CN107582530A - A kind of Kotabarb and preparation method thereof - Google Patents
A kind of Kotabarb and preparation method thereof Download PDFInfo
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- CN107582530A CN107582530A CN201710405029.1A CN201710405029A CN107582530A CN 107582530 A CN107582530 A CN 107582530A CN 201710405029 A CN201710405029 A CN 201710405029A CN 107582530 A CN107582530 A CN 107582530A
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- pregelatinized starch
- phenobarbital
- magnesium stearate
- lactose monohydrate
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Abstract
A kind of Kotabarb and preparation method thereof.It is made up of the supplementary material of following mass fraction：25~33 parts of phenobarbital, 55~65 parts of lactose monohydrate, microcrystalline cellulose：10~20 parts, pregelatinized starch：10~20 parts, magnesium stearate：0.2~1.5 part, silica：0.3~1.5 part.The present invention prepares phenobarbitone tablet using wet granulation technology, mobility of particle and compressibility prepared by the technique is good, it is up-to-standard, property is stable, the tablet rate of release is very fast, for 20min dissolution rates up to more than 90%, the medicine has significant curative effect to treatment calmness, hypnosis, anticonvulsion and Kang Dian Epilepsy in PH4.0 buffer solutions.
Description
Technical field
The invention belongs to field of pharmaceutical preparations.Specifically, the present invention relates to a kind of Kotabarb and its preparation side
Method.
Background technology
Phenobarbital (Phenobarbital), chemical name：5- ethyl -5- phenyl -2,4,6 (1H, 3H, 5H)-pyrimidines three
Ketone, molecular formula C12H12N2O3, molecular weight 232, chemical structural formula are：
Phenobarbital is hypnotic sedative agent, anticonvulsive drug, is the Typical Representative of long-acting barbiturates, and the suppression to maincenter is made
Increased with dosage, show as calmness, hypnosis, anticonvulsion and Kang Dian Epilepsy, heavy dose has bright to cardiovascular system, respiratory system
Aobvious suppression, can excessively benumb that medullary respiratory center is lethal, external electro physiology experiment see phenobarbital make the chlorine of nerve cell from
Subchannel opens, and cell crosses polarization, intends the effect like γ-aminobutyric acid (GABA), and the phenobarbital for the treatment of concentration can reduce paddy
The excitation of propylhomoserin, the inhibitory action of reinforcing gamma -amino butyric acid, suppress the cynapse of central nervous system list and polusnaptic transmission,
The high-frequency discharge of Yi Epilepsy stoves and its spread to surrounding, reduce gastric secretion, reduce stomach tension force, pass through induced glucose aldehydic acid and turn
Enzyme combination bilirubin is moved so as to reduce the concentration of bilirubin, dependence, including psychological dependence and physiological dependence can be produced.
The content of the invention
Present invention aims at provide a kind of method that phenobarbitone tablet is prepared using wet granulation technique, medicine of the present invention
For calmness, hypnosis, anticonvulsion and Kang Dian Epilepsy, there is significant curative effect.
To achieve the above object, the present invention uses following technical scheme：
A kind of Kotabarb, it is made up of the supplementary material of following mass fraction：
25~33 parts of phenobarbital, 55~65 parts of lactose monohydrate, microcrystalline cellulose：10~20 parts, pregelatinized starch：10~
20 parts, magnesium stearate：0.2~1.5 part, silica：0.3~1.5 part.
Preferably, the supplementary material includes 30 parts of phenobarbital, 60 parts of lactose monohydrate, microcrystalline cellulose according to mass parts meter
15 parts, 12 parts of pregelatinized starch, 0.5 part of magnesium stearate, 0.5 part of silica.
Present invention also offers a kind of preparation method of phenobarbital, it comprises the following steps：
Appropriate pregelatinized starch is weighed, boiling water is added, stirs, the binder aqueous solution that concentration is 8% is made, it is standby
With；
Then each supplementary material is accurately taken according to mass fraction, phenobarbital, lactose monohydrate and pregelatinized starch are placed in wet
Premix 20min in method granulator, it is then that 8% binder aqueous solution is added in granulator by several times by concentration, wet mixing 10min,
70-75 DEG C of fluidized drying of wet granular through 20 mesh sieve whole grains, adds magnesium stearate and silica, mixed to 2.0~5.5%
20min, tabletting.
