CN101849901A - Technique for preparing controlled-release preparation of zero-order release bar and preparation thereof - Google Patents
Technique for preparing controlled-release preparation of zero-order release bar and preparation thereof Download PDFInfo
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- CN101849901A CN101849901A CN201010143897A CN201010143897A CN101849901A CN 101849901 A CN101849901 A CN 101849901A CN 201010143897 A CN201010143897 A CN 201010143897A CN 201010143897 A CN201010143897 A CN 201010143897A CN 101849901 A CN101849901 A CN 101849901A
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- bar
- soluble protein
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- modified corn
- release
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Abstract
The invention belongs to a preparation technique used in the field of needing a zero-order release target, and discloses a method for preparing a biocompatible and environment-friendly bar controlled-release preparation. The method is mainly characterized by comprising the following steps of: mixing zein and medicament in a solvent such as water, alcohol and the like in a certain ratio uniformly, then extruding the mixture on an extruder to form a bar, drying the bar, coating the bar by using ethyl cellulose, chitosan, polycaprolactone and the like as a coating material, and drying the bar. The bar has good zero-order release behavior, and the release time of active ingredients of the medicament and the like can be adjusted within 8 hours to one year. The method has low processing cost, and can fully meet the requirement of industrialized production.
Description
Technical field
The invention belongs to medicine, agricultural and daily life field, especially need to use under the occasion of constant release material, and can be used for the technology of preparing of the inside and outside controlled release preparation of human body.
Background technology
The sustained release preparation is exactly that medicine or other active substances and appropriate carriers are made preparation by certain form, makes medicine or other active substance dosage by design, in the time range that requires with certain rate of release constant release.At field of medicaments, controlled release preparation is compared with traditional administering mode, and the medicine controlled releasing agent not only can reduce administration number of times, keep the concentration of blood Chinese medicine, thereby has solved the drug level problem of unstable, but also reduced drug toxicity, improved the curative effect of medicine.
The main distinction of controlled release preparation and slow releasing preparation is that controlled release preparation is to discharge medicine by zero level speed rule, and its burst size is not subjected to time effects, and rate of release is a constant speed or near constant speed, obtains blood drug level more stably.
Mostly existing controlled release preparation is osmotic pump tablet, and as antidiabetic drug glibenclamide controlled release tablet, it is craft or laser boring on coated tablet, and under the effect of label osmotic pressure, medicine diffuses in the body from the hole; The preparation method of another kind of controlled release preparation is to add porogen in tablet coating film prescription, after taking, with the porogen stripping, and stays many micropores by water, and medicine diffuses into human body from the coating membrane micropore; Utilize methods such as macromolecular material hydrogel to prepare controlled release preparation in addition.These methods can repeat stable, controlled release preparation success, practicality owing to multiple complicated reason is difficult to form, majority is among the research.
The present invention proposes a kind of bar-shaped controlled release preparation, need not punch, need not add porogen yet, the diffusion of medicine is realized in the nanoscale space that utilizes macromolecular material itself to form, bar-shaped in addition surface area ratio tablet is big, characteristics and other factors of excellent core zein water-swellable of while, thereby be prepared into a kind of novel controlled release preparation, by regulating coating prescription or excellent core preparation technology, the present invention can realize the clavate controlled release agent of the almost constant release of medicine isoreactivity material from several hours to the several months, and this clavate controlled release agent promptly can be used for the human body oral formulations and can be used for external any usefulness that needs certain material of constant release again.
Summary of the invention
The object of the present invention is to provide a kind of new controlled release preparation technology of preparing, overcome the deficiency of existing controlled release preparation preparation method, controlled release preparation inanimate object toxicity of the present invention, cheap and easy to get, preparation is simple.
The object of the present invention is achieved like this:
1. be the zero level release coating materials of framework material with the modified corn alcohol soluble protein, its composition characteristic is:
Comprise that following component and each composition weight proportioning are:
Modified corn alcohol soluble protein 30～75%
Active substance 20～65%
Coating material 5～20%
The modified corn alcohol soluble protein comprises the modifier through materials such as polyvinyl alcohol, polypyrrole alkane ketone, polyacrylic acid, oleic acid;
Active substance comprises chemical medicine, Chinese medicine extract, spice, pigment, chemical fertilizer, pesticide etc.;
Coated fertilizer comprises hypromellose (HPMC), ethyl cellulose (EC), cellulose acetate (CA and TCA), polycaprolactone (PCL), polycaprolactam, polyacrylic resin, silicone rubber, chitosan and material modified.
