CN1899276A - 大黄酸或大黄酸类化合物的复合物、其制备方法及其在制备预防肠粘连药物中的应用 - Google Patents
大黄酸或大黄酸类化合物的复合物、其制备方法及其在制备预防肠粘连药物中的应用 Download PDFInfo
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- CN1899276A CN1899276A CN 200610106515 CN200610106515A CN1899276A CN 1899276 A CN1899276 A CN 1899276A CN 200610106515 CN200610106515 CN 200610106515 CN 200610106515 A CN200610106515 A CN 200610106515A CN 1899276 A CN1899276 A CN 1899276A
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- 229910052749 magnesium Inorganic materials 0.000 description 1
- 239000011777 magnesium Substances 0.000 description 1
- 159000000003 magnesium salts Chemical class 0.000 description 1
- 239000002398 materia medica Substances 0.000 description 1
- 235000013372 meat Nutrition 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 229910000474 mercury oxide Inorganic materials 0.000 description 1
- UKWHYYKOEPRTIC-UHFFFAOYSA-N mercury(ii) oxide Chemical compound [Hg]=O UKWHYYKOEPRTIC-UHFFFAOYSA-N 0.000 description 1
- 229910021645 metal ion Inorganic materials 0.000 description 1
- 239000003094 microcapsule Substances 0.000 description 1
- 235000010755 mineral Nutrition 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 1
- TZBAVQKIEKDGFH-UHFFFAOYSA-N n-[2-(diethylamino)ethyl]-1-benzothiophene-2-carboxamide;hydrochloride Chemical compound [Cl-].C1=CC=C2SC(C(=O)NCC[NH+](CC)CC)=CC2=C1 TZBAVQKIEKDGFH-UHFFFAOYSA-N 0.000 description 1
- 230000017074 necrotic cell death Effects 0.000 description 1
- 229960002362 neostigmine Drugs 0.000 description 1
- LULNWZDBKTWDGK-UHFFFAOYSA-M neostigmine bromide Chemical compound [Br-].CN(C)C(=O)OC1=CC=CC([N+](C)(C)C)=C1 LULNWZDBKTWDGK-UHFFFAOYSA-M 0.000 description 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
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- 150000007530 organic bases Chemical group 0.000 description 1
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- 239000007800 oxidant agent Substances 0.000 description 1
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- PKUBGLYEOAJPEG-UHFFFAOYSA-N physcion Natural products C1=C(C)C=C2C(=O)C3=CC(C)=CC(O)=C3C(=O)C2=C1O PKUBGLYEOAJPEG-UHFFFAOYSA-N 0.000 description 1
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Images
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
元素 | C(%) | H(%) | N(%) | S(%) |
理论值 | 55.021 | 4.837 | 12.222 | 0.000 |
测定值 | 55.28 | 4.873 | 12.04 | 0.000 |
55.20 | 4.885 | 12.05 | 0.000 |
碳原子序号 | 化学位移(δ) | 碳原子序号 | 化学位移(δ) | 碳原子序号 | 化学位移(δ) |
4′ | 25.46(24.9) | 8 | 121.56(119.32) | 7′ | 158.28(157.5) |
3′ | 28.99(28.5) | 3 | 125.81(124.00) | 4 | 162.38(161.06) |
5′ | 42.02(41.5) | 6 | 126.26(124.40) | 5 | 162.45(161.43) |
2′ | 55.80(55.1) | 8a | 134.01(132.98) | 2-COOH | 172.02(165.06) |
10a | 116.74(115.83) | 9a | 134.13(133.50) | 1′ | 174.87(175.2) |
4a | 117.61(118.23) | 7 | 139.08(137.40) | 9 | 183.79(180.47) |
1 | 121.50(118.75) | 2 | 147.37(138.18) |
序号 | R1 | R2 | R3 | R4 | R5 | R6 | R7 | R8 |
1 | OH | COOH | OH | |||||
2 | OCH3 | OH | COOH | |||||
3 | OH | OH | COOH | OH | ||||
4 | COOH | OH | OH | OH | ||||
