CN106822015A - Acetazolamide sustained release tablets and preparation method thereof - Google Patents
Acetazolamide sustained release tablets and preparation method thereof Download PDFInfo
- Publication number
- CN106822015A CN106822015A CN201710190209.2A CN201710190209A CN106822015A CN 106822015 A CN106822015 A CN 106822015A CN 201710190209 A CN201710190209 A CN 201710190209A CN 106822015 A CN106822015 A CN 106822015A
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- Prior art keywords
- acetazolamide
- parts
- sustained release
- release tablets
- preparation
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/433—Thidiazoles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Preparation (AREA)
Abstract
The present invention proposes a kind of acetazolamide sustained release tablets, including following supplementary material：0.1~10 part of 60~80 parts of acetazolamide, 20~30 parts of hydroxypropyl methyl cellulose, 15~20 parts of Carbomer, 5~10 parts of polyvinyl alcohol, 30~40 parts of cornstarch, 0.1~2 part of lubricant and PVP.Preparation method, comprises the following steps：1) after adding pure water preparation into the corn starch solution of 8~15wt%, heating to boil cornstarch, 50~60 DEG C are cooled to and are incubated；2) acetazolamide, hydroxypropyl methyl cellulose, Carbomer, polyvinyl alcohol and PVP are sieved, is then well mixed, the corn starch solution for adding insulation carries out wet granulation；3) step 2) system particle carry out whole grain, drying, obtain acetazolamide dry particl；4) by acetazolamide dry particl and mix lubricant it is uniform after, compressing tablet, you can.Should have extraordinary release and stability, it is ensured that with the uniformity of release in vitro behavior in product body, improve the clinical efficacy of product.
Description
Technical field
The present invention relates to belong to ocular disease drug formulation art, and in particular to a kind of acetazolamide sustained release tablets and its preparation side
Method.
Background technology
Acetazolamide is a kind of carbonic anhydrase inhibitor, is mainly used in reducing intraocular pressure, suppresses ciliary body skin carbonic anhydrase
Activity, so as to reduce aqueous humor generation, declines intraocular pressure, it is adaptable to treat various types of glaucomas, such as open-angle (chronic herpes
Property) glaucoma, angle-closure glaucoma etc..
Acetazolamide is insoluble in water, and its ordinary tablet vivo biodistribution availability is low.In the case of application acetazolamide failure,
In addition to limiting the case that it is used because of its side effect, remaining because the malabsorption of medicine and cause the intraocular pressure can not be well
Control.General formulation rate of release is too fast so that peak plasma concentrations are higher, induces its many-sided side effect, such as four limbs fiber crops
It is wooden, tired, sleepy depressed, drowsiness etc..
The content of the invention
The present invention proposes a kind of acetazolamide sustained release tablets, should have extraordinary release and stability, it is ensured that production
Acetazolamide sustained release tablets good quality, it is ensured that with the uniformity of release in vitro behavior in product body, improve facing for product
Bed curative effect.
The technical proposal of the invention is realized in this way：
A kind of acetazolamide sustained release tablets, in parts by weight, including following supplementary material：
60~80 parts of acetazolamide, 20~30 parts of hydroxypropyl methyl cellulose, 15~20 parts of Carbomer, polyvinyl alcohol 5~
10 parts, 30~40 parts of cornstarch and 0.1~10 part of 0.1~2 part of lubricant and PVP.
Further, lubricant is talcum powder, magnesium stearate or zinc stearate.
It is a further object to provide a kind of preparation method of acetazolamide sustained release tablets, comprise the following steps：
1) cornstarch is added into pure water preparation into the corn starch solution of 8~15wt%, after heating is boiled, it is cooled to 50~
60 DEG C and it is incubated；
2) acetazolamide, hydroxypropyl methyl cellulose, Carbomer, polyvinyl alcohol and PVP are sieved, then mixes equal
Even, the corn starch solution for adding insulation carries out wet granulation；
3) step 2) system particle carry out whole grain, drying, obtain acetazolamide dry particl；
4) by acetazolamide dry particl and mix lubricant it is uniform after, compressing tablet, you can.
Heating PROCESS FOR TREATMENT is carried out to common corn starch, adhesive effect of the starch in sustained release agent can be improved, improved
The mouldability of tablet.
