CN104706582A - Mesalazine-containing drug composition - Google Patents
Mesalazine-containing drug composition Download PDFInfo
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- CN104706582A CN104706582A CN201310682696.6A CN201310682696A CN104706582A CN 104706582 A CN104706582 A CN 104706582A CN 201310682696 A CN201310682696 A CN 201310682696A CN 104706582 A CN104706582 A CN 104706582A
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Abstract
The present invention provides a mesalazine-containing drug composition, wherein per 60 g of the composition comprises 4 g of mesalazine, 0.04-0.1 g of a metal chelating agent, 0.1-0.5 g of an antioxidant, 0.01-0.2 g of a preservative, 0.1-0.4 g of an auxiliary suspending agent, 0.1-0.4 g of a pH value adjusting agent, and the balance of water. The enema liquid has good stability.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, relating to a kind of is the compositions of active component containing mesalazine, particularly a kind of pharmaceutical composition containing mesalazine.
Background technology
Mesalazine is a kind of common medicine for the treatment of inflamed colon inflammation, due to the therapeutic efficiency that it is excellent, worldwide be widely used, but owing to having hydroxyl and the active reactive group of carboxyl three in its structure, multiple reaction can be carried out, be easy to oxidized in process of production, lost efficacy, thus affect therapeutic effect, therefore must pass through temperature, the control of humidity, reduce the generation of chemical reaction, the content of protection effective ingredient, reduce the generation of related substance, the generation of above-mentioned chemical reaction, be mainly reflected in the change of mesalazine color, in the solution, if there is the generation of chemical reaction, the color of mesalazine solution becomes purple by the most initial milky gradually to light brown solution, finally become black, therefore, the existing preparation containing mesalazine is mostly solid preparation, be conducive to the stable of mesalazine like this, not easily variable color is gone bad, but, mesalazine Main Function position is at colon, solid preparation first will could arrive colon by gastrointestinal tract, delay the onset of action time.
Publication number be CN101721385B patent discloses a kind of mesalazine oral colon-target sustained release pharmaceutical composition, said composition comprises: slow release label a) containing mesalazine or its pharmaceutical salts or its solvate and hydrophilic matrix, and wherein mesalazine or its pharmaceutical salts are scattered in hydrophilic matrix; B) coating of acid resisting material is contained at the outside bag one deck of label; C) release in 1 hour in the simulated intestinal fluid of pH7.2 of described compositions is less than 20%, and 4 hours release 30-60%, release in 8 hours is greater than 70%.Said composition manufacturing process is simple, cost is low, at small intestinal and colon slow releasing mesalazine, reaches once-a-day colon targeting drug administration and topical therapeutic effect.
Publication number be 102784154A patent discloses a kind of Mesalazine enteric-coated tablet preparation method, this preparation method adopts nanotechnology, enteric technology and compaction of pellet technology, decrease burst size in Mesalazine enteric-coated tablet acid, add burst size in buffer, improve curative effect, extend keeping life, ensure that product quality, achieve promising result.
Publication number is that patent discloses of CN1355694 is a kind of containing the controlled release oral pharmaceutical compositions of 5-aminosalicylic acid as active component, comprise: a) inner lipotropy substrate, be made up of the material of fusing point lower than 90 DEG C, be wherein inclusive with active component at least partly; B) external hydrophilic substrate, is wherein dispersed with lipotropy substrate; C) optional other excipient.
Applicant, at a kind of pharmaceutical composition containing mesalazine of exploitation, particularly during fluid composition, has found the special formulation played a crucial role to the pharmaceutical composition quality stability of mesalazine unexpectedly.
Summary of the invention
The invention provides a kind of pharmaceutical composition containing mesalazine, in every 60g compositions, consist of the following composition: mesalazine 4g, metal-chelator 0.04g ~ 0.1g, antioxidant 0.1g ~ 0.5g, antiseptic 0.01g ~ 0.2g, suspending agent 0.1g ~ 0.4g, PH regulator 0.1g ~ 0.4g, surplus are water.
One or more preferably in disodium edetate, calcium disodium edetate of described metal-chelator, one or more preferably in sodium sulfite, sodium sulfite, sodium pyrosulfite, potassium metabisulfite, vitamin C of described antioxidant, one or more preferably in sodium benzoate, benzoic acid of described antiseptic, one or more preferably in xanthan gum, hypromellose, carbomer of described suspending agent, one or more preferably in sodium acetate, potassium acetate of described PH regulator, this pharmaceutical composition steady quality, it is substantially unchanged that room temperature places 2 years colors.