2. according to claim 1 is the preparation method of the zero level release peplos agent of framework material with the modified corn alcohol soluble protein, it is characterized in that: modified corn alcohol soluble protein and active matter pledge are blended in the ethanol equal solvent by weight ratio, stirring makes mix homogeneously, it is bar-shaped to adopt special extruder that mixture is squeezed into, and excellent drying is become semi-finished product.
3. according to claim 1 and the 2 described active substance clubs that contain, carry out peplos, the coating liquid preparation method is characterised in that:
Material therefor is bio-compatible or environment-friendly material as HPMC, EC, CA, TCA, PCL etc., gets wherein a kind of or several and makes solution and carry out peplos to containing the active substance club by usual method, and drying can obtain product of the present invention.
According to claim 1,2 and 3 described be that the bar-shaped zero level of framework material discharges the peplos agent with the modified corn alcohol soluble protein, it is characterized in that: this draw ratio that contains the active substance club is 100～0.1: 10～0.005.
According to claim 1,2 and 3 described be that the bar-shaped zero level of framework material discharges the peplos agent with the modified corn alcohol soluble protein, it is characterized in that: the active substance release behavior meets zero level and discharges or the Higuichi equation.
According to claim 1,2,3 and 4 described be that the bar-shaped zero level of framework material discharges the peplos agent with the modified corn alcohol soluble protein, it is characterized in that: this contains the active substance club and can be used for oral formulations, insecticide, balm, sustained-controll-release fertiliser etc. and need zero level to discharge purpose to use.
Advantage of the present invention and good effect are:
1. material such as used zein of the present invention is perhaps environment-friendly material of biofacies, and is cheap and easy to get;
2. by being framework material,, can realize that zero level discharges or discharges near zero level for active substance not of the same race again in the skeleton outer coatings with the modified corn alcohol soluble protein.Can make in addition medicine in vivo release time longer, drug release rate is more stable.
The specific embodiment
Below embodiments of the invention are further described:
Example one:
This coating implant comprises that following component and each composition weight proportioning are:
PEG modified corn alcohol soluble protein 50%
5-FU 40％，
EC 10％
Preparation method is:
(1) PEG modified corn alcohol soluble protein is mixed by weight ratio with 5-fluorouracil, add 50%～95% 0.2～3 times alcoholic solution in mixture, heating is stirred this mixed liquor simultaneously and was made in 30～60 minutes till the abundant mix homogeneously of this mixed liquor.
(2) adopt special extruder that mixed liquor is squeezed into club, with excellent vacuum drying 6～12 hours, this club was semi-finished product.
(3) use the 10%EC alcoholic solution as coating material, with rod coating pan coating, dry then, it is the coated slow release agent of framework material that preparation becomes with the zein.
Raw material of the present invention is the universal product on the market, and according to the coating thickness difference, drug release time can be 6～24 hours in the body.
Example two:
This coating implant comprises that following component and each composition weight proportioning are:
Polyacrylic acid modified zein 60%
Garden lavender quintessence oil 20%
Silicone rubber 20%
Preparation method is:
(1) the modified corn alcohol soluble protein is mixed by weight ratio with the Garden lavender quintessence oil, in mixture, add 95% 0.3 times ethanol, stir this mixed liquor simultaneously this is mixed till the abundant mix homogeneously.
(2) adopt special extruder that mixed liquor is squeezed into club.
(3) with 5% silicone rubber solution as coating material, with rod coating pan coating, fling to solvent.Can get fragrant rod, release time was at 2-6 month.
Example three:
This coating implant comprises that following component and each composition weight proportioning are:
Oleic acid modified corn alcohol soluble protein 40%
5-fluorouracil 40%
PCL coating material 20%
This coating implant gets preparation method:
(1) oleic acid modified corn alcohol soluble protein is mixed by weight ratio with 5-fluorouracil, add 50%～95% 0.2～3 times alcoholic solution in mixture, heating is stirred this mixed liquor simultaneously and was made in 30～60 minutes till the abundant mix homogeneously of this mixed liquor.
