CN102225046A - 透皮释药剂型 - Google Patents
透皮释药剂型 Download PDFInfo
- Publication number
- CN102225046A CN102225046A CN2011101585856A CN201110158585A CN102225046A CN 102225046 A CN102225046 A CN 102225046A CN 2011101585856 A CN2011101585856 A CN 2011101585856A CN 201110158585 A CN201110158585 A CN 201110158585A CN 102225046 A CN102225046 A CN 102225046A
- Authority
- CN
- China
- Prior art keywords
- dosage form
- acid
- hydrochloride
- purposes
- sodium
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
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- ROKRAUFZFDQWLE-UHFFFAOYSA-M sodium;1-ethyl-7-methyl-4-oxo-1,8-naphthyridine-3-carboxylate Chemical compound [Na+].C1=C(C)N=C2N(CC)C=C(C([O-])=O)C(=O)C2=C1 ROKRAUFZFDQWLE-UHFFFAOYSA-M 0.000 description 1
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- WFKJEZKHPGDCRK-UHFFFAOYSA-M sodium;2,2,2-trichloroethyl hydrogen phosphate Chemical compound [Na+].OP([O-])(=O)OCC(Cl)(Cl)Cl WFKJEZKHPGDCRK-UHFFFAOYSA-M 0.000 description 1
- FKZUETPACPDEAD-UHFFFAOYSA-M sodium;2-(1,3-dioxobenzo[de]isoquinolin-2-yl)acetate Chemical compound [Na+].C1=CC(C(N(CC(=O)[O-])C2=O)=O)=C3C2=CC=CC3=C1 FKZUETPACPDEAD-UHFFFAOYSA-M 0.000 description 1
- GNMBMOULKUXEQF-UHFFFAOYSA-M sodium;2-(3-fluoro-4-phenylphenyl)propanoate;dihydrate Chemical compound O.O.[Na+].FC1=CC(C(C([O-])=O)C)=CC=C1C1=CC=CC=C1 GNMBMOULKUXEQF-UHFFFAOYSA-M 0.000 description 1
- JXRFTGPGWGUBQB-LHOUOPCDSA-M sodium;2-[(2r,3s,4s,5r,6s)-2,4-dihydroxy-6-[(1r)-1-[(2s,5r,7s,8r,9s)-7-hydroxy-2-[(2r,5s)-5-[(2r,3s,5r)-5-[(2s,3s,5r,6s)-6-hydroxy-3,5,6-trimethyloxan-2-yl]-3-[(2s,5s,6r)-5-methoxy-6-methyloxan-2-yl]oxyoxolan-2-yl]-5-methyloxolan-2-yl]-2,8-dimethyl-1,10-d Chemical compound [Na+].O1[C@H](C)[C@@H](OC)CC[C@@H]1O[C@@H]1[C@H]([C@@]2(C)O[C@H](CC2)[C@@]2(C)O[C@]3(O[C@@H]([C@H](C)[C@@H](O)C3)[C@@H](C)[C@H]3[C@@H]([C@@H](O)[C@H](C)[C@@](O)(CC([O-])=O)O3)OC)CC2)O[C@@H]([C@@H]2[C@H](C[C@@H](C)[C@@](C)(O)O2)C)C1 JXRFTGPGWGUBQB-LHOUOPCDSA-M 0.000 description 1
- IEJDXDFBVQORAZ-CTRAYMKSSA-M sodium;2-[(2s,3s)-3-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-2-methyl-4-oxoazetidin-1-yl]oxyacetate Chemical compound [Na+].C=1SC(N)=NC=1C(=N/OC)/C(=O)N[C@H]1[C@H](C)N(OCC([O-])=O)C1=O IEJDXDFBVQORAZ-CTRAYMKSSA-M 0.000 description 1
- JGVFTSXUZPXSJY-WLWSJORBSA-M sodium;2-[(z)-[1-(2-amino-1,3-thiazol-4-yl)-2-[[1-[[3-[(5-hydroxy-4-oxo-1h-pyridine-2-carbonyl)amino]-2-oxoimidazolidin-1-yl]sulfonylcarbamoyl]-2-oxoazetidin-3-yl]amino]-2-oxoethylidene]amino]oxy-2-methylpropanoate Chemical compound [Na+].C=1SC(N)=NC=1C(=N/OC(C)(C)C([O-])=O)/C(=O)NC(C1=O)CN1C(=O)NS(=O)(=O)N(C1=O)CCN1NC(=O)C1=CC(=O)C(O)=CN1 JGVFTSXUZPXSJY-WLWSJORBSA-M 0.000 description 1
- JMHRGKDWGWORNU-UHFFFAOYSA-M sodium;2-[1-(4-chlorobenzoyl)-5-methoxy-2-methylindol-3-yl]acetate Chemical compound [Na+].CC1=C(CC([O-])=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 JMHRGKDWGWORNU-UHFFFAOYSA-M 0.000 description 1
- CWCSCNSKBSCYCS-UHFFFAOYSA-M sodium;2-[2,3-dichloro-4-(2-methylidenebutanoyl)phenoxy]acetate Chemical compound [Na+].CCC(=C)C(=O)C1=CC=C(OCC([O-])=O)C(Cl)=C1Cl CWCSCNSKBSCYCS-UHFFFAOYSA-M 0.000 description 1
- SEEXPXUCHVGZGU-UHFFFAOYSA-M sodium;2-[5-(4-chlorobenzoyl)-1,4-dimethylpyrrol-2-yl]acetate Chemical compound [Na+].C1=C(CC([O-])=O)N(C)C(C(=O)C=2C=CC(Cl)=CC=2)=C1C SEEXPXUCHVGZGU-UHFFFAOYSA-M 0.000 description 1
- DCTVJZGYZTWBLO-UHFFFAOYSA-M sodium;2-[7-(4-methylsulfanylbenzoyl)-1-benzofuran-5-yl]acetate;hydrate Chemical compound O.[Na+].C1=CC(SC)=CC=C1C(=O)C1=CC(CC([O-])=O)=CC2=C1OC=C2 DCTVJZGYZTWBLO-UHFFFAOYSA-M 0.000 description 1
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- PAKGDHCMLYSCMW-UHFFFAOYSA-M sodium;2-tetradecyloxirane-2-carboxylate Chemical compound [Na+].CCCCCCCCCCCCCCC1(C([O-])=O)CO1 PAKGDHCMLYSCMW-UHFFFAOYSA-M 0.000 description 1
- WOHSQDNIXPEQAE-QBKVZTCDSA-M sodium;3-[2-[[(1s,2r,3s,4r)-3-[4-(pentylcarbamoyl)-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]propanoate Chemical compound [Na+].CCCCCNC(=O)C1=COC([C@H]2[C@H]([C@@H]3CC[C@H]2O3)CC=2C(=CC=CC=2)CCC([O-])=O)=N1 WOHSQDNIXPEQAE-QBKVZTCDSA-M 0.000 description 1
- WTUXHNVTMYDUAM-DHHSFAMCSA-M sodium;3-[[4-[[4-hydroxy-7-[(2r,3r,4s,5r)-3-hydroxy-5-methoxy-6,6-dimethyl-4-(5-methyl-1h-pyrrole-2-carbonyl)oxyoxan-2-yl]oxy-8-methyl-2-oxochromen-3-yl]carbamoyl]-3-methyl-1h-pyrrole-2-carbonyl]amino]-7-[(2r,3r,4s,5r)-3-hydroxy-5-methoxy-6,6-dimethyl-4-( Chemical compound [Na+].O([C@@H]1[C@H](C(O[C@@H](OC=2C(=C3OC(=O)C(NC(=O)C=4C(=C(C(=O)NC=5C(OC6=C(C)C(O[C@H]7[C@@H]([C@H](OC(=O)C=8NC(C)=CC=8)[C@@H](OC)C(C)(C)O7)O)=CC=C6C=5[O-])=O)NC=4)C)=C(O)C3=CC=2)C)[C@@H]1O)(C)C)OC)C(=O)C1=CC=C(C)N1 WTUXHNVTMYDUAM-DHHSFAMCSA-M 0.000 description 1
- LFORPQYIKMHOCK-UHFFFAOYSA-M sodium;3-methylbutyl sulfate Chemical compound [Na+].CC(C)CCOS([O-])(=O)=O LFORPQYIKMHOCK-UHFFFAOYSA-M 0.000 description 1
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- DRMAOJOMESIGKD-UHFFFAOYSA-M sodium;4-[2-hydroxy-3-[4-oxo-2-(1,2,3-triaza-4-azanidacyclopenta-2,5-dien-5-yl)chromen-5-yl]oxypropoxy]benzonitrile Chemical compound [Na+].C=1C=CC=2OC(C=3[N-]N=NN=3)=CC(=O)C=2C=1OCC(O)COC1=CC=C(C#N)C=C1 DRMAOJOMESIGKD-UHFFFAOYSA-M 0.000 description 1
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- FJPYVLNWWICYDW-UHFFFAOYSA-M sodium;5,5-diphenylimidazolidin-1-ide-2,4-dione Chemical compound [Na+].O=C1[N-]C(=O)NC1(C=1C=CC=CC=1)C1=CC=CC=C1 FJPYVLNWWICYDW-UHFFFAOYSA-M 0.000 description 1
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- QORQZMBCPRBCAB-UHFFFAOYSA-N sodium;5-butan-2-yl-5-ethyl-1,3-diazinane-2,4,6-trione Chemical compound [Na+].CCC(C)C1(CC)C(=O)NC(=O)NC1=O QORQZMBCPRBCAB-UHFFFAOYSA-N 0.000 description 1
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- IQXFQHXFCSOQGI-UHFFFAOYSA-M sodium;6-acetyl-7-[5-(4-acetyl-3-hydroxy-2-propylphenoxy)pentoxy]-3,4-dihydro-2h-chromene-2-carboxylate Chemical compound [Na+].CCCC1=C(O)C(C(C)=O)=CC=C1OCCCCCOC(C(=C1)C(C)=O)=CC2=C1CCC(C([O-])=O)O2 IQXFQHXFCSOQGI-UHFFFAOYSA-M 0.000 description 1
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Abstract
本发明提供了一种透皮剂型,可以释放至少一种活性剂。该配方剂型:(i)第一种化合物,其包含有机亚砜;以及(ii)第二种化合物,选自由脂肪酸酯、脂肪酸、氮酮类化合物及其混合物所构成的组。
Description
本申请是基于以下中国专利申请的分案申请:
原案申请日:2006年8月4日
原案申请号:200680036519.9(PCT/CA2006/001271)
原案申请名称:透皮释药剂型
技术领域
本发明涉及一种透皮释药剂型。在一个特别优选的实施方式中,本发明涉及的一种包含二甲基亚砜(DMSO)和一种化合物的透皮释药剂型,该化合物选自由脂肪酸酯、脂肪酸、氮酮类化合物及其混合物所构成的组。
背景技术
透皮释药涉及到给药一种活性剂,使其透过皮肤局部或系统分布地达到受疾病侵袭的组织。透皮施用活性剂可以避免首过代谢效应,并可以减轻与将活性剂口服给药于胃肠道(GI)系统有关的一些问题。例如,口服给药非甾体抗炎药会引起显著的不良的胃肠道(GI)副作用。通过避免或减少向胃肠道释放活性剂,局部用药法可以减少胃肠道不良反应事故的发生。局部用药的形式还提供了一种简单用药的方法。
然而,皮肤是一道保护外来剂型进入皮下组织的有效屏障。在结构上,皮肤有两大主要部分:(i)相对较薄的最外层(“表皮”),和(ii)较厚的内层区域(“真皮”)。表皮的最外层(“角质层”)由填满了角蛋白的扁平的死细胞组成。角质层扁平的死细胞之间的区域填满了层状的脂质。皮肤的高度不渗透性本质主要归因于角质层。以临床活性主体浓度来释放的活性剂一般需要某些方法来减少角质层对渗透的阻碍。目前人们已经开发了许多降低角质层的屏障特性的方法。其中一种方法涉及到利用渗透促进剂。多种化学渗透促进剂已经被鉴定并得到了研究,但奇怪的是很少被成功地开发为商品剂型。
已商品化的透皮剂型的一个实例在美国专利4,575,515[Sandborn]中有描述。Sandborn讲授了一种剂型,它包含了一种药品和二甲基亚砜(DMSO),并且据称可使药品快速深入地渗透入皮下组织。
虽然Sandborn讲授的透皮剂型在该领域内有其先进之处,但仍存在改进空间。特别是与Sandborn讲授的透皮剂型相比,人们需要一种活性成分通过皮肤的通量得到提高的透皮剂型。
发明内容
本发明的目的之一是提供一种新颖的透皮剂型。
