CN101352415A - 一种醋溴茶碱口服溶液的剂型和制备方法 - Google Patents
一种醋溴茶碱口服溶液的剂型和制备方法 Download PDFInfo
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- CN101352415A CN101352415A CNA2007100584313A CN200710058431A CN101352415A CN 101352415 A CN101352415 A CN 101352415A CN A2007100584313 A CNA2007100584313 A CN A2007100584313A CN 200710058431 A CN200710058431 A CN 200710058431A CN 101352415 A CN101352415 A CN 101352415A
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- 229940100688 oral solution Drugs 0.000 title claims abstract description 33
- IPUHJDQWESJTGD-PFWPSKEQSA-N Cn1c2ncn(CC(O)=O)c2c(=O)n(C)c1=O.Nc1c(Br)cc(Br)cc1CN[C@H]1CC[C@H](O)CC1 Chemical compound Cn1c2ncn(CC(O)=O)c2c(=O)n(C)c1=O.Nc1c(Br)cc(Br)cc1CN[C@H]1CC[C@H](O)CC1 IPUHJDQWESJTGD-PFWPSKEQSA-N 0.000 title claims description 46
- 238000002360 preparation method Methods 0.000 title abstract description 21
- 239000002552 dosage form Substances 0.000 title description 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 56
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims abstract description 45
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 14
- 239000002904 solvent Substances 0.000 claims abstract description 5
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 47
- 230000000844 anti-bacterial effect Effects 0.000 claims description 20
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 17
- 229930006000 Sucrose Natural products 0.000 claims description 17
- 239000005720 sucrose Substances 0.000 claims description 17
- 229960004793 sucrose Drugs 0.000 claims description 17
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 10
- 239000003795 chemical substances by application Substances 0.000 claims description 10
- 108010011485 Aspartame Proteins 0.000 claims description 9
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 claims description 9
- 239000000605 aspartame Substances 0.000 claims description 9
- 235000010357 aspartame Nutrition 0.000 claims description 9
- 229960003438 aspartame Drugs 0.000 claims description 9
- 238000000034 method Methods 0.000 claims description 8
- 238000012856 packing Methods 0.000 claims description 7
- 235000019202 steviosides Nutrition 0.000 claims description 7
- 238000003756 stirring Methods 0.000 claims description 7
- FTLYMKDSHNWQKD-UHFFFAOYSA-N (2,4,5-trichlorophenyl)boronic acid Chemical compound OB(O)C1=CC(Cl)=C(Cl)C=C1Cl FTLYMKDSHNWQKD-UHFFFAOYSA-N 0.000 claims description 6
- UEDUENGHJMELGK-HYDKPPNVSA-N Stevioside Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1O[C@]12C(=C)C[C@@]3(C1)CC[C@@H]1[C@@](C)(CCC[C@]1([C@@H]3CC2)C)C(=O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O UEDUENGHJMELGK-HYDKPPNVSA-N 0.000 claims description 6
- 229940085605 saccharin sodium Drugs 0.000 claims description 6
- 229940013618 stevioside Drugs 0.000 claims description 6
- OHHNJQXIOPOJSC-UHFFFAOYSA-N stevioside Natural products CC1(CCCC2(C)C3(C)CCC4(CC3(CCC12C)CC4=C)OC5OC(CO)C(O)C(O)C5OC6OC(CO)C(O)C(O)C6O)C(=O)OC7OC(CO)C(O)C(O)C7O OHHNJQXIOPOJSC-UHFFFAOYSA-N 0.000 claims description 6
- 235000007119 Ananas comosus Nutrition 0.000 claims description 5
- 235000016623 Fragaria vesca Nutrition 0.000 claims description 5
- 235000011363 Fragaria x ananassa Nutrition 0.000 claims description 5
- 239000008367 deionised water Substances 0.000 claims description 5
- 229910021641 deionized water Inorganic materials 0.000 claims description 5
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims description 4
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical class OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 claims description 4
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims description 4
- 238000001914 filtration Methods 0.000 claims description 4
- 239000002304 perfume Substances 0.000 claims description 4
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims description 3
- CHHHXKFHOYLYRE-UHFFFAOYSA-M 2,4-Hexadienoic acid, potassium salt (1:1), (2E,4E)- Chemical compound [K+].CC=CC=CC([O-])=O CHHHXKFHOYLYRE-UHFFFAOYSA-M 0.000 claims description 3
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims description 3
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims description 3
