CN106236722A - A kind of preparation method of cefotiam hexetil dispersible tablet - Google Patents
A kind of preparation method of cefotiam hexetil dispersible tablet Download PDFInfo
- Publication number
- CN106236722A CN106236722A CN201610823549.XA CN201610823549A CN106236722A CN 106236722 A CN106236722 A CN 106236722A CN 201610823549 A CN201610823549 A CN 201610823549A CN 106236722 A CN106236722 A CN 106236722A
- Authority
- CN
- China
- Prior art keywords
- weight portion
- weight
- cefotiam hexetil
- carboxymethylstach sodium
- dispersible tablet
- 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.)
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Classifications
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- 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
- A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
- A61K31/546—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine containing further heterocyclic rings, e.g. cephalothin
-
- 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 the preparation method of a kind of cefotiam hexetil dispersible tablet, it comprises the following steps: weighs, prepare binding agent, make wet grain, mixed, tabletting dry, total.Be uniformly dispersed, dissolution is good, tablet is smooth, uniform, cleanliness factor is good dispersible tablet；The inventive method is simple to operate, low to the requirement of equipment, preparation is convenient, be applicable to industrialization large-scale production.
Description
Technical field
The invention belongs to field of medicine preparations, be specifically related to the preparation method of a kind of cefotiam hexetil dispersible tablet.
Background technology
In recent years, the use of Antibiotics Abroad has gradually been tended to oral administration by drug administration by injection, and newly developed go out many
Oral precursor antibiotic medicine.Cefotiam hexetil is former grinds unit for Japan Wu Tian chemical industry joint-stock company, is by injection
The antibiotic of orally available absorption after the esterification of antibiotic cefotiam.This product has a broad antifungal spectrum, equal to gram positive bacteria and negative bacterium
Demonstrate good antibacterial action.This product self there is no antibacterial action, be oral after be hydrolyzed to rapidly cephalo at intestinal mucosa and replace
Pacify (CTM) and absorbed, be transported in blood after being hydrolyzed to antibacterial activity main body cefotiam.Blood drug level is dose-dependent.
In being administered latter 24 hours, 4 O% are through renal excretion.The best to the transhipment of sputum, otorrhea, nose juice, bile, almond, skin etc..This product
Good, also without specific question in terms of safety to various infection clinical effectiveness.As the prodrug of cefotiam, it is can be wide
The general high oral cephalosporin class antibiotic of serviceability being applied to clinic.Cephalo it is hydrolyzed to rapidly after cefotiam hexetil oral administration
For peace (CTM), cefotiam is identical with the most oral cephalosporin with the antibacterial activity of negative bacterium to Grain-positive, and right
Beta-lactamase is stable.This product staphylococcus aureus to being clinically separated, coagulase negative staphylococcus, streptococcus pneumoniae,
Gonococcus, resistance to ampicillin gonococcus (AB PC), moraxelle catarrhalis, escherichia coli, citric acid Pseudomonas, Providencia,
Micrococcus scarlatinae, streptococcus agalactiae, klebsiella pneumoniae, proteus mirabilis, Hemophilus influenzae, all have relatively
Strong antibacterial activity, MIC is lower than cephalexin, Cefaclor.
Summary of the invention
It is an object of the invention to overcome the shortcoming of prior art, it is provided that the preparation side of a kind of cefotiam hexetil dispersible tablet
Method, the method is simple to operate, equipment requirements is the highest, and the cefotiam hexetil dispersible tablet of preparation is uniformly dispersed, stable in properties, disintegrate are fast
Speed, bioavailability are high.
