CN100441193C - Antipyretic and analgetic aspirin enteric-coated preparation and production thereof - Google Patents
Antipyretic and analgetic aspirin enteric-coated preparation and production thereof Download PDFInfo
- Publication number
- CN100441193C CN100441193C CNB200510012313XA CN200510012313A CN100441193C CN 100441193 C CN100441193 C CN 100441193C CN B200510012313X A CNB200510012313X A CN B200510012313XA CN 200510012313 A CN200510012313 A CN 200510012313A CN 100441193 C CN100441193 C CN 100441193C
- Authority
- CN
- China
- Prior art keywords
- enteric
- aspirin
- preparation
- antipyretic
- agent
- 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.)
- Active
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The present invention relates to a composite enteric antipyretic and analgetic aspirin preparation and a preparing method thereof, which belongs to the technical field of medicine. The preparation is used for enhancing the curative effect of aspirin and solving side effects. The present invention has the technical scheme that the preparation is compounded from aspirin as a main material, vitamin C, pharmaceutic adjuvant and enteric coating materials, wherein the main material and the adjuvant contain 10 to 70 wt% of aspirin, 7 to 44 wt% of vitamin C, 0 to 45 wt% of filling agent, 1 to 20 wt% of disintegrating agent, 0.5 to 5 wt% of lubricant, 0.8 to 10 wt% of wetting agent or binding agent and 3 to 20 wt% of enteric coating material. The preparation has an obvious enteric coating characteristics that when the preparation is put into the HCl solution of 0.1 mol/L, absolutely no medicine is released in 2 hours; when the preparation is put into phosphate buffer solution, the dissolution reaches over 90% in 45 minutes, and consequently the simulation of medicine to the intestine and the stomach, and the influence of the external environment on medicine are avoided, and the quality becomes stable.
Description
Technical field
The present invention relates to a kind of antipyretic-antalgic class medicine and preparation method thereof, belong to medical technical field.
Technical background
Aspirin is a kind of century-old old brand ntipyretic analgesic medicine of determined curative effect, and clinical practice is lasting for many years, has become the antiheumatic basic medication of domestic and international antipyretic-antalgic.In recent years, people find that again aspirin has antithrombotic characteristic, and rectal cancer, colon cancer are also had certain curative effect, take the initiation potential that aspirin can reduce rectal cancer, colon cancer 40% regularly.Along with the continuous excavation of aspirin novel clinical use, its clinical practice is also increasingly extensive.Vitamin C participates in the multiple metabolism of body, and increases the resistance of body.Both share, from pharmacological action still be in the body pharmacokinetics change to see it all is reasonably, aspirin can be competed receptor on the leukocyte film with vitamin C, suppresses leukocyte to ascorbic picked-up, the blood plasma Vitamin C content is improved, and ascorbic excretion also increases in the urine; Vitamin C then can be accelerated the absorption of aspirin, comparatively fast reaches treatment concentration, plays a role thereby quicken aspirin.
But still there are some problems in load if only aspirin and vitamin C are combined with each other simply, mainly is that aspirin is bigger to the gastrointestinal zest, easily causes digestive tract hemorrhage, gastric ulcer, even the danger of gastric perforation is arranged.Aspirin and vitamin C character less stable all in addition, aspirin is met water and easily is decomposed into salicylic acid, the easy oxidation of vitamin C.If make effervescent tablet, than being easier to the moisture absorption, thereby cause the degraded of effective ingredient, medicament contg is descended, give to produce to store and also bring great inconvenience.
Summary of the invention
The objective of the invention is to overcome the problem that has the preparation existence and a kind of good efficacy that can produce is provided, can avoid it again, be easy to produce the compound enteric coated preparation of antipyretic-antalgic storage, stable GI irritation.
Another object of the present invention provides the preparation method of this preparation.
