CN102940888B - Targeted drug delivery method of pectin colon containing lecithin - Google Patents
Targeted drug delivery method of pectin colon containing lecithin Download PDFInfo
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- CN102940888B CN102940888B CN201210448390.XA CN201210448390A CN102940888B CN 102940888 B CN102940888 B CN 102940888B CN 201210448390 A CN201210448390 A CN 201210448390A CN 102940888 B CN102940888 B CN 102940888B
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Abstract
The invention relates to a targeted drug delivery method of pectin colon containing lecithin, which comprises the following steps that (1) pectin is added into distilled water to be stirred and dissolved, then a colloidal solution is obtained, an alkali solution is added for saponification, and then a pectin solution is obtained after stirring; (2) the lecithin is added into the pectin solution to be uniformly mixed, a drug which needs to be carried is added, and ultrasonic dispersion is performed to obtain a uniform suspension; (3) the suspension is slowly dropped in a divalent metal ion salt solution with the mass concentration of 1% to 6% for gel curing reaction, and then gel balls are obtained after dropping, standing and suction filtration; and (4) the gel balls are washed with distilled water and then dried at room temperature, and then a finished product is obtained. According to the targeted drug delivery method, the pectin is used as a skeletal material, metallic ions are used as a crosslinking agent, the lecithin component is added in a compound way, the release of the drug is effectively controlled before the drug reaches colons, and the colon targeting property of gel micro pills is increased.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, relate to oral colon-target administration; More precisely, relate to a kind of medication taking pectin as framework material for medicine controlled releasing or oral colon-target administration.
Background technology
Colon targeting drug administration is mainly by drug delivery system, makes, after drug oral, not discharge in upper gi tract, drug conveying is started to disintegrate or loses and separate and discharge to human body ileocecus, in colon performance part or whole body therapeutic effect.Oral colon-target drug-delivery preparation is usually used in treating colonic diseases, as colitis, colon cancer etc., can make medicine directly discharge at diseased region, makes that medicine is more effective to play a role.
Pectin is a kind of natural macromolecule amylose, can be used as the carrier of medicine controlled releasing or oral colon-target administration.The enzymolysis type drug-supplying system that pectin makes is considered to location more accurately and reliably, and is not subject to the impact of individual variation.But the hydrophilic of pectin makes pectin base drug-supplying system easily swelling in environment and discharge in advance medicine in vivo.
In the past few years, in the time of design colon targeting drug administration system, take numerous methods to prevent that pectin base medicine from discharging in advance in upper gi tract.Pectin is by compound with other polymer, to improve hydrophobic performance; Pectin based system also can be coated by thin film or packaging technique the coating of slow release outward.The coating of different chemical composition can delay and the release of regulating drug at upper gi tract different parts, and the chemical composition of skeleton and coating polymer is to affect the key factor that colon specific drug discharges.
By retrieval, not yet find and the segmented intestine targeted relevant patent document of lecithin/pectin.
Summary of the invention
The object of the present invention is to provide a kind of pectin colon targeting drug administration method containing lecithin, this method is taking pectin as framework material, taking metal ion as cross-linking agent, by the compound lecithin fraction that adds, arrive antecolic release to control medicine, improving the segmented intestine targeted property of gel microsphere.
The object of the invention is to be achieved through the following technical solutions:
Containing a pectin colon targeting drug administration method for lecithin, step is:
(1) pectin is added to distilled water stirring and dissolving, form colloidal solution, add aqueous slkali to carry out saponification, stir and be made into pectin solution;
(2) in pectin solution, add lecithin, mix homogeneously, then add the medicine that needs carrier band, ultrasonic dispersion forms uniform suspension;
(3) above-mentioned suspension slowly being splashed into mass concentration is in 1% ~ 6% bivalent metal ion saline solution, carries out gel solidification reaction, after dripping afterwards place, sucking filtration, form gel ball;
(4) use distilled water wash gel ball, gained gel ball obtains finished product after being at room temperature dried.
And described pectin comprises hypo-methoxy pectin and hyper-methoxy pectin, high methoxyl carries out saponification processing by alkali in advance, and alkali comprises sodium hydroxide, potassium hydroxide, sodium carbonate etc., and the addition of alkali is 2% ~ 20% of pectin quality.
And the mass ratio of described lecithin and pectin is 1:4 ~ 8:4.
And the medicine of described carrier band comprises indomethacin, ketoprofen, acemetacin, mesalazine, budesonide, diclofenac sodium, the mass ratio of itself and pectin is 1:1-1:8.
