CN111407733A - Preparation method of celecoxib tablets - Google Patents
Preparation method of celecoxib tablets Download PDFInfo
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- CN111407733A CN111407733A CN202010196050.7A CN202010196050A CN111407733A CN 111407733 A CN111407733 A CN 111407733A CN 202010196050 A CN202010196050 A CN 202010196050A CN 111407733 A CN111407733 A CN 111407733A
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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
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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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
- A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
- A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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Abstract
The raw material formula of the celecoxib tablet comprises 11-12 parts by weight of lactose, 8-8.3 parts by weight of hydroxypropyl cellulose, 5-6 parts by weight of low-substituted hydroxypropyl cellulose, 1.3-1.4 parts by weight of sodium dodecyl sulfate, 1.05-1.1 parts by weight of magnesium stearate, 70-71 parts by weight of purified water and 24-26 parts by weight of celecoxib. The celecoxib tablet prepared by the invention has the advantage of easy decomposition.
Description
Technical Field
The invention belongs to the technical field of medicine preparation, and relates to a preparation method of a celecoxib tablet.
Background
Celecoxib, chemical name: 4- [5- (4-methylphenyl) -3- (trifluoromethyl) -1H-pyrazol-1-yl ] benzenesulfonamide. Celecoxib (Celecoxib) is a drug marketed by the company pfeiri in 1999 for the treatment of rheumatoid arthritis, rheumatoid arthritis and osteoarthritis. Celecoxib inhibits prostaglandin production through selectively inhibiting cyclooxygenase-2 (COX-2), thereby achieving the effects of anti-inflammation and analgesia. Since celecoxib does not inhibit cyclooxygenase-1 (COX-1), a physiological enzyme with gastrointestinal tract protection, the risk of gastrointestinal adverse reactions is obviously lower than that of the traditional non-steroidal anti-inflammatory analgesics.
The invention patent with the publication number CN109010837A discloses a celecoxib composition with high solubility, which comprises 50 percent of celecoxib and 50 percent of water-soluble excipient, wherein the water-soluble excipient comprises 1 to 3 percent of moisturizer, 80 to 90 percent of filler and 6 to 15 percent of adhesive; the moisturizer replaces the existing sodium dodecyl sulfate, a macrolide with stable structure is formed by esterification of maleic anhydride and lactose, and then 2 molecules of sodium sulfite are introduced into the macrolide through sulfonation reaction. The invention patent with the publication number of CN 103371976B discloses a solid dispersion containing celecoxib and a preparation method thereof. The solid dispersion of the present invention comprises or consists of celecoxib and copovidone.
Disclosure of Invention
The invention aims to provide a preparation method of a celecoxib tablet.
In order to achieve the above objects and other related objects, the present invention provides the following technical solutions: the preparation method of the celecoxib tablet comprises the following raw material formula, by weight, 11-12 parts of lactose, 8-8.3 parts of hydroxypropyl cellulose, 5-6 parts of low-substituted hydroxypropyl cellulose, 1.3-1.4 parts of sodium dodecyl sulfate, 1.05-1.1 parts of magnesium stearate, 70-71 parts of purified water and 24-26 parts of celecoxib;
the preparation method comprises the following steps:
step 1: adding hydroxypropyl cellulose into purified water, stirring, adding purified water, and dissolving to obtain a binding solution;
step 2: adding lactose, low-substituted hydroxypropyl cellulose, sodium dodecyl sulfate and binding solution into a stirring mixer, mixing for 1 minute, and then adding into a granulator for wet granulation to obtain granulated powder;
and step 3: putting the granulated powder into a fluidized bed dryer for drying to obtain granulated dried powder;
and 4, step 4: putting the granulated and dried powder into a granulator, and crushing by using a 1mm screen to obtain granulated powder;
and 5: putting the whole granule powder and magnesium stearate into a rotary mixer, and mixing to obtain a mixed powder;
step 6: the mixed powder is prepared into tablets by using a rotary tablet press.