First purpose of the present invention is such realization:
The compound enteric coated preparation of a kind of antipyretic-antalgic aspirin, it is made up of principal agent aspirin, vitamin C, pharmaceutic adjuvant and enteric-coating material, pharmaceutic adjuvant is divided into filler, disintegrating agent, lubricant, wetting agent and binding agent, enteric-coating material adopts the dissolved high molecular film material of beginning under the enteric environment
The unit meter is as follows by weight for described main materials and auxiliary materials:
A. aspirin 10～70%
B. vitamin C 7～44%
C. filler 0～45%
D. disintegrating agent 1～20%
E. lubricant 0.5～5%
F. wetting agent or binding agent 0.8～10%
Described filler is selected from one or both or the two or more combinations in microcrystalline Cellulose, starch, amylum pregelatinisatum, lactose, dextrin, mannitol, sucrose, the hyprolose;
Described disintegrating agent is selected from one or both or the two or more combinations in hyprolose, carboxymethylstach sodium, polyvinylpolypyrrolidone, the cross-linking sodium carboxymethyl cellulose;
Described lubricant is selected from one or both in Pulvis Talci, the micropowder silica gel;
Described wetting agent or binding agent are selected water, ethanol, starch slurry, polyvidone and cellulose family for use;
Described enteric-coating material is selected the combination of one or both or two or more materials in polyacrylic resin, acrylic resin, hydroxypropylmethyl cellulose phthalate (HPMCP), cellulose acetate phthalate (CAP), acetic acid hydroxypropyl methylcellulose succinyl ester (HPMCPAS), ethyl cellulose (EC), zein, Lac, the diketopiperazine polymer for use, and the weight of enteric-coating material is 3～20% of main ingredient weight.
The compound enteric coated preparation of above-mentioned antipyretic-antalgic aspirin, in the described compound enteric coated preparation main materials and auxiliary materials by weight the optimum ratio of unit meter be:
Aspirin 15～60%
Vitamin C 15～36%
Filler 3～36%
Disintegrating agent 2～18%
Lubricant 0.8～4%
Wetting agent or binding agent 1～8%
Enteric-coating material 5～18%
Filler preferably microcrystalline cellulose wherein; The preferred carboxymethylstach sodium of disintegrating agent; Lubricant preferably talc powder; The preferred polyvidone of wetting agent or binding agent; The preferred hydroxypropylmethyl cellulose phthalate of enteric-coating material; Plasticizer is selected polyethylene glycol 6000 for use.
The compound enteric coated preparation of above-mentioned antipyretic-antalgic aspirin, described enteric-coating material can substitute with hollow enteric hard capsule.
In order to improve the film property of enteric material, add the plasticizer of coating solution 0.1～8% in the described enteric-coating material, described plasticizer is one or more in triethyl citrate, Polyethylene Glycol, the diethyl phthalate.
For the transparency (lucifuge) of improving enteric material, the compound enteric coated preparation of above-mentioned antipyretic-antalgic aspirin, the opacifier of adding coating solution 0.1～8% in the described enteric-coating material, described opacifier is titanium dioxide, barium sulfate, calcium carbonate etc.
Another object of the present invention is achieved in that
A. prepare core material: the main ingredient crushing screening with in the above-mentioned prescription, take by weighing by formula ratio, insert mix homogeneously in the mixer, dry method or wet method prepare granule or micropill, and the qualified back of the inspection of semifinished product adds lubricant, tabletting behind the mixing;
B. prepare coating solution: with a kind of enteric material of or combination in any with dissolve with ethanol solution after, mix homogeneously adds plasticizer, opacifier as required, adjusts proper viscosity.
C. prepare enteric coated preparation:
The sheet, granule or the micropill that prepare are weighed in the rearmounted coating pan, limit spray coating solution, the limit blowing hot-air obtains enteric coated tablet, granule or micropill, granule or micropill is incapsulated get final product.
Aspirin and ascorbic compound enteric coated preparation have produced good effect among the present invention, not disintegrate in 2 hours under one's belt, enter the rapid disintegrate of enteral and become granule, thereby make aspirin enter predetermined absorption site small intestinal rapidly, reduced the stimulation of aspirin the intestines and stomach.Because the absorption of aspirin is also accelerated in ascorbic existence, therefore has advantage rapid-action, no gastrointestinal side-effect simultaneously.
Enteric effect of the present invention can be measured according to the drug release determination method that Chinese Pharmacopoeia provides.
