CN107233317B - Pharmaceutical composition containing ibuprofen arginine and preparation method thereof - Google Patents
Pharmaceutical composition containing ibuprofen arginine and preparation method thereof Download PDFInfo
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- CN107233317B CN107233317B CN201710377002.6A CN201710377002A CN107233317B CN 107233317 B CN107233317 B CN 107233317B CN 201710377002 A CN201710377002 A CN 201710377002A CN 107233317 B CN107233317 B CN 107233317B
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- arginine
- ibuprofen
- pharmaceutical composition
- composition containing
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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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
- 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
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
Abstract
The invention discloses a pharmaceutical composition containing ibuprofen arginine and a preparation method thereof, wherein the pharmaceutical composition containing ibuprofen arginine comprises the following components in parts by weight: 1 part of ibuprofen arginine, 0.5-50 parts of sucrose, 0.5-50 parts of stearic acid and 0.05-5 parts of purified water. The pharmaceutical composition containing the ibuprofen arginine has simple components, only contains two auxiliary materials of sucrose and stearic acid except the ibuprofen arginine, can effectively solve the problem that the ibuprofen arginine has pungent smell, and has good taste and low production cost. In addition, the pharmaceutical composition containing the ibuprofen arginine provided by the invention adopts water as a wetting agent, so that the problem of ethanol residue is avoided, and the medication safety of alcohol allergy patients is ensured.
Description
Technical Field
The invention relates to the field of pharmaceutical preparations, in particular to a pharmaceutical composition containing ibuprofen arginine and a preparation method thereof.
Background
The chemical name of the Ibuprofen Arginine is 2- (4-isobutylphenyl) propionic acid-L-Arginine salt, the molecular formula is C19H32N4O4, and the molecular weight is 380.48. the Ibuprofen Arginine particle is developed by Zambon S.P.A Italy, and is mainly used for toothache, dysmenorrhea, pain caused by trauma such as mobility injury, arthralgia and ligament pain, backache and headache, and fever caused by influenza.
The original product specification of the arginine ibuprofen granule discloses that the arginine ibuprofen granule comprises arginine ibuprofen, sodium bicarbonate, saccharin sodium, aspartame, apricot essence and cane sugar, but has strong pungent taste when being prepared into solution by heating water in the using process, and has the problem of compliance of patients in medication.
The Chinese patent publication No. CN1237964C discloses a method for preparing granules containing ibuprofen arginine composition, the composition comprises ibuprofen arginine, diluent and adhesive, and the problem of granule irritation is solved by coating, but the coating process is adopted, so that the production cost is increased, the requirement on equipment is high, and the method is not beneficial to industrial production.
The invention discloses arginine ibuprofen granules and a preparation method thereof in Chinese patent publication No. CN102961371B, wherein the granules comprise ibuprofen arginine, a filling agent, a taste masking agent, a binding agent, a flavoring agent, a deodorizing agent and a coloring agent, the taste of the granules is adjusted by the synergistic effect of the filling agent and the flavoring agent and the taste masking agent and the flavoring agent, the problem of irritation of the granules is solved, the taste is good, but the components of the granules are complex, and the production cost is still high. In addition, in the preparation process of the particles, an ethanol solution is used as a binder, so that certain potential safety hazards exist for patients allergic to alcohol.
Disclosure of Invention
The invention aims to solve the technical problem of providing the ibuprofen arginine granules which are low in production cost, high in safety and good in patient medication compliance and the preparation method thereof, and overcoming the defects that the ibuprofen arginine granules in the prior art have pungent smell, high production cost, potential safety hazards of medication and the like.
The technical problem to be solved by the invention is realized by the following technical scheme:
a pharmaceutical composition containing ibuprofen arginine comprises the following components in parts by weight: 1 part of ibuprofen arginine, 0.5-50 parts of sucrose, 0.5-50 parts of stearic acid and 0.05-5 parts of purified water.
Preferably, the technical scheme comprises the following components in parts by weight: 1 part of ibuprofen arginine, 1-20 parts of sucrose, 1-20 parts of stearic acid and 0.1-2 parts of purified water.
Preferably, the technical scheme comprises the following components in parts by weight: 1 part of ibuprofen arginine, 5 parts of sucrose, 2 parts of stearic acid and 0.5 part of purified water.
A preparation method of a pharmaceutical composition containing arginine ibuprofen comprises the following steps:
1) heating stearic acid to be molten, adding ibuprofen arginine, and stirring uniformly;
2) spray drying to obtain granules, and sieving;
3) adding the sieved sucrose into the particles, uniformly mixing, and sieving;
4) adding purified water as wetting agent, and sieving to obtain soft material;
5) drying and granulating the soft material to obtain the pharmaceutical composition containing the ibuprofen arginine.
Preferably, in the above technical scheme, the melting temperature of the stearic acid in the step 1) is 60-100 ℃, preferably 70-80 ℃.
Preferably, in the above technical solution, in the spray drying step of step 2): the temperature of the sample is controlled at 70-95 ℃, and preferably 85 ℃; controlling the air temperature at 20-40 ℃, preferably 30 ℃; the granules are sieved through a 60-100 mesh sieve, preferably a 80 mesh sieve.
Preferably, in the above technical scheme, in the step 3), the sucrose is sieved by a sieve with 60-100 meshes, preferably a sieve with 80 meshes.
Preferably, in the above technical scheme, the soft material in step 4) is sieved by a 60-mesh sieve.
Preferably, in the above technical solution, in step 5): the drying temperature is controlled at 40-60 ℃, preferably 50 ℃; the time is controlled to be 1-2h, preferably 1.5 h.
Preferably, in the above-described aspect, in the step 5), the whole grain step: sieving the whole granules with a 40-mesh sieve.
The technical scheme of the invention has the following beneficial effects:
(1) the pharmaceutical composition containing the ibuprofen arginine provided by the invention is simple in components, only contains two auxiliary materials of sucrose and stearic acid except the ibuprofen arginine, can effectively solve the problem that the ibuprofen arginine has pungent smell, and is good in taste and low in production cost.
(2) The pharmaceutical composition containing the ibuprofen arginine provided by the invention adopts water as a wetting agent, so that the problem of ethanol residue is avoided, and the medication safety of alcohol allergy patients is ensured.
Detailed Description
Specific examples of the invention are described in detail below to facilitate a further understanding of the invention.
All experimental procedures used in the following examples are conventional unless otherwise specified. Materials, reagents and the like used in the following examples are commercially available unless otherwise specified.
Example 1
A pharmaceutical composition containing ibuprofen arginine comprises the following components in parts by weight:
the preparation method of the pharmaceutical composition containing the arginine ibuprofen comprises the following steps:
1) heating stearic acid to melt, and controlling the temperature at 60 ℃;
2) adding ibuprofen arginine into the stearic acid molten liquid, and stirring uniformly;
3) spray drying, controlling the temperature of a sample at 70 ℃, controlling the temperature of air at 20 ℃, and sieving the obtained particles with a 60-mesh sieve;
4) sieving sucrose with 60 mesh sieve, mixing with the above granules, sieving with 40 mesh sieve, and mixing;
5) taking purified water as a wetting agent, and sieving the purified water by a 60-mesh sieve to prepare a soft material;
6) drying the soft material at 60 deg.C for 1 hr;
7) sieving with 40 mesh sieve, and grading to obtain the pharmaceutical composition containing ibuprofen arginine.
Example 2
A pharmaceutical composition containing ibuprofen arginine comprises the following components in parts by weight:
| arginine ibuprofen | 1 part of |
| Sucrose | 0.5 portion |
| Stearic acid | 0.5 portion |
| Purified water | 0.05 part |
The preparation method of the pharmaceutical composition containing the arginine ibuprofen comprises the following steps:
1) heating stearic acid to melt, and controlling the temperature at 100 ℃;
2) adding ibuprofen arginine into the stearic acid molten liquid, and stirring uniformly;
3) spray drying, controlling the temperature of a sample at 95 ℃, controlling the temperature of air at 40 ℃, and sieving the obtained particles with a 100-mesh sieve;
4) sieving sucrose with 100 mesh sieve, mixing with the above granules, sieving with 40 mesh sieve, and mixing;
5) taking purified water as a wetting agent, and sieving the purified water by a 60-mesh sieve to prepare a soft material;
6) drying the soft material at 40 deg.C for 2 hr;
7) sieving with 40 mesh sieve, and grading to obtain the pharmaceutical composition containing ibuprofen arginine.