The preferable technical scheme is as follows: the raw material formula of the celecoxib tablet comprises 11.72 parts by weight of lactose, 8.181 parts by weight of hydroxypropyl cellulose, 5.4 parts by weight of low-substituted hydroxypropyl cellulose, 1.35 parts by weight of sodium dodecyl sulfate, 1.08 parts by weight of magnesium stearate, 70.9 parts by weight of purified water and 25 parts by weight of celecoxib.
Due to the application of the technical scheme, compared with the prior art, the invention has the advantages that:
the celecoxib tablet prepared by the invention has the advantage of easy decomposition.
Detailed Description
The following description of the embodiments of the present invention is provided for illustrative purposes, and other advantages and effects of the present invention will become apparent to those skilled in the art from the present disclosure.
Example 1: preparation method of celecoxib tablets
A 1 st section: weighing section
Weighing the following raw materials: 1) lactose 200M: 11.72 kg: (1 minor batch, 6 minor batches in total) are in full 1.
2)HPC-SSL：8.181kg×1。
3) L-HPC 21 is 5.40kg (1 part in weight, 6 parts in total) in half 1.
4) And the dodecyl sodium sulfate is used as seed of S L S-P in an amount of 1.35kg (1 small batch, 6 small batches in total) and is in an amount of 1.
5) Magnesium stearate, vegetative, light, 1.08kg, in colour 1.
6) 25.00kg of celecoxib (1 small batch, 6 small batches in total) is in full 2.
In addition, the method is as follows: the allowable range of the weighing error rate is within 0.5 percent; in addition, 2: the weighing error rate is within 0.2 percent of the allowable range.
And (2) a section: granulation and drying section
1) 50.00kg of purified water was added with L8.181 kg (1% increment) of HPC-SS, followed by stirring, and 20.90kg of purified water was further added and dissolved to obtain a conjugate solution.
2) After the following raw materials were put into a high-speed stirring mixer (200L) and mixed, 13.05kg (1 small lot) of the binding liquid was added to the mixture and mixed for 1 minute for granulation, and the resultant mixture was put into a "3 mm" mesh for wet granulation to obtain a granulated powder.
Celecoxib 25.00kg1 minor batches), lactose 200M11.72kg (1 minor batch), L-HPC215.40kg (1 minor batch), sodium dodecyl sulfate seed and seed S L S-P1.35kg (1 minor batch),
3) Then, the granulated powder (2 lots) was put into a fluidized bed dryer and dried, and after the exhaust temperature reached 45 ℃, the loss on drying of the dried powder was measured, and it was confirmed that the drying was completed when the numerical value was within the control range, thereby obtaining a granulated dried powder. [ workshop section management 1 ]
[ workshop section management 1 ]: about 5g of the dried powder was taken, and the loss on drying was measured, and it was required that the loss on drying was 3.0% or less.
And a 3 rd section: finishing section
The granulated and dried powder obtained in the granulation and drying section is put into a granulator and crushed by a screen of 1mm to obtain a granulated powder.
And 4, a 4 th section: mixing section
The whole grain powder (3 batches) obtained in the whole grain working section and magnesium stearate, vegetable and lightweight [ 1.08kg ] were put into a rotary mixer (500L) and mixed [ 1 minute ] to obtain a mixed powder.
And (5) a stage: sheeting section
The resulting blend powder from the mixing section was processed using a rotary tablet press and a 8.0mm phi pestle and mortar to produce a weight [ 180.0mg ],
tablet with thickness of 2.7mm and hardness of 30N. [ workshop section management 2 ]
Section management 2: 20 tablets were sampled and the mean weight was determined, requiring 180. + -.5 mg.
Example 2: preparation method of celecoxib tablets
A 1 st section: weighing section
Weighing the following raw materials: 1) lactose 200M [ 11.72kg ] (1 in small portions, 6 in total) is added in 1.
2)HPC-SSL【8.181kg】※1。
3) L-HPC 21 (5.40 kg) (1 small batch, 6 small batches in total) is in full 1.
4) Dodecyl sodium sulfate (S L S-P) [ 1.35kg ] (1 small batch of dosage, 6 small batches in total) is added in the seed 1.
5) Magnesium stearate, vegetative, light, 1.08kg are in the same order of 1.
6) Celecoxib (25.00 kg) (1 small batch, 6 small batches in total) is in full 2.
In addition, the method is as follows: the allowable range of the weighing error rate is within 0.5 percent; in addition, 2: the weighing error rate is within 0.2 percent of the allowable range.
And (2) a section: granulation and drying section
1) And purified water (50.00 kg) was added HPC-SS L (8.181 kg) (1% increments) and stirred, and then purified water (20.90 kg) was added and dissolved to obtain a binding solution.
2) After the materials of the following notes were put into a high-speed stirring mixer (200L) and mixed, the binding solution (13.05 kg) (1 small lot) was added and mixed for granulation (1 minute), and then the mixture was put into a "3 mm" mesh for wet granulation to obtain granulated powder.
Celecoxib [ 25.00kg ] (1 minilot), lactose.200M [ 11.72kg ] (1 minilot), L-HPC 21 [ 5.40kg ] (1 minilot), sodium dodecyl sulfate (1 minilot), S L S-P [ 1.35kg ] (1 minilot),
3) Then, the granulated powder (2 lots) was put into a fluidized bed dryer and dried, and after the exhaust temperature reached [ 45 ℃ ], the loss on drying of the dried powder was measured, and it was confirmed that the drying was completed within the control range, thereby obtaining a granulated dried powder. [ workshop section management 1 ]
[ workshop section management 1 ]: about 5g of the dried powder was taken, and the loss on drying was measured, and it was required that the loss on drying was 3.0% or less.
And a 3 rd section: finishing section
The granulated and dried powder obtained in the granulation and drying section is put into a granulator and crushed by a screen of 1mm to obtain a granulated powder.
And 4, a 4 th section: mixing section
The whole grain powder (3 batches) obtained in the whole grain working section and magnesium stearate, vegetable and lightweight [ 1.08kg ] were put into a rotary mixer (500L) and mixed [ 1 minute ] to obtain a mixed powder.
And (5) a stage: sheeting section
The resulting blend powder from the mixing section was processed using a rotary tablet press and a 13.0 × 6.5.5 mm pestle and mortar to produce a weight of [ 360.0mg ],
tablet with thickness of 5.2mm and hardness of 50N. [ workshop section management 2 ]
Section management 2: 20 tablets were sampled and the mean weight was determined, requiring 360. + -.11 mg.
Example 3: preparation method of celecoxib tablets
The preparation method of the celecoxib tablet comprises the following raw material formula, by weight, 11-12 parts of lactose, 8-8.3 parts of hydroxypropyl cellulose, 5-6 parts of low-substituted hydroxypropyl cellulose, 1.3-1.4 parts of sodium dodecyl sulfate, 1.05-1.1 parts of magnesium stearate, 70-71 parts of purified water and 24-26 parts of celecoxib;
the preparation method comprises the following steps:
step 1: adding hydroxypropyl cellulose into purified water, stirring, adding purified water, and dissolving to obtain a binding solution;
step 2: adding lactose, low-substituted hydroxypropyl cellulose, sodium dodecyl sulfate and binding solution into a stirring mixer, mixing for 1 minute, and then adding into a granulator for wet granulation to obtain granulated powder;
and step 3: putting the granulated powder into a fluidized bed dryer for drying to obtain granulated dried powder;
and 4, step 4: putting the granulated and dried powder into a granulator, and crushing by using a 1mm screen to obtain granulated powder;
and 5: putting the whole granule powder and magnesium stearate into a rotary mixer, and mixing to obtain a mixed powder;
step 6: the mixed powder is prepared into tablets by using a rotary tablet press.
The preferred embodiment is: the raw material formula of the celecoxib tablet comprises 11.72 parts by weight of lactose, 8.181 parts by weight of hydroxypropyl cellulose, 5.4 parts by weight of low-substituted hydroxypropyl cellulose, 1.35 parts by weight of sodium dodecyl sulfate, 1.08 parts by weight of magnesium stearate, 70.9 parts by weight of purified water and 25 parts by weight of celecoxib.
The foregoing is illustrative of the preferred embodiment of the present invention and is not to be construed as limiting thereof in any way, and any modifications or variations thereof that fall within the spirit of the invention are intended to be included within the scope thereof.