本发明的另一个目的在于提供一种透皮剂型,其与Sandborn讲授的透皮剂型相比,透过皮肤的通量性能得到提高。
相应地,一方面,本发明提供了一种透皮剂型,其包括:(i)第一种化合物,选自机亚砜;和(ii)第二种化合物,选自由脂肪酸酯、脂肪酸、氮酮类化合物及其混合物所构成的组。
相应地,另一方面,本发明提供了一种透皮剂型,其包含:(i)第一种化合物,含有有机亚砜;和(ii)第二种化合物,含有脂肪酸。
相应地,另一方面,本发明提供了一种透皮剂型,其包含:(i)第一种化合物,含有有机亚砜;和(ii)油酸。
相应地,另一方面,本发明提供了一种透皮剂型,其包含:(i)第一种化合物,含有有机亚砜;和(ii)第二种化合物,含有氮酮类化合物。
相应地,另一方面,本发明提供了一种透皮剂型,其包含:(i)第一种化合物,含有有机亚砜;和(ii)氮酮。
附图说明
参照附图,对本发明的优选实施方式进行描述,其中:
图1是显示下述实施例1中描述的各种剂型的渗透性对比评估的示图;
图2是显示下述实施例2中描述的各种剂型的渗透性(μg/cm2)的示图;并且
图3是显示下述实施例2中描述的各种剂型的渗透性对比评估的示图。
具体实施方式
本发明提供了一种透皮剂型,可以用于至少一种活性剂的透皮转运。
本说明书中出现的术语“透皮”泛指广义的通过皮肤。更进一步,术语“透皮”和“经皮”在本说明书中可以替换使用。
术语“透皮增强剂”在此处指可以增强某种活性剂(例如一种药品)的输送性能的试剂。“透皮增强剂”用于协助将活性剂直接或间接地运送到患病部位。
术语“氮酮”和“1-十二烷基氮杂环庚-2-酮”此处可以替换使用。
在一个实施方式中,本发明提供了一种透皮剂型,其包含:(i)选自有机亚砜的第一种混合物;和(ii)第二种化合物,选自由脂肪酸酯、脂肪酸、氮酮类化合物及其混合物所构成的组。
本发明中透皮剂型的第一种化合物是有机亚砜化合物。所述有机亚砜化合物可以、但不仅限于选自由二烷基亚砜化合物、环状亚砜化合物及其混合物所构成的组。优选第一种化合物选自由二甲亚砜(DMSO)、1-甲基丙基·甲基亚砜、1,1-二甲基丙基·甲基亚砜、1,1-二甲基乙基·甲基亚砜、1-甲基丁基·甲基亚砜、1,1-二甲基丁基·甲基亚砜、1-乙基丁基·甲基亚砜、1-丙基戊基·甲基亚砜、1,3-亚丙基亚砜、1-丙基1,3-亚丙基亚砜、1-丁基1,3-亚丙基亚砜、噻吩氧化物、甲基乙基亚砜、甲基1,2-亚乙基亚砜、2-羟十一基·甲基亚砜、N-癸基甲基亚砜、及其混合物所构成的组。更优选第一种化合物选自由二甲亚砜、2-羟基十一基·甲基亚砜、癸基甲基亚砜及其混合物所构成的组。在一个优选实施方式中,第一种化合物为二甲亚砜(DMSO)。
上述的透皮剂型的一个实施方式中,所述第二种化合物是一种脂肪酸酯,选自由乙酸丁酯、十六基乳酸酯、N,N-二甲基氨基乙酸癸酯、N,N-二甲胺基异丙酸癸酯、二甘醇油酸酯、癸二酸二乙酯、丁二酸二乙酯、癸二酸二异丙酯、N,N-二甲胺基乙酸十二醇酯、(N,N-二甲胺基)丁酸十二醇酯、(N,N-二甲胺基异丙酸十二醇酯、2-(二甲胺基)丙酸十二醇酯、环氧乙烷-5-油基酯、乙酸乙酯、乙酰乙酸乙酯、乙酸丙酯、甘油单醚、甘油单月桂酸酯、甘油单油酸酯、甘油单亚油酸酯、异硬脂酸异丙酯、亚油酸异丙酯、肉豆蔻酸异丙酯、肉豆蔻酸异丙酯/脂肪酸单甘油酯组合物、肉豆蔻酸异丙酯/乙醇/L-乳酸组合物、棕榈酸异丙酯、乙酸甲酯、癸酸甲酯、月桂酸甲酯、丙酸甲酯、戊酸甲酯、1-单己酸甘油酯、单甘油酯(中等链长)、烟酸酯(苄基)、乙酸辛酯、N,N-二甲胺基乙酸辛酯、油酸辛酯、N-乙酰脯氨酸正戊醇酯、丙二醇单月桂酸酯、山梨醇二月桂酸酯、山梨醇二月桂酸酯、山梨醇单月桂酸酯、山梨醇单油酸酯、山梨醇三月桂酸酯、山梨醇三油酸酯、蔗糖椰子脂肪酸酯混合物、蔗糖单月桂酸酯、蔗糖单油酸酯、N,N-二甲胺基乙酸十四酯及其混合物所构成的组。
在一个另一个可选择的透皮剂型实施方式中,上述的第二种化合物是一种脂肪酸,可选自由链烷酸、癸酸、二酸、乙基硬脂酸、己酸、乳酸、月桂酸、反亚油酸、亚油酸、亚麻酸、叔癸酸、油酸、棕榈酸、壬酸、丙酸、异油酸、及其混合物所构成的组。
在另一个可选择的透皮剂型实施方式中,上述的第二种化合物是一种氮酮类化合物,可选自由N-酰基-六氢-2-氧-1H-氮杂、N-烷基-二氢-1,4-氧氮杂-5,7-二酮、N-烷基吗啉-2,3-二酮、N-烷基吗啉-3,5-二酮、氮杂环烷衍生物(-酮、-硫酮)、氮杂环链烯酮衍生物、1-[2-(癸基硫代)乙基]氮杂环戊烷-2-酮、N-(2,2-双羟乙基)十二胺、1-十二酰六氢-1H-氮杂、1-十二烷基氮杂环庚烷-2-酮、N-十二烷基二乙醇胺、N-十二烷基-六氢-2-硫代-1H-氮杂、N-十二烷基-N-(2-甲氧基乙基)乙酰胺,N-十二烷基-N-(2-甲氧基乙基)异丁酰胺、N-十二烷基-哌啶-2-硫酮、N-十二烷基-2-哌啶酮,N-十二烷基吡咯烷-3,5-二酮、N-十二烷基吡咯烷-2-硫酮、N-十二烷基-2-吡咯烷酮、1-法尼基氮杂环庚烷-2-酮、1-法尼基氮杂环戊烷-2-酮、1-香叶基-氮杂环庚烷-2-酮、1-香叶基氮杂环戊烷-2-酮、六氢-2-氧-氮杂-1-乙酸酯、N-(2-羟基乙基)-2-吡咯烷酮、1-十二烷基氮杂环庚烷、2-(1-壬基)-1,3-二氧戊环、1-N-辛基氮杂环庚烷-2-酮、N-(1-氧代十二烷基)-六氢-1H-氮杂、N-(1-氧代十二烷基)-吗啉,1-氧代烃基-取代氮杂环己烷、N-(1-氧代十四烷基)-六氢-2-氧-1H-氮杂、N-(1-硫代十二烷基)-吗啉、及其混合物所构成的组。
在另一个可选择的透皮剂型实施方式中,所述第二种化合物包含了上述的脂肪酸酯、脂肪酸和氮酮类化合物的混合物。
在一个实施方式中,所述第二种化合物选自由氮酮、油酸、2-(N,N-二甲胺基)丙酸十二烷酯、及其混合物所构成的组。更优选所述第二种化合物选自氮酮、油酸、及其混合物。
在另一个可选择的透皮剂型实施方式中,第一种化合物与第二种化合物的重量比在约60∶1至约1∶10范围内,优选60∶1至约1∶1,更适宜约60∶1至约5∶1,更加适宜约60∶1至约5∶1。在一个优选实施方式中,第一化合物与第二化合物的重量比的范围为约20∶1至约5∶1。
上述透皮剂型可以另外包含至少一种治疗性活性剂。
至少一种活性剂可以是抗炎药,例如非甾体抗炎药(NSAID)。所述NSAID可以选自由双氯芬酸、二氟尼酸、非诺洛芬、布洛芬、吲哚美辛、甲氯胺苯酸、萘普生、羟基保泰松、苯丁唑酮、吡氧噻嗪、舒林酸、托美汀、水杨酸和佐美酸、酮洛芬、依托度酸、氟比布洛芬、甲芬那酸、美洛昔康、萘丁美酮、噁丙嗪、苏林达克(痛立克錠)及其混合物所构成的组。其它适合的活性剂包括选择性环氧化酶-2(COX-2)类抑制剂,例如塞来昔布,罗非昔布,戊地昔布,氯美昔布,依他昔布;抗真菌药,例如:托萘酯、益康唑、环匹罗司;抗生素,例如:克林霉素;肌骨试剂,例如:丹曲林;维A酸类,例如:异维A酸;抗病毒药,例如:阿昔洛韦;血管舒张剂,例如:硝酸甘油酯,罂粟碱;荷尔蒙及其合成替代物,例如:雄激素、雌激素、胰岛素;镇静剂,例如:芬太尼、羟考酮、氢吗啡酮;局部麻醉剂,例如:利多卡因、妥卡尼、美西律和丁基-对氨基苯甲酸;抗炎药,例如:糖皮质激素;NMDA受体拮抗剂,例如:氯胺酮、右美沙芬和金刚烷胺。
其它治疗性活性剂可以包括如下:肾上腺素,肾上腺皮质激素,肾上腺皮质抑制剂,肾上腺皮质拮抗剂,氨基酸,同化激素,合成代谢兴奋剂,镇痛麻醉剂,食欲抑制剂,痤疮剂,抗肾上腺素药,抗过马来酸剂,抗阿米巴药,抗血友病药,抗心绞痛药,抗关节炎药,平喘药,抗动脉粥样硬化药,抗菌药,抗胆碱能药,抗凝血剂,抗痉挛药,抗抑郁剂,抗糖尿药,抗腹泻药剂,抗利尿剂,止吐药,抗(癫)痫药,抗纤溶药,抗真菌药,止血药,抗组胺剂,降血脂药,抗高血压药,抗降血压药,抗感染药,消炎药,抗菌剂,抗偏头痛药,抗有丝分裂药,杀真菌药,止恶心药,抗肿瘤药,抗中性白细胞减少药,抗寄生虫药,抗增殖药,安定药,抗风湿药,抗皮脂溢药,(胃)分泌抑制药,止痉挛药,抗血栓形成药,抗溃疡药,抗滤过性病原体药,食欲抑制剂,血糖调节剂,骨吸收抑制剂,支气管扩张剂,心血管类药物,类胆碱功能药物,镇静剂,诊断助剂,利尿剂,多巴胺剂,雌激素受体激动剂,纤维蛋白溶解剂,荧光剂,氧自由基清除剂,胃酸抑制剂,胃肠动力药,肾上腺皮质激素,生发剂,止血剂,组胺H2受体拮抗药,荷尔蒙,降胆固醇药,降血糖药,降血脂药,降压药,造影剂,免疫剂,免疫调理剂,免疫调节剂,免疫激活剂,免疫抑制剂,角质层分离剂,LHRH兴奋剂,情绪调节剂,粘液溶解剂,散瞳剂,鼻腔减充血剂,神经肌肉阻断剂,神经保护剂,NMDA拮抗药,非激素类固醇衍生物,纤溶酶原激活剂,血小板活化因子拮抗剂,血小板聚集抑制剂,精神药物,放射性试剂,灭疥癣药,硬化剂,镇静药,安眠镇静剂,腺苷A1受体特异性阻断剂,5-羟色胺拮抗药,5-羟色胺抑制剂,5-羟色胺受体拮抗药,类固醇,甲状腺激素,甲状腺素抑制剂,拟甲状腺素药,安定药,肌萎缩侧索硬化药,脑缺血药物,帕哲病药,不稳定型心绞痛药,血管收缩药,血管舒张药,伤口愈合剂,黄嘌呤氧化酶抑制剂,及类似物。
药物制剂的具体例子也可以包含在本发明的透皮剂型中,其可以单独或联合使用,这些制剂包含但不限于:
肾上腺素:肾上腺酮,酰胺福林-甲烷磺酸盐,盐酸安普乐定,溴莫尼定酒石酸盐,盐酸达哌拉唑,盐酸地托胺,地匹福林,盐酸多巴胺,硫酸麻黄碱,肾上腺素,重酒石酸肾上腺素,环硼肾上腺素,盐酸乙硫酰丙喹,盐酸乙基麻磺碱,氢溴酸羟苯异丙胺,可巴君,硫酸美芬丁胺,酒石酸间羟胺,盐酸美替唑啉,盐酸萘唑啉,重酒石酸萘唑啉,羟多巴胺,盐酸羟甲唑啉,盐酸去氧肾上腺素,盐酸苯丙醇胺,苯丙醇胺右美沙芬,盐酸普瑞特罗,六氢脱氧麻黄碱,盐酸伪麻黄碱,盐酸四氢唑啉,盐酸曲马唑啉和盐酸恶涕完。
肾上腺皮质激素:环丙奈德,乙酸脱氧皮质酮,去氧皮质酮新戊酸酯,醋酸地塞米松,醋酸氟氢可的松,氟甲氧缩松,氢化可的松半琥珀酸,甲基泼尼松龙琥珀酸酯,萘非可特,普昔罗米,醋酸替莫贝特,替泼尼旦。
肾上腺皮质抑制剂:氨格鲁米特;和曲洛司坦。
戒酒药:双硫仑。
肾上腺皮质拮抗剂:坎利酸钾、坎利酮、地西利酮、美利酸钾、丙利酸钾和螺内酯。
氨基酸:丙氨酸,精氨酸,天冬氨酸,肉毒碱,半胱氨酸盐酸盐、半胱氨酸,甘氨酸,组氨酸,异亮氨酸,亮氨酸,赖氨酸,赖氨酸醋酸盐,赖氨酸盐酸盐,甲硫氨酸,苯丙氨酸,脯氨酸,丝氨酸,苏氨酸,色氨酸,酪氨酸和缬氨酸。
氨基解毒剂:精谷氨酸和精氨酸盐酸盐。
肌萎缩侧索硬化剂:力路唑。
合成类固醇:勃雄二醇二丙酸酯,勃拉酮,十一烯酸勃地酮,勃金刚酯,乙雌烯醇,美替诺龙醋酸酯,勃来诺,美替诺龙庚酸酯,米勃龙,双环辛烯酸诺龙,诺勃酮,苯噻啶,奎勃龙,司腾勃龙醋酸脂,替勃龙,折仑诺。
兴奋剂:莫达非尼
止痛药:乙酰氨基苯酚,盐酸阿芬太尼,氨基苯甲酸钾,氨基苯甲酸钠,阿尼拉酯,氨苄哌替啶,盐酸氨苄哌替啶,盐酸阿尼帕米,阿尼洛泮,安替吡啉,阿司匹林,苯恶洛芬,盐酸苄达明,盐酸比西酸锝,盐酸布酚宁,马来酸溴朵林,溴芬酸钠,盐酸丁丙诺啡,布他酰胺,布替佐辛,布托啡诺,酒石酸布托诺啡,卡马西平,卡巴匹林钙,盐酸卡比芬,枸橼酸卡芬太尼,琥珀环丙法多,西拉马多,盐酸西拉马多,氯尼他秦,氯诺昔康,可待因,磷酸可待因,硫酸可待因,盐酸考曲替林,环唑辛,右培美酸,盐酸右苯恶啶,地佐辛,二氟尼柳,重酒石酸二氢可待因,二甲非他明,安乃近,盐酸多匹可明,得利尼定(Drinidene),盐酸依那朵林,依匹唑,酒石酸麦角胺,盐酸依托替芬,依托芬那酯,丁子香酚,非诺洛芬,非诺洛芬钙,枸椽酸芬太尼,氟奎氨苯酯,氟苯尼考,氟尼辛,氟尼辛葡甲胺,马来酸氟吡汀,氟达拉滨,盐酸氟伐他汀,氟比洛芬,盐酸氢吗啡酮,异丁卡因,吲哚布洛芬,酮佐辛,酮康唑,酮咯酸氨丁三醇,盐酸来托司坦,醋美沙朵,盐酸左醋美沙朵,盐酸左普匹西林,酒石酸左啡诺,盐酸洛非咪唑,草酸洛芬太尼,洛西那朵,氯诺昔康,水杨酸镁,甲芬那酸,盐酸美大麻坦,盐酸哌替啶,盐酸美普他酚,盐酸美沙酮,乙酰美沙酮,甲氧夫啉,甲氧异丁嗪,醋酸美克法胺,盐酸米姆本,盐酸米氟嗪,吗啉胍,硫酸吗啡,莫索尼定,盐酸大麻坦,盐酸纳布啡,盐酸纳美酮,纳莫雷特,盐酸南曲朵,萘普生,萘普生钠,萘普索,盐酸萘肽磷,盐酸奈西利定,盐酸诺美沙朵,盐酸奥芬溴铵,奥他酰胺,奥芬氨酯,钆贝酸奥昔香豆素,羟喹啉,盐酸羟喹啉,对苯二甲酸羟氧可待因酮,盐酸羟氢吗啡酮,培美酸,戊吗酮,喷他佐辛,盐酸喷他佐辛,乳酸喷他佐辛,盐酸非那吡啶,盐酸非尼拉朵,盐酸哌西那朵,匹那朵林,吡非尼酮,吡罗昔康乙醇胺,马来酸普拉睾酮,盐酸普地利定,盐酸普罗法朵,富马酸丙吡胺,盐酸丙氧芬,丙氧氨酚,普罗沙唑,枸橼酸普罗沙唑,酒石酸普罗吩胺,盐酸吡咯利芬,盐酸瑞芬太尼,柳胆来司,水杨酰胺,水杨酰胺镁,双水杨酯,水杨酰胺钠,甲磺酸螺朵林,舒芬太尼;枸橼酸舒芬太尼,他米巴罗汀,他尼氟酯,他洛普仑,琥珀他扎罗汀,特丁非隆;特萃达明(tetrydamine),替呋拉酸钠,盐酸替利定,硫平酸,甲磺酸托那佐辛,盐酸曲马多,盐酸曲砜那,三乙醇胺,盐酸维拉朵林,盐酸维立洛泮,伏立康唑,甲磺酸佐非康唑,二甲苯胺噻嗪盐酸,佐美酸钠,珠氯米芬。
雄激素:氟甲睾酮,甲氢睾酮,甲基睾酮,诺龙癸,苯丙酸诺龙,醋酸尼司特林,氧甲氢龙,羟甲烯龙,硅雄酮,司坦唑,睾酮,环戊丙酸睾酮,庚酸睾酮,十二酮酸睾酮,苯乙酸睾酮,丙酸睾丸酮,醋酸曲托龙。
麻药(辅助剂):羟丁酸钠。
麻醉药:阿列氟烷,盐酸丁氧普鲁卡因,苯佐卡,盐酸苯柳胺酯,盐酸布比卡因,氨苯丁酯,苦味酸氨苯丁酯,盐酸氯普鲁卡因,可卡因,盐酸可卡因,环丙烷,地氟醚,地昔卡因,环己氨磺酸二胺卡因,地布卡因,盐酸地布卡因,盐酸达克罗宁,安氟醚,甲醚,乙基氯,依替卡因,盐酸乙苯恶啶,盐酸尤普罗辛,氟乙烯醚,氟烷,对氨苯酸异丁酯,异氟烷,盐酸氯胺酮,盐酸左沙屈尔,利多卡因,盐酸利多卡因,盐酸甲哌卡因,烯丙炔巴比妥钠,甲氧氟烷,盐酸咪达唑仑,马来酸咪达唑仑,胺乙氧孕烷酮,诺考达唑,异辛胺,奥昔卡因,盐酸苯环利定,盐酸普莫卡因,盐酸丙胺卡因,盐酸普鲁卡因,丙泮尼地,盐酸丙美卡因,异丙酚,盐酸丙氧卡因,吡咯卡因,利索卡因,罗多卡因,罗谷亚胺,杨基醇,七氟醚,替福明,丁卡,盐酸丁卡,硫戊巴比妥,硫戊比妥钠,硫喷妥钠,盐酸替来他明,盐酸佐拉。
厌食化合物:右芬氟拉明。
食欲抑制剂:阿米雷司,安菲克洛尔(amphecloral),盐酸对氯苯丁胺,氯氨雷司,盐酸氯替法唑,盐酸安非拉酮,盐酸芬氟拉明,非尼米特,氟多雷司,氟氨雷司,琥珀酸左苯丙胺,马吲哚,盐酸美芬雷司,盐酸苯甲恶啉,苯(叔)丁胺和盐酸西布曲明。
拮抗剂:阿替莫单抗,阿托西班,波生坦,西咪替丁,西咪替丁盐酸,马来酸克仑硫,醋酸地特氯铵,地法胰岛素,多奈替丁,盐酸依汀替丁,法莫替丁,盐酸二氯苯氧甲基二氢咪唑,氟马西尼,醋酸艾替班特,艾考替丁(icotidine),伊拉地平,甲硫平,纳迪德,纳美芬,盐酸纳洛酮,纳曲酮,伐地平,奥昔啡烷,盐酸奥美替丁,甲磺酸奥美替丁,磺酸夸达佐辛,枸橼酸铋雷尼替丁,盐酸雷尼替丁,舒福替丁,盐酸特鲁地平,盐酸噻帕米,硫替丁,盐酸伐哌前列素,盐酸唑替丁。
垂体前叶激活剂:表美雌醇。
垂体前叶抑制剂:达那唑。
驱虫药:阿苯达唑,安太霉素,溴沙尼特,盐酸丁萘脒,布托酯,坎苯达唑,十二烷基硫酸卡班太尔,氯碘沙尼,氯生太尔,环苯达唑,敌敌畏,枸橼酸乙胺嗪,屈苯达唑,盐酸地孟汀,依苯达唑,芬苯达唑,呋罗达唑,己雷琐辛,甲苯咪唑,酒石酸莫仑太尔,氯硝柳胺,盐酸硝拉咪唑,硝旦,双羟萘酸奥克太尔,奥芬哒唑,丙氧咪唑,帕苯达唑,马来酸哌立度酯,哌嗪,枸橼酸哌嗪,哌嗪依地酸钙,丙氯诺,双羟萘酸噻嘧啶,酒石酸噻嘧啶,扑蛲灵,碘醚柳胺,司替碘铵,盐酸四咪唑,噻苯达唑,替卡波定,噻昔达唑,三氯酚哌嗪,乙烯福司,齐仑太尔。
抗痤疮药:阿达帕林;沙那西定红霉素;醋酸伊诺特隆;软甲液如水杨酸(邻羟基苯酸);水杨酸的衍生物如5-辛酰基水杨酸;间苯二酚;维A酸类,如维A酸及其衍生物(如顺式;、反式),视黄醇,视棕榈酸酯,视丙酸或视醋酸以及合成的类维A酸;含硫的D-型和L-型氨基酸及其衍生物和盐,特别是其N-乙酰衍生物,优选的例子是N-乙酰-L-半胱氨酸;硫辛酸;抗生素和抗菌剂,如过氧化苯甲酰,吡啶酮乙醇胺,四环素,2,4,4′-三氯-2’-羟基二苯醚,3,4,4′-三氯巴尼里得(3,4,4′-trichlorobanilide),壬二酸和其衍生物,苯氧基乙醇,苯氧基丙醇,苯氧基异丙醇,乙酸乙酯,克林霉素和甲基氯环素;抑制皮脂剂如黄酮类化合物;和胆酸盐如硫酸鲨胆固醇及其衍生物,脱氧胆酸和胆酸。