Described suspending agent is particularly preferably xanthan gum, carbomer, the two coupling suspending is effective, the particle size range of described pharmaceutical composition more than 90% granule is preferably 8 microns ~ 15 microns, this suspension redispersibility is good, room temperature places 3 years, and redispersibility basis is unchanged, and namely jog can be uniformly dispersed, do not lump, can constant product quality be ensured; Described pharmaceutical composition pH value ranges preferably from 3.5 ~ 5.5, is particularly preferably 4.6 ~ 4.8, and it is substantially unchanged that said composition room temperature places 3 years colors, character and outward appearance consistent with 0 day, show that quality is very stable; Aforementioned pharmaceutical compositions dosage form is preferably enema.
Detailed description of the invention
Below in conjunction with specific embodiment, the present invention is further illustrated, but this should be interpreted as that the scope of the above-mentioned theme of the present invention is only limitted to following embodiment.All technology realized based on foregoing of the present invention all belong to scope of the present invention.Adjuvant in following examples can be replaced with pharmaceutically acceptable similar adjuvant, or reduces, increases.
Embodiment 1
Prescription (specification: 60g:4g):
Preparation technology:
Get the calcium disodium edetate of recipe quantity, sodium acetate, sodium benzoate, add stirring and dissolving in appropriate purified water, under stirring, add xanthan gum and the carbomer of recipe quantity, stir swelling, add recipe quantity sodium sulfite, mesalazine, stirring and evenly mixing, homogenizing, add water to full dose, stir, fill and get final product, surveying pH value is 3.5, surveys grain diameter 90% particle size range at 8 microns to 15 microns.
Embodiment 2
Prescription (specification: 60g:4g):
Preparation technology:
Get the disodium edetate of recipe quantity, sodium acetate, sodium benzoate, add stirring and dissolving in appropriate purified water, under stirring, add xanthan gum and the carbomer of recipe quantity, stir swelling, add recipe quantity vitamin C, mesalazine, stirring and evenly mixing, homogenizing, add water to full dose, stir, fill and get final product, surveying pH value is 5.5, surveys grain diameter 90% particle size range at 8 microns to 15 microns.
Embodiment 3
Prescription (specification: 60g:4g):
Preparation technology:
Get the disodium edetate of recipe quantity, sodium acetate, sodium benzoate, add stirring and dissolving in appropriate purified water, under stirring, add xanthan gum and the carbomer of recipe quantity, stir swelling, add recipe quantity sodium pyrosulfite, mesalazine, stirring and evenly mixing, homogenizing, add water to full dose, stir, fill and get final product, surveying pH value is 4.8, surveys grain diameter 90% particle size range at 8 microns to 15 microns.
Embodiment 4
Prescription (specification: 60g:4g):
Preparation technology:
Get the disodium edetate of recipe quantity, sodium acetate, sodium benzoate, add stirring and dissolving in appropriate purified water, under stirring, add xanthan gum and the carbomer of recipe quantity, stir swelling, add recipe quantity sodium pyrosulfite, mesalazine, stirring and evenly mixing, homogenizing, add water to full dose, stir, fill and get final product, surveying pH value is 4.6, surveys grain diameter 90% particle size range at 8 microns to 15 microns.
Reference examples 1
Reference examples 1 prescription is except sodium acetate consumption, and other are consistent with embodiment 4, and reference examples 1 sodium acetate is 0.30g, and finished product detection pH value is 4.4, surveys grain diameter 90% particle size range more than 20 microns.
Reference examples 2
Reference examples 2 prescription is except sodium acetate consumption, and other are consistent with embodiment 3, and reference examples 2 sodium acetate is 0.36g, and finished product detection pH value is 5.0, surveys grain diameter 90% particle size range at 1 micron ~ 6 microns.
Test example 1
Stability test
With reference to " Chinese Pharmacopoeia 2005 version two annex medicine stability test guidelines, sample thief carries out long-term investigation test under being placed in temperature (25 DEG C), humidity (RH60%) condition, in the 0th day, December, the 24th month, the 36th month sampling, investigate its character and outward appearance, redispersibility index, embodiment 1, embodiment 2, embodiment 3 and embodiment 4 and reference examples 1, reference examples 2 result of the test see the following form.
Claims (6)
1. the pharmaceutical composition containing mesalazine, in every 60g compositions, consist of the following composition: mesalazine 4g, metal-chelator 0.04g ~ 0.1g, antioxidant 0.1g ~ 0.5g, antiseptic 0.01g ~ 0.2g, suspending agent 0.1g ~ 0.4g, PH regulator 0.1g ~ 0.4g, surplus are water.
2. pharmaceutical composition according to claim 1, it is characterized in that, described metal-chelator is selected from one or more in disodium edetate, calcium disodium edetate, described antioxidant is selected from one or more in sodium sulfite, sodium sulfite, sodium pyrosulfite, potassium metabisulfite, vitamin C, described antiseptic is selected from one or more in sodium benzoate, benzoic acid, described suspending agent is selected from one or more in xanthan gum, hypromellose, carbomer, and described PH regulator is selected from one or more in sodium acetate, potassium acetate.
