CN106137988A - A kind of metronidazole solid preparation and preparation method thereof - Google Patents
A kind of metronidazole solid preparation and preparation method thereof Download PDFInfo
- Publication number
- CN106137988A CN106137988A CN201610023708.8A CN201610023708A CN106137988A CN 106137988 A CN106137988 A CN 106137988A CN 201610023708 A CN201610023708 A CN 201610023708A CN 106137988 A CN106137988 A CN 106137988A
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- metronidazole
- mixture
- parts
- preparation
- mix homogeneously
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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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
-
- 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
- A61K31/4164—1,3-Diazoles
-
- 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
Abstract
The invention discloses a kind of metronidazole solid preparation and preparation method thereof, in parts by mass, including following components: metronidazole 30～50 parts, microcrystalline Cellulose 10～30 parts, lactose 10～30 parts, mannitol 5～10 parts, polyvinylpolypyrrolidone 5～10 parts, carboxymethyl starch sodium 5～20 parts, menthol 0.5～2 parts, micropowder silica gel 0.2～1 part, magnesium stearate 0.2～1 part.The present invention uses direct powder compression and dry granulation tablet forming technique, prepares the rapid disintegrate in saliva of metronidazole oral cavity disintegration tablet and is separated into fine particle, and drug-eluting is accelerated, and big in oral cavity and gastrointestinal tract area distributions, absorption point is many, can improve its bioavailability.For the patient such as child, old people, oral cavity disintegration tablet is taken medicine conveniently, it is not necessary to water, also need not chew, improve the compliance of patient, improve the effectiveness of clinical treatment.
Description
Technical field
The invention belongs to pharmaceutical technology field, be specifically related to a kind of metronidazole solid preparation and preparation method thereof.
Background technology
Metronidazole, chemical name is Metronidazole, for white or off-white color crystallinity powder
End, be mainly used in treatment or prevent the microbial system of above-mentioned anaerobism or local infection, as abdominal cavity, digestive tract,
The anaerobic infection at the positions such as female reproductive system, lower respiratory tract, skin and soft tissue, bone and joint, to deteriorated blood
Disease, endocarditis, infection of meninges and the colitis using antibiotic to cause are the most effective.Treatment tetanus often with
Tetanus antitoxin (TAT) is combined.Can be additionally used in oral cavity anaerobium to infect.
Existing metronidazole medicine, as Chinese patent CN101658502A disclose a kind of metronidazole sustained-release tablets and
Preparation method, improves stability and the safety of medicine release；Chinese patent CN104887636A discloses
A kind of Metronidazole Tablet and preparation method thereof, and Chinese patent CN1452963A discloses a kind of metronidazole system
Agent, although the metronidazole medicine that said method prepares has certain effect, but production cost is high, and medicine is taken
Inconvenience, effect is inconspicuous, unstable properties, especially at the treatment microbial local of anaerobism and systemic infection,
Curative effect in terms of oral cavity anaerobium infection etc. also has the biggest room for promotion.
Summary of the invention
The present invention solves the problems referred to above of the prior art, it is provided that a kind of taking convenience, low cost and to suitable
Answer metronidazole solid preparation that disease is rapid-action and preparation method thereof.
After the metronidazole oral cavity disintegration tablet that the present invention provides is oral, in oral cavity, rapid disintegrate is dispersed into microparticle or powder,
It is particularly suited for the patient of dysphagia and merges oral ulcer Disease, and said preparation arrives gastrointestinal tract
The most existing with fine particle or powder type, drug-eluting is accelerated, big at gastrointestinal tract distribution area, inhales
Sink is many, can improve its bioavailability.
For achieving the above object, the present invention is by the following technical solutions:
The first aspect of the invention is to provide a kind of metronidazole solid preparation, in parts by mass, including following group
Point:
Further, described metronidazole solid preparation, it is characterised in that in parts by mass, including following components:
Further, described metronidazole solid preparation, it is characterised in that in parts by mass, including following components:
The second aspect of the invention is to provide the preparation method of a kind of metronidazole solid preparation, uses powder direct
Tabletting, specifically includes following steps:
A, by finely ground for metronidazole mistake 80 mesh sieve；
B, by microcrystalline Cellulose, lactose, mannitol, polyvinylpolypyrrolidone, carboxymethyl starch sodium, menthol, micro-
Powder silica gel, magnesium stearate cross 40 mesh sieves respectively, standby；
C, employing equal increments method, first mix homogeneously menthol with the mannitol of equivalent, adds residue mannitol,
Mix homogeneously, obtains mixture a；
D, adding carboxymethyl starch sodium, mix homogeneously in mixture a, add polyvinylpolypyrrolidone, mixing is all
Even, obtain mixture b；
E, microcrystalline Cellulose is mixed homogeneously with lactose, add metronidazole, mix homogeneously, obtain mixture c；
F, mixture b is mixed homogeneously with mixture c, be eventually adding micropowder silica gel and magnesium stearate, cross 20 mesh
Sieve mixing；
G, carry out intermediates content detection, determine direct compression after tablet weight, obtain metronidazole solid preparation.
The third aspect of the invention is to provide the preparation method of another metronidazole solid preparation, uses dry method
Pelletizing press sheet, specifically includes following steps:
A, by finely ground for metronidazole mistake 80 mesh sieve；
B, by microcrystalline Cellulose, lactose, mannitol, polyvinylpolypyrrolidone, carboxymethyl starch sodium, menthol,
Micropowder silica gel, magnesium stearate cross 40 mesh sieves respectively, standby；
C, employing equal increments method, first mix homogeneously menthol with equivalent mannitol, adds residue mannitol,
Mix homogeneously, obtains mixture a；
D, mixture a add carboxymethyl starch sodium, mix homogeneously, add polyvinylpolypyrrolidone, mix homogeneously,
Obtain mixture b；
E, microcrystalline Cellulose are mixed homogeneously with lactose, add metronidazole mix homogeneously, obtain mixture c；
F, mixture b are mixed homogeneously with mixture c, add micropowder silica gel and the recipe quantity half of recipe quantity half
Magnesium stearate, mixing；
G, tabletting: slice, thin piece Hardness Control is 4～7kg；
H, pulverizing: pulverize with 20 mesh crushing and pelletizing machines, obtain mixed powder e after pulverizing；
I, always mix: mixed powder adds micropowder silica gel and the magnesium stearate of residue half amount；
J, carry out intermediates content detection, determine tabletting after tablet weight, obtain metronidazole solid preparation.
The metronidazole solid preparation specification using above two method to prepare be 20mg/ sheet or 50mg/ sheet or other
The specification required.
The present invention uses technique scheme, compared with prior art, has the following technical effect that the present invention adopts
With direct powder compression and dry granulation tablet forming technique, prepare the rapid disintegrate in saliva of metronidazole oral cavity disintegration tablet and divide
Dissipating for fine particle, drug-eluting is accelerated, and big in oral cavity and gastrointestinal tract area distributions, absorption point is many, can improve
Its bioavailability.For the patient such as child, old people, oral cavity disintegration tablet is taken medicine conveniently, it is not necessary to water, also need not
Chew, improve the compliance of patient, improve the effectiveness of clinical treatment.
Detailed description of the invention
The invention provides a kind of taking convenience, low cost and to the rapid-action metronidazole solid preparation of indication and
Its preparation method.Below by specific embodiment, the present invention is carried out detailed and concrete introduction, so that preferably
Understand the present invention, but following embodiment is not limiting as the scope of the invention.
The preparation of embodiment 1 metronidazole solid preparation
1.1 each amounts of components are as follows:
1.2 use direct powder compression, comprise the following steps:
A, by finely ground for 30g metronidazole mistake 80 mesh sieve；
B, by 30g microcrystalline Cellulose, 20g lactose, 8g mannitol, 8g polyvinylpolypyrrolidone, 15g carboxymethyl form sediment
Powder sodium, 2g menthol, 0.5g micropowder silica gel, 0.5g magnesium stearate cross 40 mesh sieves respectively, standby；
C, employing equal increments method, the 2g menthol after first sieving is mixed homogeneously with 2g mannitol, adds surplus
Remaining 6g mannitol, mix homogeneously, obtain mixture a；
D, in mixture a add 15g carboxymethyl starch sodium, mix homogeneously, add 8g polyvinylpolypyrrolidone,
Mix homogeneously, obtains mixture b；
E, 30g microcrystalline Cellulose is mixed homogeneously with 20g lactose, add 30g metronidazole, mix homogeneously,
Obtain mixture c；
F, mixture b is mixed homogeneously with mixture c, is eventually adding 0.6 micropowder silica gel and 0.6g magnesium stearate,
Cross 20 mesh sieve mixings；
G, carrying out intermediates content detection, determine direct compression after tablet weight, to obtain final product, prepared lot number is GY1A's
Metronidazole solid preparation, for 20mg/ sheet.