抗肾上腺素:醋丁洛尔,盐酸阿普洛尔,氨酰心安,甲苯磺酸溴苄铵,盐酸布诺洛尔,盐酸卡替洛尔,盐酸塞利洛尔,盐酸塞他洛尔,盐酸环丙洛尔,盐酸右普萘洛尔,盐酸二醋洛尔,甲磺酸二氢麦角碱,盐酸地来洛尔,盐酸艾司洛尔,盐酸已丙洛尔,盐酸芬司匹利,硫酸氟司洛尔,盐酸拉贝洛尔,盐酸左倍他洛尔,左布诺洛尔盐酸,盐酸美他洛尔,倍他乐克,倍他乐克,纳多洛尔,硫酸帕马洛尔,硫酸喷布洛尔,甲磺酸酚妥拉明,普拉洛尔,盐酸普萘洛尔,盐酸普罗克生,酒石酸索立哌汀,盐酸索他洛尔,噻吗洛尔,马来酸噻吗洛尔,盐酸替普洛尔,妥拉洛尔,盐酸佐勒汀。
抗变态反应药:氨来呫诺,息斯马来酸,盐酸氮斯汀,乙唑司特,米帕奈法唑酮,奈法唑酮钙,奈法唑酮钠,尼维美酮钠,吡嘧司特钾,喷替吉肽,吡喹诺唑,橡毒提取物,安克罗米钙,安克罗米,瑞吡司特,四唑司特葡甲胺,氯化噻丙铵,硫克司特,硫克司特钠,替普司特葡甲胺,替呫诺。
抗阿米巴病药:红霉素B,盐酸比拉米可,氯喹,盐酸氯喹,磷酸氯喹,盐酸氯胺羟喹,碘羟喹,盐酸依米丁,双碘喹啉,硫酸巴龙霉素,喹法米特,盐酸昔美汀,替克洛占,四环素和盐酸四环素。
抗雄激素药:贝诺睾酮,塞奥罗奈,复方醋酸环丙孕酮,醋酸地马孕酮,奥生多龙,托普雄酮,扎诺特隆。
抗贫血药:阿法依伯汀,β依泊汀,硫酸亚铁干粉,和亚叶酸钙。
抗心绞痛药:氨氯地平,马来酸氨氯地平,盐酸倍他洛尔,盐酸贝凡洛尔,盐酸布托丙茚,卡维,马来酸桂哌酯,琥珀酸美托洛尔,吗多明,马来酸莫那匹尔,普米洛尔,盐酸雷诺嗪,托西芬,盐酸维拉帕米。
抗焦虑药:盐酸阿达色林,阿吡坦,甲磺酸比螺酮,溴他西尼,格来色林,盐酸伊沙匹隆,马来酸米立司琼,奥西普隆,恩丹西酮,帕那普隆,泮考必利,帕秦克隆,盐酸舍氮平,枸橼酸坦度螺酮,盐酸扎螺酮。
抗关节炎药:氯德拉苯。
抗气喘药:阿鲁司特,阿鲁司特钠,布那司特,西那司特,克罗米腈钠,色甘酸钠,乙诺司特,伊萨莫索(isamoxol),富马酸酮替芬,左色满卡林,乙基洛度沙胺,洛度沙胺氨丁三醇,孟鲁司特钠,昂唑司特,奥沙巴唑,奥沙米特,吡前列素,吡前列素钾,匹罗酯,泊比司特艾得明(Pobilukast Edamine),喹唑司特,利托司特,硫鲁司特,盐酸噻拉米特,硫苯司特钠,托鲁司特,尼司特,维鲁司特,维罗茶碱扎鲁司特。
抗动脉粥样硬化药:米福酯和泰姆福龙(Timefuronc)。
抗菌药:乙酰二氨二苯砜;乙酰砜钠;阿拉米辛(alamecin);双胍啶;甲亚胺青霉素;甲亚胺青霉素美酯;阿米环素;诺氟沙星;甲磺酸诺氟沙星;丁胺卡那霉素;硫酸阿米卡星;氨基钠;氨基酸;阿莫西林;双霉素;氨苄青霉素;氨苄青霉素钠;阿帕西林钠;安普霉素;天冬菌素;硫酸阿司米星;卑霉素;阿伏霉素;阿奇霉素;阿洛西林;阿洛西林钠;盐酸巴氨西林;杆菌肽;杆菌肽亚甲基水杨酸酯;杆菌肽锌;巴波霉素;苯沙酸钙;硫酸倍他米星;比阿培南;比尼霉素;羟基吡啶硫酮马格萨菲斯(magsulfex);布替卡星;丁硫酸酰苷菌毒;硫酸卷曲霉素;卡巴多;羧二钠;羧茚满基钠;羧苄西林苯基钠;羧苄西林钾;卡芦莫南钠;头孢克洛;头孢羟氨苄;头孢孟多;羟苄四唑头孢孟;头孢孟多钠;头孢派罗(cefaparole);头孢曲秦;头孢氮氟钠;头孢唑啉;头孢唑啉钠;头孢拉宗;头孢地尼;头孢吡肟;头孢吡肟盐酸;头孢替考;头孢克肟;头孢甲肟盐酸;头孢美唑;头孢美唑钠;头孢尼西;头孢尼西钠;头孢哌酮钠;头孢雷特;头孢噻肟钠;头孢替坦;头孢替坦二钠;头孢替安盐酸;头孢西丁;头孢西丁钠;头孢咪唑;头孢咪唑钠;头孢匹胺;头孢匹胺钠;硫酸头孢匹罗;头孢泊肟酯;头孢丙烯;头孢沙定;头孢沙定钠;头孢他啶;头孢布烯头孢唑肟匹伏替;头孢唑肟钠;头孢曲松钠;头孢呋辛;头孢呋辛酯;头孢呋辛钠;氰乙酰头孢菌素钠;头孢氨苄;盐酸头孢氨苄;氨基苯乙酰头孢菌素;头孢噻啶;头孢噻吩钠;头孢匹林钠;头孢拉定;盐酸西托环素;乙酰氯霉素;氯霉素;棕榈氯霉素;氯霉素泛酸复合物;氯霉素琥珀酸钠;磷酸洗必泰;氯二甲酚;金霉素硫酸氢盐;盐酸金霉素;西诺沙星;环丙沙星;盐酸环丙沙星;西罗霉素;克拉霉素;盐酸克林沙星;克林霉素;盐酸克林霉素;盐酸克林霉素棕榈酸酯;磷酸克林霉素;氯法齐明;氯唑西林苄;邻氯青霉素钠;氯羟喹;多粘菌素E钠;硫酸粘杆菌素;香豆霉素;香豆霉素钠;氨环烷青霉素;环丝氨酸;达福普汀;氨苯砜;达托霉素;地美环素;盐酸地美环素;去甲环素;德诺芳金(denofungin);二氨藜芦啶;双氯西林;双氯西林钠;硫酸二双氢链霉素;双吡硫翁;红霉素;强力霉素;强力霉素钙;磷酸多西环素复合物;盐酸多西环素;屈克沙星钠;依诺沙星;依匹西林;差向四环素盐酸;红霉素;红霉素苯基金鸡纳酸盐;依托红霉素;琥乙红霉素;葡庚糖酸红霉素;乳糖酸红霉素;丙酸红霉素;硬脂酸红霉素;盐酸乙胺丁醇;乙硫异烟胺;氟罗沙星;氟氯西林;氟氘丙氨酸;氟甲喹;磷霉素;磷霉素氨丁三醇;呋莫西林;呋唑氯氯化物;呋唑氯酒石酸;夫西地酸钠;夫西地酸;硫酸庆大霉素;格洛莫南;短杆菌肽;碘炔三氯酚;海他西林;海他西林钾;海克西定;依巴沙星;亚胺培南;异帕米星;异康唑;异烟肼;交沙霉素;硫酸卡那霉素;吉他霉素;左呋喃他酮;左普匹西林钾;左普匹西林;洁霉素;盐酸林可霉素;洛美沙星;盐酸洛美沙星;甲磺酸洛美沙星;氯碳头孢;磺胺米隆;甲氯环素;磺基水杨酸氯甲烯土霉素;巨霉素磷酸二氢钾;美喹多司;罗培南;甲烯土霉素;盐酸甲烯土霉素;乌洛托品;马尿酸乌洛托品;孟得立酸乌洛托品;甲氧西林钠;美替普林;盐酸甲硝唑;磷酸甲硝唑;美洛西林;美洛西林钠;米诺环素;盐酸米诺环素;盐酸米林霉素;莫能菌素;莫能菌素钠;萘夫西林钠;萘啶酸钠;萘啶酸;纳他霉素;暗霉素;新霉素棕榈酸酯;硫酸新霉素;新霉素十一碳烯酸盐;硫酸奈替米星;中性霉素;尼发噻唑;硝呋拉定;硝呋地腙;硝呋太尔;硝呋隆;硝呋达齐;硝呋米特;硝呋吡醇;硝呋奎唑;硝环素;呋喃妥;硝米特;诺氟沙星;新生钠;氧氟沙星;昂托普利(onnetoprim);苯唑青霉素钠;肟莫南;肟莫南钠;欧索林酸;土霉素;土霉素钙;盐酸土霉素;帕地霉素;对氯酚;保洛霉素;培氟沙星;甲磺酸培氟沙星;培那西林;青霉素G苄;青霉素G钾;青霉素G普鲁卡因;青霉素G钠;青霉素V钾;青霉素V苄;海巴青霉素;青霉素V钾;戊齐酮钠;苯基氨基;哌拉西林钠;吡苄西林钠;吡苄西林钠;盐酸吡利霉素;盐酸匹氨西林;匹氨西林噻嘧啶;磺胺匹氨西林;硫酸多粘菌素B;紫菜霉素;普匹卡星;吡嗪酰胺;羟基吡啶硫酮锌;醋酸喹地卡明;奎奴普丁;消旋甲砜霉素;莫拉宁;雷尼霉素;雷洛霉素;瑞普米星;利福布汀;利福美坦;利福克昔;利福米特;利福平;利福喷丁;利福昔明;罗利环素;硝酸罗利环素;罗沙米星;丁酸罗沙米星;丙酸罗沙米星;罗沙米星磷酸钠;硬脂酸罗沙米星;罗索沙星;洛克沙砷;罗红霉素;山环素;山费培南钠;沙莫西林;沙匹西林;吸水真菌素;西索米星;硫酸西索米星,司帕沙星;盐酸大观霉素;螺旋霉素;盐酸司他霉素;司替霉素;硫酸链霉素;烟肼链霉素;磺胺苯;磺胺苯酰;乙酰磺胺;乙酰磺胺钠;磺胺西汀;磺胺嘧啶;磺胺嘧啶钠;磺胺多辛;磺胺林;磺胺甲基嘧啶;磺胺对甲氧嘧啶;磺胺二甲嘧啶;磺胺甲二唑;复方新诺明;磺胺间甲氧嘧啶;磺胺恶唑;磺胺酸锌;磺胺硝苯;柳氮磺胺嘧啶;磺胺异噻唑;磺胺噻唑;磺胺吡唑;磺胺异恶唑;醋磺胺异恶唑;硫代异唑二醇;磺粘菌素;硫培南;舒他西林;森西林钠;盐酸酞氨西林;替考拉宁;盐酸替马沙星;替莫西林;磷酸四环素复合物;四氧普林;甲砜霉素;甲砜霉素钾;替卡西林甲酚钠;替卡西林二钠;替卡西林单钠;氯苯异噻酮;噻碘氯铵;妥布霉素;硫酸妥布霉素;妥舒沙星;甲氧苄啶;硫酸甲氧苄啶;三重磺胺嘧啶;丙大观霉素;硫酸丙大观霉素;短杆菌素;万古霉素;盐酸万古霉素;维吉霉素;和佐尔博霉素。
抗癌辅助增强剂:阿米替林;莫沙平;霉素B;抗心律失常药物(如奎尼丁);降压药物(如利血平),钙离子Ca2+拮抗剂(如维拉帕米;钙调素抑制剂(如心可定;卡罗维林);西酞普兰);氯米帕明;氯米帕明);昔帕明;多虑平;马普替林);硝苯地平;尼群地平;非三环抗忧郁药物(如舍曲林;去甲阿米替林;普罗替林;磺基肟)和多药耐药还原剂如聚氧乙基代蓖麻油;硫醇耗竭剂(例如,丁胱;曲唑酮;三环抗忧郁药物(如丙咪嗪;三氟拉嗪;曲米帕明;帕拉诺类似物(如三苯氧胺)
抗胆石剂:单辛酸醋。
抗胆囊炎剂:鹅二醇;乌索二醇。
抗胆碱剂:枸橼酸阿尔维林;溴甲辛托品;阿托品;盐酸阿托品氧化物;硫酸阿托品;颠茄;盐酸贝那利秦;盐酸苄替米特;苯咯溴铵;比哌立登;盐酸比哌立登;乳酸比哌立登;克利溴铵;盐酸环喷托酯;右苄替米特;盐酸双环维林;盐酸双己维林;多马唑啉富马酸;依兰群;依鲁卡因;乙苄托品;盐酸尤卡托品;格隆溴铵;海特溴铵;氢溴酸后马托品;甲溴后马托品;莨菪碱;溴氢酸莨菪碱;硫酸莨菪碱;异丙碘铵;溴美喷酯铵;硝酸溴甲阿托品;美托喹嗪;氯化奥昔布宁;溴帕拉喷酯;戊哌铵硫酸甲酯;芬卡米特;泊尔定硫酸甲酯;丙谷胺;溴丙胺太林;盐酸奥昔利平;氢溴酸东莨菪碱;甲硫托铵酯;盐酸替喹胺;盐酸托芬那辛;托喹嗪;硫酸曲安吡嗪;盐酸苯海索;托吡卡胺。
抗凝血剂:安克洛酶;阿地肝素钠;比伐卢定;溴茚二酮;达肝素钠地西卢定;双香豆素;阿朴酸钠;甲磺酸奈莫司他;苯丙香豆素;亭扎肝素钠;华法林钠。
抗球虫剂:马杜霉素。
抗惊厥剂:阿布妥因;氨托利;阿托利特;布拉氨酯;桂溴胺;西替酰胺;氯硝西泮;环庚米特;地秦胺;双丙戊酸钠;依特比妥;乙琥胺;乙苯妥英;盐酸氟西泮;氟齐胺;磷苯妥英钠;加巴喷丁;伊来西胺;拉莫三嗪;硫酸镁;美芬妥英;甲苯比妥;美替妥英;甲琥胺;盐酸米拉醋胺;大麻折尼;盐酸萘咪酮;硝西泮;苯乙酰脲;苯巴比妥;苯巴比妥钠;苯琥胺;苯妥英;苯妥英钠;扑米酮;卤加比;雷利托林;盐酸立马醋胺;罗匹嗪;沙贝鲁唑;司替戊醇;舒噻嗪;托吡酯;三甲双酮;丙戊酸钠;丙戊酸;喜保宁;盐酸佐尼氯唑;和唑尼沙胺。
抗抑郁剂:阿地唑仑;甲磺酸阿地唑仑;阿拉丙酯;盐酸烯丙他明;盐酸氨甲达林;盐酸阿米替林;马来酸阿普氮平;富马酸阿扎克生;氮卓吲哚;盐酸阿齐帕明;盐酸比培那醇;盐酸安非他酮;盐酸布替林;卡罗沙酮;卡他唑酯;西科拉欣多(ciclazindol);盐酸西多塞平;甲磺酸西洛巴明;盐酸氯达酮;盐酸氯米帕明;富马酸可替宁;胺氢咔唑;盐酸苯环戊胺;盐酸环丙利多;环丙米特;甲苯磺酸达来达林;盐酸达泊西汀;马来酸苯唑吡醇;盐酸氮卓尼尔;盐酸昔帕明;右旋咪唑;德西吗芬(deximafen);盐酸二苯西平;盐酸地奥沙屈;盐酸度琉平;盐酸多塞平;盐酸度洛西汀;马来酸依氯那明;恩环丙酯;盐酸依托哌酮;盐酸泛曲酮;苯甲吗酮;富马酸非唑拉明;盐酸氟曲辛;氟西汀;盐酸氟西汀;盐酸氟洛克生;更非辛;硫酸胍诺西芬;盐酸伊马芬;盐酸咪洛克生;盐酸米帕明;盐酸茚洛秦;盐酸英曲替林;胺丙吲哚;异恶唑酰肼;富马酸氧丙咪嗪;盐酸洛非帕明;氯他拉明;马普替林;盐酸马普替林;盐酸美利曲辛;盐酸康多尔;米氮平;吗氯贝胺;硫酸莫达林;盐酸萘帕他定;盐酸奈帕咪唑;盐酸法唑酮;尼索西汀;盐酸硝呋坦;诺米芬新马来酸;盐酸去甲替林;磷酸奥克替林;奥盐酸匹哌醇;盐酸羟丙替林;奥昔哌汀;帕罗西汀;硫酸苯乙肼;盐酸吡喃达明;盐酸普立地芬;盐酸普罗林坦;盐酸普罗替林;喹哌嗪马来酸;罗利普令;盐酸塞罗西汀;盐酸舍曲林;舒必利;舒立托唑;盐酸他美曲林;富马酸坦帕明;盐酸坦达明;盐酸硫西新;托扎啉酮;盐酸托莫西汀;盐酸曲唑酮;盐酸曲苯佐明;曲米帕明马来酸;盐酸文拉法辛;盐酸维洛沙秦;盐酸齐美定;和佐美他平。
降糖药:醋酸己脲;丁福明;盐酸布他沙明;卡麦保斯(camighbose);氯磺丙脲;环格列酮;恩格列酮钠;盐酸依托福明;格列胺脲;格列波脲;格列他尼钠;格列氟胺;格列吡嗪;高血糖素;格列本脲;格列己脲;格列己脲钠;格列辛脲;格列帕脲;胰岛素;人胰岛素;人锌胰岛素;长效人胰岛素;低精蛋白人胰岛素;赖脯胰岛素;锌胰岛素;长效锌胰岛素;速效锌胰岛素;达拉内特(Dalanated)胰岛素;低精蛋白胰岛素;中性胰岛素;利诺格列;富马酸利诺格列;二甲双胍;甲基帕莫酸;帕莫酸钠;盐酸吡格列酮;酒石酸吡咯格列;人胰岛素原;醋酸司格列肽;妥拉磺脲;甲苯磺丁脲;托喷磺脲;曲格列酮;和唑泊司他。
止泻药:盐酸芬诺酯;甲泼尼龙;甲硝唑;和罗加米定。
抗利尿药:精氨加压素;醋酸去氨加压素;赖氨加压素。
解毒药:二巯丙醇;依酚氯铵;甲吡唑;左亚叶酸钙;亚甲蓝;和硫酸精蛋白。
抗痢药:盐酸司来吉兰。
止吐药:盐酸阿洛司琼;盐酸巴他必利;贝美司琼;苯喹胺;氯丙嗪;盐酸氯丙嗪;氯波必利;盐酸赛克力嗪;茶苯海明;地芬尼多;盐酸地芬尼多;芬尼嘧啶;甲磺酸多拉司琼;吗丁啉;屈大麻酚;氟美立酮;盐酸加丹司琼;格拉司琼;盐酸格拉司琼;甲磺酸卢罗司琼;盐酸美克洛嗪;盐酸甲氧氯普胺;美托哌丙嗪;丙氯拉嗪;乙二磺酸丙氯拉嗪;马来酸丙氯拉嗪;盐酸异丙嗪;硫乙拉嗪;苹果酸硫乙拉嗪;马来酸硫乙拉嗪;盐酸曲美苄胺;和盐酸美托必利。
抗癫痫药:氟齐胺;拉莫三嗪;氯瑞唑;托加比特。
抗雌激素:氯甲孕酮;盐酸萘福昔定;枸椽酸硝米芬;盐酸雷洛昔芬;枸橼酸他莫昔芬;枸橼酸托瑞米芬;甲磺酸曲沃昔芬。
抗丝素蛋白药:甲磺酸萘莫司他。
抗真菌药物:吖啶琐辛:安布替星;阿扎康唑;偶氮丝氨酸;巴西芬净;联苯苄唑;硝酸布康唑;十一(碳)烯酸钙;克念菌素;己氨胆碱-品红;氯登妥因;环吡酮;环吡酮胺;西洛芬净;顺康唑;克霉唑;铜迈星;多康唑;益康唑;硝酸益康唑;恩康唑;硝酸依托南;硝酸芬替康唑;菲利平;氟康唑;氟胞嘧啶;真菌霉素;灰黄霉素;哈霉素;伊曲康唑;卡拉真菌素;酮康唑;洛莫夫金(lomoftmgin);利地霉素;蓖麻毒素;咪康唑;硝酸咪康唑;莫能菌素;莫能菌素钠;盐酸萘替芬;硝呋太尔硝呋美隆;盐酸硝拉明;制霉菌素;辛酸;硝酸奥康唑;硝酸奥昔康唑;盐酸奥昔芬净;盐酸帕康唑;帕曲星;碘化钾;吡咯尼群;芦他霉素;血根氯铵;沙康唑;硫化硒;西奈芬净;硝酸硫康唑;疗霉舒;特康唑;福美双;噻康唑;托西拉酯;托林达酯;托萘酯;三醋汀;三嗪芬净;十一烯酸;绿黄菌素;十一烯酸锌;和盐酸齐诺康唑。
抗青光眼剂:盐酸阿普利诺辛(Alprenoxime Hydrochloride);考福新;盐酸地匹福林;盐酸大麻克酯;毛果芸香碱;珀纳宾(Pirnabine)。
止血药:聚氨葡糖。
抗血液流变药:己酮可可碱。
抗组胺药:阿伐斯汀;磷酸安他唑啉;马来酸阿扎他定;巴马斯汀;盐酸溴马秦;马来酸溴吡拉;马来酸卡比沙明;盐酸西替利嗪;马来酸氯苯那敏;氯苯那敏-磺化二乙烯苯-乙烯苯共聚物;塞马利嗪(cirmarizine);氯马斯汀;富马酸氯马斯汀;乙酰氯西拉敏;马来酸赛利拉敏;赛克力嗪;盐酸赛庚啶;右马来酸溴苯那敏;马来酸右氯苯那敏;马来酸二甲茚定;枸椽酸苯海拉明;盐酸苯海拉明;盐酸多拉斯汀;琥珀多西拉敏;依巴斯汀;盐酸非索非那定;盐酸左卡巴斯汀;氯雷他定;盐酸米安色林;诺柏斯汀;枸椽酸奥芬那君;吡拉布隆;马来酸美吡拉敏;马来酸吡咯沙敏;盐酸罗卡斯汀;罗托沙敏;盐酸他齐茶碱;替美斯汀;特非那丁;枸椽酸曲吡那敏;盐酸曲吡那敏和盐酸曲普利啶。
降脂药:考来烯胺树脂;安妥明;盐酸考来替泊;克伐他汀;达伐他汀;右甲状腺素钠;氟伐他汀钠;吉非贝齐;来西贝特;洛伐他汀;烟酸;普伐他汀钠;普罗布考;辛伐他汀;替奎安;和联苯丁酸。
抗高脂蛋白血症药:阿昔呋喃;贝洛酰胺;苯扎贝特;波克昔定;西他苯钠;环丙贝特;四甲癸二醇;卤芬酯;利贝特;美格鲁托;萘酚平;盐酸匹美汀;羟乙茶碱安妥明;替贝酸;曲洛酯。
抗高血压药:盐酸阿呋唑嗪;阿利帕胺;阿尔噻嗪;盐酸氨喹新;醋酸阿那立肽;马来酸阿替丙嗪;贝磷地尔;贝米曲啶;甲磺酸苯达洛尔;苄氟噻嗪;苄醌氯铵;硫酸倍他尼定;盐酸二氯地尔;比索洛尔;富马酸比索洛尔;盐酸布新洛尔;丁吡考胺;布噻嗪;坎沙曲里拉特;坎沙曲拉;卡托普利;西罗普利;氯噻嗪钠;西氯他宁;西拉普利;可乐定;盐酸可乐定;克罗帕米;环戊噻嗪;环噻嗪;达罗地平;硫酸异喹胍;盐酸地拉普利;硫米齐特;二氮嗪;盐酸硫氮卓酮;苹果酸硫氮酮;地替吉仑;甲磺酸多沙唑嗪;依卡曲尔;马来酸依那普利;依那普利;依那吉仑;甲磺酸恩屈嗪;依匹噻嗪;依普罗沙坦;甲磺酸依普罗沙坦;甲磺酸非诺多泮;马来酸黄酮地洛;氟地平;氟司喹南;福辛普利钠;福辛普利拉;胍那苄;醋酸胍那苄;硫酸胍那克林;硫酸胍那决尔;胍那佐定;胍那佐定单硫酸酯;硫酸胍那佐定;盐酸胍法辛;硫酸胍尼索喹;硫酸胍氯酚;盐酸胍诺克汀;胍诺沙苄;硫酸胍生;硫酸胍诺西芬;盐酸胍那克林;硫酸胍那决尔;盐酸肼屈嗪;肼屈嗪-磺化二乙烯苯-乙烯苯共聚物;氢氟噻嗪;茚达立酮吲达帕胺;盐酸吲哚普利;吲哚拉明;盐酸吲哚拉明;盐酸吲哚瑞酯;拉西地平;来尼喹新;赖诺普利;盐酸洛非西定;洛沙坦钾;盐酸洛硫嗪;美布氨酯;盐酸美加明;美沙洛尔;盐酸美沙洛尔;美沙噻嗪甲氯噻嗪甲基多巴;盐酸盐酸甲基多巴乙酯;美替洛尔;富马酸美托拉宗美托洛尔;甲基酪氨酸;米诺地尔;莫唑胺;莫唑胺;奈必洛尔;硝苯地平;奥福宁;盐酸帕吉林;帕佐昔特;盐酸培兰色林;培哚普利;盐酸酚苄明;吡那地尔;匹伏普利;泊利噻嗪;盐酸哌唑嗪;盐酸普齐地洛;盐酸喹那普利;喹普利拉;盐酸喹唑嗪;盐酸喹洛雷;盐酸喹吡罗;纽溴铵;雷米普利;蛇根木;利血平;沙普立沙坦钾;醋酸沙拉新;硝普钠;盐酸硫氧洛尔;他索沙坦;盐酸替莫普利;盐酸特拉唑嗪;特拉吉仑;噻甲压定;盐酸噻甲压定;替尼酸;替大麻酚;硫达唑嗪;盐酸噻戊托辛;三氯噻嗪;盐酸曲马唑嗪;樟磺咪芬;盐酸曲莫沙明;曲帕胺;希帕胺;盐酸扎吉仑;精氨酸佐芬普利拉。
