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伊立替康化学式伊立替康（英文名：Ibuprofen）是一种非处方药，常用于缓解轻至中度的疼痛和减轻发热。
它属于非甾体抗炎药（英文名：Non-steroidal anti-inflammatory drugs, NSAIDs）的一种。
伊立替康的化学式为C13H18O2。
1. 伊立替康的介绍伊立替康是一种白色晶体粉末，无臭，可溶于乙醇和醚，微溶于水。
它的分子式为C13H18O2，相对分子质量为206.29。
伊立替康具有镇痛、抗炎和退热的作用，是一种非鸦片类镇痛剂。
2. 伊立替康的药理作用伊立替康通过抑制环氧合酶（英文名：cyclooxygenase, COX）的活性，抑制前列腺素的合成，从而减少疼痛、炎症和发热。
它主要对COX-1和COX-2起作用，可减少组织内的前列腺素合成，减轻相关症状。
3. 伊立替康的适应症和用法用量伊立替康主要用于缓解轻度和中度疼痛，例如头痛、牙痛、肌肉痛等。
它还可用于减轻发热症状。
对于关节炎和风湿性关节炎等慢性疼痛和炎症，伊立替康的使用也较为常见。
伊立替康可口服，一般为每次200-400毫克，每日3-4次，餐后服用。
使用时应遵循医生的建议和药物说明。
4. 伊立替康的注意事项尽管伊立替康是非处方药，但在使用时仍需注意以下事项：4.1. 遵循剂量和用法用量：不要超过建议的剂量和使用频率。
过量使用可能会增加不良反应的风险。
4.2. 注意过敏反应：某些个体可能对伊立替康过敏，包括对其他NSAIDs（如阿司匹林）的过敏。
在使用该药物前，应告知医生自己是否有过敏史。
4.3. 长期使用的风险：长期或高剂量使用伊立替康可能会增加心血管事件（如心脏病和中风）的风险。
因此，应遵循医生的建议，并尽量避免长期或过量使用。
4.4. 孕妇和哺乳期妇女的使用：孕妇和哺乳期妇女在使用伊立替康前应咨询医生。
长期或过量使用可能对胎儿或婴儿产生不良影响。
4.5. 与其他药物的相互作用：伊立替康可能与其他药物发生相互作用，包括处方药和非处方药。
伊立替康1概述伊立替康（Irinotecan）为半合成水溶性喜树碱类衍生物。
本品及其代谢产物SN38为DNA拓扑异构酶Ⅰ抑制剂，其与拓扑异构酶Ⅰ及DNA形成的复合物能引起DNA单链断裂，阻止DNA复制及抑制RNA合成，为细胞周期S期特异性。
2适应证为晚期大肠癌的一线用药，也可用于术后的辅助化疗；对肺癌、乳腺癌、胰腺癌等也有一定疗效。
3临床应用单药治疗，静滴：每次350mg/m2，滴注30～90分钟，每3周1次。
根据患者具体情况可适当减量。
4不良反应本品的主要剂量限制性毒性为延迟性腹泻和中性粒细胞减少。
1.延迟性腹泻发生率为80%～90%，其中严重者占39%。
中位发生时间为用药后第5天，平均持续4天，严重者可致死。
用药24小时后出现的腹泻均应视为延迟性腹泻，一旦出现第一次水样便或腹部异常肠蠕动，应立即开始口服洛哌丁胺，首剂4mg，以后2mg，每2小时一次，至少12小时，直到末次水样便后继续用药12小时，最常用药时间不超过48小时。
若48小时后仍有腹泻，应开始预防性口服广谱抗生素（喹诺酮类）7天，并换用其他止泻治疗。
2.严重中性粒细胞减少发生率39.6%。
胃肠反应（恶心、呕吐）常见，但不严重。
中性粒细胞减少不推荐预防性应用非格司亭（G-CSF）或沙格司亭（GM-CSF）。
若第一周出现严重延迟性中性粒细胞减少，可考虑应用。
3.其他若乙酰胆碱综合征包括“早期”腹泻（24小时内出现），出汗，唾液增多，视力障碍，痉挛性腹泻，流泪。
若出现严重上述症状，可给予阿托品0.25mg皮下注射。
第一周期不主张预防性用阿托品，但若出现严重症状，包括早期腹泻，下一周期可预防性给阿托品0.25mg皮下注射。
黏膜炎，脱发，乏力，和皮肤毒性等均较轻。
4.对肝功能的影响在无进展性肝转移的患者中单药治疗，血清中短暂、轻至中度氨基转移酶、碱性磷酸酶、胆红素水平升高的发生率分别为9.2%、8.1%和1. 8%。
7.3%的患者出现短暂的轻至中度血清肌酐水平升高；在无进展性肝转移的患者中联合治疗，血清中暂时性的（1度和2度）AST、ALT、碱性磷酸酶或胆红素水平升高的发生率分别为15%、11%、11%和10%。
武汉贝尔卡生物医药有限公司产品简介
中文品名 盐酸伊立替康,(CPT-11)
CAS 号 136572-09-3
英文品名 Irinotecan HCl Trihydrate
产品编号 MB1126
三水盐酸伊立替康
分子式：C 33H 38N 4O 6.HCl .3(H 2O) 分子量：677.19
物理性状及指标：
外观：……………………淡黄色或黄色结晶性粉末
熔点：……………………250~256℃
溶解性：…………………微溶于水、乙醇和氯仿，几乎不溶于丙酮
用途及描述：科研试剂，广泛应用于分子生物学，药理学等科研方面。
伊立替康是喜树碱的半合成衍生物。
喜树碱可特异性地与拓扑异构酶I 结合，后者诱导可逆性单链断裂，从而使DNA 双链结构解旋；伊立替康及其活性代谢物SN －38可与拓扑异构酶I －DNA 复合物结合，从而阻止断裂单链的再连接。
现有研究提示，伊立替康的细胞毒作用归因于DNA 合成过程中，复制酶与拓扑异构酶I －DNA 一伊立替康（或SN －38）三联复合物相互作用，从而引起DNA 双链断裂。
哺乳动物细胞不能有效地修复这种DNA 双链断裂。
储存条件：2-8℃，避光防潮密闭干燥。
注意：我司产品为非无菌包装，若用于细胞培养，请提前做预处理，除去热原细菌，否则会导致染菌。
以上数据仅供参考交流之用。
三水盐酸伊立替康的溶解性，三水盐酸伊立替康在水中的溶解性，三水盐酸伊立替康在生理盐水中的溶解性，三水盐酸伊立替康在PBS 缓冲液中的溶解性，三水盐酸伊立替康在DMSO 、乙醇等有机溶剂中的溶解性，三水盐酸伊立替康在细胞实验方面的应用，三水盐酸伊立替康在大鼠等动物实验方面的应用。