The present invention prepares phenobarbitone tablet using wet granulation technology, and mobility of particle and compressibility prepared by the technique is equal
Well, up-to-standard, property is stable, and the tablet rate of release is very fast, in PH4.0 buffer solutions 20min dissolution rates up to 90% with
On, the medicine has significant curative effect to treatment calmness, hypnosis, anticonvulsion and Kang Dian Epilepsy.
Embodiment
In order to which the present invention is apparent to understand, with reference to specific embodiment, the invention will be further described, to help
Understand present disclosure.
Embodiment one：
Phenobarbitone tablet in the present embodiment is scored tablet, be made up of the supplementary material of following quality (2000, phenobarbital
30mg/ pieces)：It is phenobarbitone tablet 60g, lactose monohydrate 102g, microcrystalline cellulose 30g, pregelatinized starch 42g, silica 1 g, hard
Fatty acid magnesium 1g.
Preparation method：Appropriate pregelatinized starch is weighed, boiling water is added, stirs, the adhesive water that 56g concentration is 8% is made
Solution, it is standby；Then each supplementary material is accurately taken according to mass fraction, phenobarbital, lactose monohydrate and pregelatinized starch are placed in
Premix 20min in wet granulator, it is then that 8% binder aqueous solution is added in granulator by several times by concentration, wet mixing
10min, 70-75 DEG C of fluidized drying of wet granular to 2.0~5.5%, through 20 mesh sieve whole grains, add magnesium stearate and titanium dioxide
Silicon, mixes 20min, tabletting, measure 5 in pH4.0 media, 10,15,20,30min accumulation dissolution rate be followed successively by 80.2%,
90.1%th, 97.5%, 100.4%, 101.2%.
Embodiment two
Phenobarbitone tablet in the present embodiment is scored tablet, be made up of the supplementary material of following quality (2000, phenobarbital
30mg/ pieces)：Phenobarbitone tablet 60g, lactose monohydrate 108g, microcrystalline cellulose：30g, pregelatinized starch 36g, microcrystalline cellulose
30g, silica 1 g, magnesium stearate 1g.
Preparation method：Appropriate pregelatinized starch is weighed, boiling water is added, stirs, the adhesive water that 56g concentration is 8% is made
Solution, it is standby；Then each supplementary material is accurately taken according to mass fraction, phenobarbital, lactose monohydrate and pregelatinized starch are placed in
Premix 20min in wet granulator, it is then that 8% binder aqueous solution is added in granulator by several times by concentration, wet mixing
10min, 70-75 DEG C of fluidized drying of wet granular to 2.0~5.5%, through 20 mesh sieve whole grains, add magnesium stearate and titanium dioxide
Silicon, mixes 20min, tabletting, measure 5 in pH4.0 media, 10,15,20,30min accumulation dissolution rate be followed successively by 73.9%,
84.5%th, 88.3%, 96.8%, 100.9%.
Embodiment three
Phenobarbitone tablet in the present embodiment is scored tablet, be made up of the supplementary material of following quality (2000, phenobarbital
30mg/ pieces)：Phenobarbitone tablet 60g, lactose monohydrate 120g, microcrystalline cellulose：30g, pregelatinized starch 24g, microcrystalline cellulose
30g, silica 1 g, magnesium stearate 1g.
Preparation method：Appropriate pregelatinized starch is weighed, boiling water is added, stirs, the adhesive water that 56g concentration is 8% is made
Solution, it is standby；Then each supplementary material is accurately taken according to mass fraction, phenobarbital, lactose monohydrate and pregelatinized starch are placed in
Premix 20min in wet granulator, it is then that 8% binder aqueous solution is added in granulator by several times by concentration, wet mixing
10min, 70-75 DEG C of fluidized drying of wet granular to 2.0~5.5%, through 20 mesh sieve whole grains, add magnesium stearate and titanium dioxide
Silicon, mixes 20min, tabletting, measure 5 in pH4.0 media, 10,15,20,30min accumulation dissolution rate be followed successively by 68.3%,
78.9%th, 85.5%, 96.8%, 100.9%.