- 239000001630 malic acid Substances 0.000 claims description 3
- 235000011090 malic acid Nutrition 0.000 claims description 3
- 239000004302 potassium sorbate Substances 0.000 claims description 3
- 235000010241 potassium sorbate Nutrition 0.000 claims description 3
- 229940069338 potassium sorbate Drugs 0.000 claims description 3
- 230000001105 regulatory effect Effects 0.000 claims description 3
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 claims description 3
- 239000004299 sodium benzoate Substances 0.000 claims description 3
- 235000010234 sodium benzoate Nutrition 0.000 claims description 3
- 239000011975 tartaric acid Substances 0.000 claims description 3
- 235000002906 tartaric acid Nutrition 0.000 claims description 3
- QOSMNYMQXIVWKY-UHFFFAOYSA-N Propyl levulinate Chemical compound CCCOC(=O)CCC(C)=O QOSMNYMQXIVWKY-UHFFFAOYSA-N 0.000 claims description 2
- 241001481665 Protophormia terraenovae Species 0.000 claims description 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims description 2
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims description 2
- 150000002148 esters Chemical class 0.000 claims description 2
- 125000004494 ethyl ester group Chemical group 0.000 claims description 2
- 229940098779 methanesulfonic acid Drugs 0.000 claims description 2
- 150000004702 methyl esters Chemical class 0.000 claims description 2
- DCKVNWZUADLDEH-UHFFFAOYSA-N sec-butyl acetate Chemical compound CCC(C)OC(C)=O DCKVNWZUADLDEH-UHFFFAOYSA-N 0.000 claims description 2
- 239000001117 sulphuric acid Substances 0.000 claims description 2
- 235000011149 sulphuric acid Nutrition 0.000 claims description 2
- 244000099147 Ananas comosus Species 0.000 claims 1
- 240000009088 Fragaria x ananassa Species 0.000 claims 1
- 239000003814 drug Substances 0.000 abstract description 12
- ZFXYFBGIUFBOJW-UHFFFAOYSA-N theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 abstract description 11
- 230000000857 drug effect Effects 0.000 abstract description 4
- 235000019640 taste Nutrition 0.000 abstract description 4
- 229960000278 theophylline Drugs 0.000 abstract 5
- 238000009472 formulation Methods 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 238000010521 absorption reaction Methods 0.000 abstract 1
- 235000009508 confectionery Nutrition 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 235000011187 glycerol Nutrition 0.000 abstract 1
- 239000004615 ingredient Substances 0.000 abstract 1
- 239000000686 essence Substances 0.000 description 30
- 239000000243 solution Substances 0.000 description 21
- 150000007524 organic acids Chemical class 0.000 description 8
- 238000012360 testing method Methods 0.000 description 7
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
- 235000019658 bitter taste Nutrition 0.000 description 6
- 238000005516 engineering process Methods 0.000 description 5
- 229960001617 ethyl hydroxybenzoate Drugs 0.000 description 5
- NUVBSKCKDOMJSU-UHFFFAOYSA-N ethylparaben Chemical compound CCOC(=O)C1=CC=C(O)C=C1 NUVBSKCKDOMJSU-UHFFFAOYSA-N 0.000 description 5
- 239000000796 flavoring agent Substances 0.000 description 5
- GYCKQBWUSACYIF-UHFFFAOYSA-N o-hydroxybenzoic acid ethyl ester Natural products CCOC(=O)C1=CC=CC=C1O GYCKQBWUSACYIF-UHFFFAOYSA-N 0.000 description 5
- 241000234671 Ananas Species 0.000 description 4
- 241000220223 Fragaria Species 0.000 description 4
- 208000006673 asthma Diseases 0.000 description 4
- 235000019634 flavors Nutrition 0.000 description 4
- 238000005286 illumination Methods 0.000 description 4
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 4
- 229960003415 propylparaben Drugs 0.000 description 4
- QFOHBWFCKVYLES-UHFFFAOYSA-N Butylparaben Chemical compound CCCCOC(=O)C1=CC=C(O)C=C1 QFOHBWFCKVYLES-UHFFFAOYSA-N 0.000 description 3
- 230000002159 abnormal effect Effects 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
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- 206010036790 Productive cough Diseases 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 239000007864 aqueous solution Substances 0.000 description 2
- 235000019606 astringent taste Nutrition 0.000 description 2