Getting this product, is solvent with the hydrochloric acid solution 900ml of 0.1mol/L, and rotating speed is that per minute 100 changes, and turns round 2 hours, and sample is changed in another container that fills phosphate buffer (pH6.8) 900ml, measures with method.Respectively in hydrochloric acid solution 1 hour, 2 hours and change phosphate buffer over to after to get solution in 45 minutes and 60 minutes an amount of, filter, subsequent filtrate 2ml puts the 25ml measuring bottle, adds mobile phase and is diluted to scale, gets 20 μ l solution and injects chromatograph of liquid; Other gets aspirin, the vitamin C reference substance is diluted to every 1ml in right amount and contains the contrast liquid that aspirin 35.5 μ g contain Catergen 1.3 μ g, and the result is as follows:
The embodiment sample is the stripping quantity testing result in hydrochloric acid and phosphate buffer
Result of the test shows, aspirin and ascorbic compound enteric coated preparation have significant enteric characteristics: in 0.1mol/L HCl solution, almost there is not drug release to go out in 2 hours, in the solution of phosphate buffer pH6.8,45 minutes then stripping reach more than 90%, thereby avoided the stimulation of medicine, enteric film coating simultaneously to the intestines and stomach, also avoided the external environment factor to aspirin and ascorbic influence, quality is more stable.
The specific embodiment
Below provide related embodiment:
One. preparation aspirin vitamin C enteric coatel tablets embodiment:
Component embodiment 12345
A. aspirin 400 400 100 30 210
B. vitamin 240 100 240 132 21
C. filler:
Microcrystalline Cellulose 65 81
Starch 87
Lactose 200
D. disintegrating agent
Carboxymethylstach sodium 60 13.2
Hydroxypropyl cellulose 29 3 60
E. lubricant:
Pulvis Talci 88 15 1.5
Micropowder silica gel 13
F. wetting agent or binding agent
Ethanol 30
Polyvidone 75 10 2.4
Starch slurry 20
Above-mentioned prescription is 1000 a content, and unit is gram, down together.
Preparation coating solution embodiment:
Embodiment 1
Hydroxypropylmethyl cellulose phthalate 80g, polyethylene glycol 6000 12g, 80% concentration ethanol 1000ml is made into coating solution.
Embodiment 2
Hydroxypropylmethyl cellulose phthalate 40g, titanium dioxide 7.8g, 80% ethanol 800ml is made into coating solution.
Embodiment 3
Polyacrylic resin II 64g, 95% ethanol 800ml is made into coating solution.
Embodiment 4
Hydroxypropylmethyl cellulose phthalate 9g, 95% ethanol 500ml is made into coating solution.
Embodiment 5
Ethyl cellulose 5.1g, 95% ethanol 500ml is made into coating solution.
Preparation method:
Took by weighing the adjuvant of aspirin, vitamin C and mistake 100 mesh sieves of 200 mesh sieves by recipe quantity; behind the mix homogeneously; be pressed into 0.5g φ 9mm circular piece; Hardness Control is at 4-6kg; to press to such an extent that sheet stock keeps off the granule that granulation machine is made 20 order sizes with pendulum; it is even to add mix lubricant, after the inspection of semifinished product is qualified, and tabletting.
The plain sheet that makes is weighed in the rearmounted coating pan, limit spray coating solution, the limit blowing hot-air obtains enteric coated tablet.
Two. preparation aspirin vitamin C enteric coated capsule embodiment:
Component embodiment 6789
A. aspirin 200 100 200 100
B. vitamin B12 0 100 120 60
C. filler:
Microcrystalline Cellulose 66 135
Hyprolose 10
D. disintegrating agent
Carboxymethylstach sodium 8 42.5 8
Hyprolose 48.6
E. lubricant:
Pulvis Talci 8 16.5 5 1.8
F. wetting agent or binding agent
Ethanol 10
Polyvidone 10 37
Starch slurry 5
What more than provide is the prescription of 1000 preparation main ingredients, if the preparation enteric coated capsule has two kinds of approach, and the one, make the plain particles enteric coated capsule of packing into, another is to adopt the enteric coated particles conventional capsule of packing into, the former is at technology:
Take by weighing principal agent, filler, disintegrating agent by recipe quantity, add binding agent behind the mix homogeneously and granulate, drying obtains granule, after the assay was approved, adds lubricant, and the enteric coated capsule of packing into promptly gets aspirin vitamin C enteric coated capsule.
If adopt back one technology, then still need prepare coating solution, its prescription is:
Preparation coating solution embodiment 6
Polyacrylic resin II 44g, 95% ethanol 800ml is made into coating solution.
