CN109925288A - A kind of glucocorticoid medicine tablet and preparation method thereof - Google Patents
A kind of glucocorticoid medicine tablet and preparation method thereof Download PDFInfo
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- CN109925288A CN109925288A CN201711364992.6A CN201711364992A CN109925288A CN 109925288 A CN109925288 A CN 109925288A CN 201711364992 A CN201711364992 A CN 201711364992A CN 109925288 A CN109925288 A CN 109925288A
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- methylprednisolone
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- medicine tablet
- glucocorticoid medicine
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Abstract
The invention belongs to field of pharmaceutical preparations, it is related to a kind of glucocorticoid medicine tablet and preparation method thereof.The bulk pharmaceutical chemicals of the tablet are 30 ~ 40 μm of granularity D90 of methylprednisolone, the preparation method include the following steps: bulk pharmaceutical chemicals after air-flow crushing successively with filler, disintegrating agent and mix lubricant it is uniform after tabletting, obtain finished tablet.The dissolution of glucocorticoid medicine tablet made of this method is fast, and stability is high, which improves production efficiency, reduce equipment energy consumption, is suitble to industrialized production.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, and in particular to a kind of glucocorticoid medicine tablet and preparation method thereof.
Background technique
Methylprednisolone is the glucocorticoid that Upjohn company, the U.S. succeeds in developing in the 1950s, is imitated in one kind
Glucocorticoid medicine, the maintenance therapy which can be used for after some urgent patient's first aids, have anti-inflammatory, immunosupress,
The pharmacological actions such as antiallergy, Hemorrhagic shock.The anti-inflammatory effect of the medicine is stronger, is equivalent to 5 times of hydrocortisone, and the 1.4 of prednisone
Times.In glucocorticoid, the affinity of methylprednisolone and glucocorticoid receptor is most strong, and the effect of mineralocorticoid sample (such as water,
Sodium retention) it is faint, it is weaker to the inhibiting effect of hypothalamus-pituitary-adrenal axis, therefore it is light " rebound phenomenon " occur after being discontinued
It is micro-.The product is clinically widely used because of the advantages of curative effect is high, Small side effects, is the developed countries such as the U.S., Britain, Japan
The kind that pharmacopeia is persistently recorded.
Methylprednisolone clinical indication is extensive, can play to patient's state of an illness and rapidly and effectively control, and former triturate is oral
It absorbs rapidly afterwards, internal 1.5-2.3h blood concentration reaches peak value.Methylprednisolone is sensitive to high temperature and oxidizing condition, hot conditions
Lower easily dehydration generates methylprednisolone impurity G and methylprednisolone impurity D；Methylprednisolone impurity A, impurity structure are generated under oxidizing condition
It is as follows.
Methylprednisolone impurity G
Methylprednisolone impurity D (EZ)
Methylprednisolone impurity A
The peroral dosage form of methylprednisolone is mainly tablet, " the Mei Zhuo of presently commercially available product You Yuanyan company's Pfizer production
Pleasure " methylprednisolone piece (specification 4mg, 16mg) and the imitation medicine methylprednisolone piece (specification 4mg) of domestic enterprise's production.Wherein, brightness
The formulation patent of product is not disclosed in auspicious company；101804061 A of patent CN discloses the preparation method of methylprednisolone piece, in order to
Solve that amorphous methylprednisolone material flow is bad, and uniformity of dosage units is poor, and production efficiency is low, and stability is poor, when tabletting holds
Easily there is sticking, pitted skin, fracture, the low problem of tablet yield rate, which is prepared for a kind of methylprednisolone crystal form 1, and adopts
With wet granulation technology, which is added to disintegrating agent in the product to solve the problems, such as that disintegration is partially slow, but the invention is still deposited
Cumbersome in preparation process, raw material is easy to happen chemical reaction in hygrothermal environment, and composition is complicated, influences the disadvantages such as dissolution rate
End.
Summary of the invention
In view of the deficienciess of the prior art, the present invention is intended to provide a kind of novel methylprednisolone piece and preparation method,
The invention reside in improving drug dissolution, improving product stability and simplifying product formulation technique, to improve drug biology
Availability improves clinical efficacy.
