CN1228049C - 一种含吲达帕胺活性成分的缓释微丸及其制备方法 - Google Patents
一种含吲达帕胺活性成分的缓释微丸及其制备方法 Download PDFInfo
- Publication number
- CN1228049C CN1228049C CN 03129975 CN03129975A CN1228049C CN 1228049 C CN1228049 C CN 1228049C CN 03129975 CN03129975 CN 03129975 CN 03129975 A CN03129975 A CN 03129975A CN 1228049 C CN1228049 C CN 1228049C
- Authority
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- Prior art keywords
- micropill
- indapamide
- release
- slow
- release layer
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- 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.)
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- NDDAHWYSQHTHNT-UHFFFAOYSA-N indapamide Chemical compound CC1CC2=CC=CC=C2N1NC(=O)C1=CC=C(Cl)C(S(N)(=O)=O)=C1 NDDAHWYSQHTHNT-UHFFFAOYSA-N 0.000 title claims abstract description 35
- 229960004569 indapamide Drugs 0.000 title claims abstract description 35
- 238000000034 method Methods 0.000 title claims description 7
- 239000006187 pill Substances 0.000 claims abstract description 24
- 238000002360 preparation method Methods 0.000 claims abstract description 24
- 238000000576 coating method Methods 0.000 claims abstract description 21
- 239000011248 coating agent Substances 0.000 claims abstract description 20
- 239000000463 material Substances 0.000 claims abstract description 15
- 239000004014 plasticizer Substances 0.000 claims abstract description 9
- 239000000945 filler Substances 0.000 claims abstract description 7
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 33
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 claims description 19
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 19
- 239000000203 mixture Substances 0.000 claims description 16
- 239000004925 Acrylic resin Substances 0.000 claims description 13
- 229920000178 Acrylic resin Polymers 0.000 claims description 13
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 13
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 13
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 13
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims description 11
- 239000012528 membrane Substances 0.000 claims description 11
- FLKPEMZONWLCSK-UHFFFAOYSA-N diethyl phthalate Chemical compound CCOC(=O)C1=CC=CC=C1C(=O)OCC FLKPEMZONWLCSK-UHFFFAOYSA-N 0.000 claims description 10
- 239000012530 fluid Substances 0.000 claims description 10
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 10
- 229960003943 hypromellose Drugs 0.000 claims description 9
- GUBGYTABKSRVRQ-QKKXKWKRSA-N lactose group Chemical group OC1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@@H](O)[C@H](O2)CO)[C@H](O1)CO GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 9
- 239000000314 lubricant Substances 0.000 claims description 9
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 9
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 9
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 9
- 239000008101 lactose Substances 0.000 claims description 8
- 239000001856 Ethyl cellulose Substances 0.000 claims description 7
- 229920002472 Starch Polymers 0.000 claims description 7
- 239000011230 binding agent Substances 0.000 claims description 7
- 235000019325 ethyl cellulose Nutrition 0.000 claims description 7
- 229920001249 ethyl cellulose Polymers 0.000 claims description 7
- 239000003361 porogen Substances 0.000 claims description 7
- 239000008107 starch Substances 0.000 claims description 7
- 235000019698 starch Nutrition 0.000 claims description 7
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 6
- 206010056437 Parkinsonian rest tremor Diseases 0.000 claims description 6
- 229930006000 Sucrose Natural products 0.000 claims description 6
- 239000006185 dispersion Substances 0.000 claims description 6
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 6
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 6
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 6
- 239000005720 sucrose Substances 0.000 claims description 6
- 239000002202 Polyethylene glycol Substances 0.000 claims description 5
- DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical group CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 claims description 5