Preparation coating solution embodiment 7
Ethyl cellulose 48.6g, 95% ethanol 800ml is made into coating solution.
The preparation enteric coated capsule:
Take by weighing principal agent, filler, disintegrating agent by recipe quantity, add binding agent behind the mix homogeneously and granulate, drying, after the inspection of semifinished product is qualified, weigh rearmounted coating pan or fluidizing fluid-bed in, limit spray coating solution, the limit blowing hot-air obtains enteric coated particles.
Enteric coated particles is added lubricant, and the fill capsule promptly gets aspirin vitamin C enteric coated capsule.
Claims (5)
1. compound enteric coated preparation of antipyretic-antalgic aspirin, it is made up of principal agent aspirin, vitamin C, pharmaceutic adjuvant and enteric-coating material, pharmaceutic adjuvant is divided into filler, disintegrating agent, lubricant, wetting agent or binding agent, enteric-coating material adopts the dissolved high molecular film material of beginning under the enteric environment, it is characterized in that
The unit meter is as follows by weight for described main materials and auxiliary materials:
Aspirin 15～60%
Vitamin C 15～36%
Filler 3～36%
Disintegrating agent 2～18%
Lubricant 0.8～4%
Wetting agent or binding agent 1～8%
Described filler is selected microcrystalline Cellulose for use; Disintegrating agent is selected carboxymethylstach sodium for use; Lubricant is selected Pulvis Talci for use; Wetting agent or binding agent are selected polyvidone for use; Described enteric-coating material is selected hydroxypropylmethyl cellulose phthalate for use; The weight of enteric-coating material is 5～18% of main ingredient weight.
2. the compound enteric coated preparation of antipyretic-antalgic aspirin according to claim 1, it is characterized in that, the plasticizer that adds coating liquid measure 0.1～8% in the described enteric-coating material, described plasticizer are a kind of in triethyl citrate, Polyethylene Glycol, the diethyl phthalate.
3. the compound enteric coated preparation of antipyretic-antalgic aspirin according to claim 2 is characterized in that, adds the opacifier of coating liquid measure 0.1～8% in the described enteric-coating material, and described opacifier is a kind of in titanium dioxide, barium sulfate, the calcium carbonate.
4. the compound enteric coated preparation of antipyretic-antalgic aspirin according to claim 1 is characterized in that, described enteric-coating material substitutes with hollow enteric hard capsule.
5. the preparation method of the compound enteric coated preparation of antipyretic-antalgic aspirin as claimed in claim 3 is characterized in that it carries out as follows:
A. prepare core material: the main ingredient crushing screening with in the above-mentioned prescription, take by weighing by formula ratio, insert mix homogeneously in the mixer, dry method or wet method prepare granule or micropill, or add lubricant in the qualified back of the inspection of semifinished product, and tabletting is made tablet behind the mixing;
B. prepare coating solution: with a kind of enteric material of or its combination with dissolve with ethanol solution after, mix homogeneously adds plasticizer, opacifier, adjusts viscosity;
C. prepare enteric coated preparation:
The tablet, granule or the micropill that prepare are weighed in the rearmounted coating pan, limit spray coating solution, the limit blowing hot-air obtains enteric coated tablet, granule or micropill, granule or micropill is incapsulated get final product.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB200510012313XA CN100441193C (en) | 2005-01-11 | 2005-01-11 | Antipyretic and analgetic aspirin enteric-coated preparation and production thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB200510012313XA CN100441193C (en) | 2005-01-11 | 2005-01-11 | Antipyretic and analgetic aspirin enteric-coated preparation and production thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1679592A CN1679592A (en) | 2005-10-12 |
| CN100441193C true CN100441193C (en) | 2008-12-10 |
Family
ID=35066601