抗低血压药:盐酸环拉福林和盐酸米多君。
抗感染药物:阿昔洛韦;盐酸二氟沙星;艾滋病毒和其它逆转录病毒的整合酶抑制剂;月桂异喹啉铵;拉氧头孢二钠;奥硝唑;喷替米星;艾滋病毒和其它逆转录病毒的蛋白酶抑制剂;盐酸沙氟沙星。
抗感染药物(外用):酒精;盐酸氨吖啶;苄索氯铵;硫氯酚钠;溴氯唑酮;过氧化脲;西他氯铵;西吡氯铵;盐酸氯己定;度米芬;芬替克洛;氟唑氯铵;品红,碱性;呋喃唑酮;龙胆紫;哈尔奎诺(Halquinols);六氯酚;双氧水;鱼石脂;咪癸碘;碘;异丙酒精;醋酸磺胺米隆;汞林钠;氯化苯酚汞;氯化氨汞;甲苄索氯铵;呋喃西林;硝甲酚汞;盐酸奥替尼啶;奥昔氯生;奥昔氯生钠;对氯酚;樟脑;高锰酸钾;聚维酮碘;氯司帕唑;硝酸银;磺胺嘧啶银;氯氧三嗪;硫汞苯磺钠;硫柳汞;和曲氯新钾。
抗炎药:阿氯芬酸;双丙酸阿氯米松;丙缩阿尔孕酮;阿尔法淀粉酶;安西法尔;安西非特;氨芬酸钠;盐酸氨普立糖;阿那白滞素;阿尼扎芬;阿扎丙宗;巴柳氮钠;苄达酸;菠萝蛋白酶;溴哌莫;布地奈德;卡洛芬;环洛芬;辛喷他宗;克利洛芬;丙酸氯倍他索;氯倍他松丁酸;氯吡酸;氯硫卡松丙酸;醋酸可米松;可托多松;地夫可特;地奈德;去羟米松;二丙酸地塞米松;双氯芬酸钾;双氯芬酸钠;二氟拉松双乙酸钠;二氟米酮钠;二氟泼尼酯;地弗他酮;二甲基亚砜;羟西奈德;恩甲羟松;恩莫单抗;依诺利康钠;依托度酸;联苯乙酸;非那莫;芬布芬;芬氯酸;苯克洛酸;芬度柳;芬匹帕龙(fenpipalone);芬替酸;夫拉扎酮;氟扎可特;氟芬那酸;芬氟咪唑;醋酸氟尼缩松;氟可丁丁酯;醋酸氟米龙;氟喹宗;氟瑞托芬;丙酸氟替卡松;呋喃洛芬;呋罗布芬;哈西奈德;丙酸卤倍他索;醋酸卤泼尼松;布洛芬;布洛芬铝;布洛芬吡啶甲醇;伊洛达普;吲哚美辛钠;吲哚美辛;吲哚洛芬;吲哚克索;吲四唑;醋酸异氟泼尼龙;伊索克酸;伊索昔康;酮洛芬;氯诺昔康;恩波氯替泼诺;甲氯胺苯酸钠;甲氯芬那酸;甲氯松二丁酸;美沙拉嗪;美西拉宗;磺庚甲泼尼龙;吗尼氟酯;萘丁美酮;尼马宗;奥沙拉嗪钠;奥克丁;奥帕诺辛;奥沙普秦;羟布宗;盐酸瑞尼托林;戊聚糖局聚硫酸钠;布宗甘油酸钠;吡罗昔康;肉桂酸吡罗昔康;吡洛芬;泼那扎特;泼尼松龙磷酸钠;普立非酮;普罗度酸;普罗喹宗;利美索龙;氯马扎利;沙那西定;司克拉宗;丝美辛;舒多昔康;舒林酸;舒洛芬;他尼氟酯;替尼达普;替尼达普钠;替诺昔康;替昔康;特斯米德(tesimide);替可的松匹伐酯;托美丁;托美丁钠;三氯奈德;三氟米酯;和齐多美辛。
抗角质化药:度维A;罗汀;培维A。
抗疟疾药:盐酸阿莫地喹;氨喹酯;阿替夫林;氯喹;盐酸氯喹;恩波环氯胍;磷酸恩哌罗林;盐酸对卤泛曲林;硫酸羟氯喹;盐酸甲氟喹;美诺克酮;磷酸伯氨喹;乙胺嘧啶;硫酸奎宁;和替布喹。
抗菌药:氨曲南;洗必泰葡萄糖;咪唑烷脲;氨棕己胺;硝溴生;吡拉莫南钠:丙酸;吡硫翁钠;和双胆碱替吉莫南。
抗偏头痛药:盐酸纳拉曲坦;马来酸麦角克索;琥珀舒马曲坦;马来扎托司琼。
抗有丝分裂药:普达非洛。
抗真菌药:阿莫罗芬。
止吐药:盐酸布克力嗪;和乳酸赛克力嗪。
抗肿瘤药:阿西维辛;阿克拉霉素;盐酸阿考达唑;阿克罗宁;阿多来新;阿地白介素;六甲蜜胺;安波霉素;醋酸阿美蒽醌;安吖啶;阿那曲唑;安曲霉素;天冬酰胺酶;曲林菌素;阿扎胞苷;阿扎替派;阿佐霉素;巴马;苯佐替派;比卡鲁胺;盐酸比生群;二甲磺酸双奈法德;比折来新;硫酸博莱霉素;布喹那钠;溴匹立明;白消安;放线菌素C;卡普睾酮;卡醋胺;卡贝替姆;卡铂;卡氮芥;盐酸卡柔比星;卡折来新;西地芬戈;苯丁酸氮芥;顺铂;克拉屈滨;甲磺酸克里斯托(Crisnatol Mesylate);环磷酰胺;阿糖胞苷;达卡巴嗪;更生霉素;盐酸柔红霉素;地西他滨;右奥马铂;地扎胍宁;甲磺酸地扎胍宁;地吖醌;泰索帝;阿霉素;盐酸阿霉素;屈洛昔芬;枸椽酸屈洛昔芬;丙酸屈他雄酮;阿佐霉素;依达曲沙;盐酸依氟鸟氨酸;依沙芦星;恩洛铂;恩普氨酯;依匹哌啶;盐酸表阿霉素;厄布洛唑;盐酸依索比星;雌莫司汀;雌莫司汀磷酸钠;依他硝唑;乙碘[I131]油;依托泊苷;依托泊苷磷酸盐;埃托啡;盐酸法倔唑;法扎拉滨;芬维A胺;氟尿苷;磷酸氟达拉滨;氟尿嘧啶;氟西他滨;磷喹酮;福司曲星钠;吉西他滨;盐酸吉西他滨;胶体金[Au198];羟基脲;盐酸伊达比星;异环磷酰胺;伊莫福新;干扰素α-2a;干扰素α-2b;干扰素α-n3;干扰素α-nl;干扰素β-Ia;干扰素γ-Ib;异丙铂;盐酸伊立替康;异维A酸;醋酸兰瑞肽;来曲唑;醋酸亮丙瑞林;盐酸利阿唑;洛美曲索钠;洛莫司汀;盐酸洛索蒽醌;马索罗酚;美登素;盐酸氮芥;醋酸甲地孕酮;醋酸美仑孕酮;马法兰;美诺立尔;巯嘌呤;甲氨蝶呤;甲氨蝶呤钠;米托普林;美妥替哌;米丁度胺;米托克星;米托氯明;米托洁林;米托马星;丝裂霉素;米托司培;米托坦;盐酸米托;麦考酚酸;诺考达唑;诺拉霉素;奥马铂;奥昔舒仑;紫杉醇;培门冬酶;培利霉素;奈莫司汀;硫酸培洛霉素;培磷酰胺;哌泊溴烷;哌泊舒凡;盐酸吡罗蒽醌;普卡霉素;普洛美坦;卟吩姆钠;泼尼莫司汀;盐酸丙卡巴肼;嘌罗霉素;盐酸嘌罗霉素;吡唑呋喃菌素;利波腺苷;罗谷亚胺;沙芬戈;盐酸沙芬戈;司莫司汀;辛曲秦;斯帕福斯特钠(Sparfosate Sodium);司帕霉素;盐酸锗螺胺;螺莫司汀;螺铂;链黑霉素;佐星;氯化锶(锶89);磺氯苯脲;他利霉素;紫杉烷;紫杉烷二萜;特考伽兰钠(Tecogalan Sodium);替加氟;盐酸替洛蒽醌;替莫泊芬;替尼泊苷;替罗昔隆;睾内酪;西阿密普林(thiamiprine);硫唑嘌呤胺;硫鸟嘌呤;塞替派;噻唑呋林;替拉扎明;盐酸托泊替康;磷酸曲西立滨;三甲曲沙;三甲曲沙葡糖醛酸脂;曲普瑞林;盐酸妥布氯唑;尿嘧啶芥;乌瑞替派;伐普肽;维替泊芬;硫酸长春碱;硫酸长春新碱;长春地辛;硫酸长春地辛;硫酸长春匹定;硫酸长春甘酯;硫酸长春罗新;酒石酸长春瑞滨;硫酸长春罗定;硫酸长春利定;伏氯唑;折尼铂;净司他丁斯酯;和盐酸佐柔比星。
抗肿瘤化合物(附助剂):20-桥-1,25-二羟基维生素D3;5-乙炔尿嘧啶;阿比特龙;酰基富烯;腺环戊醇;ALL-TK拮抗剂;氨莫司汀;克拉度酸;阿米福汀;氨基酮戊酸;氨柔比星;阿那格雷;穿心莲内酯;血管生成抑制剂;拮抗剂D;拮抗剂G;安雷利克斯;抗雄激素;抗前列腺癌制剂;抗背部化形态发生蛋白-1;抗雌激素剂;抗恶性肿瘤剂;反义寡核苷酸;阿非迪霉素甘氨酸;凋亡基因调节剂;凋亡调节剂;脱嘌呤酸;Ara-CDP-DL-PTBA;精氨酸脱氨酶;阿苏拉林(asulacrine);阿他美坦;阿莫司汀;海洋环肽1;海洋环肽2;海洋环肽3;阿扎司琼;阿扎毒素;重氮酪氨酸;巴卡丁III衍生物;巴拉醇(balanol);BCR/ABL拮抗剂;苯并二氢卟吩;苯甲酰星孢菌素;β-内酰胺衍生物;贝塔阿勒欣(β-alethine);β-克拉霉素B;桦木酸;bFGF抑制剂;比生群;二氮丙啶精氨酸;双奈法德;比斯塔汀A(bistrateneA);布雷菲德菌素;布度钛;丁胱硫;卡泊三醇;卡弗他丁C;喜树碱衍生物;金丝雀痘白细胞介素-2;卡培他滨;酰胺-氨基氮唑;氨基三氮唑羧酸酯;CaRest MI;CARN 700;软骨源抑制剂;酪蛋白激酶抑制剂(ICOS);栗树精胺;抗菌肽B;西曲瑞克;双氢叶吩类;氯喹喔啉磺胺类药物;西卡前列素;独联体卟啉;氯米芬衍生物;考利斯霉素A(collismycinA);考利斯霉素B(collismycin B);考布他丁A4;考布他丁衍生物;考那格宁(conagenin);甘蓝海绵提取物816;克里斯纳陶(crisnatol);自念珠藻环肽8;自念珠藻环肽衍生物;库拉欣A(curacin A);环戊烷醌;环戊烷醌;莎草霉素(cypemycin);阿糖胞苷十八烷基磷酸;细胞溶解因子;磷酸己烷雌酚;达昔单抗;脱氢滴澄宁B;右异环磷酰胺;右旋维拉帕米;滴澄宁B;DIDOX 3,4-二羟荃苯并氧肟酸;二乙基瑙斯品宁(diethylnorspennine);二氢氮胞苷;二氢-9-紫杉醇;迪奥萨霉素(Dioxamycin);二苯螺内酯;甘二烷醇;杜冷丁;去氧氟尿苷;多卡霉素SA(duocarmycin SA);依布硒;依考莫司汀;依地福新;依决洛单抗;二氟甲基鸟氨酸;榄香烯;乙嘧替氟;表阿霉素;阿雌莫司汀类似物;雌激素受体激动剂;雌激素拮抗剂;依西美坦;法倔唑;氟卓斯汀;黄酮吡多;去氢表雄酮类似物;氟达拉滨;盐酸氟道儒尼星(Fluorodaunorunicin Hydrochloride);福酚美克;福美坦;福司曲星;福莫司汀;莫特沙芬钆;硝酸镓;加洛他滨;加尼瑞克;明胶酶抑制剂;谷胱甘肽抑制剂;庚磺胺类;神经调节素;六亚甲基二乙酰胺;金丝桃素;伊班膦酸;去甲氧柔红霉素;艾多昔芬;伊决孟酮;伊洛马司他;咪唑并吖啶酮;免疫刺激剂肽;肽胰岛素样生长因子-1受体抑制剂;干扰素激动剂;干扰素;白细胞介素;碘苄胍;碘化多柔比星;4-甘薯醇;伊立替康;伊罗普拉;伊索拉定;异本伽唑(isobengazole);异侯莫哈利康林(isohomohalicondrin);伊他司琼;加斯普拉诺利得(iasplakinolide,海绵生物中提取的一种环状缩肽);卡哈拉利得F(kahalalide F);片螺素-N氮醋酸;兰瑞肽;雷纳霉素(leinamycin);硫酸香菇多糖;来普斯坦;白血病抑制因子;白细胞α干扰素;亮丙瑞林+雌激素+孕酮;亮丙瑞林;左旋咪唑;利阿唑;线性多胺类似物;脂溶性糖肽;脂溶性铂化合物;噻唑啉海洋环肽7;乐铂;蚯蚓氨酸;洛美曲索;氯尼达明;洛索蒽醌;勒托替康;莫特沙芬镥;里索菲林(lysofylline);溶菌肽;美坦新;甘露莫司汀A;马立马司他;玛斯平(Maspin);基质溶酶抑制剂;基质金属蛋白酶抑制剂;麦尔巴隆;梅特勒林(meterelin);乙硫磷酶;胃复安;MIF抑制剂;米非司酮;米替福新;米立司亭;错配双链RNA;米托胍腙;二溴卫矛醇;丝裂霉素类似物;米托萘胺;米托毒素;米妥毒素(Mitotoxin)成纤维细胞生长因子-皂素;米托蒽醌;莫法罗汀;单克隆抗体,人绒毛膜促性腺激素;单磷酸类脂A+杆菌细胞壁SK;莫哌达醇;多药耐药基因抑制剂;基于治疗的多肿瘤抑制剂1;芥末抗癌剂;印度洋海绵B;结核菌细胞壁提取物;米利亚普隆(myriaporone);N-乙酰氨地那林;法瑞林;纳格瑞斯提普(nagrestip);纳洛酮+酮戊唑辛;纳帕因(napavin);纳福特平(naphterpin);那托司亭;奈达铂;奈莫柔比星;奈莫柔比星酸;中性肽链内切酶;尼鲁米特;尼萨霉素(nisamycin);一氧化氮调节剂;氮氧抗氧化剂;尼图林(nitrullyn);N-取代苯甲酰胺;06-苄基鸟嘌呤;奥琪森酮(okicenone);寡核苷酸;奥那司酮;恩丹西酮;二氯苯磺胺;奥拉素(Oracin);口腔细胞因子诱导剂;奥沙特隆;奥沙利铂;13-脱氧-10-羟基洋红霉素;紫杉醇类似物;紫杉醇衍生物;钯金胺;棕榈酰华根毒素(palmitoylrhizoxin);帕米磷酸;人参三醇;帕诺米芬;副菌铁素;帕折普汀;培地新;喷司他丁;喷司他唑;全氟溴烷;紫苏醇;奋乃静霉素(Phenazinomycin);苯乙酸;磷酸酶抑制剂;毕西巴尼;盐酸毛果芸香碱;吡喃;吡曲克辛;普雷斯汀A(placetinA);普雷斯汀B(placetin B);纤溶酶原激活物抑制因子;铂络合物;铂化合物;铂三胺络合物;丙基双吖啶酮;前列腺素J2;蛋白酶抑制剂;蛋白A-基于免疫调节物;蛋白激酶C抑制剂,蛋白激酶C抑制剂,微藻;蛋白酪氨酸磷酸酶抑制剂;嘌呤核苷磷酸抑制剂;红紫素;吡唑啉吖啶;吡哆醛血红蛋白耦联聚氧乙烯;Raf拮抗剂;雷替曲塞;雷莫;拉斯菲姆西(Ras famesyl)蛋白转移酶抑制剂;Ras基因抑制剂;Ras-GAP抑制剂;脱甲基利特里普汀(Retelliptine Demethylated);铼,Re186依替膦酸;利索新;核酶;RII维胺酸;罗希吐碱;罗莫肽;罗喹美克;卢比基酮B1(rubiginone B1)如波希尔(ruboxyl)沙芬戈;塞恩托品(saintopin);SarCNU;萨考菲托A(sarcophytol A);SDil类似物;衰老源性抑制剂-1;正义寡核苷酸;信号传导抑制剂;信号转导调制剂;单链抗原结合蛋白;西佐喃;索布佐生;硼卡钠;苯乙酸钠;扫弗洛(solverol);生长调节素结合蛋白;索纳明;膦门冬酸;斯匹卡霉素D(spicamycin D);脾脏五肽;海绵他汀1;角鲨胺;干细胞抑制剂;干细胞分裂抑制剂;斯蒂匹酰胺(stipiamide);基质分解抑制剂;萨菲诺辛(sulfinosine);超活性血管活性肠肽拮抗剂;苏拉蒂斯塔(suradista);苏拉明;苦马豆素;合成糖胺聚糖;他莫司汀;他莫昔芬锡肌松;牛磺莫司汀;特鲁拉皮里留姆(tellurapyrylium);端粒酶抑制剂;替莫唑胺;四氯十氧化物;四氮胺;白篷草三甲基硝基苯;酞胺哌啶酮;西奥考拉林(Thiocoraline,一种环二聚硫环缩肽);血小板生成素;血小板类似物;胸腺素;胸腺五肽受体激动剂;胸腺曲南;促甲状腺激素;锡乙基初紫红素;二氯二茂钛;托泊替康;托普辛亭(topsentin);托瑞米芬;全能性干细胞因子;转译抑制剂;三乙酰基胆碱;曲西立滨;托烷司琼;妥罗雄脲;酪氨酸激酶抑制剂;酪氨酸磷酸化抑制剂;UBC抑制剂;乌苯美司;泌尿生殖窦衍生生长抑制因子;尿激酶受体拮抗剂;瓦里奥林B(variolin B);载体系统,红细胞基因疗法;维拉雷琐;藜芦胺;弗丁斯(verdins);诺维本;长春磷汀;维塔辛(vitaxin,单抗);亚苄维C;净司他丁斯酯。
免疫调节药:惠尔血;来格司亭;莫拉司亭;瑞拉司亭;沙格司亭。
抗强迫症剂:马来酸氟伏沙明。
抗蠕虫剂:阿维菌素;氯舒隆;伊维菌素。
抗帕金森症药:甲磺酸苯托品;比哌立登;盐酸比哌立登;乳酸比哌立登;卡比-左旋多巴;卡金刚酸;盐酸西拉多巴;多巴金刚;盐酸普罗吩胺;拉扎贝胺;左旋多巴;盐酸洛美曲林;盐酸莫非吉兰;盐酸那高利特;硫酸帕立太特;盐酸丙环定;盐酸罗匹尼罗;托卡朋。
止泻药:盐酸地芬诺辛;地芬诺辛;氟哌醇胺;盐酸利达脒;盐酸洛哌丁胺;马来他姆;奴芬克索;樟脑鸦片酊。
抗卡氏肺孢子虫药:阿托夸酮。
抗风湿药:吡曲克辛丙脒。
抗前列腺增生药:西托糖苷。
抗原虫药:阿莫地喹;阿扎硝唑;班硝唑;无水卡硝唑;金霉素硫酸氢盐;盐酸金霉素;氟苯达唑;氟硝唑;卤夫酮氢溴酸;盐酸咪多卡;异丙硝唑;米索硝唑;吗硝唑;硝苯胂酸;异甲硝唑;舒硝唑;替硝唑。
止痒药:甲地嗪;甲地嗪盐酸;和美丙嗪酒石酸。
治牛皮癣药:阿维A;蒽;阿扎立平;卡泊三烯;放线菌酮;磷酸依那扎群;阿维A酯;富马酸利阿唑;氯萘帕林;和替泊沙林。
抗精神病药:马来酸醋奋乃静;阿仑替莫氢溴酸;阿尔哌汀;阿扎哌隆;马来酸巴氮平;苯哌利多;盐酸苄吲吡林;溴比呋辛(brofoxine,6-溴-4,4-二甲基-1,4-二氢苯并噁唑-2-酮);溴哌利多;溴哌利多癸;盐酸布他拉莫;布他哌嗪;马来布他哌嗪;马来酸卡吩嗪;盐酸卡伏曲林;氯普噻吨;桂哌林;辛曲胺;氯马克仑磷酸盐;氯哌噻吨;氯哌莫齐;氯哌帕生甲磺酸;盐酸氯哌隆;氯噻平;马来酸克劳希斯酰胺(clothixamide maleate);氯氮平;盐酸环丙奋乃静;氟哌啶;盐酸依他唑酯;非尼米特;氟西吲哚;氟甲氮平;氟奋乃静癸;氟奋乃静庚酸盐;盐酸氟奋乃静;氟司哌隆;氟司必林;氟曲林;盐酸吉伏曲林;卤培米特;氟哌啶醇;氟哌啶醇癸;伊潘立酮;盐酸咪多林;仑哌隆;马扎哌汀琥珀;美索哒嗪;美索哒嗪地平;甲硫平;咪仑哌隆;米利哌汀;盐酸吗啉酮;盐酸萘拉诺;盐酸奈氟齐特;奥卡哌酮;奥氮平;奥哌咪酮;五氟利多;喷硫平;奋乃静;哌迷清,哌氧平盐酸;匹泮哌隆;哌西他嗪;哌泊噻嗪;盐酸匹喹酮;盐酸丙嗪;瑞莫必利;盐酸瑞莫必利;盐酸林卡唑;盐酸氯氟哌醇;舍吲哚;司托哌隆;螺哌隆;硫醚嗪;盐酸硫醚嗪;氨砜噻吨;氨砜噻吨盐酸;盐酸硫哌立酮;盐酸替螺酮;三氟盐酸;三氟哌多;三氟丙嗪;盐酸三氟丙嗪;盐酸齐拉西酮。
抗风湿药:金诺芬;金硫葡糖;宾达利;氯苯扎利钠;苯基丁氮酮;吡拉唑酸;普林米特氨丁三醇;司普立糖。