- 235000019359 magnesium stearate Nutrition 0.000 claims description 5
- 229920001223 polyethylene glycol Polymers 0.000 claims description 5
- 239000001069 triethyl citrate Substances 0.000 claims description 5
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 claims description 5
- 235000013769 triethyl citrate Nutrition 0.000 claims description 5
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 4
- ZFOZVQLOBQUTQQ-UHFFFAOYSA-N Tributyl citrate Chemical compound CCCCOC(=O)CC(O)(C(=O)OCCCC)CC(=O)OCCCC ZFOZVQLOBQUTQQ-UHFFFAOYSA-N 0.000 claims description 4
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 4
- PYGXAGIECVVIOZ-UHFFFAOYSA-N Dibutyl decanedioate Chemical compound CCCCOC(=O)CCCCCCCCC(=O)OCCCC PYGXAGIECVVIOZ-UHFFFAOYSA-N 0.000 claims description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 2
- 235000021355 Stearic acid Nutrition 0.000 claims description 2
- 239000008199 coating composition Substances 0.000 claims description 2
- 239000008119 colloidal silica Substances 0.000 claims description 2
- 239000004148 curcumin Substances 0.000 claims description 2
- 229940075507 glyceryl monostearate Drugs 0.000 claims description 2
- 229920000609 methyl cellulose Polymers 0.000 claims description 2
- 239000001923 methylcellulose Substances 0.000 claims description 2
- 235000010981 methylcellulose Nutrition 0.000 claims description 2
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 claims description 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 2
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 2
- 229940093429 polyethylene glycol 6000 Drugs 0.000 claims description 2
- 239000000843 powder Substances 0.000 claims description 2
- 239000008117 stearic acid Substances 0.000 claims description 2
- 125000000185 sucrose group Chemical group 0.000 claims description 2
- 239000003814 drug Substances 0.000 abstract description 15
- 239000008280 blood Substances 0.000 abstract description 5
- 210000004369 blood Anatomy 0.000 abstract description 5
- 239000002904 solvent Substances 0.000 abstract description 3
- 239000000853 adhesive Substances 0.000 abstract 2
- 230000001070 adhesive effect Effects 0.000 abstract 2
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- 230000004584 weight gain Effects 0.000 abstract 1
- 235000019786 weight gain Nutrition 0.000 abstract 1
- 229940079593 drug Drugs 0.000 description 7
- 210000003491 skin Anatomy 0.000 description 7
- 235000010603 pastilles Nutrition 0.000 description 5
- 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 description 4
- 230000000694 effects Effects 0.000 description 4
- 238000005516 engineering process Methods 0.000 description 4
- 238000003756 stirring Methods 0.000 description 4
- 210000004204 blood vessel Anatomy 0.000 description 3
- 238000004090 dissolution Methods 0.000 description 3
- 229920000642 polymer Polymers 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Natural products OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 2
- 229920001577 copolymer Polymers 0.000 description 2
- 239000003937 drug carrier Substances 0.000 description 2
- 150000003180 prostaglandins Chemical class 0.000 description 2
- 230000001105 regulatory effect Effects 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- JIGUQPWFLRLWPJ-UHFFFAOYSA-N Ethyl acrylate Chemical compound CCOC(=O)C=C JIGUQPWFLRLWPJ-UHFFFAOYSA-N 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 description 1
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 description 1
- 206010047139 Vasoconstriction Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 229960000583 acetic acid Drugs 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 230000036772 blood pressure Effects 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 238000005660 chlorination reaction Methods 0.000 description 1
- 230000001276 controlling effect Effects 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 239000002934 diuretic Substances 0.000 description 1
- 230000001882 diuretic effect Effects 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 230000009977 dual effect Effects 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 239000012362 glacial acetic acid Substances 0.000 description 1