The purpose of the present invention is achieved through the following technical solutions: the preparation method of a kind of cefotiam hexetil dispersible tablet, its
Being characterised by, it comprises the following steps:
S1. weigh: weigh each raw material by following formula proportion, standby；Described formula is: cefotiam hexetil 100～300 weight
Part, starch 35～47 weight portion, microcrystalline Cellulose 50～70 weight portion, carboxymethylstach sodium 35～57 weight portion, lactose 1～10 weight
Amount part, L-hydroxypropylcellulose 1.3～8 weight portion, PVP K30 1.2～8.5 weight portion, silica 1 5～28 weight portion, hard
Fatty acid magnesium 1～10 weight portion, ethanol 32～50 weight portion；
S2. binding agent is prepared: ethanol is configured to the solution that concentration is 30%, and is joined by PVP K30 in ethanol solution,
Prepare binding agent；
S3. wet grain is made: by cefotiam hexetil, starch, lactose, L-hydroxypropylcellulose, account for the crystallite of microcrystalline Cellulose gross weight 70%
Cellulose, account for the carboxymethylstach sodium of carboxymethylstach sodium gross weight 60% and put into successively in granulator and be pre-mixed 1～5min, then will
Binding agent adds in the powder being pre-mixed, and stirs 3～7min, adds water and make the wet granular that mesh number is 16；
S4. being dried: loaded by wet grain in Fluidbedgranulatingdrier, controlling baking temperature is 70～80 DEG C, is dried to granule aqueous
Amount is 3～5%；
The most always mix: dried granule is added in mixer, add silicon dioxide, magnesium stearate, remaining carboxymethylstach sodium
And microcrystalline Cellulose, airtight mixing 15～25min, set the rotating speed of mixer as 5～10rad/min, i.e. prepare cefotiam
Ester dispersible tablet.
Preferably, described formula is: cefotiam hexetil 100 weight portion, starch 39.5 weight portion, microcrystalline Cellulose
60 weight portions, carboxymethylstach sodium 50 weight portion, lactose 5 weight portion, L-hydroxypropylcellulose 3.5 weight portion, PVP K30 4.5 weight
Amount part, silicon dioxide 20 weight portion, magnesium stearate 4.2 weight portion, ethanol 45 weight portion.
The invention have the advantages that
The present invention solves cefotiam hexetil at tableting processes by the lot of experiments to dispersible tablet prescription, the technique obtained
The sticking of middle appearance, sliver, take off the phenomenons such as lid, be uniformly dispersed, dissolution is good, tablet is smooth, uniform, cleanliness factor is good
Good dispersible tablet；The inventive method is simple to operate, low to the requirement of equipment, preparation is convenient, be applicable to industrialization large-scale production.
Detailed description of the invention
Below in conjunction with embodiment, the present invention will be further described, and protection scope of the present invention is not limited to following institute
State:
Embodiment 1: the preparation method of a kind of cefotiam hexetil dispersible tablet, it comprises the following steps:
S1. weigh: weigh each raw material by following formula proportion, standby；Described formula is: cefotiam hexetil 200 weight portion, starch
35 weight portions, microcrystalline Cellulose 50 weight portion, carboxymethylstach sodium 35 weight portion, lactose 1 weight portion, L-hydroxypropylcellulose 1.3 weight
Amount part, PVP K30 1.2 weight portion, silica 15 weight portion, magnesium stearate 1 weight portion, ethanol 32 weight portion.
S2. binding agent is prepared: ethanol is configured to the solution that concentration is 30%, and PVP K30 is joined ethanol solution
In, prepare binding agent；
S3. wet grain is made: by cefotiam hexetil, starch, lactose, L-hydroxypropylcellulose, account for the crystallite of microcrystalline Cellulose gross weight 70%
Cellulose, account for the carboxymethylstach sodium of carboxymethylstach sodium gross weight 60% and put into successively in granulator and be pre-mixed 1min, then will bonding
Agent adds in the powder being pre-mixed, and stirs 3min, adds water and make the wet granular that mesh number is 16；
S4. being dried: loaded in Fluidbedgranulatingdrier by wet grain, controlling baking temperature is 70 DEG C, is dried to granule water content and is
3%；
The most always mix: dried granule is added in mixer, add silicon dioxide, magnesium stearate, remaining carboxymethylstach sodium
And microcrystalline Cellulose, airtight mixing 15min, set the rotating speed of mixer as 5rad/min, i.e. prepare cefotiam hexetil dispersible tablet.