Example IV
Phenobarbitone tablet in the present embodiment is scored tablet, be made up of the raw material of following quality (2000, phenobarbital
30mg/ pieces)：Phenobarbitone tablet 60g, lactose monohydrate 120g, microcrystalline cellulose：30g, pregelatinized starch 24g, microcrystalline cellulose
30g, silica 1 g, magnesium stearate 1g.
Preparation method：Appropriate pregelatinized starch is weighed, boiling water is added, stirs, the adhesive water that 64g concentration is 8% is made
Solution, it is standby；Then each supplementary material is accurately taken according to mass fraction, phenobarbital, lactose monohydrate and pregelatinized starch are placed in
Premix 20min in wet granulator, it is then that 8% binder aqueous solution is added in granulator by several times by concentration, wet mixing
10min, 70-75 DEG C of fluidized drying of wet granular to 2.0~5.5%, through 20 mesh sieve whole grains, add magnesium stearate and titanium dioxide
Silicon, mixes 20min, tabletting, measure 5 in pH4.0 media, 10,15,20,30min accumulation dissolution rate be followed successively by 43.6,
74.5%th, 91.8%, 96.4%, 99.8%.
Embodiment five
Phenobarbitone tablet in the present embodiment is scored tablet, be made up of the raw material of following quality (2000, phenobarbital
30mg/ pieces)：Phenobarbitone tablet 60g, lactose monohydrate 120g, microcrystalline cellulose：30g, pregelatinized starch 24g, microcrystalline cellulose
30g, silica 1 g, magnesium stearate 1g.
Preparation method：Appropriate pregelatinized starch is weighed, boiling water is added, stirs, the adhesive water that 64g concentration is 8% is made
Solution, it is standby；Then each supplementary material is accurately taken according to mass fraction, phenobarbital, lactose monohydrate and pregelatinized starch are placed in
Premix 20min in wet granulator, it is then that 8% binder aqueous solution is added in granulator by several times by concentration, wet mixing
10min, 70-75 DEG C of fluidized drying of wet granular to 2.0~5.5%, through 20 mesh sieve whole grains, add magnesium stearate and titanium dioxide
Silicon, mixes 20min, tabletting, obtain 5 in pH4.0 media, 10,15,20,30min accumulation dissolution rate be followed successively by 23.8,
43.2%th, 59.6%, 70.1%, 78.9%.
Test example：Phenobarbitone tablet is prepared according to method in embodiment one~tri- and embodiment, it is molten in PH4.0 media
Go out result and see the table below 1.
The embodiment one~tri- of table 1 dissolution measurement result in PH4.0 media：
It can be found out from upper table with dissolution result, with the increase of galactose ratio, dissolution rate slows down, and analysis reason may
It is because pregelatinized starch has certain disintegrating property, with the increase of its dosage, lactose dosage reduces, slice, thin piece water swelling energy
Power reduces, therefore disintegration is slack-off, and stripping quantity reduces, and it is fast that the dissolution of embodiment one~tri- grinds piece compared with phenobarbital original.
Phenobarbitone tablet is prepared according to method in example IV~five and embodiment, dissolution result is shown in PH4.0 media
Table 2 below.
Example IV~five of table 2 dissolution measurement result in PH4.0 media：
From table 5 it was found from dissolution result, example IV grinds that dissolution result is more similar, and dissolution is qualified to phenobarbital original；
With the increase of prescription binder dosage, dissolution has declined, and analysis reason is to meet water because of pregelatinized starch to excite its viscosity,
Therefore prescription disintegration rate is slack-off, and dissolution slows down therewith.
The present invention prepares phenobarbitone tablet using wet granulation technology, and the piece is scored tablet, and composition includes bulk drug benzene bar
It is made than appropriate with lactose monohydrate, pregelatinized starch, microcrystalline cellulose, silica and magnesium stearate, wherein lactose monohydrate and shallow lake
Powder is filler, and silica is glidant, and magnesium stearate is lubricant, and starch slurry is adhesive, particle prepared by the technique
Mobility and compressibility are good, up-to-standard, and property is stable, and the tablet rate of release is very fast, in PH4.0 buffer solutions
For 20min dissolution rates up to more than 90%, the medicine has significant curative effect to treatment calmness, hypnosis, anticonvulsion and Kang Dian Epilepsy.