- 230000002209 hydrophobic effect Effects 0.000 description 1
- 230000009610 hypersensitivity Effects 0.000 description 1
- 230000001077 hypotensive effect Effects 0.000 description 1
- 230000008676 import Effects 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- IAVGMIBOMLTFSU-UHFFFAOYSA-L magnesium dioxosilane octadecanoate Chemical compound [Mg+2].O=[Si]=O.CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O IAVGMIBOMLTFSU-UHFFFAOYSA-L 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- IWVKTOUOPHGZRX-UHFFFAOYSA-N methyl 2-methylprop-2-enoate;2-methylprop-2-enoic acid Chemical compound CC(=C)C(O)=O.COC(=O)C(C)=C IWVKTOUOPHGZRX-UHFFFAOYSA-N 0.000 description 1
- 230000003204 osmotic effect Effects 0.000 description 1
- PNJWIWWMYCMZRO-UHFFFAOYSA-N pent‐4‐en‐2‐one Natural products CC(=O)CC=C PNJWIWWMYCMZRO-UHFFFAOYSA-N 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 238000003908 quality control method Methods 0.000 description 1
- 238000005070 sampling Methods 0.000 description 1
- 239000002195 soluble material Substances 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 229940124530 sulfonamide Drugs 0.000 description 1
- 150000003456 sulfonamides Chemical class 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 210000004509 vascular smooth muscle cell Anatomy 0.000 description 1
- 230000025033 vasoconstriction Effects 0.000 description 1
Images
Landscapes
- Medicinal Preparation (AREA)
Abstract
Description
1 | 2 | ||
乳糖淀粉蔗糖滑石粉硬脂酸镁 | 100g30g40g20g10g | 微晶纤维素淀粉羟丙甲纤维素二氧化硅硬脂酸镁 | 80g60g20g20g20g |
1 | 2 | ||
空白小丸吲达帕胺羟丙甲纤维素滑石粉聚乙二醇水 | 120g1.5g2g10g0.4g100ml | 空白小丸吲达帕胺聚乙烯吡咯烷酮滑石粉聚乙二醇70%乙醇 | 120g1.5g5g15g0.3g100ml |
1 | 2 | ||
含药小丸丙烯酸树脂NE30D柠檬酸三乙酯滑石粉水 | 150g20g3.5g5g150ml | 含药小丸丙烯酸树脂RS30D丙烯酸树脂RL30D柠檬酸三乙酯滑石粉水 | 150g15g1.5g3.8g11.3g135ml |
3 | 4 | ||
含药小丸乙基纤维素羟丙甲基纤维素0.1%邻苯二甲酸二乙酯75%乙醇 | 150g10g2g5g100ml | 含药小丸乙基纤维素水分散体滑石粉水 | 150g15g10g100ml |
时间(小时) | 处方1 | 处方2 | 处方3 | 处方4 |
1 | 4.7% | 3.2% | 8.7% | 7.4% |
2 | 8.6% | 5.4% | 15.4% | 20.5% |
4 | 33.6% | 30.5% | 40.6% | 46.7% |
8 | 65.4% | 57.9% | 70.1% | 67.5% |
12 | 85.4% | 70.8% | 75.6% | 75.9% |
16 | 90.7% | 85.6% | 83.2% | 80.4% |
24 | 95.4% | 94.3% | 91.5% | 92.8% |
Claims (7)
Priority Applications (1)
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CN 03129975 CN1228049C (zh) | 2003-06-03 | 2003-06-03 | 一种含吲达帕胺活性成分的缓释微丸及其制备方法 |
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CN 03129975 CN1228049C (zh) | 2003-06-03 | 2003-06-03 | 一种含吲达帕胺活性成分的缓释微丸及其制备方法 |
Publications (2)
Publication Number | Publication Date |
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CN1466945A CN1466945A (zh) | 2004-01-14 |
CN1228049C true CN1228049C (zh) | 2005-11-23 |
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CN (1) | CN1228049C (zh) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN105012275B (zh) * | 2015-08-20 | 2018-03-27 | 广东安诺药业股份有限公司 | 吲达帕胺缓释剂制备方法 |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN100396278C (zh) * | 2006-07-24 | 2008-06-25 | 冯莉萍 | 药用微丸丸芯及制备方法 |
CN102579407B (zh) * | 2012-03-30 | 2013-11-13 | 山西医科大学 | 一种吲达帕胺微球缓释胶囊制备方法 |
-
2003
- 2003-06-03 CN CN 03129975 patent/CN1228049C/zh not_active Expired - Lifetime
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN105012275B (zh) * | 2015-08-20 | 2018-03-27 | 广东安诺药业股份有限公司 | 吲达帕胺缓释剂制备方法 |
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Assignee: JIANGSU KANION PHARMACEUTICAL Co.,Ltd. Assignor: Tianjin Institute of Pharmaceutical Research Contract record no.: 2010320000502 Denomination of invention: Slow releasing micropill containing active component of indapamide and method for preparing the same Granted publication date: 20051123 License type: Exclusive License Open date: 20040114 Record date: 20100430 |
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Address after: 300193 Tianjin City, Nankai District Anshan West Road No. 308 Patentee after: Tianjin Institute of Pharmaceutical Research Co.,Ltd. Address before: 300193 Tianjin City, Nankai District Anshan West Road No. 308 Patentee before: Tianjin Institute of Pharmaceutical Research |
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