- 206010006451 bronchitis Diseases 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 208000030603 inherited susceptibility to asthma Diseases 0.000 description 2
- 238000007689 inspection Methods 0.000 description 2
- 238000011835 investigation Methods 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 2
- 238000003860 storage Methods 0.000 description 2
- 235000019605 sweet taste sensations Nutrition 0.000 description 2
- 206010011224 Cough Diseases 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- 206010062530 Increased bronchial secretion Diseases 0.000 description 1
- 206010062717 Increased upper airway secretion Diseases 0.000 description 1
- 206010067482 No adverse event Diseases 0.000 description 1
- 201000007100 Pharyngitis Diseases 0.000 description 1
- 230000001133 acceleration Effects 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 210000000621 bronchi Anatomy 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 230000001886 ciliary effect Effects 0.000 description 1
- 230000001186 cumulative effect Effects 0.000 description 1
- 238000013461 design Methods 0.000 description 1
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- 239000006185 dispersion Substances 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 229960005150 glycerol Drugs 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
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- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
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- 238000012803 optimization experiment Methods 0.000 description 1
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- 238000004806 packaging method and process Methods 0.000 description 1
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- 230000015843 photosynthesis, light reaction Effects 0.000 description 1
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Landscapes
- Medicinal Preparation (AREA)
Abstract
Description
实施例 | 醋溴茶碱(g) | 甘油和/或丙二醇(ml) | pH调节剂(适量) | 矫味剂(g) | 抑菌剂(g) |
1 | 20 | 甘油200 | 枸橼酸 | 蔗糖 300薄荷香精 适量橘子香精 适量 | 羟苯乙酯 0.5 |
2 | 10 | 丙二醇 300 | 枸橼酸 | 蔗糖 200草莓香精 适量 | 羟苯甲酯0.5 |
3 | 5 | 甘油 100丙二醇 100 | 枸橼酸 | 蔗糖 150薄荷香精 适量橘子香精 适量 | 羟苯丙酯0.3羟苯丁酯0.1 |
4 | 15 | 甘油 200 | 枸橼酸 | 蔗糖 100阿巴斯甜 0.1菠萝香精 适量薄荷香精 适量 | 羟苯甲酯0.3羟苯丁酯0.2 |
5 | 2.5 | 甘油 100丙二醇 100 | 枸橼酸 | 蔗糖 100糖精钠 0.03柠檬香精 适量 | 羟苯甲酯0.2羟苯乙酯0.2 |
6 | 1 | 甘油 200 | 枸橼酸 | 蔗糖 50阿巴斯甜 0.05草莓香精 适量薄荷香精 适量 | 羟苯乙酯0.1羟苯丙酯0.3 |
7 | 18 | 甘油 100丙二醇 100 | 枸橼酸 | 蔗糖 100甜菊甙 0.05柠檬香精 适量薄荷香精 适量 | 羟苯乙酯0.3羟苯丁酯0.2 |
8 | 13 | 甘油 200 | 枸橼酸 | 蔗糖 100阿巴斯甜 0.5菠萝香精 适量 | 苯甲酸钠3 |
9 | 8 | 丙二醇 200 | 枸橼酸 | 蔗糖 200橘子香精 适量 | 羟苯丙酯0.5 |
10 | 3 | 甘油 300 | 枸橼酸 | 阿巴斯甜 1 | 山梨酸钾3 |
11 | 2 | -- | 枸橼酸 | 甜菊甙 0.1 | 羟苯丁酯0.5 |
12 | 10 | -- | 枸橼酸 | 蔗糖 450薄荷香精 适量 | 羟苯甲酯0.2羟苯丙酯0.3 |
Claims (10)
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CN2007100584313A CN101352415B (zh) | 2007-07-26 | 2007-07-26 | 一种醋溴茶碱口服溶液的剂型和制备方法 |
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CN2007100584313A CN101352415B (zh) | 2007-07-26 | 2007-07-26 | 一种醋溴茶碱口服溶液的剂型和制备方法 |
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CN101352415A true CN101352415A (zh) | 2009-01-28 |
CN101352415B CN101352415B (zh) | 2011-11-23 |
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Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN104771358A (zh) * | 2014-01-14 | 2015-07-15 | 江苏柯菲平医药股份有限公司 | 一种茶碱乙酸氨溴索注射剂及其制备方法 |
CN106727590A (zh) * | 2016-01-04 | 2017-05-31 | 石家庄学院 | 一种稳定的吸入用茶碱乙酸氨溴索溶液 |
CN110141550A (zh) * | 2019-07-09 | 2019-08-20 | 武汉兴华智慧医药科技有限公司 | 一种左氧氟沙星口服溶液及其制备方法 |
CN115645366A (zh) * | 2022-11-15 | 2023-01-31 | 山东济坤生物制药有限公司 | 一种氨溴特罗口服溶液及其制备工艺 |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN100525770C (zh) * | 2003-05-13 | 2009-08-12 | 沈阳药科大学 | 一种含茶碱和沙丁胺醇活性组分的口服复方缓释制剂及制备工艺 |
-
2007
- 2007-07-26 CN CN2007100584313A patent/CN101352415B/zh not_active Expired - Fee Related
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN104771358A (zh) * | 2014-01-14 | 2015-07-15 | 江苏柯菲平医药股份有限公司 | 一种茶碱乙酸氨溴索注射剂及其制备方法 |
CN106727590A (zh) * | 2016-01-04 | 2017-05-31 | 石家庄学院 | 一种稳定的吸入用茶碱乙酸氨溴索溶液 |
CN110141550A (zh) * | 2019-07-09 | 2019-08-20 | 武汉兴华智慧医药科技有限公司 | 一种左氧氟沙星口服溶液及其制备方法 |
CN115645366A (zh) * | 2022-11-15 | 2023-01-31 | 山东济坤生物制药有限公司 | 一种氨溴特罗口服溶液及其制备工艺 |
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