JPS56127338A - Basic amino acid salt of diclofenac and suppository containing the same - Google Patents
Basic amino acid salt of diclofenac and suppository containing the sameInfo
- Publication number
- JPS56127338A JPS56127338A JP3108080A JP3108080A JPS56127338A JP S56127338 A JPS56127338 A JP S56127338A JP 3108080 A JP3108080 A JP 3108080A JP 3108080 A JP3108080 A JP 3108080A JP S56127338 A JPS56127338 A JP S56127338A
- Authority
- JP
- Japan
- Prior art keywords
- diclofenac
- salt
- amino acid
- formula
- lysine
- 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
- DCOPUUMXTXDBNB-UHFFFAOYSA-N diclofenac Chemical compound OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl DCOPUUMXTXDBNB-UHFFFAOYSA-N 0.000 title abstract 6
- 229960001259 diclofenac Drugs 0.000 title abstract 5
- -1 amino acid salt Chemical class 0.000 title abstract 2
- 239000000829 suppository Substances 0.000 title abstract 2
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 abstract 3
- 239000004475 Arginine Substances 0.000 abstract 2
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 abstract 2
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 abstract 2
- 239000004472 Lysine Substances 0.000 abstract 2
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 abstract 2
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 abstract 2
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 abstract 1
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 abstract 1
- 150000001413 amino acids Chemical class 0.000 abstract 1
- 230000000202 analgesic effect Effects 0.000 abstract 1
- 239000000730 antalgic agent Substances 0.000 abstract 1
- 239000002260 anti-inflammatory agent Substances 0.000 abstract 1
- 230000001741 anti-phlogistic effect Effects 0.000 abstract 1
- 239000002221 antipyretic Substances 0.000 abstract 1
- 229940125716 antipyretic agent Drugs 0.000 abstract 1
- 239000008280 blood Substances 0.000 abstract 1
- 210000004369 blood Anatomy 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000000463 material Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 210000004400 mucous membrane Anatomy 0.000 abstract 1
- 210000000664 rectum Anatomy 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- RPACBEVZENYWOL-XFULWGLBSA-M sodium;(2r)-2-[6-(4-chlorophenoxy)hexyl]oxirane-2-carboxylate Chemical compound [Na+].C=1C=C(Cl)C=CC=1OCCCCCC[C@]1(C(=O)[O-])CO1 RPACBEVZENYWOL-XFULWGLBSA-M 0.000 abstract 1
- 230000000638 stimulation Effects 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
Abstract
NEW MATERIAL:Basic amino acid salt of 2-(2,6-dichloroanilino)phenylacetic acid (general name: Diclofenac).
EXAMPLE: Diclofenac 1-lysine salt.
USE: Antiphlogistic, analgesic and antipyretic agent for rectal administration. It can be absorbed rapidly through rectum, gives high concentration in blood, and also gives extremely low stimulation to mucous membranes. The distinctive character of this compound is that the side effects such as gastroenteric disorder of the Diclofenac Na salt for oral administation are improved by converting to a suppository preparation.
PROCESS: The reaction of Diclofenac with a basis amino acid, e.g. lysine, arginine, histidine etc., in water-containing methanol gives a salt of formula I (Y is a group of formula II and n is 4 when lysine is used; Y is a group of formula III and n is 3 when arginine is used; Y is a group of formula IV and n is 1 when histidine is used).
COPYRIGHT: (C)1981,JPO&Japio
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP3108080A JPS56127338A (en) | 1980-03-10 | 1980-03-10 | Basic amino acid salt of diclofenac and suppository containing the same |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP3108080A JPS56127338A (en) | 1980-03-10 | 1980-03-10 | Basic amino acid salt of diclofenac and suppository containing the same |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS56127338A true JPS56127338A (en) | 1981-10-06 |
| JPH0223527B2 JPH0223527B2 (en) | 1990-05-24 |
Family
ID=12321441
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP3108080A Granted JPS56127338A (en) | 1980-03-10 | 1980-03-10 | Basic amino acid salt of diclofenac and suppository containing the same |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS56127338A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS56138115A (en) * | 1980-03-31 | 1981-10-28 | Teijin Ltd | Suppository containing acidic amino acid or derivative thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5089517A (en) * | 1973-12-18 | 1975-07-18 | ||
| JPS50126818A (en) * | 1974-03-07 | 1975-10-06 | ||
| JPS54109942A (en) * | 1978-02-13 | 1979-08-29 | Mitsui Toatsu Chem Inc | Preparation of phenylacetic acid derivative |
-
1980
- 1980-03-10 JP JP3108080A patent/JPS56127338A/en active Granted
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5089517A (en) * | 1973-12-18 | 1975-07-18 | ||
| JPS50126818A (en) * | 1974-03-07 | 1975-10-06 | ||
| JPS54109942A (en) * | 1978-02-13 | 1979-08-29 | Mitsui Toatsu Chem Inc | Preparation of phenylacetic acid derivative |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS56138115A (en) * | 1980-03-31 | 1981-10-28 | Teijin Ltd | Suppository containing acidic amino acid or derivative thereof |
| JPH0242809B2 (en) * | 1980-03-31 | 1990-09-26 |
Also Published As
| Publication number | Publication date |
|---|---|
| JPH0223527B2 (en) | 1990-05-24 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ATE195417T1 (en) | PHARMACEUTICAL COMPOSITION CONTAINING IBUPROFEN SALT | |
| ES8306321A1 (en) | Cream preparation. | |
| JPS55147236A (en) | Optical resolution of ( )-mandelic acid | |
| JPS56127338A (en) | Basic amino acid salt of diclofenac and suppository containing the same | |
| JPS5312835A (en) | Preparation of 2-(3-phenoxyphenyl) propionic acid | |
| JPS52131551A (en) | Synthesis of alpha-phenylpropionic acid derivatives | |
| JPS5665816A (en) | Acetylsalicylate pharmaceutical for injection | |
| JPS5646838A (en) | 2- 2-fluoro-4-biphenylyl propionic acid-cyclodextrin clathrate compound | |
| JPS5668672A (en) | Novel 2-acetoxybenzamide derviative, its preparation, and pharmaceutical containing said derviative as effective component | |
| JPS56147761A (en) | Salt compound consisting of acetylsalicylic acid and diguanidine, its preparation and agent containing the same as active constitutent | |
| SE8204792D0 (en) | N-METHYL-D-GLUCAMINE SALT OF 3,4-DIHYDRO-5-METHYL-6- (2-METHYL-PROPYL) -4-OXOTIENO (2,3-D) PYRIMIDIN-2-CARBOXYLIC ACID AND PHARMACEUTICAL COMPOSITION CONTAINING THIS SALT | |
| FR2322544A1 (en) | RELEASE OF ETHYLENE IN PLANTS BY AN IMPROVED MIXTURE CONTAINING 2-CHLORO-ETHYLPHOSPHONIC ACID | |
| JPS5257129A (en) | Process for hydroquinone | |
| ATE35536T1 (en) | CYSTEINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM. | |
| JPS5528953A (en) | Racemization of optically active alpha-substituted arylacetic acid | |
| JPS56150034A (en) | Preparation of 3,4,5-trimethoxybenzaldehyde | |
| JPS5484522A (en) | Racemization of optically active amino acid ester | |
| JPS5223058A (en) | Preparation of indanylpropionic acid derivatives | |
| JPS5340734A (en) | Preparation of phenylacetic acid derivatives | |
| JPS5246037A (en) | Process for preparation of 2-(p-isobutylphenyl)propionic acid | |
| JPS5271439A (en) | Synthesis of phenylacetic acid derivatives | |
| GR3015937T3 (en) | Salts of the 2-(2,6-dichloroanilino)-phenylacetic acid, process for their preparation and their application as pharmaceutical preparations for topical use. | |
| JPS52100438A (en) | Preparation of alpha-phenylcarboxylic acids | |
| JPS5495734A (en) | Antiphlogistic analgesic agent | |
| JPS5515458A (en) | Hypotensive agent |