5 | COOH | OH | OH | OH | ||||
6 | COOH | OH | OH | OCH3 | ||||
7 | OCH3 | OH | COOH | OCH3 | OCH3 | OH | ||
8 | OCH3 | OH | COOH | OCH3 | OCH3 | OCH3 | ||
9 | OCH3 | OH | COOH | OH | OCH3 | OH | ||
10 | OCH3 | OH | COOH | OH | ||||
11 | OH | COOH | OH | OCH3 | OH | |||
12 | OH | COOH | OH | OH | OH | |||
13 | OCH3 | COOH | OH | |||||
14 | OCH3 | COOH | OH | |||||
15 | OH | OH | COOH | |||||
16 | OH | COOH | OH | |||||
17 | OH | OH | COOH | OH | ||||
18 | OH | COOH | OCH3 | OH | ||||
19 | OH | COOH | CH3 | OH | OH | |||
20 | OH | COOH | OH | OH | ||||
21 | OH | COOH | OH | OH | COOH | OH | ||
22 | OH | COOH | OH | OH | ||||
23 | OH | COOH | OH | OCH3 | OH | |||
24 | OH | COOH | OH | OH | OH | |||
25 | OH | OH | COOH | |||||
26 | OH | COOH | ||||||
27 | OH | COOH | OH | |||||
38 | OH | COOH | OH | OH | ||||
29 | OH | COOH | OH | OH | ||||
30 | OH | OCH3 | OH | COOH | ||||
31 | OH | COOH | OH | OH | ||||
32 | COOH | |||||||
33 | OH | COOH | OH | OCH3 | OH |
34 | OH | COOH | OH | |||||
35 | OH | COOH | OH | |||||
36 | OH | OH | OH | COOH | OH | |||
37 | OH | OH | COOH | OH | ||||
38 | OH | COOH | OH | OH | OH | |||
39 | OH | OH | OCH3 | COOH | OH | |||
40 | OH | OCH3 | COOH | OH | ||||
41 | OH | OH | COOH | OCH3 | OH | |||
42 | OH | COOH | OH | OCH3 | OH | OH | ||
43 | OH | COOH | OH | OH | OCH3 | |||
44 | OH | COOH | ||||||
45 | OH | COOH | OH | OCH3 | OCH3 |
化合物 | 浓度 | pH值 | 澄清度 | 说明 |
大黄酸钠盐 | 2.0mg/ml | 9-10 | 澄清 | 制剂pH值偏高,药学上不接受 |
大黄酸钠盐 | 2.0mg/ml | 6-7 | 不澄清 | 制剂不澄清,药学上不接受 |
大黄酸钾盐 | 2.0mg/ml | 9-10 | 澄清 | 制剂pH值偏高,药学上不接受 |
大黄酸钾盐 | 2.0mg/ml | 6-7 | 不澄清 | 制剂不澄清,药学上不接受 |
大黄酸精氨酸复合物 | 2.0mg/ml | 6-7 | 澄清 | pH值、澄清度符合药学上的要求 |
大黄酸赖氨酸复合物 | 2.0mg/ml | 6-7 | 澄清 | pH值、澄清度符合药学上的要求 |
大黄酸氨基葡萄糖复合物 | 2.0mg/ml | 6-7 | 澄清 | pH值、澄清度符合药学上的要求 |
大黄酸葡甲胺复合物 | 2.0mg/ml | 6-7 | 澄清 | pH值、澄清度符合药学上的要求 |
大黄酸肉毒碱复合物 | 2.0mg/ml | 6-7 | 澄清 | pH值、澄清度符合药学上的要求 |
大黄酸川芎嗪复合物 | 2.0mg/ml | 6-7 | 澄清 | pH值、澄清度符合药学上的要求 |
含大黄酸50%有效部位钠盐 | 2.0mg/ml | 9-11 | 澄清 | 制剂pH值偏高,药学上不接受 |
含大黄酸50%有效部位钠盐 | 2.0mg/ml | 6-7 | 不澄清 | 制剂不澄清,药学上不接受 |
含大黄酸50%有效部位钾盐 | 2.0mg/ml | 9-11 | 澄清 | 制剂pH值偏高,药学上不接受 |
含大黄酸50%有效部位钾盐 | 2.0mg/ml | 6-7 | 不澄清 | 制剂不澄清,药学上不接受 |
含大黄酸50%有效部位精氨酸复合物 | 2.0mg/ml | 6-7 | 澄清 | pH值、澄清度符合药学上的要求 |
含大黄酸50%有效部位赖氨酸复合物 | 2.0mg/ml | 6-7 | 澄清 | pH值、澄清度符合药学上的要求 |
含大黄酸50%有效部位氨基葡萄糖复合物 | 2.0mg/ml | 6-7 | 澄清 | pH值、澄清度符合药学上的要求 |
含大黄酸50%有效部位葡甲胺复合物 | 2.0mg/ml | 6-7 | 澄清 | pH值、澄清度符合药学上的要求 |
组别 | 剂量(mg/kg) | 吸光值 |
模型对照组氢化可的松大黄酸精氨酸大剂量组大黄酸精氨酸小剂量组大黄酸钠组 | -40241212 | 0.606±0.1510.312±0.097**0.455±0.105**0.476±0.096*0.494±0.134* |
组别 | 剂量(mg/kg) | 肉牙净重(mg) |
模型对照组消炎痛组大黄酸精氨酸大剂量组大黄酸精氨酸小剂量组大黄酸钠组 | -10241212 | 19.20±3.5212.21±2.43**13.64±2.47**15.23±3.60**15.87±3.31** |
组别 | 剂量(mg/kg) | 推进率(%) |
模型对照组吗丁林对照组大黄酸精氨酸大剂量组大黄酸精氨酸小剂量组大黄酸钠组 | -9241212 | 45.63±10.155.42±9.6**66.47±9.7**53.81±8.9**51.69±7.1** |
等级 | 等级粘连状况 |
0IIIIIIIV | 完全无粘连内脏间或内脏与腹壁间1条粘连带内脏间或内脏与腹壁间2条粘连带多于2条粘连带而内脏未直接粘连至腹壁内脏直接粘连到腹壁,不管粘连带多少 |
组别 | 剂量(mg/kg) | 粘连程度分级 | ||||
0 | I | II | III | IV | ||
模型对照组地塞米松组大黄酸精氨酸大剂量组大黄酸精氨酸小剂量组大黄酸钠组 | 101266 | 01311 | 02544 | 28232 | 71233 | 30012 |
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