And described bivalent metal ion salt comprises hydrochlorate or the sulfate of calcium ion, zinc ion, iron ion.
Advantage of the present invention and good effect are:
1, the present invention adds lecithin can effectively reduce the swellability of pectin gel micropill, and the drug carrying ability of pectin gel micropill and the sustained release performance in simulated intestinal fluid are significantly improved.
2, the present invention is after compound lecithin, lecithin/pectin gel micropill cumulative release rate in small intestinal simulated solution is starkly lower than simple pectin gel micropill, in small intestinal simulated solution, 8h cumulative release rate is reduced to below 5%, and lecithin/pectin gel micropill is also better than simple pectin gel micropill at high temperature and illumination stability inferior.
Detailed description of the invention
Below by detailed description of the invention, the present invention is described further, but should not be construed as limitation of the invention.Those of ordinary skill in the art, according to technique scheme, can also make amendment, replacement, the change of various ways.All amendments of doing based on above-mentioned technological thought, replacement, change all belong to scope of the present invention.
The percentage ratio of following each embodiment is mass percent.
The crude drug of following each embodiment, only taking indomethacin as example, can be ketoprofen, acemetacin, mesalazine, budesonide, diclofenac sodium in addition.
Embodiment 1:
A kind of preparation method of the lecithin/calcium pectinate micropill containing indomethacin: step is:
(1) pectin 0.4g, adds 8ml distilled water, forms colloidal solution, adds the NaOH solution saponification of 2ml 3%, stirs and is made into pectin solution;
(2) add 0.3g lecithin, stir it is mixed homogeneously with pectin solution, indomethacin crude drug 0.1g is added in pectin solution, ultrasonic it is uniformly dispersed;
(3) this suspension is slowly splashed in 6% calcium chloride solution, carry out gelling curing reaction, placement after dripping completes, sucking filtration, form gel ball;
(4) above-mentioned gel ball distilled water wash 2 ~ 3 times, the dry finished product that obtains.
Embodiment 2:
A kind of preparation method of the lecithin/calcium pectinate micropill containing indomethacin: step is:
(1) pectin 0.4g, adds 8ml distilled water, forms colloidal solution, adds the NaOH solution saponification of 2ml 2%, stirs and is made into pectin solution;
(2) add 0.3g lecithin, stir it is mixed homogeneously with pectin solution, indomethacin crude drug 0.15g is added in pectin solution, ultrasonic it is uniformly dispersed;
(3) this suspension is slowly splashed in 6% calcium chloride solution, carry out gelling curing reaction, placement after dripping completes, sucking filtration, form gel ball;
(4) above-mentioned gel ball distilled water wash 2 ~ 3 times, the dry finished product that obtains.
Embodiment 3:
A preparation method that contains lecithin/pectin zinc micropill of indomethacin, step is:
(1) pectin 0.4g, adds 8ml distilled water, forms colloidal solution, adds the NaOH solution saponification of 2ml 2%, stirs and is made into pectin solution;
(2) add 0.3g lecithin, treat that it mixs homogeneously with pectin solution, indomethacin crude drug 0.1g is added in pectin solution, ultrasonic it is uniformly dispersed;
(3) suspension is slowly splashed in 5% liquor zinci chloridi, carry out gelling curing reaction, placement after dripping completes, sucking filtration, form gel ball;
(4) above-mentioned gel ball distilled water wash 2 ~ 3 times, the dry finished product that obtains.
Embodiment 4:
A preparation method that contains lecithin/pectin zinc micropill of indomethacin, step is:
(1) pectin 0.4g, adds 8ml distilled water, forms colloidal solution, adds the NaOH solution saponification of 2ml2%, stirs and is made into pectin solution.
(2) add 0.5g lecithin, treat that it mixs homogeneously with pectin solution, indomethacin crude drug 0.1g is added in pectin solution, ultrasonic it is uniformly dispersed;
(3) suspension is slowly splashed in 6% liquor zinci chloridi, carry out gelling curing reaction, placement after dripping completes, sucking filtration, form gel ball;
(4) above-mentioned gel ball distilled water wash 2 ~ 3 times, the dry finished product that obtains.