The skeleton retarding agent of sustained release tablets of the invention is hydroxypropyl methyl cellulose, Carbomer and polyvinyl alcohol.Hydroxypropyl
Methylcellulose has good hydrophily with polyvinyl alcohol.Contain a large amount of carboxyls in Carbomer structure, meet water energy and form gel,
The free carboxy of Carbomer, can provide proton, and hydrogen bond can be formed with gastrointestinal mucosa after forming gel, stick on gastrointestinal wall,
So as to extend holdup time of the medicine in intestines and stomach.Cornstarch with skeleton retarding agent of the invention after heating by matching somebody with somebody
Conjunction can effectively control the rate of release of medicine, it is to avoid the too fast release of medicine.
The acetazolamide sustained release tablets toxic and side effect prepared using technical solution of the present invention is few, is easy to patient's long-term treatment, and
Improve the compliance of medication.The acetazolamide sustained release tablets of technical solution of the present invention preparation are taken, daily can once be protected
24 hours internal active drug concentration of card, and it is secondary instead to reduce the higher poison for causing of peak plasma concentrations that ordinary preparation brought
Should.Using acetazolamide sustained release tablets of the present invention, significantly reduce preparation differences between batches and improve the stability of sample.
Specific embodiment
Embodiment 1
A kind of acetazolamide sustained release tablets, in parts by weight, including following supplementary material：
70 parts of acetazolamide, 25 parts of hydroxypropyl methyl cellulose, 18 parts of Carbomer, 7 parts of polyvinyl alcohol, cornstarch 36
7 parts of part, 1.2 parts of magnesium stearate and PVP.
Preparation method, comprises the following steps：
1) after adding pure water preparation into the corn starch solution of 12wt%, heating to boil cornstarch, 56 DEG C are cooled to simultaneously
Insulation；
2) acetazolamide, hydroxypropyl methyl cellulose, Carbomer, polyvinyl alcohol and PVP are sieved, then mixes equal
Even, the corn starch solution for adding insulation carries out wet granulation；
3) step 2) system particle carry out whole grain, drying, obtain acetazolamide dry particl；
4) after acetazolamide dry particl is well mixed with magnesium stearate, compressing tablet, you can.
Embodiment 2
A kind of acetazolamide sustained release tablets, in parts by weight, including following supplementary material：
60 parts of acetazolamide, 20 parts of hydroxypropyl methyl cellulose, 15 parts of Carbomer, 5 parts of polyvinyl alcohol, cornstarch 40
1 part of part, 0.3 part of talcum powder and PVP.
Preparation method, comprises the following steps：
1) after adding pure water preparation into the corn starch solution of 8wt%, heating to boil cornstarch, 50 DEG C are cooled to and are protected
Temperature；
2) acetazolamide, hydroxypropyl methyl cellulose, Carbomer, polyvinyl alcohol and PVP are sieved, then mixes equal
Even, the corn starch solution for adding insulation carries out wet granulation；
3) step 2) system particle carry out whole grain, drying, obtain acetazolamide dry particl；
4) after acetazolamide dry particl is well mixed with talcum powder, compressing tablet, you can.
Embodiment 3
A kind of acetazolamide sustained release tablets, in parts by weight, including following supplementary material：
80 parts of acetazolamide, 30 parts of hydroxypropyl methyl cellulose, 20 parts of Carbomer, 10 parts of polyvinyl alcohol, cornstarch 40
10 parts of part, 2 parts of zinc stearate and PVP.
Preparation method, comprises the following steps：
1) after adding pure water preparation into the corn starch solution of 15wt%, heating to boil cornstarch, 60 DEG C are cooled to simultaneously
Insulation；
2) acetazolamide, hydroxypropyl methyl cellulose, Carbomer, polyvinyl alcohol and PVP are sieved, then mixes equal
Even, the corn starch solution for adding insulation carries out wet granulation；
3) step 2) system particle carry out whole grain, drying, obtain acetazolamide dry particl；
4) after acetazolamide dry particl is well mixed with zinc stearate, compressing tablet, you can.