抗血吸虫药:盐酸贝恩酮;海恩酮;盐酸硫蒽酮;尼立达唑;奥沙尼喹;恩波副品红;和盐酸特罗扎林。
消炎防腐药:氯喔星;梨酮/吡罗克酮;吡罗克酮乙醇胺;和间苯二酚一乙酸酯。
前列腺素类药:阿巴前列素;地前列素;硫酸苯辛替明;奥曲肽;醋酸奥曲肽;奥美拉唑钠;利奥前列素;曲莫前列素。
解痉药:司洛碘铵;盐酸替扎尼定。
抗血栓药:盐酸阿那格雷;达肝素钠;达那肝素钠;盐酸达唑氧苯;硫酸依非加群;依诺肝素钠;伊非曲班;伊非曲班钠;和三苯格雷。
镇咳药:苯佐那酯;枸椽酸布他米酯;盐酸氯苯达诺;可待因磺化二乙烯苯-乙烯苯共聚物;可多克辛;右美沙芬;氢溴酸右美沙芬;右美沙芬磺化二乙烯苯-乙烯苯共聚物;乙基咳宁;愈创哌特;重酒石酸二氢可待因酮;二氢可待因酮磺化二乙烯苯-乙烯苯共聚物;左丙氧芬乙-苯磺酸盐;那可丁;硝酸哌美立特;匹哌氮酯;硫酸琥甲哌酯。
抗溃疡药:醋谷胺铝;卡地姆碘;盐酸西曲酸酯;依尼前列素;依索喹胺;兰索拉唑;拉伏替丁琥珀;米索前列醇;尼扎替丁;诺利溴铵;潘托拉唑;哌法宁;盐酸哌仑西平;雷贝拉唑钠;瑞前列醇;盐酸罗沙替丁醋酸酯;硫糖铝;硫糖酯钾;和托利咪酮。
抗泌尿病药:半胱胺;盐酸半胱胺;和枸橼酸氢钾钠。
抗病毒药物:乙酰化甘露聚糖;阿昔洛韦;阿昔洛韦钠;阿德福韦;阿洛夫定;阿韦舒托;盐酸金刚烷胺;阿拉诺丁;阿立酮;阿替韦啶甲磺酸;阿夫立定;西多福韦;西潘茶碱;盐酸阿糖胞苷;地拉韦啶甲磺酸;地昔洛韦;羟肌苷;二噁沙利;依度尿苷;恩韦拉登;恩韦肟;泛昔洛韦;法莫汀盐酸;非西他滨;非阿尿苷;磷利酯;膦甲酸钠;膦乙醇钠;更昔洛韦;更昔洛韦钠;碘苷;草酸乙酯;拉米夫定;洛布卡韦;盐酸美莫汀;美替沙腙;奈韦拉平;喷昔洛韦;吡罗达韦;利巴韦林;盐酸金刚乙胺;甲磺酸沙奎那韦;盐酸索金刚胺;索立夫定;维司托隆;盐酸替洛隆;曲氟尿苷;盐酸万乃洛韦;阿糖腺苷;磷酸阿糖腺苷;阿糖腺苷磷酸钠;韦罗肟;扎西他滨;齐多夫定;和净韦肟。
食欲抑制剂:盐酸右芬氟拉明;酒石酸苯甲曲秦;和盐酸芬特明。
良性前列腺增生的治疗剂:盐酸坦索罗辛。
血糖调节剂:醋酸己脲和格列吡嗪;氯磺丙脲和人胰岛素。
骨吸收抑制剂:阿仑膦酸钠;依替膦酸钠二钠;和帕米膦酸二钠。
支气管扩张药:沙丁胺醇;硫酸沙丁胺醇;马来酸阿扎那托;盐酸巴米茶碱;甲磺酸比托特罗;布他前列素;盐酸卡布特罗;盐酸氯丙那林;甲磺酸可尔特罗;多沙前列素;多索茶碱;二羟丙茶碱;恩丙茶碱;麻黄碱;盐酸麻黄素;非诺特罗;盐酸苯呤司特;愈甘醚茶碱;硫酸海索那林;盐酸胡喹嗪;异丙托溴铵;异他林;盐酸异他林;甲磺酸异他林;盐酸异丙肾上腺素;硫酸异丙肾上腺素;奥西那林磺化二乙烯苯-乙烯苯共聚物;硫酸奥西那林;甲磺酸尼司特罗;胆茶碱;富马酸吡库特罗;盐酸吡库特罗;醋酸吡布特罗;盐酸吡布特罗;盐酸丙卡特罗;硫酸伪麻黄碱;夸唑定;硫酸夸唑定;消旋肾上腺素;盐酸消旋肾上腺素;盐酸瑞普特罗;利米特罗氢溴酸;沙美特罗;沙美特罗昔萘酸盐;盐酸索特瑞醇;盐酸磺酰特罗;草酸舒洛昔芬;硫酸特布他林;茶碱;异丙氧蒽酸钠;嗪多群;盐酸净特罗。
碳酸酐酶抑制剂:乙酰唑胺;乙酰唑钠;双氯酚胺;多佐胺盐酸;醋甲唑胺;和盐酸司佐胺。
心脏抑制剂:盐酸乙酰卡尼;乙酰胆碱氯化物;阿克索胺;腺苷;胺碘酮;阿普林定;盐酸阿普林定;富马酸阿替利特;二盐酸阿齐利特;比地索胺;马来酸布卡尼;布色酮;克冠酸钠;卡泊酸;西苯唑啉;琥珀酸西苯唑啉;磷酸氯非铵;地索布胺;丙吡胺;磷酸丙吡胺;多非利特;羟布林;醋酸依地福龙;托西依米铵;盐酸恩卡尼;醋酸氟卡尼;富马酸伊布利特;盐酸英地卡尼;富马酸依帕利特;盐酸劳拉义明;盐酸劳卡尼;硫酸甲氧苯汀;盐酸美西律;莫地卡尼;莫雷西嗪;奥昔拉定;盐酸吡美诺;吡拉酰胺;普拉氯铵;盐酸普鲁卡因胺;盐酸普罗帕酮;吡诺林;喹度溴铵;葡萄糖酸奎尼丁;硫酸奎尼丁;盐酸司美利特;马来酸舒立卡尼;妥卡尼;盐酸妥卡尼;和群司卡尼。
保心药:右雷佐生;和曲氟嗪。
强心药:阿托地近;氨力农;贝莫拉旦;布托巴胺;卡巴折伦;琥珀卡沙群;去乙酰毛花苷;洋地黄;洋地黄毒苷;地高辛;多巴酚丁胺;盐酸多巴酚丁胺;乳糖醛巴酚丁胺/道布特咪;酒石酸多巴酚丁胺;依诺昔酮;盐酸伊马唑旦;吲哚利旦;盐酸伊索马唑;乳糖酸左多巴酚丁胺;硫酸利沙齐农;美多力农;米力农;盐酸培力农;匹莫苯;匹罗昔酮;普啉索旦;海葱次苷;喹齐酮;盐酸他佐洛尔;和维司力农。
心血管药剂:多培沙明;和盐酸多培沙明。
脑缺血药剂:盐酸右啡烷。
利胆剂:去氢胆酸;芬西布醇;羟甲香豆素;哌普唑林;辛卡利特;托莰非。
胆碱能药:醋克利定;氯贝胆碱;卡巴胆碱;地美溴铵;右泛醇;碘依可酯;异氟磷;氯醋甲胆碱;甲硫酸新斯的明;溴新斯的明;水杨酸毒扁豆碱;硫酸毒扁豆碱;硝酸毛果芸香碱;和溴吡斯的明。
胆碱能激动药:呫诺美林;和酒石酸呫诺美林。
胆碱酯酶减活化剂:双复磷;氯解磷定;碘解磷定;和甲磺酸解磷定。
球虫抑制药:阿普西特;甲基盐霉素;生度米星;和生度米星钠。
认知辅剂:甲磺酸双氢麦角碱;吡拉西坦;盐酸普拉西坦;硫酸普拉西坦;和盐酸他克林。
认知增强剂:盐酸贝西吡啶;利诺;和西波吡啶。
造影剂:硫酸钡;泛影葡胺钠;赤藓红钠;碘番酸;碘泊酸钠;甲双吡丙酮;和酪泮酸钠。
诊断辅助物:对氨马尿酸钠;阿那佐林钠;阿氯苯宁;苯替酪胺;青霉素聚赖氨酸;布替膦四钠;丁苯宁;球孢菌素;可的瑞林;绵羊萃夫鲁特(ovine triflutate);促肾上腺皮质激素氢氧化锌;促肾上腺皮质激素,里坡希特利(Repository);泛影葡胺葡甲胺;泛影酸;锡克试验用白喉毒素;地索苯宁;乙碘油;依替菲宁;依沙美肟;吡磷铁钠;菲立磁;佛卢莫瑟(ferumoxsil,一种口服造影剂);荧光素;荧光素钠;钆贝葡胺;钆双胺;钆喷酸二甲葡胺;钆特醇;钆弗塞胺;组胞浆菌素;盐酸英普咪定;靛胭脂;吲哚花青绿;硫酸碘[I123]苄胍;碘苯扎酸;碘卡酸葡甲胺酯;碘卡酸;碘西他酸;碘达胺;碘达胺葡甲胺;胆影酸葡甲胺;碘克沙醇;碘沙酸葡甲胺;碘沙酸;碘格利酸;碘葡醇;碘葡胺;碘甘卡酸;碘葡胺;碘海醇;碘美普尔;碘帕醇;碘喷托;碘苯酯;碘普西酸;碘普罗酸;碘吡多;碘吡酮;碘西法酸;碘丝酸;碘西胺葡甲胺;碘磺拉酸;碘酞硫;碘替酸;碘他拉葡甲胺;碘他拉钠;碘他拉酸;碘曲仑;碘曲西酸;碘佛醇;碘克沙钠;碘克沙葡甲胺;碘克沙酸;碘昔兰;羟泛影酸;碘泊酸钠;异丙苯甘酸;异磺胺蓝;白细胞分型血清;利多苯宁;甲溴菲宁;葡甲胺;甲泛葡胺;甲泛影钠;酒石酸甲双吡丙酮;腮腺炎皮肤试验抗原;喷替酸;丙碘酮;喹那定蓝;锡克试验对照品(灭活白喉毒素);醋酸舍莫瑞林;碘[I123]化钠;镝双胺;焦磷酸亚锡;锡硫胶体;二巯丁二酸;醋酸特立帕肽;替曲膦;甲苯磺丁脲钠;结核菌素;和木糖。
利尿剂:安布茶碱;安布赛特;盐酸阿米洛利;阿佐利明;阿佐寒米;溴克利那;布美他尼;氯噻嗪;氯噻酮;克拉唑亚胺(clazolimine);氯索隆;依他尼酸钠;依他尼酸;依托唑啉;芬喹唑;呋塞米;氢氯噻嗪;硝酸异山梨酯;甘露醇;美夫西特;胆茶碱;吡咯他尼;螺沙宗;托拉塞米;氨苯蝶啶;三氟洛辛和尿素。
多巴胺剂:异波帕胺。
杀外寄生虫药:伏蚁灵;扑灭司林。
催吐剂:盐酸阿扑吗啡。
酶抑制剂:30珀里格内特钠(30polignate sodium);乙磺酸;阿司他丁钠;抑肽酶;盐酸苯那普利;贝那普利拉;贝奴司他;溴隐亭;甲磺酸溴隐亭;西司他丁钠;氟法胺;地麦角腈;甲磺酸麦角腈;左环丝氨酸;赖苯普利;喷托普利;胃酶抑素;培哚普利;淀粉硫酸钠;索比尼尔;盐酸螺普利;螺普利拉;泰勒拉瑙(taleranol,α-玉米赤霉醇);替普罗肽;托法胺;佐芬普利钙。
雌激素:氯烯雌醚;己二烯雌酚;己烯雌酚;磷酸己烯雌酚;马烯雌(甾)酮;雌二醇;环戊丙酸雌二醇;庚酸雌二醇;十一酸雌二醇;戊酸雌二醇;雌秦醇氢溴酸;雌三醇;雌呋酯;雌激素(共轭);雌激素(酯化);雌酮;哌嗪雌酮硫酯;炔雌醇;芬雌酸;美雌醇;尼尔雌醇;和炔雌醚。
纤溶药:阿尼普酶;乳酸比索布啉;和纤维蛋白酶。
氧自由基清除剂:培戈汀。
胃酸抑制剂:兰索拉唑,泮托拉唑和奥美拉唑。
胃肠动力剂:西沙比利。
糖皮质激素:安西奈德;二丙酸倍氯米松;倍他米松;醋酸倍他米松;苯甲酸倍他米松;倍他米松二丙酸酯;倍他米松磷酸钠;戊酸倍他米松;甘珀酸钠;醋酸氯可托龙;新戊酸氯可托龙;氯泼尼醇;促肾上腺皮质激素;醋酸可的松;可的伐唑;地西龙;地西奈德;地塞米松;地塞米松磷酸钠;二氟可龙;新戊酸二氟可龙;氟氯奈德;氟米松;新戊酸氟米松;氟尼缩松;氟轻松;醋酸氟轻松;氟可龙;己氟可龙;氟米龙;氟培龙醋酸;氟泼尼龙;戊酸氟泼尼龙;氟氢缩松;福莫可他;氢化可的松;醋酸氢化可的松;氢化可的松丁丙酸酯;丁酸氢化可的松;氢化可的松磷酸钠;氢化可的松琥珀酸钠;戊酸氢化可的松;甲羟松;醋酸甲泼尼龙;甲泼尼龙磷酸钠;甲泼尼龙琥珀酸钠;尼伐可醇;醋酸帕拉米松;泼尼卡酯;泼尼松龙;醋酸泼尼松龙;半琥珀酸泼尼松龙;泼尼松龙琥珀酸钠;泼尼松龙叔丁基乙酸酯;泼尼松;泼尼松龙;丙酸替卡贝松;曲洛奈德;苯曲安奈德;曲安奈德;曲安奈德钠;曲安奈德双醋酸酯;和己曲安奈德。
促性腺物质:醋酸布舍瑞林;枸橼酸克罗米芬;醋酸加尼瑞克;醋酸戈那瑞林;盐酸戈那瑞林;绒促性素;和尿促性素。
刺激毛发生长药:氨基己酸;米诺止血;盐酸奥沙香豆素;硫马林;凝血酶;和氨甲环酸。
激素:17-α-二氢马萘雌(甾)酮;17-α-二氢马烯雌酮;17-α-雌二醇;17-β-雌二醇;17-羟孕酮;雄烯二酮;克罗米酚;替可克肽;脱氢表雄酮;二氢睾酮;去氢马烯雌酮;炔诺醇;卵泡调节蛋白;卵泡刺激素;制卵泡素;戈那道萃宁(Gonadoctrinins);戈那瑞林;促性腺激素;韩氏更年期(Han memopausal)促性腺激素;人绒毛膜促性腺激素;胰岛素生长因子;亮丙瑞林;左炔诺孕酮;促黄体生成激素;促黄体激素释放激素及类似物;甲孕酮;甲地孕酮;二甲诺龙;炔诺酮;异炔诺酮;甲基炔诺酮;卵母细胞成熟抑制剂;催产素;垂体后叶;孕酮;松弛素;醋酸丝拉克肽;猪丙氨生长素;人蛋氨生长素;生长激素;猪诺生长素;牛度生长素;三苯氧胺;尿促卵泡素和血管升压素。
降胆固醇药:利非贝罗。
降血糖药:达格列酮钠;和格列美脲。
降血脂药:阿扎兰司他;考来酮;舒福姆;和联苯利平。
降压药:维前列醇。
免疫试剂:抗狂犬病血清;抗蛇毒血清;抗蛇毒血清(响尾蛇毒);卡介苗疫苗;肉毒中毒抗毒素;霍乱疫苗;白喉抗毒素;白喉类毒素;吸附精制白喉类毒素;免疫球蛋白;B型肝炎免疫球蛋白;乙型肝炎病毒灭活疫苗;流感病毒疫苗;麻疹病毒活疫苗;A群脑膜炎球菌多糖疫苗;C群脑膜炎球菌多糖疫苗;腮腺炎病毒活疫苗;百日咳免疫球蛋白;百日咳疫苗;百日咳疫苗吸附;鼠疫疫苗;脊髓灰质炎病毒灭活疫苗;脊髓灰质炎疫苗口服活;狂犬病免疫球蛋白;狂犬病疫苗;Rho(D)免疫球蛋白;风疹病毒活疫苗;天花疫苗;破伤风抗毒素;破伤风免疫球蛋白;破伤风类毒素;破伤风类毒素吸附;伤寒疫苗;牛痘免疫球蛋白;水痘带状疱疹免疫球蛋白;和黄热病疫苗。
免疫调节剂:二甲氨丙醇醋氨苯酸;咪喹莫特;干扰素β-1b;利索茶碱;霉酚酸酯;和醋肽铜。
免疫调节药:氮双吡咯;甲磺酸法奈替唑;法奈替唑;盐酸奥沙米索;磷酸利司硫醇;胸腺;和噻氯咪索。
免疫增强药:洛索立宾;和替西白介素。
免疫抑制剂:硫唑嘌呤;硫唑嘌呤钠;环孢菌素;达曲班;三盐酸胍立莫司;西罗莫司;普乐可复。
阳痿治疗辅助药:盐酸地来夸明。
抑制剂:阿卡波糖;阿托伐他汀钙;苄丝肼;溴克立新;卡比多巴;克拉维酸钾;达美格雷;多西苯醌;依前列醇;依前列醇钠;爱普列特;非那雄胺;氟比洛芬钠;呋格雷酸钠;鲁非罗尼;米格列醇;奥利司他;盐酸匹马吉定;吡吗格雷;泊那司他;利多格雷;舒巴坦苄;舒巴坦匹酯;舒巴坦钠;马来酸舒罗吖啶;三唑巴坦;三唑巴坦钠;盐酸噻氯匹定;甲磺酸替拉扎特;托瑞司他;马来酸维吖啶;齐罗硅酮;齐留通。
溶角蛋白剂:铝克洛沙;尿囊素铝;二苯并噻吩;香豆素;莫维A胺;二乙醇胺匹考群;水杨酸;舒马罗汀;扎罗汀;四羟醌;和维甲酸。
黄体激素释放激素激动剂:地洛瑞林;戈舍瑞林;组氨瑞林;醋酸黄体瑞林;醋酸法瑞林。
肝脏疾病治疗药:马洛替酯。
黄体溶解素:芬前列林。
记忆佐剂:盐酸莫沙明;和利巴米诺。
心理表现增强剂:阿尼西坦。
精神性能强化剂:酚加宾。
粘液溶解药:乙酰半胱氨酸;羧甲司坦;和多米奥醇。
粘膜保护剂:米索前列醇。
散瞳药:贝瑞福林。
鼻腔充血剂:盐酸奈马唑啉;伪麻黄碱磺化二乙烯苯-乙烯苯共聚物。
抗精神病药物:富马酸度奥哌隆;与利培酮。
神经肌肉阻断剂:阿地平;苯磺酸顺阿屈库铵;多库氯铵;戈拉碘铵;氯二甲箭毒;米库氯铵;泮库溴铵;哌库溴铵;罗库溴铵;氯化琥珀胆碱;氯筒箭毒碱;和维库溴铵。
神经保护药:马来佐环平。
甲基门冬氨酸拮抗药:塞福太。
非甾类固醇衍生物:琥珀孕烯醇酮。
子宫收缩药:卡贝缩官素;卡甲基;卡氨丁三醇;地诺前列素;地诺前列素氨丁三醇;诺前列酮;马来酸麦角;甲烯前列素;马来甲麦角新碱;和硫酸司巴丁。
帕哲病药:替鲁膦酸钠二钠。
孕酮:醋苯阿尔孕酮;醋酸阿马地酮;醋酸阿那孕酮;醋酸氯地孕酮;烯孕醇;醋酸氯孕酮;醋酸氯美孕酮;去氧孕烯;地美炔酮;地屈孕酮;炔孕酮;炔诺醇双乙酸钠;依托孕烯;醋酸氟孕酮;孕氯酮;孕二烯酮;己酸孕诺酮;孕三烯酮;卤孕酮;己酸羟孕酮;利奈孕酮;美屈孕酮;甲孕酮;双乙酸甲诺醇;炔诺酮醋酸酯;诺孕酪;诺孕美特;苯丙酸奥索孕酮;醋酸奎孕醇;奎孕酮;和替孕醇。
前列腺素类药:氯前列烯醇钠;氟前列醇钠;吉美前列素;芬前列林;和硫前列酮。
前列腺生长抑制剂:喷托孟。
临促甲状腺素:普罗瑞林。
精神治疗药:米那普林。
放射性试剂:碘[I125]纤维蛋白原;氟[F18]脱氧葡糖;氟[F18]多巴;碘[I125]人血清白蛋白;碘[I131]人血清白蛋白;碘[I123]苄胍;碘[I131]达胺钠;碘[I131]安替比林;碘[I131]胆固醇;碘[I123]马尿酸钠盐;碘[I125]马尿酸钠盐;碘[I131]马尿酸钠盐;碘[I125]奥酮;碘[I131]奥酮;碘[I123]非他胺盐酸;碘[I125]美丁;碘[I131]美丁;碘[I125]他拉钠;碘[I131]他拉钠;碘[I131]酪氨酸;碘[I125]塞罗宁;碘[I131]塞罗宁;汞[Hg197]丙醇醋酸盐;汞[Hg203]丙醇醋酸盐;汞[Hg197]丙醇醋酸盐;硒[Se75]蛋氨酸;锝[99mTc]三硫化锑胶体;比西酸锝[99mTc];锝[99mTc]呋膦;锝[99mTc]依替膦酸钠;依沙美肟锝[99mTc];锝[99mTc]呋膦;葡庚糖酸锝[99mTc];利多苯宁锝[99mTc];甲溴菲宁锝[99mTc];[99mTc]锝美罗酸;[99mTc]锝美罗酸二钠;巯替肽锝[99mTc];[99mTc]羟亚甲基二膦酸锝;喷替酸钙钠锝[99mTc];喷替酸钙钠钙三钠盐锝[99mTc];锝[99mTc]司他比;西硼肟锝[99mTc];[99mTc]锝琥巯酸;[99mTc]锝胶体硫;替肟锝[99mTc];替曲膦锝[99mTc];贝硫肽锝[99mTc];[I125]甲状腺素;C甲状腺素[I131];碘[I131]托泊酮;碘[I125]三油酸甘油酯和碘[I131]托泊酮三油酸甘油酯。
调节药:骨化二醇;降钙素;骨化三醇;氯膦酸;双氢速甾醇;依替膦酸;奥昔磷酸;吡膦酸钠;利塞膦酸钠;和司骨化醇。
松弛剂:盐酸阿地芬宁;阿库氯铵;氨茶碱;阿珠莫林钠;巴氯酚;盐酸苯佐他明;卡立普多;氯苯甘油氨酯;氯唑沙宗;环桂氟胺;桂美君;克鲁达诺林(clodanolene);盐酸环苯扎林;丹曲洛林;丹曲洛林钠;非那拉胺;盐酸非尼啶醇;盐酸非托西酯;盐酸黄酮哌酯;氟乙西泮;氟美吗酮;己芴溴铵;盐酸异戊拉明;劳氨酯;盐酸美贝维林;盐酸美舒令;美他沙酮;盐酸匹美噻吨;美索巴莫;苹果酸盐萘甲羟胺;马来酸奈来扎林;盐酸罂粟碱;盐酸哌泊索仑;喹他酯;利托君;盐酸利托君;罗咯定;茶碱甘氨酸钠;盐酸昔芬那米(thiphenamil hydrochloride);和希洛班。
营养重分剂:西马特罗。
抗疥螨药:双甲脒;克罗米通。
硬化剂:乙醇胺油酸;角肝油酸钠;苄糖苷。
镇静剂:丙酰马嗪。
镇静安眠药:阿洛巴比妥;阿洛米酮;阿普唑仑;异戊巴比妥钠;苯他西泮;溴替唑仑;仲丁比妥;仲丁比妥钠;布他比妥;卡普脲;卡波氯醛;三氯乙醛甜菜碱;水化氯醛;盐酸甲氨二氮卓;盐酸氯哌酮;氯乙双酯;环丙西泮;盐酸德克拉莫(dexclamol hydrochloride);地莫西泮;氯醛比林;安定乙氯维诺;依托咪酯;非诺班;氟硝西泮;福司肼;格鲁米特;哈拉西泮;仑内特西泮(Lon-netazepam);甲氯喹酮;甲丙氨酯;安眠酮;咪达氟;聚乙醛;异戊巴比妥;戊巴比妥钠;哌拉平;普拉西泮;夸西泮;瑞氯西泮;咯来米特;司可巴比妥;司可巴比妥钠;舒普罗酮;曲卡唑酯;马来酸曲匹泮;三唑仑;三甲氧苯醋酰胺;三氯福司钠;曲美托嗪;乌达西泮;扎莱普隆;盐酸唑拉西泮;和酒石酸唑吡坦。