3. pharmaceutical composition according to claim 2, is characterized in that, described suspending agent is xanthan gum, carbomer, and the particle size range of described pharmaceutical composition more than 90% granule is 8 microns ~ 15 microns.
4. the pharmaceutical composition according to any one of claim 1,2,3, described medicine composition dosage form is enema.
5. the pharmaceutical composition according to any one of claim 1,2,3, described pharmaceutical composition pH value scope is 3.5 ~ 5.5.
6. pharmaceutical composition according to claim 5, described enema pH value scope is 4.6 ~ 4.8.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310682696.6A CN104706582A (en) | 2013-12-12 | 2013-12-12 | Mesalazine-containing drug composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310682696.6A CN104706582A (en) | 2013-12-12 | 2013-12-12 | Mesalazine-containing drug composition |
Publications (1)
| Publication Number | Publication Date |
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| CN104706582A true CN104706582A (en) | 2015-06-17 |
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| CN201310682696.6A Pending CN104706582A (en) | 2013-12-12 | 2013-12-12 | Mesalazine-containing drug composition |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105878177A (en) * | 2016-05-12 | 2016-08-24 | 中国人民解放军广州军区武汉总医院 | Mesalazine temperature-sensitive gel enema and preparation method thereof |
| CN107854436A (en) * | 2017-11-02 | 2018-03-30 | 广州市桐晖药业有限公司 | Mesalazine granule |
| CN113350277A (en) * | 2021-06-30 | 2021-09-07 | 广东科伦药业有限公司 | Mesalazine gargle for treating chemotherapy oral mucositis and preparation method thereof |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1312368A1 (en) * | 2001-11-19 | 2003-05-21 | Dr. Falk Pharma Gmbh | Composition comprising mesalazine for the treatment of inflammatory bowel diseases |
| JP2006036660A (en) * | 2004-07-23 | 2006-02-09 | Wakamoto Pharmaceut Co Ltd | Hardly soluble pharmaceutical-containing aqueously suspended thermogelling preparation |
| CN101610670A (en) * | 2006-11-03 | 2009-12-23 | 萨利克斯药品公司 | The preparation and the purposes of 2-hydroxyl-5-phenylazobenzoic acid derivatives |
| CN102238868A (en) * | 2008-10-03 | 2011-11-09 | 福尔克博士药物有限责任公司 | Compositions and methods for the treatment of bowel diseases with granulated mesalamine |
| WO2013059768A1 (en) * | 2011-10-20 | 2013-04-25 | Aptalis Pharma U.S., Inc. | Therapeutic agents for treating gastrointestinal disorders associated with inflammation of the gastrointestinal tract |
-
2013
- 2013-12-12 CN CN201310682696.6A patent/CN104706582A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1312368A1 (en) * | 2001-11-19 | 2003-05-21 | Dr. Falk Pharma Gmbh | Composition comprising mesalazine for the treatment of inflammatory bowel diseases |
| JP2006036660A (en) * | 2004-07-23 | 2006-02-09 | Wakamoto Pharmaceut Co Ltd | Hardly soluble pharmaceutical-containing aqueously suspended thermogelling preparation |
| CN101610670A (en) * | 2006-11-03 | 2009-12-23 | 萨利克斯药品公司 | The preparation and the purposes of 2-hydroxyl-5-phenylazobenzoic acid derivatives |
| CN102238868A (en) * | 2008-10-03 | 2011-11-09 | 福尔克博士药物有限责任公司 | Compositions and methods for the treatment of bowel diseases with granulated mesalamine |
| WO2013059768A1 (en) * | 2011-10-20 | 2013-04-25 | Aptalis Pharma U.S., Inc. | Therapeutic agents for treating gastrointestinal disorders associated with inflammation of the gastrointestinal tract |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105878177A (en) * | 2016-05-12 | 2016-08-24 | 中国人民解放军广州军区武汉总医院 | Mesalazine temperature-sensitive gel enema and preparation method thereof |
| CN105878177B (en) * | 2016-05-12 | 2019-07-23 | 中国人民解放军广州军区武汉总医院 | Mesalazine thermo-sensitive gel enema fluid and preparation method thereof |
| CN107854436A (en) * | 2017-11-02 | 2018-03-30 | 广州市桐晖药业有限公司 | Mesalazine granule |
| CN113350277A (en) * | 2021-06-30 | 2021-09-07 | 广东科伦药业有限公司 | Mesalazine gargle for treating chemotherapy oral mucositis and preparation method thereof |
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