Test example
The sustained release tablets that experiment is prepared using embodiment 1, by the medicine stability of States Pharmacopoeia specifications investigate method investigate (referring to
Two C of annex Ⅺ Ⅹ of Pharmacopoeia of People's Republic of China 2010 edition), it has been experimentally confirmed what is prepared using technical solution of the present invention
Acetazolamide sustained release tablets have high stability, are compared with existing product and prior art with remarkable result (experiment number
According to referring to table 1, table 2 and table 3).
The study on the stability of product acetazolamide sustained release tablets of the present invention under the hot conditions of table 1
The study on the stability of product acetazolamide sustained release tablets of the present invention under the super-humid conditions of table 2
The study on the stability of product acetazolamide sustained release tablets of the present invention under the conditions of the strong illumination of table 3
Presently preferred embodiments of the present invention is the foregoing is only, is not intended to limit the invention, it is all in essence of the invention
Within god and principle, any modification, equivalent substitution and improvements made etc. should be included within the scope of the present invention.
Claims (3)
1. a kind of acetazolamide sustained release tablets, it is characterised in that in parts by weight, including following supplementary material：
60~80 parts of acetazolamide, 20~30 parts of hydroxypropyl methyl cellulose, 15~20 parts of Carbomer, 5~10 parts of polyvinyl alcohol,
0.1~10 part of 30~40 parts of cornstarch, 0.1~2 part of lubricant and PVP.
2. acetazolamide sustained release tablets according to claim 1, it is characterised in that lubricant be talcum powder, magnesium stearate or
Person's zinc stearate.
3. the preparation method of acetazolamide sustained release tablets as claimed in claim 1, it is characterised in that comprise the following steps：
1) after adding pure water preparation into the corn starch solution of 8~15wt%, heating to boil cornstarch, 50~60 DEG C are cooled to
And be incubated；
2) acetazolamide, hydroxypropyl methyl cellulose, Carbomer, polyvinyl alcohol and PVP are sieved, is then well mixed, then
Adding the corn starch solution of insulation carries out wet granulation；
3) step 2) system particle carry out whole grain, drying, obtain acetazolamide dry particl；
4) by acetazolamide dry particl and mix lubricant it is uniform after, compressing tablet, you can.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710190209.2A CN106822015A (en) | 2017-03-27 | 2017-03-27 | Acetazolamide sustained release tablets and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710190209.2A CN106822015A (en) | 2017-03-27 | 2017-03-27 | Acetazolamide sustained release tablets and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106822015A true CN106822015A (en) | 2017-06-13 |
Family
ID=59130284
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710190209.2A Pending CN106822015A (en) | 2017-03-27 | 2017-03-27 | Acetazolamide sustained release tablets and preparation method thereof |
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| CN (1) | CN106822015A (en) |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2256587A (en) * | 1991-06-11 | 1992-12-16 | American Cyanamid Co | Acetazolamide in sustained release form |
| CN102949377A (en) * | 2012-11-28 | 2013-03-06 | 河南中帅医药科技发展有限公司 | Acetazolamide sustained-release capsule and preparation method thereof |
| CN104434837A (en) * | 2014-12-05 | 2015-03-25 | 海南卫康制药(潜山)有限公司 | Acetazolamide composition lyophilized tablet and preparation method thereof |
-
2017
- 2017-03-27 CN CN201710190209.2A patent/CN106822015A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2256587A (en) * | 1991-06-11 | 1992-12-16 | American Cyanamid Co | Acetazolamide in sustained release form |
| CN102949377A (en) * | 2012-11-28 | 2013-03-06 | 河南中帅医药科技发展有限公司 | Acetazolamide sustained-release capsule and preparation method thereof |
| CN104434837A (en) * | 2014-12-05 | 2015-03-25 | 海南卫康制药(潜山)有限公司 | Acetazolamide composition lyophilized tablet and preparation method thereof |
Non-Patent Citations (2)
| Title |
|---|
| B.SRINIVAS等: "Design and evaluation of extended release capsules of acetazolamide using eudragit RS100 and eudragit RL100", 《INDO AMERICAN JOURNAL OF PHARMACEUTICAL RESEARCH》 * |
| 张炳盛等: "《中药药剂学》", 28 February 2013 * |
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| PB01 | Publication | ||
| PB01 | Publication | ||
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Application publication date: 20170613 |