CN110893174A - Preparation method of diclofenac sodium enteric-coated tablets - Google Patents
Preparation method of diclofenac sodium enteric-coated tablets Download PDFInfo
- Publication number
- CN110893174A CN110893174A CN201911226937.XA CN201911226937A CN110893174A CN 110893174 A CN110893174 A CN 110893174A CN 201911226937 A CN201911226937 A CN 201911226937A CN 110893174 A CN110893174 A CN 110893174A
- Authority
- CN
- China
- Prior art keywords
- diclofenac sodium
- enteric
- preparation
- percent
- 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.)
- Pending
Links
- 229960001193 diclofenac sodium Drugs 0.000 title claims abstract description 41
- JGMJQSFLQWGYMQ-UHFFFAOYSA-M sodium;2,6-dichloro-n-phenylaniline;acetate Chemical compound [Na+].CC([O-])=O.ClC1=CC=CC(Cl)=C1NC1=CC=CC=C1 JGMJQSFLQWGYMQ-UHFFFAOYSA-M 0.000 title claims abstract description 41
- 239000002662 enteric coated tablet Substances 0.000 title claims abstract description 28
- 238000002360 preparation method Methods 0.000 title claims abstract description 13
- 239000003826 tablet Substances 0.000 claims abstract description 17
- 239000004925 Acrylic resin Substances 0.000 claims abstract description 10
- 229920000178 Acrylic resin Polymers 0.000 claims abstract description 10
- 239000000314 lubricant Substances 0.000 claims abstract description 9
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 16
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 12
- 235000019359 magnesium stearate Nutrition 0.000 claims description 6
- 238000001035 drying Methods 0.000 claims description 4
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 3
- 238000007873 sieving Methods 0.000 claims description 3
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 claims description 2
- 239000000741 silica gel Substances 0.000 claims description 2
- 229910002027 silica gel Inorganic materials 0.000 claims description 2
- 238000005303 weighing Methods 0.000 claims description 2
- 239000000843 powder Substances 0.000 claims 1
- 239000000463 material Substances 0.000 abstract description 8
- 239000003814 drug Substances 0.000 abstract description 6
- 230000000694 effects Effects 0.000 abstract description 5
- 238000000034 method Methods 0.000 abstract description 5
- 229940079593 drug Drugs 0.000 abstract description 4
- 230000008569 process Effects 0.000 abstract description 4
- 210000002784 stomach Anatomy 0.000 description 5
- 208000002193 Pain Diseases 0.000 description 3
- 239000006185 dispersion Substances 0.000 description 3
- 210000001035 gastrointestinal tract Anatomy 0.000 description 3
- 230000000638 stimulation Effects 0.000 description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 230000001154 acute effect Effects 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 230000000968 intestinal effect Effects 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 210000000813 small intestine Anatomy 0.000 description 2
- 229910002012 Aerosil® Inorganic materials 0.000 description 1
- 208000006820 Arthralgia Diseases 0.000 description 1
- 206010006811 Bursitis Diseases 0.000 description 1
- 206010013935 Dysmenorrhoea Diseases 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 201000005569 Gout Diseases 0.000 description 1
- 206010018634 Gouty Arthritis Diseases 0.000 description 1
- 206010019233 Headaches Diseases 0.000 description 1
- 206010023232 Joint swelling Diseases 0.000 description 1
- 206010028391 Musculoskeletal Pain Diseases 0.000 description 1
- 208000000112 Myalgia Diseases 0.000 description 1
- 208000007613 Shoulder Pain Diseases 0.000 description 1
- 208000006045 Spondylarthropathies Diseases 0.000 description 1
- 208000004760 Tenosynovitis Diseases 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000000202 analgesic effect Effects 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 206010003246 arthritis Diseases 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 238000000748 compression moulding Methods 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 239000002702 enteric coating Substances 0.000 description 1
- 238000009505 enteric coating Methods 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 210000004051 gastric juice Anatomy 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 231100000869 headache Toxicity 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000009776 industrial production Methods 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 201000008482 osteoarthritis Diseases 0.000 description 1
- 230000002085 persistent effect Effects 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 239000008055 phosphate buffer solution Substances 0.000 description 1
- 210000001187 pylorus Anatomy 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 201000003068 rheumatic fever Diseases 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- 210000004872 soft tissue Anatomy 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 201000005671 spondyloarthropathy Diseases 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 208000004371 toothache Diseases 0.000 description 1
- 230000008733 trauma Effects 0.000 description 1
- 230000000472 traumatic effect Effects 0.000 description 1
Classifications
-
- 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
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
-
- 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
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
-
- 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]
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention relates to a preparation method of diclofenac sodium enteric-coated tablets. The diclofenac sodium enteric-coated tablet comprises the following components in percentage by weight: 18 to 52 percent of diclofenac sodium, 100 to 5546 to 80 percent of acrylic resin L and 0.3 to 2 percent of lubricant, wherein the sum of the components reaches 100 percent. The diclofenac sodium tablet prepared by the invention has the advantages of small auxiliary material dosage, good stability, simple process, small drug property side effect and good safety.
Description
Technical Field
The invention belongs to the technical field of medicines, and particularly relates to a preparation method of diclofenac sodium enteric-coated tablets.
Background
Diclofenac sodium is a common anti-inflammatory analgesic. It is used for relieving rheumatoid arthritis and osteoarthritis. Acute stage or persistent joint swelling and pain symptoms of various chronic arthritis such as spondyloarthropathy, gouty arthritis, rheumatic arthritis and the like; various soft tissue rheumatalgia, such as shoulder pain, tenosynovitis, bursitis myalgia, traumatic pain after exercise, etc.; acute mild and moderate pain such as: pain after surgery, trauma, strain, etc.; primary dysmenorrhea, toothache, headache, etc.
Whether a large-dose or small-dose diclofenac sodium tablet is used for a long time, the main side effect of the diclofenac sodium tablet is stimulation to the gastrointestinal tract, the most common method for solving the problem is to prepare the enteric-coated tablet, but the common enteric-coated tablet can generate the intestinal side effect due to rapid disintegration and dissolution even when reaching the intestine, the tablet is greatly influenced by the stomach and pyloric sphincter, and researches show that the time from the stomach to the small intestine is different from 15 minutes to 7 hours, so that unstable blood concentration is easily caused, the local concentration of the small intestine is overhigh, and the intestinal stimulation is aggravated.
Disclosure of Invention
Aiming at the technical problems, the invention provides a preparation method of diclofenac sodium enteric-coated tablets, which has the advantages of small using amount of auxiliary materials, good stability and simple process.
In order to solve the technical problems, the invention adopts the following technical scheme: the preparation method of the diclofenac sodium enteric-coated tablet comprises the following components in percentage by weight:
diclofenac sodium 18-52%
Acrylic resin L100-5546% -80%
0.3 to 2 percent of lubricant,
the sum of the components reaches 100 percent;
weighing diclofenac sodium and acrylic resin L100-55, dissolving in ethanol, drying, and sieving to obtain diclofenac sodium enteric-coated tablet dispersoid; the diclofenac sodium enteric-coated tablet dispersoid is uniformly mixed with a lubricant and directly tabletted to obtain the diclofenac sodium enteric-coated tablet.
Further: each tablet contains 25-100mg of diclofenac sodium.
The lubricant is one or more of magnesium stearate, micropowder silica gel and talcum powder.
The lubricant is magnesium stearate.
The diclofenac sodium enteric-coated tablet and the preparation method thereof have the following advantages:
(1) the auxiliary material variety is less, and the tablet stability is high. The invention only adopts enteric material and lubricant, and does not add any other auxiliary material, thus improving the stability of diclofenac sodium;
(2) the acid resistance is good, and the product can be quickly dissolved out in phosphate buffer solution with pH value of 6.8. In vitro release degree experiments show that:
the tablet of the invention can release less than 1.5 percent in 0.1 mol/L hydrochloric acid for 2 hours, and the tablet is complete and has no change in appearance;
in phosphate buffer at pH 6.8, the tablets erode quickly and the drug dissolves quickly.
(3) Does not need enteric coating, has simple preparation process and is suitable for industrial production.
In addition, the diclofenac sodium tablet has the main side effect of stimulating gastrointestinal tracts after being used for a long time, and the enteric-coated tablet can reduce the local stimulation of the medicine to the stomach and also reduce the damage of gastric juice to the medicine. The diclofenac sodium enteric-coated tablet does not disintegrate in stomach, can be absorbed in intestinal tract, and has low irritation to stomach. The diclofenac sodium and the acrylic resin L100-55 are dissolved in ethanol, and are dried and sieved, so that the materials can be fully and uniformly mixed, and meanwhile, the problem of caking is well avoided by adopting the acrylic resin L100-55. Ethanol is used as the most common organic reagent, is widely applied in the field of tablets, has comprehensive safety protection measures and does not have serious potential safety hazard. At the same time, the volatility of ethanol determines that it has little solvent remaining after drying.
Therefore, the diclofenac sodium tablet obtained by the invention has the advantages of small auxiliary material dosage, good stability, simple process, small drug property side effect and good safety.
Detailed Description
The invention is further illustrated by the following examples. The formulation and preparation method of the present invention are for illustration and not for limitation, and the simple modification of the formulation and preparation method of diclofenac sodium enteric-coated tablet based on the concept of the present invention is within the scope of the present invention.
Example 1
Dissolving 100g of diclofenac sodium and 100-55100 g of acrylic resin L in 500mL of ethanol by stirring, drying for 24 hours at 40 ℃ in a vacuum oven, crushing, and sieving with a 30-mesh sieve to obtain a diclofenac sodium enteric-coated tablet dispersion; dispersing enteric-coated tablet with hard gelatin
Mixing magnesium stearate, and compression molding with rotary tablet press.
Example 2
25g of diclofenac sodium and 100-55100 g of acrylic resin are stirred and dissolved in 1000mL of ethanol, dried for 24 hours at 45 ℃ in a vacuum oven, crushed and sieved by a 24-mesh sieve to obtain a diclofenac sodium enteric-coated tablet dispersoid; the obtained enteric-coated tablet dispersion is uniformly mixed with 1.2g of magnesium stearate and 1.0 g of aerosil, and is compressed and molded by a rotary tablet machine.
Example 3
The above examples 1 to 3 were prepared as follows
50g of diclofenac sodium and 100-55150 g of acrylic resin are stirred and dissolved in 500mL of ethanol, dried for 24 hours at 40 ℃ in a vacuum oven, crushed and sieved by a 30-mesh sieve to obtain a diclofenac sodium enteric-coated tablet dispersoid; the obtained enteric tablet dispersion was mixed with 0.6 g of magnesium stearate, and compression-molded by a rotary tablet press.
The diclofenac sodium enteric-coated tablet prepared by the invention has the advantages of small auxiliary material dosage, good stability, simple process, small drug effect and good safety.
Claims (3)
1. The preparation method of the diclofenac sodium enteric-coated tablet comprises the following components in percentage by weight:
diclofenac sodium 18-52%
Acrylic resin L100-5546% -80%
0.3 to 2 percent of lubricant,
the sum of the components reaches 100 percent;
weighing diclofenac sodium and acrylic resin L100-55, dissolving in ethanol, drying, and sieving to obtain diclofenac sodium enteric-coated tablet dispersoid; the diclofenac sodium enteric-coated tablet dispersoid is uniformly mixed with a lubricant and directly tabletted to obtain the diclofenac sodium enteric-coated tablet.
2. The preparation method of diclofenac sodium enteric-coated tablets according to claim 1, characterized in that: each tablet contains diclofenac sodium 25-100 mg.
