CN1608620A - 双环醇固体分散体 - Google Patents
双环醇固体分散体 Download PDFInfo
- Publication number
- CN1608620A CN1608620A CN 200310101890 CN200310101890A CN1608620A CN 1608620 A CN1608620 A CN 1608620A CN 200310101890 CN200310101890 CN 200310101890 CN 200310101890 A CN200310101890 A CN 200310101890A CN 1608620 A CN1608620 A CN 1608620A
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- Prior art keywords
- bicyclol
- solid dispersion
- pvp
- medicine
- physical mixture
- Prior art date
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- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 title abstract description 7
- 125000002619 bicyclic group Chemical group 0.000 title abstract 3
- 239000006185 dispersion Substances 0.000 title abstract 2
- 239000007787 solid Substances 0.000 title 1
- 239000007962 solid dispersion Substances 0.000 claims abstract description 124
- MTHSVFCYNBDYFN-UHFFFAOYSA-N diethylene glycol Chemical compound OCCOCCO MTHSVFCYNBDYFN-UHFFFAOYSA-N 0.000 claims abstract description 10
- 239000008118 PEG 6000 Substances 0.000 claims abstract description 6
- 229920002584 Polyethylene Glycol 6000 Polymers 0.000 claims abstract description 6
- KXMTXZACPVCDMH-UHFFFAOYSA-N methyl 4-[5-(hydroxymethyl)-7-methoxy-1,3-benzodioxol-4-yl]-7-methoxy-1,3-benzodioxole-5-carboxylate Chemical compound COC(=O)C1=CC(OC)=C2OCOC2=C1C1=C2OCOC2=C(OC)C=C1CO KXMTXZACPVCDMH-UHFFFAOYSA-N 0.000 claims description 186
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 26
- 229920001983 poloxamer Polymers 0.000 claims description 26
- 229960000502 poloxamer Drugs 0.000 claims description 26
- 239000000463 material Substances 0.000 claims description 21
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 9
- 229920002594 Polyethylene Glycol 8000 Polymers 0.000 claims description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims description 7
- KXGVEGMKQFWNSR-UHFFFAOYSA-N deoxycholic acid Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)C(O)C2 KXGVEGMKQFWNSR-UHFFFAOYSA-N 0.000 claims description 6
- 150000007524 organic acids Chemical class 0.000 claims description 6
- 229920001030 Polyethylene Glycol 4000 Polymers 0.000 claims description 4
- BHQCQFFYRZLCQQ-UHFFFAOYSA-N (3alpha,5alpha,7alpha,12alpha)-3,7,12-trihydroxy-cholan-24-oic acid Natural products OC1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)C(O)C2 BHQCQFFYRZLCQQ-UHFFFAOYSA-N 0.000 claims description 3
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 claims description 3
- 239000004380 Cholic acid Substances 0.000 claims description 3
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims description 3
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 claims description 3
- 239000002775 capsule Substances 0.000 claims description 3
- BHQCQFFYRZLCQQ-OELDTZBJSA-N cholic acid Chemical compound C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 BHQCQFFYRZLCQQ-OELDTZBJSA-N 0.000 claims description 3
- 235000019416 cholic acid Nutrition 0.000 claims description 3
- 229960002471 cholic acid Drugs 0.000 claims description 3
- 229960004106 citric acid Drugs 0.000 claims description 3
- 235000015165 citric acid Nutrition 0.000 claims description 3
- KXGVEGMKQFWNSR-LLQZFEROSA-N deoxycholic acid Chemical compound C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 KXGVEGMKQFWNSR-LLQZFEROSA-N 0.000 claims description 3
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- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical class O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 claims description 3
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- -1 polyethylene pyrrolidone Polymers 0.000 claims description 2
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- CTKXFMQHOOWWEB-UHFFFAOYSA-N Ethylene oxide/propylene oxide copolymer Chemical compound CCCOC(C)COCCO CTKXFMQHOOWWEB-UHFFFAOYSA-N 0.000 description 20
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- JMZOMFYRADAWOG-UHFFFAOYSA-N methyl 7-methoxy-4-(7-methoxy-5-methoxycarbonyl-1,3-benzodioxol-4-yl)-1,3-benzodioxole-5-carboxylate Chemical compound COC(=O)C1=CC(OC)=C2OCOC2=C1C1=C2OCOC2=C(OC)C=C1C(=O)OC JMZOMFYRADAWOG-UHFFFAOYSA-N 0.000 description 4
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- 239000008280 blood Substances 0.000 description 3
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- 239000012153 distilled water Substances 0.000 description 3