Specifically, the present invention adopts the following technical scheme:
It uses air-flow crushing to granularity for 30 ~ 40 μm of D90 methylprednisolone bulk pharmaceutical chemicals, crosses 60 meshes, filler is crossed into 60 meshes
It is uniformly mixed afterwards with methylprednisolone, sequentially adds disintegrating agent and mix lubricant is uniform.
The content of each composition of methylprednisolone tablets are as follows:
Methylprednisolone 4.0%
Filler 93.0%
Disintegrating agent 2.0%
Lubricant 1.0%
Filler in prescription is the one or more of lactose monohydrate, cornstarch.
Disintegrating agent in prescription is crospovidone, the one or more of low-substituted hydroxypropyl cellulose.
Lubricant in prescription is the one or more of magnesium stearate, calcium stearate.
A kind of methylprednisolone tablets are made by above-mentioned preparation method.
Compared with prior art, the present invention by adopting the above technical scheme has the advantage that
For the low feature of methylprednisolone solubility, the present invention by by bulk pharmaceutical chemicals be micronized and use direct tablet compressing technique with
Improve the dissolution rate of product；The characteristics of dehydration and oxidative degradation easily occurs for methylprednisolone simultaneously, the present invention passes through
Medicament contact hygrothermal environment is avoided using direct tablet compressing technique, the impurity of control methylprednisolone piece increases.
Compared with prior art, methylprednisolone tablets of the present invention and its preparation process have the following advantages that and significantly
Progressive: improve the dissolution rate of drug, enhance the stability of drug, improve production efficiency, reduce equipment energy
Consumption is suitble to industrialized production.
Detailed description of the invention
Fig. 1 is the 1 lower three kind of dissolution rate schematic diagram of tablet in an aqueous medium of embodiment；
Fig. 2 is 60 DEG C of tablet A high temperature placements, 30 days related material patterns prepared by embodiment 1；
Fig. 3 is that original grinds 60 DEG C of tablet B high temperature placements, 30 days related material patterns；
Fig. 4 is 60 DEG C of tablet C high temperature placements, 30 days related material patterns；
Fig. 5 is the 2 lower three kinds of dissolution rate schematic diagrames of tablet in an aqueous medium of embodiment.
Specific embodiment
The technical solution in the present invention is made below in conjunction with specific embodiments further elucidated above.Unless otherwise saying
Bright, reagent used in the following example, material, instrument etc. can be obtained by routine business means.
Embodiment 1:
It feeds intake according to 10000
Formula: methylprednisolone 40g
Lactose monohydrate 720g
Cornstarch 210g
Crospovidone 20g
Magnesium stearate 10g
Preparation process:
1) bulk pharmaceutical chemicals crush: crushing air-flow 1.0Mpa, charging rate 0.6kg/h, raw material carry out again after crushing D90 by several times
Average, average rear D90 is at 30 ~ 40 μm.
2) it is fed intake in terms of preparing 10000, the above-mentioned auxiliary material of recipe quantity in addition to crospovidone, magnesium stearate point
60 meshes are not crossed, are mixed with above-mentioned methylprednisolone micro mist, three-dimensional mixer is used when mixing, and revolving speed 10rpm is mixed 15 minutes.
3) crospovidone of recipe quantity is added, revolving speed 10rpm is mixed 10 minutes.
4) magnesium stearate of recipe quantity is added, revolving speed 10rpm is mixed 10 minutes, carries out tabletting.
1 tablet A of above-described embodiment, original is taken to grind methylprednisolone tablets B, and the domestic commercially available country is commercially available according to patent CN
The tablet C of the preparation method preparation of methylprednisolone piece, progress methylprednisolone piece dissolution curve measurement in 101804061 A, as a result
Such as Fig. 1.
As shown in Figure 1, under the conditions of paddle method 50rpm, aqueous medium in 900ml, makes sample A by oneself and original grinds methylprednisolone piece B
Dissolution curve it is consistent, the amount of dissolution of the sample C in 5min will be lower than A and B.