(2) adopt special extruder that mixed liquor is squeezed into club, with excellent vacuum drying 6～12 hours.
(3) add acetic acid ethyl dissolution with biodegradation material PCL and become 10% solution as coating material, with rod coating pan coating, dry then, it is the coating implant of framework material that preparation becomes with the zein.According to the coating thickness difference, drug release time can be 6～24 months in the body.
Claims (6)
1. be the zero level release coating materials of framework material with the modified corn alcohol soluble protein, its composition characteristic is:
Comprise that following component and each composition weight proportioning are:
Modified corn alcohol soluble protein 30～75%
Active substance 20～65%
Coating material 5～20%
The modified corn alcohol soluble protein comprises the modifier through materials such as polyvinyl alcohol, polypyrrole alkane ketone, polyacrylic acid, oleic acid;
Active substance comprises chemical medicine, Chinese medicine extract, spice, pigment, chemical fertilizer, pesticide etc.;
Coated fertilizer comprises hypromellose (HPMC), ethyl cellulose (EC), cellulose acetate (CA and TCA), polycaprolactone (PCL), polycaprolactam, polyacrylic resin, silicone rubber, chitosan and material modified.
2. according to claim 1 is the preparation method of the zero level release peplos agent of framework material with the modified corn alcohol soluble protein, it is characterized in that: modified corn alcohol soluble protein and active matter pledge are blended in the ethanol equal solvent by weight ratio, stirring makes mix homogeneously, it is bar-shaped to adopt special extruder that mixture is squeezed into, and excellent drying is become semi-finished product.
3. according to claim 1 and the 2 described active substance clubs that contain, carry out peplos, the coating liquid preparation method is characterised in that: material therefor is bio-compatible or environment-friendly material as HPMC, EC, CA, TCA, PCL etc., get wherein a kind of or several and make solution and carry out peplos to containing the active substance club by usual method, drying can obtain product of the present invention.
According to claim 1,2 and 3 described be that the bar-shaped zero level of framework material discharges the peplos agent with the modified corn alcohol soluble protein, it is characterized in that: this draw ratio that contains the active substance club is 100～0.1: 10～0.005.
According to claim 1,2 and 3 described be that the bar-shaped zero level of framework material discharges the peplos agent with the modified corn alcohol soluble protein, it is characterized in that: the active substance release behavior meets zero level and discharges or the Higuichi equation.
According to claim 1,2,3 and 4 described be that the bar-shaped zero level of framework material discharges the peplos agent with the modified corn alcohol soluble protein, it is characterized in that: this contains the active substance club and can be used for oral formulations, insecticide, balm, sustained-controll-release fertiliser etc. and need zero level to discharge purpose to use.
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201010143897A CN101849901A (en) | 2010-04-08 | 2010-04-08 | Technique for preparing controlled-release preparation of zero-order release bar and preparation thereof |
| CN2011100963763A CN102232921A (en) | 2010-04-08 | 2011-04-08 | Technique for preparing rod-like sustained-release preparation by using blending-modified corn zein as skeleton material and preparation prepared by technique |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201010143897A CN101849901A (en) | 2010-04-08 | 2010-04-08 | Technique for preparing controlled-release preparation of zero-order release bar and preparation thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101849901A true CN101849901A (en) | 2010-10-06 |
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Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201010143897A Pending CN101849901A (en) | 2010-04-08 | 2010-04-08 | Technique for preparing controlled-release preparation of zero-order release bar and preparation thereof |