注射用盐酸拓扑替康【药品名称】通用名称：注射用盐酸拓扑替康英文名称：Topotecan Hydrochloride for Injection【成份】本品主要成份为盐酸拓扑替康。
【适应症】小细胞肺癌。
晚期转移性卵巢癌经一线化疗失败者。
【用法用量】1 剂量:推荐剂量为1.2mg/m2/日，静脉输注30分钟。
持续5天，21天为一疗程，治疗中严重的中性粒细胞减少症患者，在其后的疗程中剂量减少0.2mg/m2或与G-CSF同时使用。
使用从第6天开始，即在持续5天使用本品后24小时后再用G-CSF。
2 注射液配制:用无菌注射用水1ml溶解本品1mg比例溶解本品，按1.2mg/m2/日剂量抽取药液，用0.9％氯化钠或5％葡萄糖注射液稀释后静脉输注。
3 特殊人群的剂量调整肝功能不全者:肝功能不全（血浆胆红素1.5～10mg/dl）患者，血浆清除率降低，但一般不需剂量调整。
肾功能不全者:对轻微肾功能不全（CLcr40～60ml/分钟）一般不需剂量调整，中度肾功能不全（CLcr20～39ml/分钟）剂量调为0.6mg/m2，没有足够资料可证明在严重肾功能不全者可否使用。
老年人:除非肾功能不全，一般不作剂量调整。
【不良反应】1.血液系统：有白细胞减少、血小板减少、贫血等反应。
骨髓抑制（主要是中性粒细胞）是本品的剂量限制性毒性，治疗期间要监测外周血象，在治疗中中性粒细胞恢复至>；1500个/mm3，血小板恢复至100000个/mm3，血红蛋白恢复至9.0g/dl方可继续使用（必要时可使用G-CSF或输注成分血）。
与其它细胞毒药物联合应用时可加重骨髓抑制。
2.消化系统：恶心、呕吐、腹泻、便秘、肠梗阻、腹痛、口腔炎、厌食。
3.皮肤及附件：脱发、偶见严重的皮炎及搔痒。
4.神经肌肉：头痛、关节痛、肌肉痛、全身痛、感觉异常。
5.呼吸系统：可致呼吸困难。
虽然尚不能肯定是否会因此造成死亡，但应引起医生的重视。
6.肝脏：有时出现肝功能异常，转氨酶升高。
Irinotecan Hydrochloride(eye'' ri noe tee' kan hye'' droe klor' ide).C33H38N4O6·HCl·3H2O Anhydrous: 623.14 Trihydrate: 677.18[1,4′-Bipiperidine]-1′-carboxylic acid, 4,11-diethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-1H-pyrano[3′,4′:6,7]indolizino[1,2-b]quinolin-9-yl ester, monohydrochloride, trihydrate, (S)-;(+)-7-Ethyl-10-hydroxycamptothecine 10-[1,4′-bipiperidine]-1′-carboxylate, monohydrochloride, trihydrate [136572-09-3].DEFINITIONIrinotecan Hydrochloride contains NLT 98.0% and NMT 102.0% of C33H38N4O6·HCl, calculated on the anhydrous basis.IDENTIFICA TION• A. Infrared Absorption 〈197K〉• B. The retention time of the major peak of the Sample solution corresponds to the irinotecan (S-enantiomer) peak in the Identification solution, as obtained in the test for Limit of Irinotecan Hydrochloride Enantiomer.• C. Identification Tests—General, Chloride 〈191〉: A 2-mg/mL solution meets the requirements of the tests. ASSAY•ProcedureSolution A: 2.8 g/L of monobasic sodium phosphate monohydrate and 1.8 g/L of 1-octanesulfonic acid sodium salt monohydrate in waterMobile phase: Acetonitrile, methanol, and Solution A (17:24:59)Diluent: Use Mobile phase adjusted with diluted hydrochloric acid to a pH of 3.65 ± 0.15.Standard solution: 1 mg/mL of USP Irinotecan Hydrochloride RS in DiluentSample solution: 1 mg/mL of Irinotecan Hydrochloride in DiluentChromatographic system(See Chromatography 〈621〉, System Suitability.)Mode: LCDetector: UV 255 nmColumn: 4.6-mm × 25-cm; 5-µm packing L1Column temperature: 40°Flow rate: 1.5 mL/minInjection size: 15 µLSystem suitabilitySample: Standard solutionSuitability requirementsTailing factor: NMT 1.5Relative standard deviation: NMT 2.0%AnalysisSamples: Standard solution