CN102440963A - Allopurinol sustained release pellet and preparation method thereof - Google Patents
Allopurinol sustained release pellet and preparation method thereof Download PDFInfo
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- CN102440963A CN102440963A CN2011103861615A CN201110386161A CN102440963A CN 102440963 A CN102440963 A CN 102440963A CN 2011103861615 A CN2011103861615 A CN 2011103861615A CN 201110386161 A CN201110386161 A CN 201110386161A CN 102440963 A CN102440963 A CN 102440963A
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- allopurinol
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Abstract
The invention relates to an allopurinol sustained release pellet, which does not need to adopt special equipment, and comprises allopurinol, sustained release material and hydrophobicbase with the mass ratio of 1%-50%. The hydrophobicbase can adjust the drug release, concretely, after the sustained release pellet enters the body, the sustained release pellet is limited due to the entering of water, so the drug release is slowed down, and the function of retarding the drug release is played.
Description
Technical field
The present invention relates to a kind of allopurinol new sustained release micropill.Specifically, this micropill is regulated drug release jointly through hydrophobic base and slow-release material, and the micropill drug release homogeneity of preparation is good, and micropill outward appearance rounding, good fluidity.
Background technology
Micropill is meant all kinds of pills of diameter less than 2.5mm, can be made into rapid release or slow-release micro-pill according to different needs.At present the emphasis of research is a slow-release micro-pill, and slow-release micro-pill is to be mixed and made into or to process earlier common ball core by medicine and blocker then to wrap release-controlled film again and form.Micropill can be suppressed in flakes, also can micropill be loaded on and process capsule in the capsule.Slow release, controlled release micro pill are a kind of novel forms that develops rapidly in the world; It is steady with blood drug level, toxic and side effects is little, take number of times few, can take together with liquid, characteristics such as relative low price receive numerous doctors and patient's welcome deeply; Market prospect is very good, will become a main trend slow, the controlled release preparation development.At present, the release mechanism according to slow-release micro-pill is divided into usually: 1) waxiness, insoluble macromolecular scaffold micropill release mechanism; 2) contain the coating membrane release mechanism of porogen; 3) resin type micropill release mechanism 4) pulsed release micropill release mechanism pulsatile drug delivery system (pulsatile release system) with the timing controlled mode in gastrointestinal tract specific part (like stomach, colon) release; Its release mode meets the human body circadian rhythm and changes, and is a frontier of recent pharmaceutical preparation research.
Wherein, Micropill for adopting waxiness, insoluble macromolecular scaffold micropill release mechanism is many; The technical scheme that adopts also respectively has characteristics; For example, the mixture that application number CN97198537.5 discloses employing cera alba, valproic acid (allopurinol) and surfactant composition stirs in the water-bearing media of pH=4.5, and the colleague remains on the melt temperature that is higher than wax with the temperature of mixture.During cooling, owing to the spheroidal particle that disperses to form is solidified into microspheres form, yet, adopt this scheme, need when mixing, keep temperature stabilization, comparatively loaded down with trivial details during preparation, and need professional high temperature resistant equipment, cost is higher.
Allopurinol mainly uses in gout outbreak interval and chronic phase, is applicable to that uricopoiesis is too much, irritated or invalid to uricosuric, and the constitutional and the secondary gout patient that should not use uricotelic drugs (if any renal insufficiency), with the control hyperuricemia.This medicine also can share with uricosuric, to strengthen curative effect, is specially adapted to the serious and fair patient of renal function of tophus.Because this medicine need be taken for a long time, is particularly suitable for being prepared into sustained-release preparation.
Summary of the invention
Main purpose of the present invention has been to provide a kind of allopurinol slow-release micro-pill that need not to adopt special installation, comprises that allopurinol, slow-release material, mass ratio are the hydrophobic base of 1%-50%.This hydrophobic base can be regulated drug release, and specifically, after in this slow-release micro-pill entering body, because the entering of moisture is restricted, the release of medicine is slowed down, and plays the effect that blocking medicine discharges.
Further, said hydrophobic base is waxiness or fatty acid and ester or Polyethylene Glycol or organic acid.Specifically, lyophobic dust is stearic acid or Brazil wax or glyceryl monostearate or stearyl alcohol or propylene glycol or paraffin.Use above-mentioned hydrophobic base, can form the hydrophobicity skeleton, moisture gets into micropill inside through the space of this skeleton, forms Concentraton gradient thereby make medicine be able to dissolving, and medicine discharges gradually.And the inventor finds that surprisingly when using a certain amount of above-mentioned material, it can make that at a certain temperature micropill has certain deformation, and at process collision postcooling, the micropill that makes is rounding more, and hardness is moderate, is fit to further coating or tabletting.Therefore, preferably this hydrophobic base can produce certain deformation more than or equal to 40 ℃.And hydrophobic base produces the temperature of deformation preferably less than 500 ℃.