Embodiment 2: the preparation method of a kind of cefotiam hexetil dispersible tablet, it comprises the following steps:
S1. weigh: weigh each raw material by following formula proportion, standby；Described formula is: cefotiam hexetil 100 weight portion, starch
47 weight portions, microcrystalline Cellulose 70 weight portion, carboxymethylstach sodium 57 weight portion, lactose 10 weight portion, L-hydroxypropylcellulose 8 weight
Part, PVP K30 8.5 weight portion, silicon dioxide 28 weight portion, magnesium stearate 10 weight portion, ethanol 50 weight portion；
S2. binding agent is prepared: ethanol is configured to the solution that concentration is 30%, and is joined by PVP K30 in ethanol solution,
Prepare binding agent；
S3. wet grain is made: by cefotiam hexetil, starch, lactose, L-hydroxypropylcellulose, account for the crystallite of microcrystalline Cellulose gross weight 70%
Cellulose, account for the carboxymethylstach sodium of carboxymethylstach sodium gross weight 60% and put into successively in granulator and be pre-mixed 5min, then will bonding
Agent adds in the powder being pre-mixed, and stirs 7min, adds water and make the wet granular that mesh number is 16；
S4. being dried: loaded in Fluidbedgranulatingdrier by wet grain, controlling baking temperature is 80 DEG C, is dried to granule water content and is
5%；
The most always mix: dried granule is added in mixer, add silicon dioxide, magnesium stearate, remaining carboxymethylstach sodium
And microcrystalline Cellulose, airtight mixing 25min, set the rotating speed of mixer as 10rad/min, i.e. prepare cefotiam hexetil dispersion
Sheet.
Embodiment 3: the preparation method of a kind of cefotiam hexetil dispersible tablet, it comprises the following steps:
S1. weigh: weigh each raw material by following formula proportion, standby；Described formula is: cefotiam hexetil 250 weight portion, starch
15 weight portions, microcrystalline Cellulose 55 weight portion, carboxymethylstach sodium 52 weight portion, lactose 8 weight portion, L-hydroxypropylcellulose 3 weight
Part, PVP K30 8 weight portion, silica 18 weight portion, magnesium stearate 9 weight portion, ethanol 48 weight portion；
S2. binding agent is prepared: ethanol is configured to the solution that concentration is 30%, and is joined by PVP K30 in ethanol solution,
Prepare binding agent；
S3. wet grain is made: by cefotiam hexetil, starch, lactose, L-hydroxypropylcellulose, account for the crystallite of microcrystalline Cellulose gross weight 70%
Cellulose, account for the carboxymethylstach sodium of carboxymethylstach sodium gross weight 60% and put into successively in granulator and be pre-mixed 2min, then will bonding
Agent adds in the powder being pre-mixed, and stirs 4min, adds water and make the wet granular that mesh number is 16；
S4. being dried: loaded in Fluidbedgranulatingdrier by wet grain, controlling baking temperature is 73 DEG C, is dried to granule water content and is
4%；
The most always mix: dried granule is added in mixer, add silicon dioxide, magnesium stearate, remaining carboxymethylstach sodium
And microcrystalline Cellulose, airtight mixing 18min, set the rotating speed of mixer as 7rad/min, i.e. prepare cefotiam hexetil dispersible tablet.
Embodiment 4: the preparation method of a kind of cefotiam hexetil dispersible tablet, it comprises the following steps:
S1. weigh: weigh each raw material by following formula proportion, standby；Described formula is: cefotiam hexetil 300 weight portion, starch
39.5 weight portions, microcrystalline Cellulose 60 weight portion, carboxymethylstach sodium 50 weight portion, lactose 5 weight portion, L-hydroxypropylcellulose 3.5
Weight portion, PVP K30 4.5 weight portion, silicon dioxide 20 weight portion, magnesium stearate 4.2 weight portion, ethanol 45 weight portion；
S2. binding agent is prepared: ethanol is configured to the solution that concentration is 30%, and is joined by PVP K30 in ethanol solution,
Prepare binding agent；
S3. wet grain is made: by cefotiam hexetil, starch, lactose, L-hydroxypropylcellulose, account for the crystallite of microcrystalline Cellulose gross weight 70%
Cellulose, account for the carboxymethylstach sodium of carboxymethylstach sodium gross weight 60% and put into successively in granulator and be pre-mixed 4min, then will bonding
Agent adds in the powder being pre-mixed, and stirs 6min, adds water and make the wet granular that mesh number is 16；
S4. being dried: loaded in Fluidbedgranulatingdrier by wet grain, controlling baking temperature is 78 DEG C, is dried to granule water content and is
4.8%；
The most always mix: dried granule is added in mixer, add silicon dioxide, magnesium stearate, remaining carboxymethylstach sodium
And microcrystalline Cellulose, airtight mixing 22min, set the rotating speed of mixer as 8rad/min, i.e. prepare cefotiam hexetil dispersible tablet.
Claims (2)
1. the preparation method of a cefotiam hexetil dispersible tablet, it is characterised in that it comprises the following steps:
S1. weigh: weigh each raw material by following formula proportion, standby；Described formula is: cefotiam hexetil 100～300 weight
Part, starch 35～47 weight portion, microcrystalline Cellulose 50～70 weight portion, carboxymethylstach sodium 35～57 weight portion, lactose 1～10 weight
Amount part, L-hydroxypropylcellulose 1.3～8 weight portion, PVP K30 1.2～8.5 weight portion, silica 1 5～28 weight portion, hard
Fatty acid magnesium 1～10 weight portion, ethanol 32～50 weight portion；
S2. binding agent is prepared: ethanol is configured to the solution that concentration is 30%, and is joined by PVP K30 in ethanol solution,
Prepare binding agent；
S3. wet grain is made: by cefotiam hexetil, starch, lactose, L-hydroxypropylcellulose, account for the crystallite of microcrystalline Cellulose gross weight 70%
Cellulose, account for the carboxymethylstach sodium of carboxymethylstach sodium gross weight 60% and put into successively in granulator and be pre-mixed 1～5min, then will
Binding agent adds in the powder being pre-mixed, and stirs 3～7min, adds water and make the wet granular that mesh number is 16；
S4. being dried: loaded by wet grain in Fluidbedgranulatingdrier, controlling baking temperature is 70～80 DEG C, is dried to granule aqueous
Amount is 3～5%；
The most always mix: dried granule is added in mixer, add silicon dioxide, magnesium stearate, remaining carboxymethylstach sodium
And microcrystalline Cellulose, airtight mixing 15～25min, set the rotating speed of mixer as 5～10rad/min, i.e. prepare cefotiam
Ester dispersible tablet.
The preparation method of a kind of cefotiam hexetil dispersible tablet the most as claimed in claim 1, it is characterised in that described formula is:
Cefotiam hexetil 100 weight portion, starch 39.5 weight portion, microcrystalline Cellulose 60 weight portion, carboxymethylstach sodium 50 weight portion, lactose
5 weight portions, L-hydroxypropylcellulose 3.5 weight portion, PVP K30 4.5 weight portion, silicon dioxide 20 weight portion, magnesium stearate 4.2
Weight portion, ethanol 45 weight portion.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610823549.XA CN106236722A (en) | 2016-09-14 | 2016-09-14 | A kind of preparation method of cefotiam hexetil dispersible tablet |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610823549.XA CN106236722A (en) | 2016-09-14 | 2016-09-14 | A kind of preparation method of cefotiam hexetil dispersible tablet |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106236722A true CN106236722A (en) | 2016-12-21 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610823549.XA Pending CN106236722A (en) | 2016-09-14 | 2016-09-14 | A kind of preparation method of cefotiam hexetil dispersible tablet |
Country Status (1)
| Country | Link |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1004318A2 (en) * | 1991-06-21 | 2000-05-31 | Takeda Chemical Industries, Ltd. | Cyclodextrin composition |
| CN102370621A (en) * | 2010-08-19 | 2012-03-14 | 北京润德康医药技术有限公司 | Solid preparation with cefotiam hexetil as active component |
| CN105193753A (en) * | 2015-10-30 | 2015-12-30 | 成都通德药业有限公司 | Preparation method of azithromycin dispersible tablets |
-
2016
- 2016-09-14 CN CN201610823549.XA patent/CN106236722A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1004318A2 (en) * | 1991-06-21 | 2000-05-31 | Takeda Chemical Industries, Ltd. | Cyclodextrin composition |
| CN102370621A (en) * | 2010-08-19 | 2012-03-14 | 北京润德康医药技术有限公司 | Solid preparation with cefotiam hexetil as active component |
| CN105193753A (en) * | 2015-10-30 | 2015-12-30 | 成都通德药业有限公司 | Preparation method of azithromycin dispersible tablets |
Non-Patent Citations (1)
| Title |
|---|
| 褚良，等: "盐酸头孢替安酯的聚合物检查方法的建立与验证", 《哈尔滨医药》 * |
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| PB01 | Publication | ||
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| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20161221 |