Claims (4)
1. a preparation method for lecithin/pectin micropill of pastille, is characterized in that: step is:
(1) pectin is added to distilled water stirring and dissolving, form colloidal solution, add aqueous slkali to carry out saponification, stir and be made into pectin solution;
(2) in pectin solution, add lecithin, mix homogeneously, then add the medicine that needs carrier band, ultrasonic dispersion forms uniform suspension;
(3) above-mentioned suspension slowly being splashed into mass concentration is in 1%～6% bivalent metal ion saline solution, carries out gel solidification reaction, after dripping afterwards place, sucking filtration, form gel ball;
(4) use distilled water wash gel ball, gained gel ball obtains finished product after being at room temperature dried;
The mass ratio of described lecithin and pectin is 1:4～8:4.
2. the preparation method of lecithin/pectin micropill of pastille according to claim 1, it is characterized in that: described pectin is selected from hypo-methoxy pectin and hyper-methoxy pectin, high methoxyl carries out saponification processing by alkali in advance, alkali is selected from sodium hydroxide, potassium hydroxide or sodium carbonate, and the addition of alkali is 2%～20% of pectin quality.
3. the preparation method of lecithin/pectin micropill of pastille according to claim 1, it is characterized in that: the medicine of described carrier band is selected from indomethacin, ketoprofen, acemetacin, mesalazine, budesonide or diclofenac sodium, the mass ratio of itself and pectin is 1:1-1:8.
4. the preparation method of lecithin/pectin micropill of pastille according to claim 1, is characterized in that: described bivalent metal ion salt is selected from hydrochlorate or the sulfate of calcium ion, zinc ion, iron ion.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210448390.XA CN102940888B (en) | 2012-11-12 | 2012-11-12 | Targeted drug delivery method of pectin colon containing lecithin |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201210448390.XA CN102940888B (en) | 2012-11-12 | 2012-11-12 | Targeted drug delivery method of pectin colon containing lecithin |
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| Publication Number | Publication Date |
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| CN102940888A CN102940888A (en) | 2013-02-27 |
| CN102940888B true CN102940888B (en) | 2014-09-24 |
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Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104367588B (en) * | 2014-11-29 | 2017-02-22 | 山西医科大学 | Dexamethasone, pectin and zinc combined gel oral colon-specific drug delivery pellet |
| CN108851084B (en) * | 2018-06-06 | 2021-06-15 | 福建省农业科学院农业工程技术研究所 | Colon positioning micelle loaded with quercetin and preparation method thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN86108429A (en) * | 1985-12-20 | 1988-01-20 | 沃纳-兰伯特公司 | Confection or active material induction system |
| CN1284838A (en) * | 1998-01-08 | 2001-02-21 | 大塚食品株式会社 | Gelled foods and process for producing the same |
| CN1326784A (en) * | 2000-06-07 | 2001-12-19 | 张昊 | Colon-releasing oral biological preparation |
| CN1676164A (en) * | 2004-03-31 | 2005-10-05 | 张昊 | Colon positioned-release oral insulin self-micro emulsion formulation and capsule containing it |
-
2012
- 2012-11-12 CN CN201210448390.XA patent/CN102940888B/en not_active Expired - Fee Related
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN86108429A (en) * | 1985-12-20 | 1988-01-20 | 沃纳-兰伯特公司 | Confection or active material induction system |
| CN1284838A (en) * | 1998-01-08 | 2001-02-21 | 大塚食品株式会社 | Gelled foods and process for producing the same |
| CN1326784A (en) * | 2000-06-07 | 2001-12-19 | 张昊 | Colon-releasing oral biological preparation |
| CN1676164A (en) * | 2004-03-31 | 2005-10-05 | 张昊 | Colon positioned-release oral insulin self-micro emulsion formulation and capsule containing it |
Non-Patent Citations (6)
| Title |
|---|
| "Interactions between food components and drugs Part 8: Effect of pectins and bile acid preparations forming stable mixed micelles on transport of quinine in vitro";B. Fritzsch et al;《pharmazie》;20001231;第55卷(第1期);59-61 * |
| "不同离子交联果胶凝胶微丸溶胀及释药性质研究";张良珂等;《生物医学工程学杂志》;20091031;第26卷(第5期);1030-1033 * |
| "果胶基口服结肠靶向给药系统的研究进展";刘健等;《现代化工》;20110228;第31卷(第2期);25-28 * |
| B. Fritzsch et al."Interactions between food components and drugs Part 8: Effect of pectins and bile acid preparations forming stable mixed micelles on transport of quinine in vitro".《pharmazie》.2000,第55卷(第1期), |
| 刘健等."果胶基口服结肠靶向给药系统的研究进展".《现代化工》.2011,第31卷(第2期), |
| 张良珂等."不同离子交联果胶凝胶微丸溶胀及释药性质研究".《生物医学工程学杂志》.2009,第26卷(第5期), |
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