Further, this hydrophobic base can soften or become fluid state at a certain temperature or be made up of eutectic.
Specifically, said slow-release material is hydrophilic framework material or erodible framework material.
Further, the selection hydrophobic base is 1%-30%, is preferably 5%-15%.
The present invention further provides a kind of method for preparing of said allopurinol slow-release micro-pill, it is characterized in that, allopurinol, slow-release material and hydrophobic base are placed wet mixing pelletizer; Spray into adhesive or wetting agent, make soft, with soft just extrude round as a ball; Dry materials with round as a ball promptly gets.Temperature during preferably, with dry materials is the temperature that hydrophobic base produces deformation.
The specific embodiment
Below come further to explain or explanation content of the present invention through embodiment.Described embodiment has been merely and has helped to understand content of the present invention, should not be understood that the qualification to purport of the present invention and protection domain.
Drug release determination method of the present invention is release medium referring to two appendix XD first methods of Chinese Pharmacopoeia version in 2010 with water.
Embodiment 1
The ball core is formed:
Process 1000 preparation units through being prepared as follows method:
(1) ball core preparation places wet mixing pelletizer with allopurinol, slow-release material and hydrophobic base, sprays into certain water gaging, and the system soft material is extruded soft material round as a ball, with 70 ℃ of dryings of round as a ball material, promptly gets.
Adopt two appendix XD first methods of Chinese Pharmacopoeia version in 2010 to measure the release degree of said preparation, measure the result and see table 1.
Embodiment 2
The ball core is formed:
Allopurinol 200g
Cane sugar powder 30g
Brazil wax 230g
Process 1000 preparation units through being prepared as follows method:
(1) ball core preparation places wet mixing pelletizer with allopurinol, slow-release material and hydrophobic base, sprays into certain water gaging, and the system soft material is extruded soft material round as a ball, with 55 ℃ of dryings of round as a ball material, promptly gets.
Adopt two appendix XD first methods of Chinese Pharmacopoeia version in 2010 to measure the release degree of said preparation, measure the result and see table 1.
Embodiment 3
The ball core is formed:
Process 1000 preparation units through being prepared as follows method:
(1) ball core preparation places wet mixing pelletizer with allopurinol, slow-release material and hydrophobic base, sprays into certain water gaging, and the system soft material is extruded soft material round as a ball, with 75 ℃ of dryings of round as a ball material, promptly gets.
Adopt two appendix XD first methods of Chinese Pharmacopoeia version in 2010 to measure the release degree of said preparation, measure the result and see table 1.
Embodiment 4
The ball core is formed:
Allopurinol 200g
Microcrystalline Cellulose 101 10g
Glyceryl monostearate 90g
Process 1000 preparation units through being prepared as follows method:
(1) ball core preparation places wet mixing pelletizer with allopurinol, slow-release material and hydrophobic base, sprays into certain water gaging, and the system soft material is extruded soft material round as a ball, with 55 ℃ of dryings of round as a ball material, promptly gets.
Adopt two appendix XD first methods of Chinese Pharmacopoeia version in 2010 to measure the release degree of said preparation, measure the result and see table 1.
Embodiment 5
The ball core is formed:
Process 1000 preparation units through being prepared as follows method:
(1) ball core preparation places wet mixing pelletizer with allopurinol, slow-release material and hydrophobic base, sprays into certain water gaging, and the system soft material is extruded soft material round as a ball, with 45 ℃ of dryings of round as a ball material, promptly gets.
Adopt two appendix XD first methods of Chinese Pharmacopoeia version in 2010 to measure the release degree of said preparation, measure the result and see table 1.
To sum up, said preparation unit is meant the micropill of preparation is dressed up capsule or added suitable adjuvant and process tablet.
Each embodiment drug accumulation release degree of table 1
What need explanation is that above embodiment is just to illustrating the present invention.Under the prerequisite that does not depart from spirit of the present invention and essence, those skilled in the art can design multiple alternative of the present invention and improvement project, and it all should be understood to be within protection scope of the present invention.
Claims (10)
1. an allopurinol slow-release micro-pill comprises that principal agent, slow-release material, mass ratio are the hydrophobic base of 1%-50%.
2. the said allopurinol slow-release micro-pill of claim 1 is characterized in that, said hydrophobic base is waxiness or fatty acid and ester or Polyethylene Glycol or organic acid.
3. the said allopurinol slow-release micro-pill of claim 2 is characterized in that, lyophobic dust is stearic acid or Brazil wax or glyceryl monostearate or stearyl alcohol or propylene glycol or paraffin.
4. each allopurinol of claim 1-3 is stated slow-release micro-pill, it is characterized in that, hydrophobic base is 1%-30%, is preferably 5%-15%.
5. the said allopurinol slow-release micro-pill of claim 1-4, this hydrophobic base can produce certain deformation more than or equal to 40 ℃.
6. the said allopurinol slow-release micro-pill of claim 5 is characterized in that, hydrophobic base produces the temperature of deformation less than 500 ℃.
7. the said allopurinol slow-release micro-pill of claim 6 is characterized in that, said deformation is because hydrophobic base is softening or become fluid state or be made up of eutectic.
8. each said allopurinol slow-release micro-pill of claim 1-7 is characterized in that, said slow-release material is hydrophilic framework material or erodible framework material.
9. the method for preparing of each said allopurinol slow-release micro-pill of claim 1-8 is characterized in that, principal agent, slow-release material and hydrophobic base are placed wet mixing pelletizer; Spray into adhesive or wetting agent, make soft, with soft just extrude round as a ball; Dry materials with round as a ball promptly gets.
10. the method for preparing of the said allopurinol slow-release micro-pill of claim 9, the temperature during with dry materials are the temperature that hydrophobic base produces deformation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011103861615A CN102440963A (en) | 2011-11-29 | 2011-11-29 | Allopurinol sustained release pellet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011103861615A CN102440963A (en) | 2011-11-29 | 2011-11-29 | Allopurinol sustained release pellet and preparation method thereof |
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| Publication Number | Publication Date |
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| CN102440963A true CN102440963A (en) | 2012-05-09 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN2011103861615A Pending CN102440963A (en) | 2011-11-29 | 2011-11-29 | Allopurinol sustained release pellet and preparation method thereof |
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| CN (1) | CN102440963A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103142602A (en) * | 2013-03-15 | 2013-06-12 | 汤日波 | Application of allopurinol in preparing medicines after atrial fibrillation catheter ablation |
| CN103417506A (en) * | 2013-06-24 | 2013-12-04 | 深圳翰宇药业股份有限公司 | Allopurinol sustained-release pellet and preparation method and preparation thereof |
| CN104288127A (en) * | 2014-11-04 | 2015-01-21 | 周有财 | Allopurinol sustained release capsule and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1739522A (en) * | 2004-12-17 | 2006-03-01 | 范敏华 | Slowly releasing allopurinol tablet and its prepn |
| CN101288659A (en) * | 2007-04-18 | 2008-10-22 | 王雷波 | Floating type pellets in stomach and preparation method thereof |
| CN101652128A (en) * | 2007-03-02 | 2010-02-17 | 法纳姆公司 | Sustained release compositions using wax-like materials |
-
2011
- 2011-11-29 CN CN2011103861615A patent/CN102440963A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1739522A (en) * | 2004-12-17 | 2006-03-01 | 范敏华 | Slowly releasing allopurinol tablet and its prepn |
| CN101652128A (en) * | 2007-03-02 | 2010-02-17 | 法纳姆公司 | Sustained release compositions using wax-like materials |
| CN101288659A (en) * | 2007-04-18 | 2008-10-22 | 王雷波 | Floating type pellets in stomach and preparation method thereof |
Non-Patent Citations (2)
| Title |
|---|
| 潘卫三 主编: "《新药制剂技术》", 31 October 2004, 北京：化学工业出版社, article ""4.3.2 蜡质骨架片"、"4.4 微丸型缓控释制剂"" * |
| 陆彬 主编: "《药物新剂型与新技术》", 30 April 1998, 北京：人民卫生出版社, article ""生物溶蚀性骨架材料"" * |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103142602A (en) * | 2013-03-15 | 2013-06-12 | 汤日波 | Application of allopurinol in preparing medicines after atrial fibrillation catheter ablation |
| CN103142602B (en) * | 2013-03-15 | 2014-12-10 | 汤日波 | Application of allopurinol in preparing medicines after atrial fibrillation catheter ablation |
| CN103417506A (en) * | 2013-06-24 | 2013-12-04 | 深圳翰宇药业股份有限公司 | Allopurinol sustained-release pellet and preparation method and preparation thereof |
| CN103417506B (en) * | 2013-06-24 | 2016-08-10 | 深圳翰宇药业股份有限公司 | A kind of Allopurinol sustained release pellet and preparation method thereof and preparation |
| CN104288127A (en) * | 2014-11-04 | 2015-01-21 | 周有财 | Allopurinol sustained release capsule and preparation method thereof |
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Address after: 100083 A building, block 15, Tiangong building, No. 30, Haidian District, Beijing, Xueyuan Road Applicant after: Beijing Kexin Bicheng Medicine Science & Technology Developing Co., Ltd. Address before: 100190, room 1410, satellite building, No. 63, Zhichun Road, Beijing, Haidian District Applicant before: Beijing Kexin Bicheng Medicine Science & Technology Developing Co., Ltd. |
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Application publication date: 20120509 |