选择性腺苷A1拮抗剂:阿帕茶碱。
羟色胺拮拉剂:酒石酸阿坦色林;安麦角;酮色林;和利坦色林。
羟色胺抑制剂:盐酸辛那色林;芬克洛宁;甲磺酸二甲替嗪;和托西米定。
羟色胺受体拮抗剂:盐酸托烷色林。
类固醇:乙呋地塞米松;和糠酸莫米松。
兴奋剂:安福萘酸;硫酸苯丙胺;硫酸二甲胺嗪;盐酸阿布他明;阿扎苯胺;咖啡因;蓝肽;蓝肽二乙胺;富马酸达佐必利;
右旋安非他命;硫酸右旋安非他命;盐酸二氟嗪;盐酸二甲弗林;盐酸多沙普仑;香草二乙胺;醋酸乙色胺;盐酸芬乙茶碱;盐酸氟巴尼酯;氟替尔;磷酸组胺;盐酸茚屈林;美非沙胺;盐酸甲基苯丙胺;盐酸哌甲酯;匹莫林;盐酸吡咯戊酮;扎莫特罗;和富马酸扎莫特罗。
抑制剂:氨氟替唑;秋水仙碱;他唑非隆。
症状性多发性硬化症:氨吡啶。
增效剂:盐酸普罗地芬。
甲状腺激素:甲状腺素钠;塞罗宁钠;复方甲状腺素。
甲状腺抑制剂:甲巯咪唑;和丙硫氧嘧啶。
拟甲状腺素药:盐酸甲状米登。
镇定剂:溴西泮;盐酸丁螺环酮;环氯唑仑;克拉唑仑;氯巴占;二钾氯氮卓;一钾氯氮卓;地莫西泮;美托咪啶;盐酸恩西拉嗪;吉哌隆盐酸;奥芬氨酯;盐酸羟嗪;双羟萘酸羟嗪;凯他唑仑;劳拉西泮;氯扎封;洛沙平;丁二酸洛沙平;盐酸美达西泮;大麻隆;尼索氨酯;奥沙西泮;喷他氨酯;匹仑哌隆;利帕西泮;咯利普兰;硫西泮;盐酸他克拉明;替马西泮;三氟巴占;泰巴氨酯;和戊诺酰胺。
不稳定型心绞痛药:盐酸替罗非班。
排尿酸药:苯溴马隆;伊替马唑;丙磺舒;磺吡酮。
血管收缩剂:血管紧张素酰胺;苯赖加压素;美西麦角;和马来美西麦角。
血管扩张剂:前列地尔;盐酸氮氯嗪;硫酸巴美生;盐酸苄普地尔;布替利嗪;枸椽酸西替地尔;盐酸卡波罗孟;氯硝甘油;潘生丁;氢普拉明;丁四硝酯;非洛地平;盐酸氟桂利嗪;福司地尔;海索苯定;烟酸肌醇;盐酸异丙沙明;硝酸异山梨酯;单硝酸异山梨酯;盐酸异克舒令;利多氟嗪;甲苯地尔;富马酸甲苯地尔;二盐酸咪贝弗雷地;盐酸米氟嗪;米克昔定;草酸萘呋胺酯;盐酸尼卡地平;尼麦角;尼可呋酯;烟碱醇;尼莫地平;尼索地平;羟苯甘氨酸;盐酸氧烯洛尔;戊四醇四硝酸酯;己酮可可碱;戊硝醇;马来酸戊硝醇;吲哚洛尔;哌多明;普尼拉明;丙帕硝酯;舒洛地尔;盐酸特罗地林;盐酸替普地尔;盐酸妥拉唑林;烟胺羟丙茶碱。
创伤药:尿囊素。
伤口愈合剂:厄索夫明。
黄嘌呤氧化酶抑制剂:别嘌呤;和奥昔嘌醇。
其他药剂,包括:1-α-氟代雌二醇;1-α-黄毒苷;异雌三醇;1-α-雌二醇;17-β-雌二醇;1α-羟维生素D2,1-癸烷吡咯烷酮;1-十二烷吡咯烷酮;22-氯化钙三醇;2CVV;2′-Nor-cGMP;3-异丁基γ-氨基丁酸;6-FUDCA(熊脱氧胆酸);7-甲氧基他克林(9-氨基-7-甲氧基-1,2,3,4-四氢吖啶);硫酸阿巴卡韦;阿巴诺喹;阿贝卡尔;阿卡地新;阿坎酸;盐酸醋丁洛尔;醋氯芬酸;阿昔拓米普利格醇(acetomepregenol);醋碘苯酸钠;N-二乙酰半胱氨酸;醋洋地黄毒苷;乙酰左旋肉碱;醋美沙朵;阿昔莫司;阿昔替酯;萘二磺乙乳胆铵;阿考烟肼;阿伐斯汀;金刚芬酯;阿达色林;阿德福韦酯;阿地米屈;腺苷蛋氨酸;补体D;阿屈非尼;阿拉普利;阿拉达辛(aladapcin);阿拉丙酯;甲磺酸阿拉曲沙星;白吞叶青素;白蛋白铬[铬51]酸盐;人血清白蛋白;白蛋白碘[I125]化血清;白蛋白碘[I131]化血清;阿德卡尔霉素(aldecalmycin);阿仑磷酸;阿仑替莫;骨化醇;阿夫唑嗪;阿糖苷酶;阿利那斯汀;阿利维A酸;绿藜芦碱;别嘌呤钠;阿莫曲坦苹果酸;阿洛司琼;α-埃德松(alpha idosone);α-生育酚;α-生育酚醋酸酯;阿舍西隆;阿舍西隆B;金刚烷胺-HCI;安贝氯铵;阿洛米松;甲硫阿美铵;安非他酮;氨氟沙星;盐酸氨基酮戊酸;氨基酸树脂复合物;盐酸胺碘酮;氨磺必;氨氯地平;铵乳酸;苯丙胺己二酸;安非他明天门冬氨酸;苯丙胺树脂复合物;安吡昔康;氨普那韦;糊精;4-噻唑甲酸;阿纳耐因(ananain);阿那立肽;磷酸阿尼利定;茴茚二酮;双炔失碳酯;阿帕多林(apadoline);阿帕泛;阿可乐定;阿瑞匹坦;阿普硫钠;牛抑肽酶;阿替加奈;阿雷地平;阿贝卡星;阿比朵尔;阿布他明;槟榔单宁B1;阿加曲班;阿立哌醇;阿立哌唑;阿罗洛尔;盐酸阿替卡因;抗坏血酸;阿西马朵林;阿斯帕拉酮(aspalatone);阿斯珀呋喃(asperfuran,一种羟基苯并呋喃衍生物);阿扑西林;硫酸阿扎那韦;S-氨酰心安;阿替韦啶;盐酸托莫西汀;阿特盘宁B(atpenin B);阿曲肌醇;奥略巴西定A(aureobasidin A);阿伏苯宗;印楝素;壬二酸;氮卓斯汀;阿折地平;阿齐利特;二水阿奇霉素;氨曲南;巴卡亭III;白花猪母菜甙A;白花猪母菜甙B;巴特波拉明(bactobolamine);巴拉齐朋;巴黑霉素(balhimycin);巴洛沙星;巴柳氮;班布特罗;宝藿甙I;巴尼地平;巴布司特;白僵菌;贝卡普勒明;贝康唑;二丙酸倍氯米松水合物;贝氟沙通;贝利那明(bellenamine);本芴醇;贝尼地平;本托奎坦(bentoquatam);苯并异恶唑;本曹达新(benzoidazoxan);过氧化苯甲酰;盐酸苄非他明;盐酸苯喹胺;苯扎托品;苯甲酸苄酯;苄青霉素-聚赖氨酸;苄普地尔;波拉坦(beractant);贝前列素;柏拉非农;柏托沙米;贝西吡啶;β-胡萝卜素;无水甜菜碱;倍他米隆;倍他洛尔;盐酸倍他唑;贝凡洛尔;倍克洛汀;二苯美仑;比卡林;比马前列素;比弥昔(bimithil);比螺酮;生物素;α-2-百瑟罗霉素(bioxalomycin alpha2);比立哌隆;比沙雷米;二吖丙啶基精胺;双苯并咪唑A;双苯并咪唑B;碱式水杨酸铋;比斯特拉米德D(bistramide D);比斯特拉米德K(bistramide K);波尔定碱;波吲洛尔;硼替佐米;布雷菲尔得菌素;溴莫尼;布林佐胺;溴芬酸;布新洛尔;布地品;布那唑嗪;布替萘芬;盐酸布替萘芬;丙酸布替可特;卡麦角林;枸椽酸咖啡因;胡桐素A;人降钙素;鲑鱼降钙素;钙;醋酸钙;葡庚糖酸钙;甲泛影钙;猪肺磷脂;卡莫格雷;坎地沙坦;坎地沙坦西来替昔酯;坎沙曲拉;卡罗单抗;辣椒素;卡马西平;卡巴索霉素C(Carbazomycin C);卡贝缩宫素;卡比多巴/左旋多巴;3-脱氧-2-烯鸟苷;羧甲基β-1,3-葡聚糖;卡培立肽;卡替洛尔;卡芦莫南;卡伏曲林;醋酸卡泊芬净;西巴西坦;头孢羟氨苄/头孢羟氨苄半水化合物;头孢卡品酯;甲苯磺酸喷替头孢达肟;头孢托仑酯;盐酸头孢吡肟(精氨酸剂型);头孢他美;头孢他美酯;头孢三唑;头孢瑞南;头孢米诺;头孢地嗪;头孢噻利;头孢替安;头孢替安己酯;头孢唑兰;头孢匹罗;头孢磺啶;头孢他啶(精氨酸剂型);头孢他啶钠;头孢特仑;头孢二水;头孢曲松;雷公藤红素;塞来考昔;瑟里卡里姆(celikalim);塞利洛尔;纤维素磷酸钠;西帕西定A(cepacidine A);西文氯胺;西立伐他汀;西立伐他汀钠;舍托肝素钠;西替地尔;西替利嗪;十六烷基醇;盐酸西维美林;汞丙脲[Hg197];氯美扎酮;克劳奥林素A(chloroorienticin A);克劳奥林素B(chloroorienticin B);维生素D3;考来烯胺;α绒毛膜促性腺激素;磷酸铬[P32];木瓜凝乳酶;糜蛋白酶;西苯唑啉;环索奈德;环丙洛尔;西兰司琼;西尼地平;西洛雷定;西洛他唑;西托溴铵;西尼必利;西诺西泮;西前列烯;单水西沙比利;苯磺顺阿曲库胺;西替克新;西酞普兰;西酞普兰氢溴酸;胞二磷胆碱;α-赛垂米辛(citreamicin alpha);黄皮酰胺;克利溴铵;克林沙星;氯美噻唑;氯吡格雷;硫酸氢氯吡格雷;氯化钴[Co57];氯化钴[Co60];盐酸考来维仑;考利斯提米德(colestimide,一种胆汁结合剂);棕榈胆磷;卡姆普利斯塔丁(complestatin);康提那斯托(contignasterol);康陶洛斯塔丁(contortrostatin);促肾上腺皮质激素氢氧化锌;克萨灵(cosalane);克斯塔陶里德(costatolide);可替宁;库马霉素;醋酸绿藜安;绿藜安单宁酸;丘卡玛里德(cucumariosid);硫酸热凝胶;丘略欣(curiosin);维生素B12;维生素B12[Co57],维生素B12[Co58];维生素B12[Co60];塞科拉辛(cyclazosin);环西道法韦;环苯扎林;环丁A(Cyclobut A);环丁-G(Cyclobut G);环己酰;塞克鲁欣(cyclosin);环硫杂嘧啶;环氮霉素;盐酸赛克立明;去乙酰环丙氯地孕酮;半胱胺酒石酸氢盐;细胞松弛素B;放线菌素D;大豆黄酮;大豆异黄酮;达那肝素钠;毛瑞香素;达哌唑;达匹坦;达非那新;道鲁欣(darlucin);达西多明;枸椽酸柔红霉素;DdUTP;十烃溴铵;葡铁钠钙;甲磺酸去铁胺;脱氢膜海鞘素B;地拉普利;地来夸明;地发哌嗪;地莫匹醇;氯化翠雀啶;脱氧吡啶啉;地泼罗酮;酯肽霉素;德伦环烷;硫酸皮肤素;地舍平;地西卢定;地洛他定;去氨加压素;脱氧胺碘酮;脱氧核糖核酸酶;重酒石酸地他义铵;右旋酮洛芬;右氯谷胺;盐酸去甲基苯;盐酸右雷佐生;右索他洛尔;糊精2-硫酸;右旋安非他命己二酸;右旋安非他命树脂复合物;右旋安非他命糖酸盐;葡萄糖;双氯芬酸蒂格利(diclofenac digolil);曲尾藓素;地诺孕素;二乙基高精胺;二乙基去甲精胺;盐酸地芬诺辛;D1受体激动剂;地尔硫;二甲前列腺铝;二甲基高精胺;地来西坦;十四酰卵磷脂;甲硫二苯马尼;浙皮海绵内酯;双丙戊酸;道卡帕宁(docarparnine);1-二十二烷醇;多甲磺酸拉司琼单水化物;多米曲班;盐酸多奈;多佐胺;多司马酯;多他利嗪;多沙唑嗪;度骨化醇;德拉库林(draculin);卓斯珀林冬(drosperidone);屈螺酮;屈他维林;阿昔菲利酯(acephyllinate);屈噁昔康;度他雄胺;依比拉肽;乙溴替丁;依卡派特;依卡倍特;埃克斯特龙(ecdisteron);蛇毒C-型凝集素;蛇毒锯鳞蝰素;海鞘素722;海鞘素729;海鞘素743;依达拉奉;哌嗪依地酸钙;铁依地酸钠;埃巴单抗;依决洛单抗;依发韦仑;依非加群;依福地平;乙呱仑;依降钙素;来曲普坦;来曲普坦氢溴酸;依高地平;依利罗地;依尔替酸;依马卡林;依美斯汀;依美斯汀延胡索酸;乙格列酯;依莫白介素;恩曲他滨;依那普利;依那扎群;恩夫韦地;恩格列酮;恩他卡朋;肠抑素;依普利酮;依普利酮;依斯的明;替非巴肽;厄多司坦;麦角钙化(固)醇;艾生利特;厄他培南钠;赤藓醇;草酸依地普仑;埃索美拉唑镁;乙磺普隆;依坦特罗;乙沙西嗪;乙氯维诺;炔己蚁胺;乙炔基雌二醇;依索唑胺;盐酸依替卡因;依替唑仑;依曲巴明;埃弗米诺米辛(Eveminomicin);艾沙瑞林;替米贝;法里夫金(faerieftmgin);泛托法隆;泛昔洛韦;法罗培南;法西多曲;法舒地尔;非多托秦;非尔氨酯;非诺贝特;非诺多泮;芬司匹利;芬太尼;芬替康唑;非普地醇;吡磷铁钠;佛里斯汀(ferristene);佛里珊(ferrixan);枸椽酸亚铁[Fe59];盐酸非索非那定;碘[I125]纤维蛋白原;纤溶酶;氟卡尼;氟丁特罗;氟辛克生;氟卓斯汀;氟罗布芬;氟氧头孢;氟苯尼考;氟非宁;夫劳娜斯塔(flornastat);氟沙地尔;氟[F18]脱氧葡糖;氟美西诺;氟桂利嗪;弗洛卡里三醇(fluocalcitriol);R-氟西汀;L-氟西汀;氟洛克生;氟吡汀;氟比洛芬酯;氟红霉素;氟他胺;氟曲马唑;氟伐他汀;氟伏沙明;叶酸;α促滤泡素;α/β促滤泡素;福米韦生钠;磺达肝素钠;福拉沙坦;福莫特罗;富马酸福莫特罗;R,R-福莫特罗;福辛普利;磷苯妥英;琥珀夫罗曲坦;氟维司群;呋塞米;钆贝酸;钆布醇;钆双胺-竹叶黄酮DTPA;钆喷甲葡胺;钆特酸;加兰他马来酸;氢溴酸加兰他马来酸;加丹司琼;戈洛帕米;伽莫林酸(gamolenic acid);加替沙星;吉非替尼;甲磺酸吉米沙星;吉妥珠单抗奥唑米星;吉哌隆;吉立索泮;格拉莫德;醋酸格拉替雷;兰萼丙素;盐酸胰高血糖素;重组盐酸胰高血糖素;重组胰高血糖素;葡糖酸内酯;格鲁塔吡喃酮(glutapyrone);谷胱甘肽二硫化物;格里考品(glycopine);格里考普利(glycopril);醋酸戈舍瑞林;格帕沙星;盐酸格帕沙星;愈创木酚;盐酸胍;软海绵素B;对卤泛曲林;哈勒蒙(halomon,一种多卤化单萜化合物);乳酸氟哌啶醇;卤泼尼松;哈特马鲁比金A(hatomarubigin A);哈特马鲁比金B(hatornambigin B);哈陶那米辛(hatornamicin);哈陶那鲁比金A(hatornarubigin A);哈陶那鲁比金B(hatornarubigin B);肝素钙;肝素钠;甲硫己环铵甲基硫酸盐;因盐酸海克卡因;醋酸组氨瑞林;透明质酸酶;盐酸氢可他酯;氢化可的松睾酮;氢化可的松普如比尤酯(probutate);苯二酚;羟钴胺;羟丙基纤维素;羟芪巴脒;依西双溴丙脒;伊巴倔那钠;伊菠加因;异丁司特;布洛芬钾;艾考糊精;伊利马醌(illimaquinone);伊洛前列素;甲磺酸伊马替尼;咪达普利;伊米达辛尼(imidazenil);伊米苷酶;双羟萘酸丙米嗪;乳酸氨力农;吲达帕胺;茚地那韦;硫酸茚地那韦;羟喹啉铟[In111];喷替酸铟[In111]二钠;喷曲肽[In111]试剂盒;吲哚美辛;法呢吲哚美辛;吲哚美辛钠;伊诺特隆;伊诺加群;伊诺莫单抗;速效胰岛素制剂;精蛋白速效胰岛素制剂;甘精胰岛素;赖脯精蛋白胰岛素;干扰素α;干扰素α-NI;干扰素-β;干扰素-βlal;干扰素γ-1A;干扰素γ-1B;干扰素Ω;复合干扰素;白细胞-3;白细胞介素-1;白细胞介素-Iβ;白细胞介素-10;白细胞介素-11;白细胞介素-12;白细胞介素15;白细胞介素-2;白细胞介素-4;白细胞介素-5;白细胞介素-7;白细胞介素-8;白细胞介素-α;内因子;菊糖;转化糖;碘苄胍硫酸[I131];碘比醇;碘达胺葡甲胺;胆影酸钠;埃德米劳里德(iodoamiloride);碘[I123]马尿酸钠;碘[I131]马尿酸钠;碘[I123]非他胺盐酸;碘拉醇;碘普罗胺;碘吡多;碘美普尔;碘[I125]他拉钠;碘赛特;碘格利酸钠;依帕利特;伊培沙宗;伊匹达克林;4-药薯醇;依普拉芬;伊沙匹隆;伊贝沙坦;伊洛沙星;右旋糖酐铁;铁蔗糖;伊替马唑;伊沙司坦;伊波格雷;异帕米星;异弗洛西斯品(isofloxythepin);异丙乌诺前列酮;伊他美林;伊托必利;R-酮洛芬;S-酮洛芬;酮咯酸;乳梨醇;拉替福新(lactivicin);乳果糖;拉埃内克;拉呋替丁;拉诺康唑;兰吡立松;拉米非班;拉莫三嗪;拉坦前列素;拉特里汀(lateritin);月桂氮酮;来氟米特;洛美沙星;来明拉唑;来那西普;来匹卢定;瘦素;乐卡地平;来立司琼;来米地平;来索吡琼;来曲珠利;吉他霉素;盐酸左旋沙丁胺醇;酒石酸左洛啡烷;盐酸左旋咪唑;左倍他洛尔;左布诺洛尔;左布比卡因;盐酸左旋布比卡因;卡巴斯汀;左卡尼汀;左羟丙哌嗪;左氧氟沙星;无水萘磺酸左丙氧芬;左美洛昔芬;左莫普洛尔;左西孟旦;左舒必利;林丹;利奈唑酮;利诺曲班;林西多明;林替曲特;林托必利;脂肪酶;利沙必利;锂碳酸盐;枸椽酸锂;洛度沙胺;洛美利嗪;氯那唑酸;洛匹那韦;氯戊米特;洛沙坦;氯西加酮;氯替泼诺;罗韦拉得;盐酸洛沙平;LpdR;芦贝鲁唑;镥;2-苯基-N-乙酰色胺;利地霉素;溶葡球菌酶;蛙皮抗菌肽二胺;醋酸镁;醋酸镁硼酸;厚朴酚;马拉硫磷;马洛特克洛明(mallotochromene);马洛特加盘宁(mallottojaponin);锰福地吡;锰福地吡三钠;马尼地平;曼尼瓦霉素A(maniwamycin A);甘露醇;手霉素E;手霉素L;马哌斯汀;马提克8708(martek 8708);马提克92211(martek92211);马瑟托里德(massetolide);甲泛影葡甲胺;美洛昔康;盐酸马法兰;萘氢醌二磷酸钠;维生素K3;甲基强的松;甲基对苯二酚;汞撒利钠;美司那;盐酸二甲双胍;乙胺太林铵;美沙比妥;盐酸甲氧胺;美绍瑟酮(methoxatone);甲氧补骨脂素;甲东莨菪铵;甲氯噻嗪;甲基多巴;R-α甲基组胺;甲基肌苷;醋丙甲泼尼龙;甲乙哌酮;美提帕尼德(metiparnide);盐酸美替洛尔;美托拉腙;富马酸美托洛尔;S-美托洛尔;酒石酸美托洛尔;美曲磷酯;甲泛影镁;甲泛影酸;一水美洛西林钠;米歇拉宁B(michellarnine B);麦洛考林A(microcolin A);米多君;麦格司他;米拉美林;米拉美林;米屈肼;米那普仑;米利酮乳酸;米欧卡霉素;米普拉苷;米氟嗪;米非司酮;密散普利(mixanpril);咪唑斯汀;咪唑立宾;莫昔普利;盐酸莫昔普利;莫达非尼;莫米松;一水糠酸莫米松;莫诺苯宗;孟替瑞林;莫雷西嗪;盐酸莫雷西嗪;莫沙帕明;莫沙斯汀;促动内脂;盐酸莫西沙星;莫昔普令;莫索尼定;莫匹罗星;莫匹罗星钙;盐酸霉酚酸酯;那氟沙星;那屈肝素钙;那法多替得(nafadotride,多巴胺D3受体部分性拮抗剂);萘莫司他;萘哌地尔;那格列钒;盐酸纳美芬;盐酸纳曲酮;萘二磺乙乳胆铵;奈沙加群;纳拉曲坦;那沙普酶;那格列奈;内特普拉瑟(nateplasel);甲磺酸奈非那韦;奈西立肽;烟酰胺;烟碱;聚丙烯酸尼古丁;尼培替丁;尼拉伏林;乳链菌肽;硝唑尼特;硝替卡朋;尼替西农;S-尼群地平;呋喃妥水合物;呋喃妥因钠;粗晶呋喃妥因;呋喃西林;硝酸甘油;壬苯醇醚-9;甲基孕酮;辛基甲氧基肉桂酸;奥美沙坦酯;奥洛他定;奥洛他定盐酸;奥普力农;奥沙拉嗪;奥美拉唑镁;R-恩丹西酮法;口服海普格里米克斯(oral hypoglyceremics);盐酸奥芬太尼;奥斯他韦磷酸盐;奥腾折帕;奥沙米索;奥沙普钾;奥卡西平;奥昔康唑;奥拉西坦;奥索地平;羟苯宗;奥昔布宁;盐酸羟苄利明;奥芬溴铵;奥扎格雷;帕洛尔宁(palauarnine);帕利那韦;盐酸帕洛诺司琼;低分子肝素钠;帕那美新;胰脂肪酶;帕尼培南;帕尼培南;潘诺林(pannorin,由毡状金孢霉产生的一种新的辅酶A还原酶抑制剂);帕诺米芬;泛硫乙胺;泮托拉唑钠;泛酸;甲乙双酮;帕立骨化醇;帕马苷;帕米格雷;盐酸帕罗西汀;甲磺酸帕罗西汀;欧苷菊;帕珠沙星;牛培加酶;培维索孟;吡嘧司特;吡嘧司特钾;喷昔洛韦钠;青霉胺;潘它夫西地;五肽胃泌素;喷他脒;依西双溴丙脒;喷替酸钙三钠[Yb 169];喷替吉肽;酒石酸喷托铵;戊聚糖;珀弗里森(perflexane);顺滑剂;全氟丙烷;培高利特;甲磺酸培高利特;培哚普利拉;培美酸;哌罗匹隆;2,5二甲基芬太尼;苯茚二酮;马来酸非尼拉;盐酸芬美曲秦;芬诺图西弗林(phenotoxifvline);苯羟基丙氨酸;芬苏昔那(phensuccinal);芬特明树脂复合物;甲磺酸酚妥拉明;苯丙酮康唑;福林酸式酒石酸盐;长效苯妥英钠;速效苯妥英钠;磷酸;维生素K1;哌西那朵;胡黄连提取物;吡库特罗;匹多莫德;匹西卡因胺;匹马吉定;吡美莫司;匹米前列素;松属素;吡格列酮;胡椒基丁醚/增效醚;吡吲哚;吡美诺;吡咯司特;聚磷酸雌二醇;聚乙二醇3350;聚四氟乙烯;猪肺磷脂;酸钾氯化物;盐酸普拉克索;吡喹酮;哌唑嗪;丙胺卡因;普鲁卡乙氧汞林;氯胍盐酸;丙帕锗;丙戊茶碱;丙内酯;盐酸丙酰马嗪;L-丙二酰卡米丁(propionylcamitine,L-);丙吡仑;丙吡仑+对乙酰氨基酚;丙哌维林;普罗斯卓汀(prostratin);抗菌肽;水解蛋白;盐酸普罗托醇;普罗托萨夫沙星(protosufloxacin,一种抗爱滋病单酯物);普卢利沙星;除虫菊酯;维生素B6;盐酸吡多辛;夸西泮;奎的平;富马酸喹硫平;喹夫拉朋;喹高利特;喹卡酯;喹乙宗;奎尼丁聚半乳糖醛酸;雷洛昔芬;雷马曲班;雷奈酸;雷诺嗪;雷帕库溴铵;瑞卡南;瑞加韦单抗;瑞格;瑞西那明;里森弗拉毒素(resinferatoxin);浆膜蛋白;瑞肝素钠;瑞维齐农;核黄素;核黄素磷酸酯钠;利卡司琼;利洛吡司;金刚乙胺;利美索龙;利莫罗近;利奥地平;替美司坦;利塞膦酸;利喷西平;利替培南酯;利替培南;利托那韦;酒石酸利斯的明;苯甲酸利扎曲普坦;尼波弗拉迪(rnibefradil);尼法求里姆氯化物(rnivacurium chloride);罗非考昔;罗他霉素;罗匹尼罗;罗比卡因;罗比卡因盐酸一水合物;罗喹美克;孟加拉玫瑰钠[I131];马来酸罗格列酮;罗沙替丁;罗克吲哚;氯化铷[Rb82];芦氟沙星;卢帕替丁(rupatidine);卢扎朵仑;药酵母蔗糖;红花油;沙非罗尼;R-沙丁胺醇;R-沙那西定;来昔决南钐[Sm153]五钠盐;山费培南;沙普立沙坦;沙丙蝶呤;沙奎那韦;沙格菲托A(sarcophytol A);沙格司亭;沙美利定;山帕曲拉;沙格雷酯;沙芦普酶;沙特力农;沙替格雷;喷地肽沙妥莫单抗;东莨菪碱;胰泌素;硒[Se75]蛋氨酸;司美利特;舍莫瑞林;司莫地尔;舍他康唑;舍曲林;盐酸舍曲林;司普替林;盐酸司维拉姆;司韦单抗;司佐胺;枸橼酸西地那非;西立匹特;西替普酶;磺胺嘧啶银;西孟坦;瓦斯康;瓦斯康-纤维素;西硝地尔;辛纳比道(sinnabidol);西帕曲近;辛伐他汀;生长调节素C;重组生长激素;山梨醇;生长介素B;人蛋氨生长素;生长激素;索他洛尔;斯陶若鲍林(Staurosporine);司替罗宁;斯哚巴丁;氯化锶[Sr89];修斯邦(succibun);磺胺;磺胺苯吡唑;磺胺吡啶;亚砜胺;阿地砜钠;硫;舒他西林;舒托必利;舒马曲坦;舒替兰酶;西马克里姆(symakalim);他布比妥;坦度螺酮;单宁酸;塔普金(tapgen);他前列烯;酒石酸;扎司特;马来酸替加色罗;替仑西平;替美司坦;替米沙坦;替莫普利;富马酸替诺福韦酯;替诺柳;替吡吲哚;特拉唑嗪;盐酸特比萘芬;特拉伏沙;特麦角脲;特利加压素;特罗地林;特他洛尔;布昔酸睾酮(Testosterone Bucielate);溴化亚铊T1201;硫胺素;盐酸硫胺;硫非君;硫玛里醇(Thiomarinol);硫丙咪胺;氨硫脲;通佐溴胺;甲状腺球蛋白;促甲状腺激素;α促甲状腺素;噻加宾;盐酸噻加宾;噻萘普汀;贴帕芬(Tiapafant);噻氯匹定;替诺洛尔;替利洛尔;替洛芬阿酯;替鲁膦酸;硫普罗宁;噻托溴铵;替兰达迪金(Tirandalydigin);替拉扎特;替罗非班;替罗匹胺;醋酸生育酚;酒石酸托特罗定;托拉塞米;特拉芬宁(Trafennin);群多普利;硫酸反苯环丙胺;曲伏前列素;曲托喹酚;盐酸曲唑酮;曲前列环素钠;托可维A酸;氨苯蝶啶;三辛精;毛透明蛋白;α天花粉蛋白;三氯生;曲地氯(Tridihexethyl Chloride);曲恩汀;盐酸曲恩汀;三黄素;曲美孕酮;盐酸左旋咪唑;3-氧补骨脂素;曲普瑞林扑酸盐;三乙醇胺多肽油酸凝析油;特罗珀第平(trombodipine);氨丁三醇;缓血酸胺;千里光酸托品酯;丙大观霉素;曲伐沙星;甲磺酸曲伐沙星;曲韦定;妥卡雷琐;妥洛特罗;泰隆基宁(tylogenin);四丁酚醛;恩地氯化物;恩地氯铵碘;异丙乌诺前列酮;乌拉地尔;尿素[碳13];尿素[碳14];尿嘧啶核苷三磷酸;万乃洛韦;戊地昔布;盐酸缬更昔洛韦;丙戊酸镁;丙戊酸半钠;戊柔比星;缬沙坦;伐米胺;瓦纳带因(vanadeine);瓦尼诺醇(vaninolol);升压素单宁酸盐;文拉法辛;(S)维拉帕米;绿藜芦;菲洛珊(veroxan);菲昔比诺(vexibinol);枸椽酸长春布宁;长春布宁树脂;长春考酯;长春西汀;枸椽酸长春西汀;长春培醇;硫酸紫霉素;维生素A;维生素A棕榈酸酯;维生素E;维生素K;伏立康唑;伏高利特;法林钾;珍米洛非班;希莫洛芬;彦伽宾(yangarnbin);扎普利;扎考必利;R-扎考必利法;扎鲁司特;扎螺酮;扎托洛芬;扎那米韦;扎那米韦;扎吉仑;扎替雷定;扎托司琼;折那司他;净司他丁斯酯;齐拉西酮;甲磺酸齐拉西酮;唑来膦酸;佐米曲坦;唑吡坦;佐匹克隆;S-佐匹克隆;佐洛哌隆;和佐替平。
还有其它的医药品例子,列举在2000年MedAd News 19期56-60页中,以及《医师案头参考》(The Physicians Desk Reference,53rd.Edition,pages 792-796,Medical Economics Company(1999))中。
在本发明的另一个实施方式中,提供了一种透皮剂型,其包含一种非甾族抗炎药(NSAID),所述NSAID具有以Franz扩散池(Franz渗透池,Franz池)程序测定的至少约2μg/cm2·hr的通量。在进一步的实施方式中,该透皮剂型具有以Franz扩散池程序测定的至少3μg/cm2-hr的通量。而在更进一步的实施方式中,该透皮剂型具有以Franz扩散池程序测定的至少约4μg/cm2-hr的通量。在一个优选实施方式中,该透皮剂型具有以Franz扩散池程序测定的至少约5μg/cm2-hr的通量。所述Franz扩散池程序包括了使用人类尸体皮肤。
在另一个可选择的实施方式中,本发明提供了一种透皮剂型,其包含一种非甾族抗炎药(NSAID),具有以Franz扩散池程序测定的至少约2-5μg/cm2·hr的通量。可在所述透皮剂型中使用的NSAIDS例子已在上面描述过。
上述的包含一种非甾体抗炎药(NSAID)、具有以Franz扩散池程序测定的至少约2-5μg/cm2·hr的通量的透皮剂型可以进一步包含:(i)第一种化合物,选自有机亚砜;和(ii)第二种化合物,选自由脂肪酸酯、脂肪酸、氮酮类化合物及其混合物所构成的组。可选用的脂肪酸酯、脂肪酸、氮酮类化合物的例子参见上述。另外,第一种与第二种化合物的重量比如上所述可以在约50∶1-约10∶1的范围之内,优选约10∶1-约20∶1,更优选约5∶1-约20∶1。
此处所述的透皮剂型还可以包含一种或多种药学上可接受的载体/赋形剂。适合用于此处讨论的透皮剂型的载体/赋形剂已为本领域人员所熟知,其包括,但不仅限于:增溶剂,例如C2-C8的直链和支链醇、二醇、和三醇;增湿剂和保湿剂,诸如甘油、氨基酸及氨基酸衍生物、聚氨基酸及其衍生物、吡咯烷酮羧酸及其盐和衍生物;表面活性剂,诸如十二烷基磺酸钠、山梨醇单月桂酸酯;乳化剂,如十六醇、硬脂醇;增稠剂,如甲基纤维素、乙基纤维素、羟甲基纤维素、羟丙基纤维素、聚乙烯吡咯烷酮、聚乙烯醇和丙烯酸酯聚合物。
渗透增强效果可以用本领域公知的技术测定。测定方法的一个例子在如下的实施例中有描述。
在本发明的一个优选实施方式中,所述透皮剂型包含了DMSO和油酸,其中DMSO对油酸的重量比落入前述的范围内。
在本发明的另一个可选择的优选实施方式中,所述透皮剂型包含了DMSO和氮酮,其中DMSO对氮酮的重量比落入前述的范围内。
优选所述透皮剂型包含了至少一种活性剂。合适的活性剂的例子前已述及。更优选至少一种活性剂包含了一种非甾族抗炎药(NSAID)。可用于本发明透皮剂型中的NSAIDs的合适的例子前已述及。例如,上述的剂型可以包括双氯芬酸,尤其是双氯芬酸钠,作为至少一种活性剂。
所述透皮剂型的一个实施方式优选包含重量占剂型高达约45%的DMSO、重量占剂型约5%的油酸、和作为活性剂的双氯芬酸钠。应理解,平衡的剂型还可以包含至少一种药学可接受的载体/赋形剂。例如,剂型可能还可以包含乙醇、丙二醇、聚乙二醇300中的至少一种,和至少一种保湿剂。
上述透皮剂型还可以包含丙二醇。丙二醇在该剂型中的重量比可以为1%-25%w/w。
另外,所述透皮剂型还可以包含乙醇和/或聚乙二醇300。乙醇在该剂型中的重量比可以为1%-25%w/w。聚乙二醇300在该剂型中的重量比可以为1%-80%w/w。此外,所述透皮剂型还可以包含至少一种增湿剂/保湿剂。
在更进一步的实施方式中,所述剂型包含了占剂型重量约45%的DMSO、占剂型重量约10%的油酸、和双氯芬酸钠。应当理解,为了达到平衡,剂型还可以另外包含至少一种如上所述药学可接受的载体/赋形剂。
在更进一步的实施方式中,所述剂型包含了占剂型重量约45%的DMSO、占剂型重量约5%的氮酮、和双氯芬酸钠。应当理解,该剂型还可以另外包含至少一种药学可接受的载体/赋形剂。例如,剂型还可以包含乙醇、丙二醇、聚乙二醇300中的至少一种,和至少一种保湿剂。
上述透皮剂型还可以包含丙二醇。丙二醇在该剂型中的重量比可以为1%-25%w/w。另外,所述透皮剂型还可以包含乙醇和/或聚乙二醇300。乙醇在该剂型中的重量比可以为1%-25%w/w。聚乙二醇300在该剂型中的重量比可以为1%-80%w/w。此外,所述透皮剂型还可以包含至少一种增湿剂/保湿剂。
在更进一步的实施方式中,所述剂型包含了占剂型重量约45%的DMSO、占剂型重量约2%的氮酮、和双氯芬酸钠。应当理解,该剂型还可以另外包含至少一种如上所述药学可接受的载体/赋形剂。
在更进一步的实施方式中,所述剂型包含了占剂型重量约30%的DMSO、占剂型重量约5%的氮酮、和双氯芬酸钠。应当理解,该剂型还可以另外包含至少一种如上所述药学可接受的载体/赋形剂。
在本发明的一个实施方式中,所述透皮剂型至少包含了一种活性剂、DMSO、氮酮、乙醇、丙二醇、聚乙二醇300、和一种保湿剂。特别是,该剂型包含:
(i)25%-90%w/w的DMSO;
(ii)1%-10%w/w的氮酮;
(iii)1%-25%w/w的乙醇;
(iv)1%-25%w/w的丙二醇;
(v)1%-80%w/w的聚乙二醇300;
(vi)至少一种保湿剂;和
(vii)至少一种活性剂。
在更进一步的实施方式中,该剂型包含:
(viii)30%-45%w/w的DMSO;
(ix)2%-5%w/w的氮酮;
(x)1%-25%w/w的乙醇;
(xi)1%-25%w/w的丙二醇;
(xii)1%-80%w/w的聚乙二醇300;
(xiii)至少一种保湿剂;和
(xiv)至少一种活性剂。
在本发明的另一个可选择的一个实施方式中,所述透皮剂型至少包含了一种活性剂、DMSO、油酸、乙醇、丙二醇、聚乙二醇300、和一种保湿剂。特别是,该剂型包含:
(i)25%-90%w/w的DMSO;
(ii)1%-10%w/w的油酸;
(iii)1%-25%w/w的乙醇;
(iv)1%-25%w/w的丙二醇;
(v)1%-80%w/w的聚乙二醇300;
(vi)至少一种保湿剂;和
(vii)至少一种活性剂。
在更进一步的实施方式中,该剂型包含:
(viii)30%-45%w/w的DMSO;
(ix)5%-10%w/w的油酸;
(x)1%-25%w/w的乙醇;
(xi)1%-25%w/w的丙二醇;
(xii)1%-80%w/w的聚乙二醇300;
(xiii)至少一种保湿剂;和
(xiv)至少一种活性剂。
本发明提供了一种改进的透皮剂型,用于将至少一种活性剂转运进入系统循环。改进之处在于通过形成制剂并且合并了DMSO、以及氮酮和油酸中的至少一种,进而增强了渗入效应。这种增强的效应将在下面进行讨论,并在实例和随附的图1中展示。
下面的实施例提供了一种比较:根据本发明的一种新的改进的透皮剂型,其中包含了双氯芬酸钠作为活性成分,与Nuvo研究公司(Nuvo Research Inc.)(原Dimethaid研究公司)公司生产的包含双氯芬酸钠作为活性剂的透皮剂型进行比较。
实施例一
材料
猪皮:Lampire生物实验室,宾夕法尼亚州Pipersville市
配方:4种配方,详述见下
HPLC使用装置:安捷仑1100,附带自动进样器
HPLC溶剂:高效液相色谱级纯水,高效液相色谱级纯乙腈,高效液相色谱级纯磷酸
HPLC柱:Ci8反相色谱柱
制备出表1中列出的剂型。从表1中可以看出,对照1不含油酸,对照2/3不含DMSO。相应的,对照1,对照2,对照3只是为了用于对比,并不包含在本发明中。
表1
表1中的每种剂型都使用Franz扩散池测试其在猪皮中的渗透情况,见下述。
在Franz扩散池具有容量为5ml的受体孔,用于连接全层猪皮(从佩里科学公司Perry Scientific获得)。猪皮的毛发被剔除,并用水冲洗干净,且去除了皮下脂肪。供体孔面积为约0.5cm2。受体孔内填充了等渗的含0.01%叠氮化钠的磷酸盐缓冲溶液。Franz扩散池边缘涂有真空脂,以确保完全密封,并用弹簧夹(SS#18VWR80073-350)以均匀的压力夹紧。Franz扩散池组装好后,猪皮用PBS缓冲溶液进行预水合,时间为45分钟。除去PBS后,将200μl剂型施加于供体孔。Franz扩散池的受体孔保持在37℃(皮肤表面温度在30℃左右),并使用搅拌棒持续搅拌。计算通量率,假设供体孔半径为0.4cm(即,面积为0.503cm2)。高效液相色谱测定双氯芬酸的校准曲线斜率是115.6AUC/(μg双氯芬酸/ml)。
该试验结果见表2。除对照1外,所有的剂型均在t=24hrs和t=48hrs时从受体孔中取样。对照1的样品在t=48hrs时从受体孔中取样。测量重复5次。
表2
剂型 | 24hrs时的通量(μg/hr/cm2) | 48hrs时的通量(μg/hr/cm2) |
对照1 | 0.003 | 0.004 |
对照2 | 0.03 | 0.07 |
对照3 | 0.08 | 0.11 |
A | 0.07 | 0.39 |
B | 0.14 | 0.87 |
这些结果表明,与对照1和对照2相比,剂型A的通量显著提高。此外,这些结果还表明,与对照1和对照3相比,剂型B的通量显著提高.