It takes 1 tablet A of above-described embodiment, original to grind methylprednisolone tablets B, and sprinkles Buddhist nun according to first in 101804061 A of patent CN
The preparation method of imperial piece prepare tablet C place influence factor test, investigate high temperature (60 DEG C), illumination (visible light 4500 ±
90 μ w.hr/cm of 500Lux.hr ultraviolet light2), place 30 days under the conditions of high humidity (75%RH, 92.5%RH), wherein under hot conditions
Impurity variation is obvious, as a result such as Fig. 2,3,4.
1 tablet A of example and original grind 30 days impurity of sample B high temperature without rising appreciably, and tablet C high temperature places 30 days rear impurities
It is significant to increase, especially impurity D, therefore it is more excellent using the stability that the preparation process in this example prepares methylprednisolone tablets,
It is consistent that product quality is ground with original.Data such as table 1,2,3.
1 example of table, 1 tablet A high temperature places 0 day and 30 days related material results
N.D. it indicates to be not detected
2 original of table grinds sample B high temperature and places 0 day and 30 days related material results
N.D. it indicates to be not detected
3 tablet C high temperature of table places 0 day and 30 days related material results
N.D. it indicates to be not detected
Embodiment 2:
It feeds intake according to 10000
Formula:
Methylprednisolone 40g
Lactose monohydrate 930g
Low-substituted hydroxypropyl cellulose 20g
Calcium stearate 10g
Preparation process:
1) bulk pharmaceutical chemicals crush: crushing air-flow 1.0Mpa, charging rate 0.6kg/h, raw material carry out again after crushing D90 by several times
Average, average rear D90 is at 30 ~ 40 μm.
2) it is fed intake in terms of preparation 10000, the lactose monohydrate of recipe quantity is crossed into 60 meshes, it is micro- with above-mentioned methylprednisolone
Powder mixing, three-dimensional mixer is used when mixing, and revolving speed 10rpm is mixed 15 minutes.
3) low-substituted hydroxypropyl cellulose of recipe quantity is added, revolving speed 10rpm is mixed 10 minutes.
4) calcium stearate of recipe quantity is added, revolving speed 10rpm is mixed 10 minutes, carries out tabletting.
2 tablet A of above-described embodiment, original is taken to grind methylprednisolone tablets B, and domestic commercially available according to patent CN 101804061
The tablet C of the preparation method preparation of methylprednisolone piece, progress methylprednisolone piece dissolution curve measurement in A, as a result such as Fig. 5.
As shown in Figure 5, under the conditions of paddle method 50rpm, aqueous medium in 900ml, makes sample A by oneself and original grinds methylprednisolone piece B
Dissolved corrosion it is consistent.
It takes 2 tablet A of above-described embodiment, original to grind methylprednisolone tablets B, and sprinkles Buddhist nun according to first in 101804061 A of patent CN
The preparation method of imperial piece prepare tablet C place influence factor test, investigate high temperature (60 DEG C), illumination (visible light 4500 ±
90 μ w.hr/cm of 500Lux.hr ultraviolet light2), place 30 days under the conditions of high humidity (75%RH, 92.5%RH), wherein under hot conditions
Impurity variation is obvious, data such as table 4,5,6.
4 example of table, 2 tablet A high temperature places 0 day and 30 days related material results
N.D. it indicates to be not detected
5 original of table grinds sample B high temperature and places 0 day and 30 days related material results
N.D. it indicates to be not detected
6 tablet C high temperature of table places 0 day and 30 days related material results
N.D. it indicates to be not detected.
Claims (7)
1. a kind of glucocorticoid medicine tablet and preparation method thereof, which is characterized in that prepare the glucocorticoid medicine tablet
Bulk pharmaceutical chemicals be 30 ~ 40 μm of granularity D90 of methylprednisolone.
2. glucocorticoid medicine tablet according to claim 1 and preparation method thereof, which is characterized in that the tablet includes
Methylprednisolone, filler, disintegrating agent and lubricant.
3. glucocorticoid medicine tablet according to claim 2 and preparation method thereof, which is characterized in that the filler
For the one or more of lactose monohydrate, cornstarch.
4. glucocorticoid medicine tablet according to claim 2 and preparation method thereof, which is characterized in that the disintegrating agent
For crospovidone, the one or more of low-substituted hydroxypropyl cellulose.
5. glucocorticoid medicine tablet according to claim 2 and preparation method thereof, which is characterized in that the lubricant
For the one or more of magnesium stearate, calcium stearate.
