FR2518880A1 - Compositions therapeutiques a activite choleretique, contenant a titre de principe actif, des derives de l'acide cholanique - Google Patents
Compositions therapeutiques a activite choleretique, contenant a titre de principe actif, des derives de l'acide cholanique Download PDFInfo
- Publication number
- FR2518880A1 FR2518880A1 FR8217523A FR8217523A FR2518880A1 FR 2518880 A1 FR2518880 A1 FR 2518880A1 FR 8217523 A FR8217523 A FR 8217523A FR 8217523 A FR8217523 A FR 8217523A FR 2518880 A1 FR2518880 A1 FR 2518880A1
- Authority
- FR
- France
- Prior art keywords
- active ingredient
- therapeutic compositions
- activity
- acid
- iii
- 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.)
- Granted
Links
- 239000004480 active ingredient Substances 0.000 title claims abstract description 10
- 239000000203 mixture Substances 0.000 title claims abstract description 8
- 230000001225 therapeutic effect Effects 0.000 title claims description 7
- 230000000694 effects Effects 0.000 title description 3
- 150000001830 cholanoic acids Chemical class 0.000 title 1
- 230000001989 choleretic effect Effects 0.000 claims abstract description 8
- 150000001875 compounds Chemical class 0.000 claims description 10
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 4
- 229940127557 pharmaceutical product Drugs 0.000 claims description 3
- 230000000295 complement effect Effects 0.000 claims 1
- RUDATBOHQWOJDD-UHFFFAOYSA-N (3beta,5beta,7alpha)-3,7-Dihydroxycholan-24-oic acid Natural products OC1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)CC2 RUDATBOHQWOJDD-UHFFFAOYSA-N 0.000 abstract description 14
- RUDATBOHQWOJDD-UZVSRGJWSA-N ursodeoxycholic 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)CC1 RUDATBOHQWOJDD-UZVSRGJWSA-N 0.000 abstract description 14
- 229960001661 ursodiol Drugs 0.000 abstract description 13
- 239000000047 product Substances 0.000 description 11
- 210000000941 bile Anatomy 0.000 description 10
- 239000002775 capsule Substances 0.000 description 8
- RPKLZQLYODPWTM-KBMWBBLPSA-N cholanoic acid Chemical compound C1CC2CCCC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@@H](CCC(O)=O)C)[C@@]1(C)CC2 RPKLZQLYODPWTM-KBMWBBLPSA-N 0.000 description 7
- 229920000084 Gum arabic Polymers 0.000 description 6
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 6
- 229920002472 Starch Polymers 0.000 description 6
- 235000010489 acacia gum Nutrition 0.000 description 6
- 239000000205 acacia gum Substances 0.000 description 6
- 239000011777 magnesium Substances 0.000 description 6
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 6
- 239000000546 pharmaceutical excipient Substances 0.000 description 6
- 239000008107 starch Substances 0.000 description 6
- 235000019698 starch Nutrition 0.000 description 6
- 241000700159 Rattus Species 0.000 description 5
- 241001465754 Metazoa Species 0.000 description 4
- 239000002253 acid Substances 0.000 description 4
- 244000171897 Acacia nilotica subsp nilotica Species 0.000 description 3
- 241000978776 Senegalia senegal Species 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 239000000377 silicon dioxide Substances 0.000 description 3
- 239000000725 suspension Substances 0.000 description 3
- 239000000454 talc Substances 0.000 description 3
- 229910052623 talc Inorganic materials 0.000 description 3
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
- 150000007513 acids Chemical class 0.000 description 2
- 231100000460 acute oral toxicity Toxicity 0.000 description 2