and Sample solutionCalculate the percentage of irinotecan hydrochloride (C33H38N4O6·HCl) in the portion of Irinotecan Hydrochloride taken:Result = (r U/r S) × (C S/C U) × 100r U = = peak area from the Sample solutionr S = = peak area from the Standard solutionC S = = concentration of USP Irinotecan Hydrochloride RS in the Standard solution (mg/mL)C U = = concentration of Irinotecan Hydrochloride in the Sample solution (mg/mL)Acceptance criteria: 98.0%–102.0% on the anhydrous basisIMPURITIES•Residue on Ignition 〈281〉: NMT 0.1%•Heavy Metals, Method II 〈231〉: NMT 10 ppmChange to read:•Limit of Irinotecan Hydrochloride EnantiomerMobile phase: Hexane, dehydrated alcohol, and diethylamine (250:250:1)Diluent: Dehydrated alcohol and diethylamine (250:1)System suitability solution: 0.1 mg/mL each of USP Irinotecan Hydrochloride RS and USP Irinotecan Related Compound D RS in DiluentIdentification solution: 1 mg/mL of USP Irinotecan Hydrochloride RS in Diluent. [Note—This solution is used for Identification test B. ]Standard solution: 1.5 µg/mL of USP Irinotecan Related Compound D RS in DiluentSensitivity solution: 0.5 µg/mL of USP Irinotecan Related Compound D RS in Diluent, from the Standard solution Sample solution: 1 mg/mL of Irinotecan Hydrochloride in DiluentChromatographic system(See Chromatography 〈621〉, System Suitability.)Mode: LCDetector: UV 370 nmColumn: 4.6-mm × 25-cm; 10-µm packing L40Flow rate: 1.0 mL/minInjection size: 20 µLSystem suitabilitySamples: System suitability solution, Standard solution, and Sensitivity solution[Note—The relative retention times for irinotecan related compound D (R-enantiomer) and irinotecan (S-enantiomer) are 0.7 and 1.00, respectively. ]Suitability requirementsResolution: NL T 2.5 between irinotecan related compound D and irinotecan, System suitability solutionRelative standard deviation: NMT 5.0%,(RB 1-Oct-2010) Standard solutionSensitivity: The irinotecan related compound D peak should be visible, Sensitivity solutionAnalysisSamples: Standard solution and Sample solutionCalculate the percentage of irinotecan hydrochloride R-enantiomer in the portion of Irinotecan Hydrochloride taken: Result = (r U/r S) × (C S/C U) × 100r U = = peak area of irinotecan related compound D from the Sample solutionr S = = peak area of irinotecan related compound D from the Standard solutionC S = = concentration of USP Irinotecan Related CompoundD RS in the Standard solution (mg/mL)C U = = concentration of Irinotecan Hydrochloride in the Sample solution (mg/mL)Acceptance criteriaR-enantiomer: NMT 0.15%Add the following:[Note—On the basis of the synthetic route, perform either Organic Impurities Procedure 1 or Organic Impurities Procedure 2. ] (RB 1-Oct-2010)Change to read:•Organic Impurities Procedure 1 (for Material Labeled as Produced by a Synthetic Process)(RB 1-Oct-2010) Mobile phase, Diluent, Sample solution, and Chromatographic system: Proceed as directed in the Assay.System suitability stock solution: 0.01 mg/mL each of USP Irinotecan Related Compound B RS and USP Irinotecan Related Compound C RS in methanolSystem suitability solution: 1.0 µg/mL each of USP Irinotecan Related Compound B RS and USP Irinotecan Related Compound C RS in Diluent, from System suitability stock solutionStandard solution: 2.0 µg/mL of USP Irinotecan Hydrochloride RS in DiluentSensitivity solution: 0.5 µg/mL of USP Irinotecan Hydrochloride RS in DiluentSystem suitabilitySamples: System suitability solution, Standard solution, and Sensitivity solutionSuitability requirementsResolution: NL T 1.1 between irinotecan related compound B and irinotecan related compound C, System suitability solutionRelative standard deviation: NMT 2.0%, Standard solutionSignal-to-noise ratio: NL T 10, Sensitivity solutionAnalysisSamples: Sample solution and Standard solutionCalculate the percentage of each impurity in the portion of Irinotecan Hydrochloride taken:Result = (r U/r S) × (C S/C U) × 100r U = = peak area of each impurity from the Sample solutionr S = = peak area of irinotecan from the Standard solutionC S = = concentration of irinotecan hydrochloride in the Standard solution (mg/mL)C U = = concentration of Irinotecan Hydrochloride in the Sample solution (mg/mL)Acceptance criteriaIndividual impurities: See Table 1. [Note—Disregard any impurity peaks less than 0.05%. ]Table 1Add the following:•Organic Impurities Procedure 2 (for Material Labeled as Produced by a Semi-synthetic Process)Solution A: 2.72 g/L of monobasic potassium phosphate in water. Adjust with dilute phosphoric acid (1 in 20) to a pH of 3.5 ± 0.05.Solution B: Acetonitrile and methanol (3:2)Mobile phase: See Table 2.Table 2Diluent: Acetonitrile, methanol, and Solution A (1:1:2)System suitability solution: 0.1 mg/mL each of USP Irinotecan Hydrochloride RS and USP Irinotecan Related Compound A RS in DiluentStandard solution: 1 µg/mL of USP Irinotecan Hydrochloride RS in DiluentSample solution: 1 mg/mL of Irinotecan Hydrochloride in DiluentChromatographic system(See Chromatography 〈621〉, System Suitability.)Mode: LCDetector: UV 220 nmColumn: 4.6-mm × 25-cm; 5-µm