| CN2011100963763A Pending CN102232921A (en) | 2010-04-08 | 2011-04-08 | Technique for preparing rod-like sustained-release preparation by using blending-modified corn zein as skeleton material and preparation prepared by technique |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2011100963763A Pending CN102232921A (en) | 2010-04-08 | 2011-04-08 | Technique for preparing rod-like sustained-release preparation by using blending-modified corn zein as skeleton material and preparation prepared by technique |
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Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104387213A (en) * | 2014-10-21 | 2015-03-04 | 金正大生态工程集团股份有限公司 | Biodegradable controlled-release coated urea and preparation method thereof |
| CN106242848A (en) * | 2016-08-30 | 2016-12-21 | 贵州开磷集团股份有限公司 | A kind of leguminous plant Special slow release fertilizer and preparation method thereof |
| CN107441500A (en) * | 2017-09-19 | 2017-12-08 | 云智前沿科技发展（深圳）有限公司 | Colon targeting drug administration oral formulations film-forming composition and preparation method, application process |
| CN107827654A (en) * | 2017-11-28 | 2018-03-23 | 芜湖四高农业科技有限公司 | A kind of radish composite fertilizer for improving soil texture |
| CN108299109A (en) * | 2018-04-17 | 2018-07-20 | 史丹利化肥遂平有限公司 | A kind of long-acting leafy vegetable special fertilizer and preparation method thereof |
| CN111434643A (en) * | 2019-01-14 | 2020-07-21 | 石河子大学 | Slow/controlled release fertilizer prepared based on natural protein and preparation method and application thereof |
| CN113582782A (en) * | 2021-08-13 | 2021-11-02 | 贵州省烟草科学研究院 | Segmented-absorption fully-degradable coated rod fertilizer for cigarettes and preparation method thereof |
| CN115735938A (en) * | 2022-11-21 | 2023-03-07 | 广东省科学院微生物研究所(广东省微生物分析检测中心) | Dopamine-modified prochloraz polycaprolactone nanosphere and preparation method and application thereof |
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| CN103242088A (en) * | 2013-04-25 | 2013-08-14 | 苏州谷力生物科技有限公司 | Slow-release leaf surface selenium fertilizer |
| CN105967921A (en) * | 2016-02-25 | 2016-09-28 | 马鞍山市全润农业科技有限公司 | Modified-Chinese-chestnut-protein-coated slow-release medicinal fertilizer |
| CN108997060B (en) * | 2018-09-12 | 2021-09-03 | 石河子大学 | Coated slow-release fertilizer chelating medium and trace elements based on humic acid materials and preparation method and application thereof |
| CN109350609A (en) * | 2018-11-14 | 2019-02-19 | 常州大学 | A kind of preparation of chitosan package zeins nanoparticle and the application for loading acacetin sodium salt |
-
2010
- 2010-04-08 CN CN201010143897A patent/CN101849901A/en active Pending
-
2011
- 2011-04-08 CN CN2011100963763A patent/CN102232921A/en active Pending
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104387213A (en) * | 2014-10-21 | 2015-03-04 | 金正大生态工程集团股份有限公司 | Biodegradable controlled-release coated urea and preparation method thereof |
| CN106242848A (en) * | 2016-08-30 | 2016-12-21 | 贵州开磷集团股份有限公司 | A kind of leguminous plant Special slow release fertilizer and preparation method thereof |
| CN107441500A (en) * | 2017-09-19 | 2017-12-08 | 云智前沿科技发展（深圳）有限公司 | Colon targeting drug administration oral formulations film-forming composition and preparation method, application process |
| CN107827654A (en) * | 2017-11-28 | 2018-03-23 | 芜湖四高农业科技有限公司 | A kind of radish composite fertilizer for improving soil texture |
| CN108299109A (en) * | 2018-04-17 | 2018-07-20 | 史丹利化肥遂平有限公司 | A kind of long-acting leafy vegetable special fertilizer and preparation method thereof |
| CN111434643A (en) * | 2019-01-14 | 2020-07-21 | 石河子大学 | Slow/controlled release fertilizer prepared based on natural protein and preparation method and application thereof |
| CN113582782A (en) * | 2021-08-13 | 2021-11-02 | 贵州省烟草科学研究院 | Segmented-absorption fully-degradable coated rod fertilizer for cigarettes and preparation method thereof |
| CN115735938A (en) * | 2022-11-21 | 2023-03-07 | 广东省科学院微生物研究所(广东省微生物分析检测中心) | Dopamine-modified prochloraz polycaprolactone nanosphere and preparation method and application thereof |
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| Publication number | Publication date |
|---|---|
| CN102232921A (en) | 2011-11-09 |
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Open date: 20101006 |