Claims (2)
1. A preparation method of celecoxib tablets is characterized by comprising the following steps: the raw material formula of the celecoxib tablet comprises 11-12 parts by weight of lactose, 8-8.3 parts by weight of hydroxypropyl cellulose, 5-6 parts by weight of low-substituted hydroxypropyl cellulose, 1.3-1.4 parts by weight of sodium dodecyl sulfate, 1.05-1.1 parts by weight of magnesium stearate, 70-71 parts by weight of purified water and 24-26 parts by weight of celecoxib;
the preparation method comprises the following steps:
step 1: adding hydroxypropyl cellulose into purified water, stirring, adding purified water, and dissolving to obtain a binding solution;
step 2: adding lactose, low-substituted hydroxypropyl cellulose, sodium dodecyl sulfate and binding solution into a stirring mixer, mixing for 1 minute, and then adding into a granulator for wet granulation to obtain granulated powder;
and step 3: putting the granulated powder into a fluidized bed dryer for drying to obtain granulated dried powder;
and 4, step 4: putting the granulated and dried powder into a granulator, and crushing by using a 1mm screen to obtain granulated powder;
and 5: putting the whole granule powder and magnesium stearate into a rotary mixer, and mixing to obtain a mixed powder;
step 6: the mixed powder is prepared into tablets by using a rotary tablet press.
2. The method of preparing a celecoxib tablet according to claim 1, wherein: the raw material formula of the celecoxib tablet comprises 11.72 parts by weight of lactose, 8.181 parts by weight of hydroxypropyl cellulose, 5.4 parts by weight of low-substituted hydroxypropyl cellulose, 1.35 parts by weight of sodium dodecyl sulfate, 1.08 parts by weight of magnesium stearate, 70.9 parts by weight of purified water and 25 parts by weight of celecoxib.
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| Application Number | Priority Date | Filing Date | Title |
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| CN202010196050.7A CN111407733A (en) | 2020-03-19 | 2020-03-19 | Preparation method of celecoxib tablets |
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| CN202010196050.7A CN111407733A (en) | 2020-03-19 | 2020-03-19 | Preparation method of celecoxib tablets |
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Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20020119193A1 (en) * | 2000-08-18 | 2002-08-29 | Le Trang T. | Oral fast-melt formulation of a cyclooxygenase-2 inhibitor |
| CN102920676A (en) * | 2012-12-04 | 2013-02-13 | 山东省立医院 | Celecoxib chewable tablet and preparation method thereof |
| CN104027319A (en) * | 2014-06-25 | 2014-09-10 | 万特制药(海南)有限公司 | Celecoxib dispersible tablet and preparation method thereof |
| CN105343030A (en) * | 2015-12-16 | 2016-02-24 | 钟柏根 | Celecoxib capsule and preparation method thereof |
| CN107115313A (en) * | 2017-07-03 | 2017-09-01 | 福建省福抗药业股份有限公司 | A kind of celecoxib composition and preparation method thereof |
| WO2018111991A1 (en) * | 2016-12-14 | 2018-06-21 | Druggability Technologies Ip Holdco Limited | Pharmaceutical composition containing celecoxib |
-
2020
- 2020-03-19 CN CN202010196050.7A patent/CN111407733A/en active Pending
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20020119193A1 (en) * | 2000-08-18 | 2002-08-29 | Le Trang T. | Oral fast-melt formulation of a cyclooxygenase-2 inhibitor |
| CN102920676A (en) * | 2012-12-04 | 2013-02-13 | 山东省立医院 | Celecoxib chewable tablet and preparation method thereof |
| CN104027319A (en) * | 2014-06-25 | 2014-09-10 | 万特制药(海南)有限公司 | Celecoxib dispersible tablet and preparation method thereof |
| CN105343030A (en) * | 2015-12-16 | 2016-02-24 | 钟柏根 | Celecoxib capsule and preparation method thereof |
| WO2018111991A1 (en) * | 2016-12-14 | 2018-06-21 | Druggability Technologies Ip Holdco Limited | Pharmaceutical composition containing celecoxib |
| CN107115313A (en) * | 2017-07-03 | 2017-09-01 | 福建省福抗药业股份有限公司 | A kind of celecoxib composition and preparation method thereof |
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Application publication date: 20200714 |