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB200510012313XA Active CN100441193C (en) | 2005-01-11 | 2005-01-11 | Antipyretic and analgetic aspirin enteric-coated preparation and production thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN100441193C (en) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100413502C (en) * | 2006-09-15 | 2008-08-27 | 天津市中央药业有限公司 | Hypertension treating medicine |
| CN101596166B (en) * | 2008-06-04 | 2011-08-17 | 永信药品工业(昆山)有限公司 | Aspirin enteric-coated pellet |
| CN101496903B (en) * | 2009-02-23 | 2010-11-17 | 四川珍珠制药有限公司 | Coating solution of medicament for reducing stimulation of medicament to stomach |
| CN104356101A (en) * | 2014-11-07 | 2015-02-18 | 李玉成 | Calcium acetylsalicylate ascorbate and preparation method thereof |
| CN104352444A (en) * | 2014-11-20 | 2015-02-18 | 哈尔滨圣吉药业股份有限公司 | Aspirin-vitamin C enteric micropellet and preparation method thereof |
| CN106880639A (en) * | 2015-12-15 | 2017-06-23 | 上海星泰医药科技有限公司 | Aspirin and compound enteric-coated of vitamin C and preparation method thereof |
| CN109394708B (en) * | 2017-08-17 | 2021-10-08 | 西安棣加生物科技有限公司 | Oral rapidly-disintegrating heart disease first-aid tablet and 3D printing method and application thereof |
| CN107737151B (en) * | 2017-12-01 | 2020-06-30 | 皖南医学院 | Compound snakegourd fruit-aspirin stomach enteric-coated pellet capsule as well as preparation method and application thereof |
-
2005
- 2005-01-11 CN CNB200510012313XA patent/CN100441193C/en active Active
Non-Patent Citations (6)
| Title |
|---|
| 国家药品标准. 国家药典委编，5页，化学工业出版社. 2003 国家药品标准. 国家药典委编，9页，化学工业出版社. 2003 药剂学. 奚念朱，323-325页，人民卫生出版社. 1996 |
| 国家药品标准. 国家药典委编，5页，化学工业出版社. 2003 * |
| 国家药品标准. 国家药典委编，9页，化学工业出版社. 2003 * |
| 维生素C对阿斯匹林的血药浓度及药物动力学的影响. 吴金虎等.中国药学杂志，第30卷第1期. 1995 |
| 维生素C对阿斯匹林的血药浓度及药物动力学的影响. 吴金虎等. 中国药学杂志，第30卷第1期. 1995 * |
| 药剂学. 奚念朱，323-325页，人民卫生出版社. 1996 * |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1679592A (en) | 2005-10-12 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN100441193C (en) | Antipyretic and analgetic aspirin enteric-coated preparation and production thereof | |
| JP4088420B2 (en) | Colon selective drug delivery composition and pharmaceutical preparation using polysaccharides | |
| AU633220B2 (en) | Coated solid medicament form having releasability in large intestine | |
| AU628754B2 (en) | Therapeutic agents | |
| CN101466359B (en) | Fast release paracetamol tablets | |
| CN104069502B (en) | Compound skeleton material and its pharmaceutical composition | |
| NO315686B1 (en) | Composition for releasing a drug to the colon | |
| CN105658207A (en) | Pharmaceutical composition containing dimethyl fumarate for administration at a low daily dose | |
| JPS593447B2 (en) | Manufacturing method for long-acting oral drugs | |
| CN101502491B (en) | Dirithromycin enteric-coated formulation | |
| PL207776B1 (en) | Modified release pharmaceutical composition | |
| CN103285017B (en) | Compound isosorbide mononitrate aspirin sustained-release capsule preparation and preparation method | |
| CN108348472A (en) | The tablet containing high dose mesalazine of optimization | |
| CA2533165A1 (en) | Gellan gum based oral controlled release dosage forms- a novel platform technology for gastric retention | |
| CA2877190C (en) | Medicament form for release of active ingredients | |
| CN101347413A (en) | Quetiapine sustained release tablets and method of preparing the same | |
| CN101636153A (en) | Time-specific delayed/pulsatile release dosage forms | |
| PL213804B1 (en) | Therapeutic system comprising amoxicillin and clavulanic acid | |
| JP2002193792A (en) | Film-coated tablet and erosion preventing composition | |
| JP3122478B2 (en) | Lower gastrointestinal release oral formulation | |
| GB2352172A (en) | Orally administered dose unit comprising a drug with an outer coating of an enteric polymer, which allows co-administered food to separate from the dose unit | |
| CN101780054A (en) | Compound sustained-release preparation and preparation method thereof | |
| JP2524497B2 (en) | Persistent solid agent | |
| CN101530406A (en) | Compound enteric-coated preparation and preparation method thereof | |
| WO2003037296A2 (en) | Methods and dosage forms for improving the bioavailability of therapeutic agents |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant |