CN105963259A - Method for preparing ibuprofen microspheres through normal-pressure filtration - Google Patents
Method for preparing ibuprofen microspheres through normal-pressure filtration Download PDFInfo
- Publication number
- CN105963259A CN105963259A CN201610350570.2A CN201610350570A CN105963259A CN 105963259 A CN105963259 A CN 105963259A CN 201610350570 A CN201610350570 A CN 201610350570A CN 105963259 A CN105963259 A CN 105963259A
- Authority
- CN
- China
- Prior art keywords
- ibuprofen
- microspheres
- microsphere
- water
- normal
- 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
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
- A61K9/14—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
- A61K9/1682—Processes
-
- 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
Abstract
The invention provides a method for preparing ibuprofen microspheres through normal-pressure filtration, belonging to the field of pharmaceutical preparation technical study. The method comprises the following steps: adding ibuprofen into deionized water, heating to 80-100 DEG C and preserving heat for 6-24h, and cooling to 0 DEG C; shaking the solution; filtering with filter paper under normal pressure at a speed of 5-11ml per minute; and drying for 24h at 40 DEG C to obtain the ibuprofen microspheres. In the method, the adopted raw material is single, no chemical aid is involved, and the guarantee of ibuprofen purity is promoted. With high density, the ibuprofen microspheres can suspend in water or sink to the bottom, and the efficiency of the technologies such as follow-up coating, tabletting and encapsulation of ibuprofen can be improved. The ibuprofen microspheres can increase the solubility of ibuprofen in water and improve the absorption and utilization of drugs.
Description
Technical field
The present invention provides a kind of method using natural filtration to prepare ibuprofen microsphere, belongs to drug preparation technique research field.
Background technology
As anti-inflammatory drug, ibuprofen for antiinflammatory, analgesia, rheumatism and the treatment of the disease such as antipyretic, its shortcoming is that dissolubility is low in water, bitter in the mouth, the half-life short (1.8-2 hour), patient needs frequent medication.Therefore develop slow release formulation to reduce administration number of times, i.e. realized by modes such as coating, suspendible and gels.Ibuprofen crude drug crystal is needle-like, density is little, hydrophobicity is strong, the most floating, and poor fluidity, easy sticking mould during compression molding, bring great inconvenience to subsequent techniques such as ibuprofen coating, tabletting and micropills processed.Using the methods such as melt molding, emulsion-diffusion method and melted-extrusion molding to be processed into by ibuprofen granular, the efficiency of subsequent technique will be greatly improved.
During the melt molding of ibuprofen, typically can add diluent and reduce the eutectic composition of melt temperature, ibuprofen melt being stirred into granular under high speed shear effect in the aqueous solution of low temperature.The chemical assistant that this process is used can affect the purity of ibuprofen to a certain extent, and the shot-like particle sphericity that during high speed shear, ibuprofen melt is formed is low, and the mobility of ibuprofen grain reduces.Up to the present, during melt molding, the research report of ibuprofen microsphere is prepared without chemical assistant considerably less.
Summary of the invention
It is an object of the invention to provide a kind of method using natural filtration to prepare ibuprofen microsphere, for achieving the above object, pass through following steps:
(1) ibuprofen is added in deionized water, then be warming up to insulation 6 ~ 24h after 80 ~ 100 C, be cooled to 0 C；
(2) will be after the solution that step (1) prepares shake 2 minutes under the speed of 250 ~ 280 rpms, through filter paper natural filtration, more i.e. obtain ibuprofen microsphere after dry 24h at 40 DEG C.
Wherein, in step (1), ibuprofen content in deionized water is 8.89 ~ 35.56 gram per liter.The speed filtered when filtering in step (2) be 5 ~ 11 milliliters per minute.
The size of ibuprofen microsphere can be regulated and controled by the speed of shake and the rate of filtration.
The beneficial effects of the present invention is:
1, the raw material that this method is used is single, without chemical assistant, the beneficially guarantee of ibuprofen purity；
2, the technique that this method is used is simple, and the deionized water that preparation solution is used can reuse after filtering, it is easy to industrialized production；
3, the ibuprofen Microsphere Size controllable that this method prepares, size is homogeneous；
4, the ibuprofen microsphere that this method prepares can improve ibuprofen dissolubility in water, improves absorption and the utilization of medicine；
5, this method prepares ibuprofen microsphere good fluidity, consistency height can suspend in water or sink to the bottom, and can improve the follow-up coating of ibuprofen microsphere, tabletting and the process efficiency such as encapsulated.
Accompanying drawing explanation
Fig. 1 is the SEM electron scanning micrograph of the ibuprofen microsphere of embodiment 1 preparation.
Detailed description of the invention
Embodiment 1
(1) 0.40 gram of ibuprofen is put in 45 ml deionized water, after being warming up to 100 C and being incubated 6h, be cooled to 0 C；
(2) through filter paper natural filtration after shaking 2 minutes under the solution that will prepare through step (1) is with the speed of 250 rpms, the rate of filtration be 11 milliliters per minute, then after 40 C are dried 24h, i.e. obtain ibuprofen microsphere.
Ibuprofen is at water float, and after dissolving 72 hours under 37 C in the phosphate buffer of pH=7.2, the dissolubility of ibuprofen is about 50 micro-gram per liter.And ibuprofen microsphere suspends in water or sinks to the bottom, after dissolving 72 hours under 37 C in the phosphate buffer of pH=7.2, the dissolubility of ibuprofen microsphere is about 77 micro-gram per liter.
Embodiment 2
(1) 1.60 grams of ibuprofen are put in 45 ml deionized water, after being warming up to 100 C and being incubated 6h, be cooled to 0 C；
(2) through filter paper natural filtration after shaking 2 minutes under the solution that will prepare through step (1) is with the speed of 280 rpms, the rate of filtration be 5 milliliters per minute, then after 40 C are dried 24h, i.e. obtain ibuprofen microsphere.
Ibuprofen suspends in water, and after dissolving 72 hours under 37 C in the phosphate buffer of pH=7.2, the dissolubility of ibuprofen is about 50 micro-gram per liter.And ibuprofen microsphere sinks to the bottom in water, after dissolving 72 hours under 37 C in the phosphate buffer of pH=7.2, the concentration of ibuprofen microsphere is about 83 micro-gram per liter.
Claims (2)
1. the method using natural filtration to prepare ibuprofen microsphere, is characterized in that comprising the following steps:
Ibuprofen is added in deionized water by step 1., and the content making ibuprofen is 8.89 ~ 35.56 gram per liter, then is warming up to insulation 6 ~ 24h after 80 ~ 100 C, is cooled to 0 C；
After the solution prepared through step 1 is shaken 2 minutes under the speed of 250 ~ 280 rpms by step 2., through filter paper natural filtration, more i.e. obtain ibuprofen microsphere after dry 24h under 40 C.
A kind of method using natural filtration to prepare ibuprofen microsphere the most as claimed in claim 1, it is characterised in that: in step 2 during natural filtration filter speed be 5 ~ 11 milliliters per minute.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610350570.2A CN105963259A (en) | 2016-05-25 | 2016-05-25 | Method for preparing ibuprofen microspheres through normal-pressure filtration |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610350570.2A CN105963259A (en) | 2016-05-25 | 2016-05-25 | Method for preparing ibuprofen microspheres through normal-pressure filtration |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105963259A true CN105963259A (en) | 2016-09-28 |
Family
ID=56956974
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610350570.2A Pending CN105963259A (en) | 2016-05-25 | 2016-05-25 | Method for preparing ibuprofen microspheres through normal-pressure filtration |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105963259A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109956860A (en) * | 2019-03-08 | 2019-07-02 | 天津大学 | Preparation method of ibuprofen spherical crystal |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5869101A (en) * | 1994-01-28 | 1999-02-09 | Gebro Borschek Gesellschaft M.B.H. | Process for the preparation of S(+)-ibuprofen-particles |
| CN105193731A (en) * | 2014-05-30 | 2015-12-30 | 华东理工大学 | Ibuprofen particle, ibuprofen preparation and preparation method of ibuprofen particle |
-
2016
- 2016-05-25 CN CN201610350570.2A patent/CN105963259A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5869101A (en) * | 1994-01-28 | 1999-02-09 | Gebro Borschek Gesellschaft M.B.H. | Process for the preparation of S(+)-ibuprofen-particles |
| CN105193731A (en) * | 2014-05-30 | 2015-12-30 | 华东理工大学 | Ibuprofen particle, ibuprofen preparation and preparation method of ibuprofen particle |
Non-Patent Citations (1)
| Title |
|---|
| 杨明，等: "《药剂学》", 31 August 2014, 中国医药科技出版社 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109956860A (en) * | 2019-03-08 | 2019-07-02 | 天津大学 | Preparation method of ibuprofen spherical crystal |
| CN109956860B (en) * | 2019-03-08 | 2022-03-01 | 天津大学 | Preparation method of ibuprofen spherical crystal |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN102924539B (en) | Method for preparing trehalose crystals | |
| JPS5858145A (en) | Microcapsule with fast releasability and preparation thereof | |
| WO2021196535A1 (en) | Large-particle spherical salt and preparation method therefor | |
| CN102382082B (en) | Novel potassium sodium dehydroandroan drographolide succinate compound and drug combination thereof | |
| CN107041874A (en) | A kind of fucoxanthin microcapsules and its preparation technology | |
| CN101914035B (en) | Method for preparing oxytetracycline hydrochloride | |
| CN104788472B (en) | One water Cefazolin sodium spheroidal particle and its crystallization preparation method | |
| CN105963259A (en) | Method for preparing ibuprofen microspheres through normal-pressure filtration | |
| CN102320954B (en) | Method for preparing ibuprofen with large crystal form | |
| WO2024087551A1 (en) | Method for preparing silver nanowires using soft template method | |
| CN106045843B (en) | The production technology of racemic ketoprofen isoleucine calcium | |
| CN103549635A (en) | Preparation method of resistant starch nutritional carrier based on metal-organic framework as well as product thereof | |
| CN105852131A (en) | Method for preparing organic food processing standard meeting fish oil microcapsules | |
| CN107823144A (en) | A kind of preparation method of high-purity mannitol vertical compression particle | |
| CN1351869A (en) | Method for preparing nanometer level pearli powder | |
| CN102058548B (en) | Ambroxol hydrochloride composition for injection and preparation method thereof | |
| CN103755609B (en) | Crystal formation of tartaric acid valnemulin and preparation method thereof | |
| CN103694280B (en) | From containing the method extracting glucosamine hydrochloride glucosamine hydrochloride mother liquid | |
| CN102525976B (en) | Method for preparing strontium ranelate orally disintegrating tablets with fluidized bed | |
| CN104402705B (en) | Spherical calcium citrate, and preparation method and application thereof | |
| CN103087138B (en) | Ginsenoside C-K monohydrate crystal and preparation method thereof | |
| CN103536575B (en) | Acetylcysteine composition capsule | |
| CN108653214B (en) | Cefdinir granules and preparation method thereof | |
| CN106361708A (en) | High-density micropill core and preparation method thereof | |
| CN109535022B (en) | Preparation method for improving fluidity of L-carnitine fumarate |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into 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: 20160928 |