1.3 use dry granulation tablettings, specifically include following steps:
A, by finely ground for 30g metronidazole mistake 80 mesh sieve；
B, by 30g microcrystalline Cellulose, 20g lactose, 8g mannitol, 8g polyvinylpolypyrrolidone, 15g carboxymethyl form sediment
Powder sodium, 2g menthol, 0.5g micropowder silica gel, 0.5g magnesium stearate cross 40 mesh sieves respectively, standby；
C, employing equal increments method, the 2g menthol after first sieving is mixed homogeneously with 2g mannitol, adds surplus
Remaining 6g mannitol, mix homogeneously, obtain mixture a；
D, in mixture a add 15g carboxymethyl starch sodium, mix homogeneously, add 8g polyvinylpolypyrrolidone,
Mix homogeneously, obtains mixture b；
E, 30g microcrystalline Cellulose is mixed homogeneously with 20g lactose, add 30g metronidazole, mix homogeneously,
Obtain mixture c；
F, mixture b are mixed homogeneously with mixture c, add 0.3g micropowder silica gel and 0.3g magnesium stearate, mixing；
G, tabletting: slice, thin piece Hardness Control is 4～7kg；
H, pulverizing: pulverize with 20 mesh crushing and pelletizing machines, obtain mixed powder e after pulverizing；
I, always mix: mixed powder adds remaining 0.3g micropowder silica gel and 0.3g magnesium stearate；
J, carrying out intermediates content detection, determine tabletting after tablet weight, to obtain final product, prepared lot number is the first nitre of GY2A
Azoles solid preparation, for 20mg/ sheet.
The preparation of embodiment 2 metronidazole solid preparation
2.1 each amounts of components are as follows:
2.2 preparation methoies: using direct powder compression, concrete operation step is same as in Example 1,
Prepared lot number is the metronidazole solid preparation of GY1B, for 20mg/ sheet.
2.3 preparation methoies: using dry granulation tabletting, concrete operation step is same as in Example 1, prepare
Lot number is the metronidazole solid preparation of GY2B, for 20mg/ sheet.
The preparation of embodiment 3 metronidazole solid preparation
3.1 each amounts of components are as follows:
3.2 preparation methoies: using direct powder compression, concrete operation step is same as in Example 1,
Prepared lot number is the metronidazole solid preparation of GY1C, for 20mg/ sheet.
3.3 preparation methoies: using dry granulation tabletting, concrete operation step is same as in Example 1, prepare
Lot number is the metronidazole solid preparation of GY2C, for 20mg/ sheet.
Comparative example 1 uses the preparation method of Chinese patent CN101658502A, prepares and embodiment of the present invention 1-3
The metronidazole sustained-release tablets that tablet weight is identical, for 20mg/ sheet.
Comparative example 2 uses the preparation method of Chinese patent CN104887636A, prepares and embodiment of the present invention 1-3
The Metronidazole Tablet that tablet weight is identical, for 20mg/ sheet.
Comparative example 3 uses the preparation method of Chinese patent CN1452963A, prepares and embodiment of the present invention 1-3 sheet
The Protostat that heavy phase is same, for 20mg/ sheet.
Analyze and measure:
(lot number is respectively as follows: to prepare above-described embodiment 1-3 six batch sample respectively according to two kinds of preparation methoies of the present invention
GY1A, GY1B, GY1C, GY2A, GY3B, GY3C), and right with take existing technique to prepare
Ratio 1-3 sample carries out conventional sense, testing result such as following table:
From above-mentioned detection date comprision, use the metronidazole solid preparation (mouth that the inventive method prepares
Disintegrating tablet) taking convenience, in good taste, dissolution release is fast, can significantly improve bioavailability, and preparation method is simple
Feasible, processing step is simple, and low cost is suitable for promotion and application widely.
Being described in detail the specific embodiment of the present invention above, but it is intended only as example, the present invention is also
It is not restricted to particular embodiments described above.To those skilled in the art, any the present invention is carried out
Equivalent modifications and substitute the most all among scope of the invention.Therefore, without departing from the spirit of the present invention and model
Enclose lower made impartial conversion and amendment, all should contain within the scope of the invention.
Claims (4)
1. a metronidazole solid preparation, it is characterised in that in parts by mass, including following components:
Metronidazole solid preparation the most according to claim 1, it is characterised in that in parts by mass, including with
Lower component:
3. the preparation method of metronidazole solid preparation as claimed in claim 1, it is characterised in that use powder direct
Tabletting, specifically includes following steps:
A, by finely ground for metronidazole mistake 80 mesh sieve；
B, by microcrystalline Cellulose, lactose, mannitol, polyvinylpolypyrrolidone, carboxymethyl starch sodium, menthol, micro-
Powder silica gel, magnesium stearate cross 40 mesh sieves respectively, standby；
C, employing equal increments method, first mix homogeneously menthol with the mannitol of equivalent, adds residue mannitol,
Mix homogeneously, obtains mixture a；
D, adding carboxymethyl starch sodium, mix homogeneously in mixture a, add polyvinylpolypyrrolidone, mixing is all
Even, obtain mixture b；
E, microcrystalline Cellulose is mixed homogeneously with lactose, add metronidazole, mix homogeneously, obtain mixture c；
F, mixture b is mixed homogeneously with mixture c, be eventually adding micropowder silica gel and magnesium stearate, cross 20 mesh
Sieve mixing；
G, carry out intermediates content detection, determine direct compression after tablet weight, obtain metronidazole solid preparation.
4. the preparation method of metronidazole solid preparation as claimed in claim 1, it is characterised in that use dry granulation
Tabletting, specifically includes following steps:
A, by finely ground for metronidazole mistake 80 mesh sieve；
B, by microcrystalline Cellulose, lactose, mannitol, polyvinylpolypyrrolidone, carboxymethyl starch sodium, menthol,
Micropowder silica gel, magnesium stearate cross 40 mesh sieves respectively, standby；
C, employing equal increments method, first mix homogeneously menthol with equivalent mannitol, adds residue mannitol,
Mix homogeneously, obtains mixture a；
D, mixture a add carboxymethyl starch sodium, mix homogeneously, add polyvinylpolypyrrolidone, mix homogeneously,
Obtain mixture b；
E, microcrystalline Cellulose are mixed homogeneously with lactose, add metronidazole mix homogeneously, obtain mixture c；
F, mixture b are mixed homogeneously with mixture c, add micropowder silica gel and the recipe quantity half of recipe quantity half
Magnesium stearate, mixing；
G, tabletting: slice, thin piece Hardness Control is 4～7kg/cm2；
H, pulverizing: pulverize with 20 mesh crushing and pelletizing machines, obtain mixed powder e after pulverizing；
I, always mix: mixed powder e adds micropowder silica gel and the magnesium stearate of residue half amount；
J, carry out intermediates content detection, determine tabletting after tablet weight, obtain metronidazole solid preparation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610023708.8A CN106137988A (en) | 2016-01-14 | 2016-01-14 | A kind of metronidazole solid preparation and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610023708.8A CN106137988A (en) | 2016-01-14 | 2016-01-14 | A kind of metronidazole solid preparation and preparation method thereof |
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| Publication Number | Publication Date |
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| CN106137988A true CN106137988A (en) | 2016-11-23 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201610023708.8A Pending CN106137988A (en) | 2016-01-14 | 2016-01-14 | A kind of metronidazole solid preparation and preparation method thereof |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109276551A (en) * | 2018-11-28 | 2019-01-29 | 武汉长联来福制药股份有限公司 | A kind of Ornidazole oral disintegrating tablet and preparation method thereof |
| CN109620813A (en) * | 2019-02-21 | 2019-04-16 | 武汉同济现代医药科技股份有限公司 | A kind of oral solid tablet and preparation method thereof containing metronidazole |
| CN110101675A (en) * | 2019-05-07 | 2019-08-09 | 安徽金太阳生化药业有限公司 | A kind of preparation method of Metronidazole Tablet |
| CN110917161A (en) * | 2019-12-31 | 2020-03-27 | 北京鑫开元医药科技有限公司 | Metronidazole tablet and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1817346A (en) * | 2006-03-28 | 2006-08-16 | 陈益智 | Benzoyl metronidazole dispersion tablets and preparation thereof |
| CN104887636A (en) * | 2015-06-16 | 2015-09-09 | 吉林万通药业集团郑州万通复升药业股份有限公司 | Metronidazole tablet and preparation method thereof |
-
2016
- 2016-01-14 CN CN201610023708.8A patent/CN106137988A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1817346A (en) * | 2006-03-28 | 2006-08-16 | 陈益智 | Benzoyl metronidazole dispersion tablets and preparation thereof |
| CN104887636A (en) * | 2015-06-16 | 2015-09-09 | 吉林万通药业集团郑州万通复升药业股份有限公司 | Metronidazole tablet and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 张奇编: "《军用药物制剂工程学》", 30 April 2012 * |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109276551A (en) * | 2018-11-28 | 2019-01-29 | 武汉长联来福制药股份有限公司 | A kind of Ornidazole oral disintegrating tablet and preparation method thereof |
| CN109620813A (en) * | 2019-02-21 | 2019-04-16 | 武汉同济现代医药科技股份有限公司 | A kind of oral solid tablet and preparation method thereof containing metronidazole |
| CN110101675A (en) * | 2019-05-07 | 2019-08-09 | 安徽金太阳生化药业有限公司 | A kind of preparation method of Metronidazole Tablet |
| CN110917161A (en) * | 2019-12-31 | 2020-03-27 | 北京鑫开元医药科技有限公司 | Metronidazole tablet and preparation method thereof |
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Application publication date: 20161123 |