Example 3
A pharmaceutical composition containing ibuprofen arginine comprises the following components in parts by weight:
| arginine ibuprofen | 1 part of |
| Sucrose | 20 portions of |
| Stearic acid | 20 portions of |
| Purified water | 2 portions of |
The preparation method of the pharmaceutical composition containing arginine ibuprofen is the same as that in example 1.
Example 4
A pharmaceutical composition containing ibuprofen arginine comprises the following components in parts by weight:
| arginine ibuprofen | 1 part of |
| Sucrose | 1 part of |
| Stearic acid | 1 part of |
| Purified water | 0.1 part |
The preparation method of the pharmaceutical composition containing arginine ibuprofen is the same as that in example 2.
Example 5
A pharmaceutical composition containing ibuprofen arginine comprises the following components in parts by weight:
| arginine ibuprofen | 1 part of |
| Sucrose | 5 portions of |
| Stearic acid | 2 portions of |
| Purified water | 0.5 portion |
The preparation method of the pharmaceutical composition containing the arginine ibuprofen comprises the following steps:
1) heating stearic acid to melt, and controlling the temperature at 75 ℃;
2) adding ibuprofen arginine into the stearic acid molten liquid, and stirring uniformly;
3) spray drying, controlling the temperature of a sample at 85 ℃, controlling the temperature of air at 30 ℃, and sieving the obtained particles with a 80-mesh sieve;
4) sieving sucrose with 80 mesh sieve, mixing with the above granules, sieving with 40 mesh sieve, and mixing;
5) taking purified water as a wetting agent, and sieving the purified water by a 60-mesh sieve to prepare a soft material;
6) drying the soft material at 50 deg.C for 1.5 h;
7) sieving with 40 mesh sieve, and grading to obtain the pharmaceutical composition containing ibuprofen arginine.
Comparative example 1
A pharmaceutical composition containing ibuprofen arginine comprises the following components in parts by weight:
| arginine ibuprofen | 1 part of |
| Sucrose | 0.5 portion |
| Polyvinylpyrrolidone | 0.5 portion |
| Purified water | 0.05 part |
The preparation method of the pharmaceutical composition containing the arginine ibuprofen comprises the following steps:
1) heating polyvinylpyrrolidone to melt, and controlling the temperature at 100 ℃;
2) adding ibuprofen arginine into the stearic acid molten liquid, and stirring uniformly;
3) spray drying, controlling the temperature of a sample at 95 ℃, controlling the temperature of air at 40 ℃, and sieving the obtained particles with a 100-mesh sieve;
4) sieving sucrose with 100 mesh sieve, mixing with the above granules, sieving with 40 mesh sieve, and mixing;
5) taking purified water as a wetting agent, and sieving the purified water by a 60-mesh sieve to prepare a soft material;
6) drying the soft material at 40 deg.C for 2 hr;
7) sieving with 40 mesh sieve, and grading.
Comparative example 2
A pharmaceutical composition containing ibuprofen arginine comprises the following components in parts by weight:
| arginine ibuprofen | 1 part of |
| Sucrose | 5 portions of |
| Polyethylene glycol 6000 | 2 portions of |
| Purified water | 0.5 portion |
The preparation method of the pharmaceutical composition containing the arginine ibuprofen comprises the following steps:
1) heating polyethylene glycol 6000 to melt, and controlling the temperature at 80 ℃;
2) adding ibuprofen arginine into the stearic acid molten liquid, and stirring uniformly;
3) spray drying, controlling the temperature of a sample at 85 ℃, controlling the temperature of air at 30 ℃, and sieving the obtained particles with a 80-mesh sieve;
4) sieving sucrose with 180 mesh sieve, mixing with the above granules, sieving with 40 mesh sieve, and mixing;
5) taking purified water as a wetting agent, and sieving the purified water by a 60-mesh sieve to prepare a soft material;
6) drying the soft material at 50 deg.C for 1.5 h;
7) sieving with 40 mesh sieve, and grading.
The pharmaceutical compositions containing ibuprofen arginine according to the invention, prepared according to the above-described examples 1-5 and comparative examples 1-2, were analyzed:
(1) the samples obtained in examples 1 to 5 and comparative examples 1 to 2 were examined for pungent odor and taste, and the results are shown in Table 1 (odor and taste evaluation):
table 1 odor and mouthfeel evaluation
The above test results show that the products of examples 1-5 have significantly better odor and mouthfeel than the comparative product.