6. glucocorticoid medicine tablet according to claim 2 and preparation method thereof, which is characterized in that including following step
It is rapid:
(1) bulk pharmaceutical chemicals crush: taking methylprednisolone bulk pharmaceutical chemicals, through air-flow crushing to 30 ~ 40 μm of D90, cross 60 meshes；
(2) filler is crossed into 60 meshes, is uniformly mixed with the methylprednisolone in step (1)；
(3) disintegrating agent is uniformly mixed with the material in step (2)；
(4) mix lubricant is added in (3) and uniformly carries out tabletting afterwards.
7. glucocorticoid medicine tablet according to claim 2 and preparation method thereof, which is characterized in that each composition contains
Amount are as follows:
Methylprednisolone 4.0%
Filler 93.0%
Disintegrating agent 2.0%
Lubricant 1.0%.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113304115A (en) * | 2021-06-07 | 2021-08-27 | 辰欣药业股份有限公司 | Prednisone acetate micro-tablets and preparation method thereof |
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|---|---|---|---|---|
| WO1987005804A1 (en) * | 1986-04-01 | 1987-10-08 | The Upjohn Company | Methylprednisolone/sodium carboxymethyl starch tablet composition |
| CN101804061A (en) * | 2010-04-01 | 2010-08-18 | 天津金耀集团有限公司 | New methylprednisolone tablets and crystal form and preparation method thereof |
| CN101987082A (en) * | 2010-07-16 | 2011-03-23 | 钟术光 | Solid preparation and preparation method thereof |
| CN104546701A (en) * | 2014-12-27 | 2015-04-29 | 云南盟生药业有限公司 | Methylprednisolone sodium succinate solution and preparation method thereof |
| CN104721160A (en) * | 2015-03-27 | 2015-06-24 | 贾红瑞 | Prednisone acetate tablet and preparation method thereof |
| CN104721162A (en) * | 2015-04-02 | 2015-06-24 | 天津泛博生物科技有限公司 | Prednisone oral pulsatile tablet and preparation method thereof |
| CN106963739A (en) * | 2017-03-27 | 2017-07-21 | 华益药业科技(安徽)有限公司 | Prednisolone oral disnitegration tablet and preparation method thereof |
| CN107049969A (en) * | 2017-03-01 | 2017-08-18 | 华益药业科技(安徽)有限公司 | A kind of prednisolone piece and preparation method thereof |
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2017
- 2017-12-18 CN CN201711364992.6A patent/CN109925288A/en active Pending
Patent Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1987005804A1 (en) * | 1986-04-01 | 1987-10-08 | The Upjohn Company | Methylprednisolone/sodium carboxymethyl starch tablet composition |
| CN101804061A (en) * | 2010-04-01 | 2010-08-18 | 天津金耀集团有限公司 | New methylprednisolone tablets and crystal form and preparation method thereof |
| CN101987082A (en) * | 2010-07-16 | 2011-03-23 | 钟术光 | Solid preparation and preparation method thereof |
| CN104546701A (en) * | 2014-12-27 | 2015-04-29 | 云南盟生药业有限公司 | Methylprednisolone sodium succinate solution and preparation method thereof |
| CN104721160A (en) * | 2015-03-27 | 2015-06-24 | 贾红瑞 | Prednisone acetate tablet and preparation method thereof |
| CN104721162A (en) * | 2015-04-02 | 2015-06-24 | 天津泛博生物科技有限公司 | Prednisone oral pulsatile tablet and preparation method thereof |
| CN107049969A (en) * | 2017-03-01 | 2017-08-18 | 华益药业科技(安徽)有限公司 | A kind of prednisolone piece and preparation method thereof |
| CN106963739A (en) * | 2017-03-27 | 2017-07-21 | 华益药业科技(安徽)有限公司 | Prednisolone oral disnitegration tablet and preparation method thereof |
Non-Patent Citations (2)
| Title |
|---|
| 孟胜男等: "《药剂学》", 31 January 2012, 上海科学技术出版社 * |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113304115A (en) * | 2021-06-07 | 2021-08-27 | 辰欣药业股份有限公司 | Prednisone acetate micro-tablets and preparation method thereof |
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Application publication date: 20190625 |