packing L1Flow rate: 1 mL/minInjection size: 10 µLSystem suitabilitySamples: System suitability solution and Standard solutionSuitability requirementsResolution: NL T 3.0 between irinotecan and irinotecan related compound A, System suitability solutionRelative standard deviation: NMT 2.0%, Standard solutionAnalysisSamples: Standard solution and Sample solutionCalculate the percentage of each impurity in the portion of Irinotecan Hydrochloride taken:Result = (r U/r S) × (C S/C U) × (1/F) × 100r U = = peak area of each individual impurity from the Sample solutionr S = = peak area of irinotecan from the Standard solutionC S = = concentration of USP Irinotecan Hydrochloride RS in the Standard solution (mg/mL)C U = = concentration of Irinotecan Hydrochloride in the Sample solution (mg/mL)F = = relative response factor for each individual impurity (see Table 3)Acceptance criteriaIndividual impurities: See Table 3. [Note—Disregard any unspecified impurity peaks less than 0.05%. ]Table 3(RB 1-Oct-2010)SPECIFIC TESTS•Microbial Enumeration Tests 〈61〉and Tests for Specified Microorganisms 〈62〉: The total aerobic microbial count does not exceed 1000 cfu/g, and the total combined molds and yeasts count does not exceed 100 cfu/g.•Water Determination, Method I〈921〉: Between 7.0% and 9.0%ADDITIONAL REQUIREMENTS•Packaging and Storage: Preserve in tight, light-resistant containers, and store at controlled room temperature.Add the following:•Labeling: If a test for Organic Impurities other than Procedure 1 is used, the labeling states the test with which the article complies.(RB 1-Oct-2010)Change to read:•USP Reference Standards 〈11〉USP Irinotecan Hydrochloride RSUSP Irinotecan Related Compound A RS(S)-4-Ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione.C20H16N2O5364.35(RB 1-Oct-2010)USP Irinotecan Related Compound B RS(S)-4,11-Diethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione.C22H20N2O5392.40USP Irinotecan Related Compound C RS(S)-9-[(1,4'-Bipiperidine)-1'-carbonyloxy]-4-methyl-11-ethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-1H-pyrano[3' ,4':6,7]indolizino[1,2-b]quinoline hydrochloride.C32H36N4O6·HCl 609.11USP Irinotecan Related Compound D RS(R)-9-[(1,4'-Bipiperidine)-1'-carbonyloxy]-4,11-diethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-1H-pyrano[3',4':6,7 ]indolizino[1,2-b]quinoline hydrochloride, trihydrate.C33H38N4O6·HCl·3 H2O 677.18Auxiliary Information— Please check for your question in the FAQs before contacting USP.USP34–NF29 Page 3189USP34–NF29 Supplement : No. 1 Page 4974。