实施例2
材料:
人类尸体皮肤:男性,美国组织和细胞公司Male US Tissue and Cell,Inc.,编号06713,06600,07043
剂型:Dimethaid,A-E
HPLC型号:Hewlett Packard 1100
高效液相色谱溶剂:
水,高效液相色谱级,J.T.Baker;
乙腈,高效液相色谱级,Acros;
冰醋酸/磷酸Sigma-Aldrich
高效液相色谱柱:反相C8,由Dimethaid提供
渗透性测量
表3
测量渗透通量的步骤为Franz扩散池程序,如Franz,TJ在Percutaneous absorption:on the relevance of in vitro data.JInvest derm 1975,64;190-195.中所述。垂直的Franz扩散池(受体容量5.1ml-PermeGear,Bethlehem市,宾夕法尼亚州),供体面积为0.64cm2。测量池的受体器含有等渗磷酸盐缓冲液,并用磁搅拌器进行搅拌,转速为600rpm(在100ml水溶解1片得到PBS缓冲溶液)。人的皮肤样本被置于扩散池中,并在实验前用PBS预水合一个小时。在Franz扩散池内进行体外渗透人体尸皮肤(3种供体)的测试,每个剂型重复施用3次,每个剂型都应用于三种供体。简单来说,每种剂型都取15μl施涂于皮肤上,并用玻璃棒扩散开。每次取样前后都去除气泡。每次采集400μl样本后都改换新鲜PBS。根据这些稀释液进行计算。采样时间分别如下:
剂型A至C:0、4、8、10、12、24、36
剂型D:0、8、10、12、22、24、26、36
剂型E:在0、8、10、12、22、23、24、36
在0和8hr进行应用测试。在第二次应用前取出8小时的样品。高效液相色谱法分析和随后的计算得到渗透参数,包括通量(J)和强化率(ER)。
如图1和2所示,剂型A和B显示出最高的增强效果,与对照样D和E相比,其渗透双氯芬酸钠的滞后时间最少。使用t检验进行统计分析,结果显示,A和B在通量和Q24上不存在显著差异。将剂型A和B与C、D、E比较,结果表明,A和B对双氯芬酸钠有显著较高的通量和Q24。
表4包括了剂型A到E的试验数据,其中ER=强化率=剂型A的通量/剂型D的通量,n=重复次数,在括号里的值是标准偏差。
表4
剂型 | A(n=8) | B(n=7) | C(n=6) | D(n=6) | E(n=7) |
滞后时间(hr) | 7.2(±2.0) | 8.7(±2.6) | 12.1(±1.3) | 13.3(±0.2) | 9.5(±1.4) |
通量(μg/cm2.hr) | 5.9(±1.7) | 5.7(±1.4) | 2.6(±0.63) | 0.4(±0.02) | 1.4(±0.6) |
相比D之ER* | 14.7 | 14.2 | 6.5 | ||
相比E之ER | 4.6 | 4.0 | 1.8 | ||
Q24(μg/cm2) | 96.8(±40.2) | 83.8(±32.7) | 26.4(±6.9) | 4.5(±0.2) | 17.9(±7.5) |
实施例3
材料
人类尸体皮肤:男性,美国组织和细胞公司Male US Tissue and Cell,Inc.,编号06713,06600,07043;
剂型:Dimethaid,A-E
高效液相色谱型号:Hewlett Packard 1100;
高效液相色谱溶剂:
水,高效液相色谱级,JT.Baker;
乙腈,高效液相色谱级,Acros;
冰醋酸/磷酸,Sigma-Aldrich;
高效液相色谱柱:反相C8,由dimethaid提供。
渗透测量
表5提供了剂型3A到3F的详细组成。这些剂型将按照下述方法进行测试。
表5
用上文讨论过的Franz扩散池程序测量渗透性能。Franz扩散池的受体孔容量为3ml,与分层厚皮尸体皮肤(0.015″-0.018″,AlIo Source)一起使用。供体孔面积为0.5cm2。受体孔内充满了含0.01%叠氮化钠的等渗磷酸盐缓冲溶液。Franz扩散池边缘涂有一层真空脂以确保完全密封,并用弹簧夹(SS#18VWR80073-350)以均匀压力夹紧。Franz扩散池组装好后,使皮肤用PBS预水合45分钟。然后除去PBS,将200μl的剂型施加于供体孔。Franz扩散池的受体孔保持在37℃(皮肤表面上的温度在30℃),用搅拌棒持续搅拌。在t=24hrs和t=48hrs时从受体孔中取样。测量重复5次。用高效液相色谱分析受体液体中的双氯芬酸钠含量。
此测试的结果见表6。t=24hr和t=48hr时分别从受体孔采集样本。测量重复5次。
表6
剂型 | 24hrs时的通量(μg/hr/cm2) | 48hrs时的通量(μg/hr/cm2) |
3A | 9.59 | 10.70 |
3B | 6.54 | 7.80 |
3C | 4.70 | 6.67 |
3D | 5.31 | 8.46 |
3E | 5.15 | 8.53 |
3F | 2.26 | 4.36 |
3G | 1.63 | 2.57 |
根据本发明制备的透皮剂型可以以本领域已知的任何手段施涂于皮肤,包括,但不仅限于:利用气雾剂、喷雾剂、带泵包、刷子、棉签、或其他涂药器具。优选涂药器可以提供一种固定的或浮动的读数表用来测定使用剂量,例如能测定剂量的气雾剂、测定蓄能剂量的泵,或者提供一种手动测定剂量的泵。优选药物传送系统施涂于人或动物皮肤,所覆盖的释药表面积约为10-800cm2,优选约10-400cm2,更优选约10-200cm2。释药优选用局部有剂量读数表、的喷雾剂进行,其同时配备了驱动器喷嘴和罩子,该装置可共同精确控制使用量和/或均一度。罩子的一个作用就是使得喷嘴处于预定高度之上,并垂直于施用药物的皮肤。这个作用同样可以通过间隔棒或此类器具实现。罩子的另一个作用是封闭上述皮肤区域,旨在避免或限制药物反弹和/或释药系统向周围环境释放药物而造成的损失。优选罩子限定的区域基本上是圆形的。
该药物释放系统可以是一个具有或没有滚轴的单位体积分配器,或其他类型的涂药器。也可能有必要对未处理的皮肤施涂许多剂量,以获取期望效果。
尽管本发明的具体实施方式在说明性实施例中被详细描述,但这些描述不是用于进行限制。因此,参照本发明的公开,对例举实施例进行各种改进,以及本发明的其它实施方式,对本领域技术人员而言是显而易见的。因此,附后的权利要求涵盖了任何此类改进或具体实施方式。进一步而言,此处所有的权利要求以引用的方式并入优选实施方式的说明中。
本文所提及的任何公开、专利和专利申请都是以全文引用的方式并入,其引用程度就如同将每一个别公开、专利或专利申请具体且个别地以全文引用的方式并入。
Claims (43)
1.一种透皮剂型的用途,用于提高人体中至少一种活性剂的透皮渗入,所述剂型包含:
(i)第一种化合物选自由二甲亚砜(DMSO)、甲基乙基亚砜、甲基1,2-亚乙基亚砜及其混合物所构成的组;
(ii)第二种化合物选自由脂肪酸、氮酮类化合物及其混合物所构成的组,其中
所述脂肪酸选自由反亚油酸、亚油酸、亚麻酸、油酸、异油酸及其混合物所构成的组,以及
所述氮酮类化合物选自由1-[2-(癸基硫代)乙基]氮杂环戊烷-2-酮、氮酮、1-法尼基氮杂环庚烷-2-酮、1-法尼基氮杂环戊烷-2-酮、1-香叶基-氮杂环庚烷-2-酮、1-香叶基氮杂环戊烷-2-酮、1-N-辛基氮杂环庚烷-2-酮及其混合物所构成的组;以及
(iii)至少一种治疗性的活性剂,所述活性剂为非甾族抗炎药,其中所述非甾族抗炎药选自由双氯芬酸、甲氯胺苯酸、甲芬那酸、双氯芬酸钠、双氯芬酸钾、甲氯胺苯酸钠及其混合物所构成的组。
2.一种透皮剂型的用途,用于人体中至少一种活性剂的转运,所述剂型包含:
(i)第一种化合物选自由二甲亚砜(DMSO)、甲基乙基亚砜、甲基1,2-亚乙基亚砜及其混合物所构成的组;
(ii)第二种化合物选自由脂肪酸、氮酮类化合物及其混合物所构成的组,其中
所述脂肪酸选自由反亚油酸、亚油酸、亚麻酸、油酸、异油酸及其混合物所构成的组,以及
所述氮酮类化合物选自由1-[2-(癸基硫代)乙基]氮杂环戊烷-2-酮、氮酮、1-法尼基氮杂环庚烷-2-酮、1-法尼基氮杂环戊烷-2-酮、1-香叶基-氮杂环庚烷-2-酮、1-香叶基氮杂环戊烷-2-酮、1-N-辛基氮杂环庚烷-2-酮及其混合物所构成的组;以及
(iii)至少一种治疗性的活性剂,所述活性剂为非甾族抗炎药,其中所述非甾族抗炎药选自由双氯芬酸、甲氯胺苯酸、甲芬那酸、双氯芬酸钠、双氯芬酸钾、甲氯胺苯酸钠及其混合物所构成的组。
3.如权利要求2所述的用途,其特征在于,所述透皮剂型用于将至少一种活性剂直接或间接地运送到患病部位。
4.如权利要求2所述的用途,其特征在于,所述透皮剂型用于将至少一种活性剂转运进入系统循环。
5.如权利要求1或2所述的用途,其特征在于,所述剂型施涂于人或动物皮肤,所覆盖的表面积为10-800cm2、10-400cm2或10-200cm2。
6.如权利要求1至3中任一项所述的用途,其特征在于,所述非甾族抗炎药是双氯芬酸钠。
7.如权利要求1至3中任一项所述的用途,其特征在于,所述第一种化合物是二甲亚砜。
8.如权利要求1至3中任一项所述的用途,其特征在于,所述第二种化合物为氮酮。
9.如权利要求1至3中任一项所述的用途,其特征在于,所述第二种化合物为油酸。
10.如权利要求1至3中任一项所述的用途,其特征在于,所述第一种化合物与所述第二种化合物的重量比在50∶1至5∶1的范围内。
11.如权利要求10所述的用途,其特征在于,所述第一种化合物与所述第二种化合物的重量比在20∶1至5∶1的范围内。
12.如权利要求1至3中任一项所述的用途,其特征在于,所述剂型通过气雾剂、带泵包、刷子或棉签被施涂到皮肤上。
13.如权利要求12所述的用途,其特征在于,所述气雾剂为喷雾剂。
14.如权利要求1至3中任一项所述的用途,其特征在于,所述剂型具有以Franz扩散池程序测定的至少2μg/cm2·hr的通量。
15.如权利要求14所述的用途,其特征在于,所述剂型具有以Franz扩散池程序测定的至少3μg/cm2·hr的通量。
16.如权利要求15所述的用途,其特征在于,所述剂型具有以Franz扩散池程序测定的至少4μg/cm2·hr的通量。
17.如权利要求16所述的用途,其特征在于,所述剂型具有以Franz扩散池程序测定的至少5μg/cm2·hr的通量。
18.如权利要求14所述的用途,其特征在于,所述剂型具有以Franz扩散池程序测定的2-5μg/cm2·hr的通量。
19.如权利要求1或2所述的用途,其特征在于,所述剂型包含DMSO作为第一种化合物和氮酮作为第二种化合物,其中DMSO和氮酮的重量比在50∶1至10∶1的范围内。
20.如权利要求19所述的用途,其特征在于,所述DMSO和氮酮的重量比在20∶1至10∶1的范围内。
21.如权利要求20所述的用途,其特征在于,所述NSAID为双氯芬酸钠。
22.如权利要求1至3中任一项所述的用途,其特征在于,所述剂型进一步包含至少一种药学上可接受的载体。
23.如权利要求1或2所述的用途,其特征在于,所述透皮剂型包含:
(i)在剂型中重量百分数为25%-90%的DMSO;
(ii)在剂型中重量百分数为1%-10%的氮酮;
(iii)在剂型中重量百分数为1%-25%的乙醇;
(iv)在剂型中重量百分数为1%-25%的丙二醇;
(v)在剂型中重量百分数为1%-80%的聚乙二醇300;
(vi)至少一种保湿剂;和
(vii)至少一种活性剂,所述活性剂为非甾族抗炎药,其中所述非甾族抗炎药选自由双氯芬酸、甲氯胺苯酸、甲芬那酸、双氯芬酸钠、双氯芬酸钾、甲氯胺苯酸钠、及其混合物所构成的组。
24.如权利要求23所述的用途,其特征在于,所述DMSO在剂型中的重量百分数为30%-45%。
25.如权利要求23或24所述的用途,其特征在于,所述氮酮在剂型中的重量百分数为2%-5%。
26.如权利要求23所述的用途,其特征在于,所述非甾族抗炎药为双氯芬酸钠。
27.如权利要求1或2所述的用途,其特征在于,所述透皮剂型包含:
(i)在剂型中重量百分数为45.5%的DMSO;
(ii)在剂型中重量百分数为5%的氮酮;以及
(iii)双氯芬酸钠。
28.如权利要求27所述的用途,其特征在于,所述剂型进一步包含丙二醇、甘油、乙醇和PEG300中的至少一种。
29.如权利要求1或2所述的用途,其特征在于,所述透皮剂型包含:
(i)在剂型中重量百分数为45.5%的DMSO;
(ii)在剂型中重量百分数为2%的氮酮;和
(iii)双氯芬酸钠。
30.如权利要求29所述的用途,其特征在于,所述剂型进一步包含丙二醇、甘油、乙醇和PEG300中的至少一种。
31.如权利要求1或2所述的用途,其特征在于,所述透皮剂型包含:
(i)在剂型中重量百分数为30%的DMSO;
(ii)在剂型中重量百分数为5.0%的氮酮;和
(iii)双氯芬酸钠。
32.如权利要求31所述的用途,其特征在于,所述剂型进一步包含丙二醇、甘油、乙醇和PEG300中的至少一种。
33.如权利要求1或2所述的用途,其特征在于,所述剂型包含DMSO作为第一种化合物和油酸作为第二种化合物,其中DMSO和油酸的重量比在10∶1至5∶1的范围内。
34.如权利要求33所述的用途,其特征在于,所述抗炎药为双氯芬酸钠。
35.如权利要求33或34所述的用途,其特征在于,所述剂型进一步包含至少一种药学上可接受的载体。
36.如权利要求1或2所述的用途,其特征在于,所述剂型包含:
(i)在剂型中重量百分数为25%-90%的DMSO;
(ii)在剂型中重量百分数为1%-10%的油酸;
(iii)在剂型中重量百分数为1%-25%的乙醇;
(iv)在剂型中重量百分数为1%-25%的丙二醇;
(v)在剂型中重量百分数为1%-80%的聚乙二醇300;
(vi)至少一种保湿剂;和
(vii)至少一种活性剂,所述活性剂为非甾族抗炎药,其中所述非甾族抗炎药选自由双氯芬酸、甲氯胺苯酸、甲芬那酸、双氯芬酸钠、双氯芬酸钾、甲氯胺苯酸钠、及其混合物所构成的组。
37.如权利要求36所述的用途,其特征在于,所述DMSO在剂型中的重量百分数为30%-45%。
38.如权利要求36所述的用途,其特征在于,所述油酸在剂型中的重量百分数为5%-10%。
39.如权利要求36至38中任一项所述的用途,其特征在于,所述非甾族抗炎药为双氯芬酸钠。
40.如权利要求1或2所述的用途,其特征在于,所述剂型包含:
(i)在剂型中重量百分数为45.5%的DMSO;
(ii)在剂型中重量百分数为5%的油酸;和
(iii)双氯芬酸钠。
41.如权利要求40所述的用途,其特征在于,所述剂型进一步包含丙二醇、甘油、乙醇和PEG300中的至少一种。
42.如权利要求1或2所述的用途,其特征在于,所述剂型包含:
(i)在剂型中重量百分数为45.5%的DMSO;
(ii)在剂型中重量百分数为10%的油酸;和
(iii)双氯芬酸钠。
43.如权利要求42所述的用途,其特征在于,所述剂型进一步包含丙二醇、甘油、乙醇和PEG300中的至少一种。
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KR100433614B1 (ko) * | 2000-06-16 | 2004-05-31 | 주식회사 태평양 | 친수성 또는 염의 형태로 된 약물을 함유하는 경피흡수제제 |
US20040175415A1 (en) * | 2003-03-05 | 2004-09-09 | Chan Alvin C. | Formulations and methods of delivery of intact tocopheryl succinate to humans |
US20040241217A1 (en) * | 2003-05-29 | 2004-12-02 | Yee-Chien Liu | Method for administration of immune modulators in systemic and localized immune disorders |
US20070269379A1 (en) * | 2003-07-23 | 2007-11-22 | Samir Mitragotri | Penetration Enhancer Combinations for Transdermal Delivery |
-
2006
- 2006-08-04 US US12/063,028 patent/US20080319092A1/en not_active Abandoned
- 2006-08-04 CA CA002617934A patent/CA2617934A1/en not_active Abandoned
- 2006-08-04 WO PCT/CA2006/001271 patent/WO2007016766A1/en active Application Filing
- 2006-08-04 CN CN2006800365199A patent/CN101296691B/zh not_active Expired - Fee Related
- 2006-08-04 EP EP06775058A patent/EP1909772A4/en not_active Withdrawn
- 2006-08-04 CN CN2011101585856A patent/CN102225046A/zh active Pending
Cited By (7)
Publication number | Priority date | Publication date | Assignee | Title |
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CN107441069A (zh) * | 2012-02-28 | 2017-12-08 | 日绊株式会社 | 贴附剂 |
CN107920989A (zh) * | 2015-06-08 | 2018-04-17 | 考里安国际公司 | 用于透皮递送阿立哌唑的制剂 |
CN107670022A (zh) * | 2017-09-06 | 2018-02-09 | 华中农业大学 | 一种催产素透皮剂及其制备方法和应用 |
CN107670022B (zh) * | 2017-09-06 | 2020-07-10 | 华中农业大学 | 一种催产素透皮剂及其制备方法和应用 |
CN110833546A (zh) * | 2018-08-17 | 2020-02-25 | 中国科学院上海生命科学研究院 | 通佐溴胺在治疗胃癌中的用途 |
CN110833546B (zh) * | 2018-08-17 | 2022-06-28 | 中国科学院分子细胞科学卓越创新中心 | 通佐溴胺在治疗胃癌中的用途 |
CN114652734A (zh) * | 2022-03-31 | 2022-06-24 | 李红梦 | 一种祛痘的药物组合物及其制备方法 |
Also Published As
Publication number | Publication date |
---|---|
CA2617934A1 (en) | 2007-02-15 |
CN101296691B (zh) | 2011-07-27 |
WO2007016766A1 (en) | 2007-02-15 |
CN101296691A (zh) | 2008-10-29 |
EP1909772A1 (en) | 2008-04-16 |
EP1909772A4 (en) | 2011-07-13 |
US20080319092A1 (en) | 2008-12-25 |
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