H; C Scentration, in mg per mL, of Doxazosin Mesylate in the Assayis the concentration, in mg per mL, of USP Doxazosin Mesylatepreparation; and r U and r S are the peak responses obtained from RS in the Standard solution; C T is the concentration, in mg perthe Assay preparation and the Standard preparation, respectively. mL, of Doxazosin Mesylate in the Test solution; r i is the peakresponse of doxazosin related compound G or doxazosin re-lated compound H in the Test solution; and r S is the peak re-sponse of USP Doxazosin Mesylate RS in the Standard solution.Assay—Doxazosin TabletsSolvent A—Dissolve 5g of phosphoric acid (84%–86%) in100mL of water.» Doxazosin Tablets contain an amount of dox-Solvent B—Use acetonitrile.azosin mesylate equivalent to not less than 90.0 Solvent C—Use water.percent and not more than 110.0 percent of the Solvent D—Prepare a mixture of 100mL of Solvent B and 2g labeled amount of doxazosin (C23H25N5O5).of phosphoric acid (84%–86%).Mobile phase—Use variable mixtures of degassed Solvent A,Packaging and storage—Preserve in tight containers. Solvent B, and Solvent C, as directed for Chromatographic system.USP Reference standards 〈11〉—Make adjustments if necessary (see System Suitability underUSP Doxazosin Mesylate RSChromatography 〈621〉).Identification—The retention time of the major peak in the System suitability solution—Dissolve accurately weighed quan-chromatogram of the Assay preparation corresponds to that in tities of USP Doxazosin Related Compound A RS and USP Dox-the chromatogram of the Standard preparation, as obtained in azosin Related Compound B RS in approximately 2.5mL ofthe Assay.Solvent D. Further dilute this solution quantitatively, and step-wise if necessary, with Solvent C and Solvent D to obtain a finalsolution having a known concentration of 12µg per mL of each。