3. The preparation method of diclofenac sodium enteric-coated tablets according to claim 1, characterized in that: the lubricant is one or more of magnesium stearate, micro-powder silica gel and talcum powder.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201911226937.XA CN110893174A (en) | 2019-12-04 | 2019-12-04 | Preparation method of diclofenac sodium enteric-coated tablets |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201911226937.XA CN110893174A (en) | 2019-12-04 | 2019-12-04 | Preparation method of diclofenac sodium enteric-coated tablets |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN110893174A true CN110893174A (en) | 2020-03-20 |
Family
ID=69787277
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201911226937.XA Pending CN110893174A (en) | 2019-12-04 | 2019-12-04 | Preparation method of diclofenac sodium enteric-coated tablets |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN110893174A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111700872A (en) * | 2020-07-20 | 2020-09-25 | 华益药业科技(安徽)有限公司 | Diclofenac enteric-coated tablet and processing technology thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4948581A (en) * | 1989-02-17 | 1990-08-14 | Dojin Iyaku-Kako Co., Ltd. | Long acting diclofenac sodium preparation |
| AU7537000A (en) * | 1999-10-01 | 2001-05-10 | Norton Healthcare Ltd | Anti-inflammatory pharmaceutical formulations |
| CN106109426A (en) * | 2016-06-23 | 2016-11-16 | 广东肇庆星湖生物科技股份有限公司 | A kind of diclofenac sodium enteric-coated tablets and preparation method thereof |
| CN109646412A (en) * | 2018-12-12 | 2019-04-19 | 中国药科大学 | A kind of enteric Pharmaceutical composition and its preparation method and application |
-
2019
- 2019-12-04 CN CN201911226937.XA patent/CN110893174A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4948581A (en) * | 1989-02-17 | 1990-08-14 | Dojin Iyaku-Kako Co., Ltd. | Long acting diclofenac sodium preparation |
| AU7537000A (en) * | 1999-10-01 | 2001-05-10 | Norton Healthcare Ltd | Anti-inflammatory pharmaceutical formulations |
| CN106109426A (en) * | 2016-06-23 | 2016-11-16 | 广东肇庆星湖生物科技股份有限公司 | A kind of diclofenac sodium enteric-coated tablets and preparation method thereof |
| CN109646412A (en) * | 2018-12-12 | 2019-04-19 | 中国药科大学 | A kind of enteric Pharmaceutical composition and its preparation method and application |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111700872A (en) * | 2020-07-20 | 2020-09-25 | 华益药业科技(安徽)有限公司 | Diclofenac enteric-coated tablet and processing technology thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Jindal et al. | Synthesis of thiolated alginate and evaluation of mucoadhesiveness, cytotoxicity and release retardant properties | |
| CN101584673A (en) | Levetiracetam tablet and preparation method | |
| CN103610658B (en) | Immunomodulator slow-release preparation and preparation method thereof | |
| CN110507620B (en) | Compound glucosamine sulfate dispersible tablet and preparation method thereof | |
| CN102952280A (en) | Hydroxypropyl methylcellulose copolymer for preparing plant capsules and preparation method thereof | |
| CN106109426A (en) | A kind of diclofenac sodium enteric-coated tablets and preparation method thereof | |
| CN110893174A (en) | Preparation method of diclofenac sodium enteric-coated tablets | |
| KR102224087B1 (en) | Slow-release solid oral compositions | |
| CN102488686B (en) | Compound alpha-keto acid tablet and preparation process thereof | |
| CN110893175A (en) | Diclofenac sodium enteric-coated tablet | |
| CN103263395A (en) | Telmisartan tablet preparation and preparation method thereof | |
| CN107375938B (en) | Glucosamine hydrochloride adhesive, tablets and preparation method thereof | |
| CN103961351A (en) | Preparation method of amoxicillin and clavulanate potassium tablets | |
| Kotadiya et al. | Colon targeted moringa gum compression coated tablets of capecitabin: a factorial approach | |
| CN103781473A (en) | Oral formulations containing hyaluronic acid for sustained drug release | |
| JP2004137183A (en) | Oral administration medicine, health food product or nutritional medicine composition containing glucosaminoglycan or its salt | |
| CN103142533B (en) | Enteric coated tablet of etoposide | |
| CN115192535A (en) | Mexicam enteric-coated tablet and preparation method thereof | |
| CN103127019B (en) | Florfenicol dispersible tablet as well as preparation method and application thereof | |
| JP4864369B2 (en) | Method for stabilizing thiamines | |
| CN104644587A (en) | Preparation method of medicine composition for treating cardiovascular disease | |
| CN103142545B (en) | Enteric capsule of etoposide | |
| Siddiqui et al. | Studies on fruit pectin in the development of tablet formulations of ibuprofen | |
| KR100944121B1 (en) | Fast-acting pharmaceutical composition comprising soy polysaccharide | |
| CN117530928A (en) | A kind of preparation method of aceclofenac sustained-release tablets |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20200320 |