- 239000003613 bile acid Substances 0.000 description 2
- 239000003833 bile salt Substances 0.000 description 2
- 230000008859 change Effects 0.000 description 2
- 239000000731 choleretic agent Substances 0.000 description 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000008101 lactose Substances 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- 231100000419 toxicity Toxicity 0.000 description 2
- 230000001988 toxicity Effects 0.000 description 2
- 238000005303 weighing Methods 0.000 description 2
- HTSGKJQDMSTCGS-UHFFFAOYSA-N 1,4-bis(4-chlorophenyl)-2-(4-methylphenyl)sulfonylbutane-1,4-dione Chemical compound C1=CC(C)=CC=C1S(=O)(=O)C(C(=O)C=1C=CC(Cl)=CC=1)CC(=O)C1=CC=C(Cl)C=C1 HTSGKJQDMSTCGS-UHFFFAOYSA-N 0.000 description 1
- GIYAQDDTCWHPPL-UHFFFAOYSA-N 4-amino-5-bromo-N-[2-(diethylamino)ethyl]-2-methoxybenzamide Chemical compound CCN(CC)CCNC(=O)C1=CC(Br)=C(N)C=C1OC GIYAQDDTCWHPPL-UHFFFAOYSA-N 0.000 description 1
- 102000013142 Amylases Human genes 0.000 description 1
- 108010065511 Amylases Proteins 0.000 description 1
- 0 C1C=*2*1*CC2 Chemical compound C1C=*2*1*CC2 0.000 description 1
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical class [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 1
- 108090000317 Chymotrypsin Proteins 0.000 description 1
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 description 1
- 102000004882 Lipase Human genes 0.000 description 1
- 108090001060 Lipase Proteins 0.000 description 1
- 239000004367 Lipase Substances 0.000 description 1
- 102000057297 Pepsin A Human genes 0.000 description 1
- 108090000284 Pepsin A Proteins 0.000 description 1
- 241000212342 Sium Species 0.000 description 1
- YTGJWQPHMWSCST-UHFFFAOYSA-N Tiopronin Chemical compound CC(S)C(=O)NCC(O)=O YTGJWQPHMWSCST-UHFFFAOYSA-N 0.000 description 1
- 108010058907 Tiopronin Proteins 0.000 description 1
- WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 description 1
- 235000019418 amylase Nutrition 0.000 description 1
- 229940025131 amylases Drugs 0.000 description 1
- 229940069428 antacid Drugs 0.000 description 1
- 239000003159 antacid agent Substances 0.000 description 1
- 230000001458 anti-acid effect Effects 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 229940093761 bile salts Drugs 0.000 description 1
- 229960001034 bromopride Drugs 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- RUDATBOHQWOJDD-BSWAIDMHSA-N chenodeoxycholic 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)CC1 RUDATBOHQWOJDD-BSWAIDMHSA-N 0.000 description 1
- 229960001091 chenodeoxycholic acid Drugs 0.000 description 1
- 235000012000 cholesterol Nutrition 0.000 description 1
- 229960002376 chymotrypsin Drugs 0.000 description 1
- 210000001953 common bile duct Anatomy 0.000 description 1
- 230000029087 digestion Effects 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 230000002183 duodenal effect Effects 0.000 description 1
- NLFBCYMMUAKCPC-KQQUZDAGSA-N ethyl (e)-3-[3-amino-2-cyano-1-[(e)-3-ethoxy-3-oxoprop-1-enyl]sulfanyl-3-oxoprop-1-enyl]sulfanylprop-2-enoate Chemical compound CCOC(=O)\C=C\SC(=C(C#N)C(N)=O)S\C=C\C(=O)OCC NLFBCYMMUAKCPC-KQQUZDAGSA-N 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 239000013067 intermediate product Substances 0.000 description 1
- 230000008991 intestinal motility Effects 0.000 description 1
- 229940080428 lactose 200 mg Drugs 0.000 description 1
- 239000008141 laxative Substances 0.000 description 1
- 229940125722 laxative agent Drugs 0.000 description 1
- 235000019421 lipase Nutrition 0.000 description 1
- 239000000395 magnesium oxide Substances 0.000 description 1
- CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 description 1
- AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 229930182817 methionine Natural products 0.000 description 1
- 229960004503 metoclopramide Drugs 0.000 description 1
- TTWJBBZEZQICBI-UHFFFAOYSA-N metoclopramide Chemical compound CCN(CC)CCNC(=O)C1=CC(Cl)=C(N)C=C1OC TTWJBBZEZQICBI-UHFFFAOYSA-N 0.000 description 1
- 230000007170 pathology Effects 0.000 description 1
- 229940111202 pepsin Drugs 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- GOZDTZWAMGHLDY-UHFFFAOYSA-L sodium picosulfate Chemical compound [Na+].[Na+].C1=CC(OS(=O)(=O)[O-])=CC=C1C(C=1N=CC=CC=1)C1=CC=C(OS([O-])(=O)=O)C=C1 GOZDTZWAMGHLDY-UHFFFAOYSA-L 0.000 description 1
- 229960005077 sodium picosulfate Drugs 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 238000011287 therapeutic dose Methods 0.000 description 1
- 229960004402 tiopronin Drugs 0.000 description 1
- -1 tryp sine Proteins 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT25874/81A IT1142639B (it) | 1981-12-29 | 1981-12-29 | Composizioni terapeutiche ad attivita' coleretica contenenti come principio attivo derivati dall'acido colanico |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| FR2518880A1 true FR2518880A1 (fr) | 1983-07-01 |
| FR2518880B1 FR2518880B1 (https=) | 1985-04-19 |
Family
ID=11217997
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FR8217523A Granted FR2518880A1 (fr) | 1981-12-29 | 1982-10-20 | Compositions therapeutiques a activite choleretique, contenant a titre de principe actif, des derives de l'acide cholanique |
Country Status (4)
| Country | Link |
|---|---|
| JP (1) | JPS58118514A (https=) |
| DE (1) | DE3239444A1 (https=) |
| FR (1) | FR2518880A1 (https=) |
| IT (1) | IT1142639B (https=) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0273469A1 (en) * | 1986-11-28 | 1988-07-06 | Gipharmex S.p.A. | Oral pharmaceutical compositions with sustained release |
| EP0571338A1 (en) * | 1992-05-18 | 1993-11-24 | EUDERMA S.r.l. | Pharmaceutical oral controlled release composition comprising small pellets of bile acids |
-
1981
- 1981-12-29 IT IT25874/81A patent/IT1142639B/it active
-
1982
- 1982-10-20 FR FR8217523A patent/FR2518880A1/fr active Granted
- 1982-10-25 DE DE19823239444 patent/DE3239444A1/de not_active Withdrawn
- 1982-12-02 JP JP57210673A patent/JPS58118514A/ja active Pending
Non-Patent Citations (1)
| Title |
|---|
| CHEMICAL ABSTRACTS, vol. 53, no. 3, 10 février 1959, colonnes 2415-2416, résumé 2416a-e, COLUMBUS, OHIO (US), * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0273469A1 (en) * | 1986-11-28 | 1988-07-06 | Gipharmex S.p.A. | Oral pharmaceutical compositions with sustained release |
| EP0571338A1 (en) * | 1992-05-18 | 1993-11-24 | EUDERMA S.r.l. | Pharmaceutical oral controlled release composition comprising small pellets of bile acids |
| US5422124A (en) * | 1992-05-18 | 1995-06-06 | Euderma S.R.L. | Pharmaceutical oral controlled release composition comprising small pellets of bile acids |
Also Published As
| Publication number | Publication date |
|---|---|
| FR2518880B1 (https=) | 1985-04-19 |
| DE3239444A1 (de) | 1983-07-07 |
| IT8125874A0 (it) | 1981-12-29 |
| IT1142639B (it) | 1986-10-08 |
| JPS58118514A (ja) | 1983-07-14 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| ST | Notification of lapse |