(2) According to the specification of the drug import standard JX20020151, the samples of the examples and the comparative examples are examined for properties, content difference, solubility, free ibuprofen and content, and the results are in accordance with the specification and are detailed in Table 2 (sample examination).
Table 2 sample examination
The above test results show that the products of examples 1-5 are significantly better than the comparative product in controlling the free ibuprofen as an impurity.
(3) Possibility of industrial utilization
In the pharmaceutical composition containing the ibuprofen arginine, the ibuprofen arginine particles with no pungent smell and good taste can be obtained by applying the sucrose and the stearic acid as the auxiliary materials, and the production cost is obviously lower than that of the ibuprofen arginine particles disclosed in the prior art, so that the ibuprofen arginine particle has an obvious industrial effect. In addition, the pharmaceutical composition containing the ibuprofen arginine disclosed by the invention does not adopt an ethanol solvent, so that the medication safety of alcohol allergy patients is improved, and the pharmaceutical composition has good social benefits.
Although the present invention has been described with reference to the above embodiments, it should be understood that the present invention is not limited thereto, and various changes and modifications may be made by those skilled in the art without departing from the spirit and scope of the present invention.
Claims (1)
1. The pharmaceutical composition containing the ibuprofen arginine is characterized by comprising the following components in parts by weight: 1 part of ibuprofen arginine, 5 parts of sucrose, 2 parts of stearic acid and 0.5 part of purified water;
the preparation method of the pharmaceutical composition containing the arginine ibuprofen comprises the following steps:
1) heating stearic acid to melt, and controlling the temperature at 75 ℃;
2) adding ibuprofen arginine into the stearic acid molten liquid, and stirring uniformly;
3) spray drying, controlling the temperature of a sample at 85 ℃, controlling the temperature of air at 30 ℃, and sieving the obtained particles with a 80-mesh sieve;
4) sieving sucrose with 80 mesh sieve, mixing with the above granules, sieving with 40 mesh sieve, and mixing;
5) taking purified water as a wetting agent, and sieving the purified water by a 60-mesh sieve to prepare a soft material;
6) drying the soft material at 50 deg.C for 1.5 h;
7) sieving with 40 mesh sieve, and grading to obtain the pharmaceutical composition containing ibuprofen arginine.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710377002.6A CN107233317B (en) | 2017-05-25 | 2017-05-25 | Pharmaceutical composition containing ibuprofen arginine and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710377002.6A CN107233317B (en) | 2017-05-25 | 2017-05-25 | Pharmaceutical composition containing ibuprofen arginine and preparation method thereof |
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| CN107233317A CN107233317A (en) | 2017-10-10 |
| CN107233317B true CN107233317B (en) | 2020-07-24 |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1054508C (en) * | 1987-05-14 | 2000-07-19 | 格拉克索集团有限公司 | Method for preparing pharmaceutical composition |
| CN1528278A (en) * | 2003-10-15 | 2004-09-15 | 杭州容立医药科技有限公司 | Method for preparing composition granules containing ibuprofen amino guanidyl valeric acid |
| WO2008090038A1 (en) * | 2007-01-22 | 2008-07-31 | Masterfarm, S.L. | Pulverulent pharmaceutical composition comprising ibuprofen and a polyalcohol |
-
2017
- 2017-05-25 CN CN201710377002.6A patent/CN107233317B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1054508C (en) * | 1987-05-14 | 2000-07-19 | 格拉克索集团有限公司 | Method for preparing pharmaceutical composition |
| CN1528278A (en) * | 2003-10-15 | 2004-09-15 | 杭州容立医药科技有限公司 | Method for preparing composition granules containing ibuprofen amino guanidyl valeric acid |
| WO2008090038A1 (en) * | 2007-01-22 | 2008-07-31 | Masterfarm, S.L. | Pulverulent pharmaceutical composition comprising ibuprofen and a polyalcohol |
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| Publication number | Publication date |
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| CN107233317A (en) | 2017-10-10 |
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Effective date of registration: 20200824 Address after: 325025 no.360 Binhai 25th Road, Xinghai street, Wenzhou Economic and Technological Development Zone, Wenzhou City, Zhejiang Province Patentee after: HAIHE PHARMA Co.,Ltd. WENZHOU Address before: 100871, 8 floor, No. 18 Zhongguancun Avenue, Beijing, Haidian District, 05-148 Patentee before: BEIJING WANPENG LANGGE MEDICINE TECHNOLOGY Co.,Ltd. |
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