Claims (3)
1. a kind of Kotabarb, it is characterised in that be made up of the supplementary material of following mass fraction：
25~33 parts of phenobarbital, 55~65 parts of lactose monohydrate, microcrystalline cellulose：10~20 parts, pregelatinized starch：10~20
Part, magnesium stearate：0.2~1.5 part, silica：0.3~1.5 part.
2. Kotabarb according to claim 1, it is characterised in that：The supplementary material includes benzene according to mass parts meter
30 parts of barbital, 60 parts of lactose monohydrate, 15 parts of microcrystalline cellulose, 12 parts of pregelatinized starch, 0.5 part of magnesium stearate, silica
0.5 part.
3. a kind of preparation method of phenobarbital, it is characterised in that it comprises the following steps：
Appropriate pregelatinized starch is weighed, boiling water is added, stirs, the binder aqueous solution that concentration is 8% is made, it is standby；
Then each supplementary material is accurately taken according to mass fraction, phenobarbital, lactose monohydrate and pregelatinized starch are placed in wet method system
Premix 20min in grain machine, it is then that 8% binder aqueous solution is added in granulator by several times by concentration, wet mixing 10min, wet
70-75 DEG C of fluidized drying of grain through 20 mesh sieve whole grains, adds magnesium stearate and silica, mixed to 2.0~5.5%
20min, tabletting.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201710405029.1A CN107582530A (en) | 2017-06-01 | 2017-06-01 | A kind of Kotabarb and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201710405029.1A CN107582530A (en) | 2017-06-01 | 2017-06-01 | A kind of Kotabarb and preparation method thereof |
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| CN107582530A true CN107582530A (en) | 2018-01-16 |
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Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006046933A1 (en) * | 2004-10-26 | 2006-05-04 | Viktor Olexandrovych Rybchuk | Sedative and spasmolytic medicinal agent and method for the production thereof (variants) |
| CN1819819A (en) * | 2003-05-07 | 2006-08-16 | 阿克纳公司 | Highly plastic granules for making fast melting tablets |
| CN101190225A (en) * | 2006-11-29 | 2008-06-04 | 天津市润拓生物技术有限公司 | Phenobarbitone chewable tablets for dog or cat |
| CN104147020A (en) * | 2014-08-08 | 2014-11-19 | 青岛中仁药业有限公司 | Anti-epileptic medicine composition and preparation method thereof |
| CN104288231A (en) * | 2014-10-23 | 2015-01-21 | 三峡大学仁和医院 | Medicine for treating refractory epilepsy |
| CN105147632A (en) * | 2015-09-30 | 2015-12-16 | 合肥华方医药科技有限公司 | Phenobarbital orally disintegrating tablets and preparation method thereof |
-
2017
- 2017-06-01 CN CN201710405029.1A patent/CN107582530A/en active Pending
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1819819A (en) * | 2003-05-07 | 2006-08-16 | 阿克纳公司 | Highly plastic granules for making fast melting tablets |
| WO2006046933A1 (en) * | 2004-10-26 | 2006-05-04 | Viktor Olexandrovych Rybchuk | Sedative and spasmolytic medicinal agent and method for the production thereof (variants) |
| CN101190225A (en) * | 2006-11-29 | 2008-06-04 | 天津市润拓生物技术有限公司 | Phenobarbitone chewable tablets for dog or cat |
| CN104147020A (en) * | 2014-08-08 | 2014-11-19 | 青岛中仁药业有限公司 | Anti-epileptic medicine composition and preparation method thereof |
| CN104288231A (en) * | 2014-10-23 | 2015-01-21 | 三峡大学仁和医院 | Medicine for treating refractory epilepsy |
| CN105147632A (en) * | 2015-09-30 | 2015-12-16 | 合肥华方医药科技有限公司 | Phenobarbital orally disintegrating tablets and preparation method thereof |
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Application publication date: 20180116 |