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- JTEGQNOMFQHVDC-NKWVEPMBSA-N lamivudine Chemical compound O=C1N=C(N)C=CN1[C@H]1O[C@@H](CO)SC1 JTEGQNOMFQHVDC-NKWVEPMBSA-N 0.000 description 3
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- LPLVUJXQOOQHMX-QWBHMCJMSA-N glycyrrhizinic acid Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@@H]1C([C@H]2[C@]([C@@H]3[C@@]([C@@]4(CC[C@@]5(C)CC[C@@](C)(C[C@H]5C4=CC3=O)C(O)=O)C)(C)CC2)(C)CC1)(C)C)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O LPLVUJXQOOQHMX-QWBHMCJMSA-N 0.000 description 1
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Images
Abstract
Description
试验号 | 1 | 2 | 3 | 4 |
药物:PVP | 1∶2 | 1∶4 | 1∶6 | 1∶8 |
药物投量 | 2g | 2g | 2g | 2g |
PVP投量 | 4g | 8g | 12g | 16 |
试验号 | 1 | 2 | 3 | 4 |
药物:PVP | 1∶2 | 1∶4 | 1∶6 | 1∶8 |
药物投量 | 2g | 2g | 2g | 2g |
PVP投量 | 4g | 8g | 12g | 16 |
试验号 | 1 | 2 | 3 | 4 |
药物∶PEG | 1∶4 | 1∶6 | 1∶8 | 1∶10 |
药物投量 | 2g | 2g | 2g | 2g |
PEG投量 | 8g | 12g | 16g | 20g |
试验号 | 1 | 2 | 3 | 4 |
药物∶PEG | 1∶4 | 1∶6 | 1∶8 | 1∶10 |
药物投量 | 2g | 2g | 2g | 2g |
PEG投量 | 8g | 12g | 16g | 20g |
试验号 | 1 | 2 | 3 | 4 |
药物∶Poloxemer188 | 1∶4 | 1∶6 | 1∶8 | 1∶10 |
药物投量 | 2g | 2g | 2g | 2g |
Poloxemer188投量 | 8g | 12g | 16g | 20g |
试验号 | 1 | 2 | 3 | 4 |
药物∶Poloxemer188 | 1∶4 | 1∶6 | 1∶8 | 1∶10 |
药物投量 | 2g | 2g | 2g | 2g |
Poloxemer188投量 | 8g | 12g | 16g | 20g |
样品 | 饱和溶液浓度25℃(μg/ml) | 样品 | 饱和溶液浓度25℃(μg/ml) |
双环醇原料(100目) | 28.72 | ||||
PVP物理混合物 | 1∶2 | 22.30 | PVP固体分散体 | 1∶2 | 452.8 |
1∶4 | 25.38 | 1∶4 | 432.5 | ||
1∶6 | 27.33 | 1∶6 | 462.8 | ||
1∶8 | 26.75 | 1∶8 | 478.9 | ||
PEG物理混合物 | 1∶4 | 26.31 | PEG固体分散体 | 1∶4 | 56.24 |
1∶6 | 27.49 | 1∶6 | 62.20 | ||
1∶8 | 27.83 | 1∶8 | 67.42 | ||
1∶10 | 29.25 | 1∶10 | 70.04 | ||
Poloxamer物理混合物 | 1∶4 | 28.13 | Poloxamer固体分散体 | 1∶4 | 58.34 |
1∶6 | 30.40 | 1∶6 | 65.64 | ||
1∶8 | 31.29 | 1∶8 | 64.70 | ||
1∶10 | 35.14 | 1∶10 | 64.73 |
Claims (8)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
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CNB2003101018907A CN100435791C (zh) | 2003-10-23 | 2003-10-23 | 双环醇固体分散体 |
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Application Number | Priority Date | Filing Date | Title |
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CNB2003101018907A CN100435791C (zh) | 2003-10-23 | 2003-10-23 | 双环醇固体分散体 |
Publications (2)
Publication Number | Publication Date |
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CN1608620A true CN1608620A (zh) | 2005-04-27 |
CN100435791C CN100435791C (zh) | 2008-11-26 |
Family
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Application Number | Title | Priority Date | Filing Date |
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CNB2003101018907A Expired - Lifetime CN100435791C (zh) | 2003-10-23 | 2003-10-23 | 双环醇固体分散体 |
Country Status (1)
Country | Link |
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CN (1) | CN100435791C (zh) |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2006015546A1 (fr) * | 2004-08-11 | 2006-02-16 | Institute Of Mataria Medica, Chinese Academy Of Medical Sciences | Utilisation de bicyclol pour produire un medicament capable de prevenir et/ou traiter l’alcoolisme aigu et une lesion d’intestin d’alcoolisme aigu ou chronique |
CN102091052B (zh) * | 2009-12-15 | 2012-11-07 | 北京协和药厂 | 双环醇双层渗透泵控释片剂及其制备方法 |
CN101524349B (zh) * | 2007-09-20 | 2014-01-15 | 中国医学科学院药物研究所 | 双环醇的磷脂复合物及其制备方法 |
CN114073680A (zh) * | 2020-08-13 | 2022-02-22 | 北京协和药厂 | 一种双环醇干混悬剂 |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
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US4868207A (en) * | 1988-07-28 | 1989-09-19 | Taisho Pharmaceutical Co., Ltd. | Bis (methylenedioxy) biphenyl compounds useful for the treatment of liver diseases |
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2003
- 2003-10-23 CN CNB2003101018907A patent/CN100435791C/zh not_active Expired - Lifetime
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2006015546A1 (fr) * | 2004-08-11 | 2006-02-16 | Institute Of Mataria Medica, Chinese Academy Of Medical Sciences | Utilisation de bicyclol pour produire un medicament capable de prevenir et/ou traiter l’alcoolisme aigu et une lesion d’intestin d’alcoolisme aigu ou chronique |
CN101524349B (zh) * | 2007-09-20 | 2014-01-15 | 中国医学科学院药物研究所 | 双环醇的磷脂复合物及其制备方法 |
CN102091052B (zh) * | 2009-12-15 | 2012-11-07 | 北京协和药厂 | 双环醇双层渗透泵控释片剂及其制备方法 |
CN114073680A (zh) * | 2020-08-13 | 2022-02-22 | 北京协和药厂 | 一种双环醇干混悬剂 |
CN114073680B (zh) * | 2020-08-13 | 2023-08-15 | 北京协和药厂 | 一种双环醇干混悬剂 |
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