CN102940888A - 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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- CN102940888A CN102940888A CN201210448390XA CN201210448390A CN102940888A CN 102940888 A CN102940888 A CN 102940888A CN 201210448390X A CN201210448390X A CN 201210448390XA CN 201210448390 A CN201210448390 A CN 201210448390A CN 102940888 A CN102940888 A CN 102940888A
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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 the oral colon-target administration; More precisely, relate to a kind of medication take pectin as framework material for medicine controlled releasing or oral colon-target administration.
Background technology
Colon targeting drug administration mainly is by drug delivery system, make drug oral after, do not discharge in upper gi tract, drug conveying beginning disintegrate or erosion to the human body ileocecus are separated and are discharged, in colon performance part or whole body therapeutic effect.The oral colon-target drug-delivery preparation is usually used in treating colonic diseases, such as colitis, colon cancer etc., medicine is directly discharged 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 the location more accurately and reliably, and is not subjected to the impact of individual variation.But the hydrophilic of pectin makes easily swelling and discharge in advance medicine in the environment in vivo of pectin base drug-supplying system.
In the past few years, when design colon targeting drug administration system, taked 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; The 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 the 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 publication 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 that contains lecithin, this method is take pectin as framework material, take metal ion as cross-linking agent, by compound adding lecithin fraction, arrive antecolic release with the control medicine, improving the segmented intestine targeted property of gel microsphere.
The objective of the invention is to be achieved through the following technical solutions:
A kind of pectin colon targeting drug administration method that contains lecithin, step is:
⑴ add the distilled water stirring and dissolving with pectin, forms colloidal solution, adds aqueous slkali and carry out saponification, stirs and be made into pectin solution;
⑵ add lecithin in pectin solution, mix homogeneously adds the medicine that needs carrier band again, and ultra-sonic dispersion forms uniform suspension;
⑶ slowly splash into mass concentration with above-mentioned suspension is in 1% ~ 6% bivalent metal ion saline solution, carries out gel solidification reaction, places afterwards after dripping, sucking filtration, forms gel ball;
⑷ distilled water wash gel ball, the gained gel ball at room temperature obtains finished product after the drying.
And described pectin comprises hypo-methoxy pectin and hyper-methoxy pectin, and high methoxyl carries out saponification by alkali in advance to be processed, 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, and 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 the swellability that lecithin can reduce the pectin gel micropill effectively, 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 behind compound lecithin, lecithin/pectin gel micropill cumulative release rate in the small intestinal simulated solution is starkly lower than simple pectin gel micropill, 8h cumulative release rate is reduced to below 5% in the small intestinal simulated solution, and lecithin/pectin gel micropill is also better than simple pectin gel micropill at high temperature and illumination stability inferior.
The specific embodiment
Below the present invention is described further by the specific embodiment, but should not be construed as limitation of the invention.Those of ordinary skills can also make modification, replacement, the change of various ways according to technique scheme.All modification, replacement, changes of doing based on above-mentioned technological thought 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 can be ketoprofen, acemetacin, mesalazine, budesonide, diclofenac sodium only take indomethacin as example in addition.
Embodiment 1:
The preparation method of a kind of lecithin that contains indomethacin/calcium pectinate micropill: step is:
⑴ pectin 0.4g adds the 8ml distilled water, forms colloidal solution, adds the NaOH solution saponification of 2ml 3%, stirs and is made into pectin solution;
⑵ add 0.3g lecithin, stirs to make itself and pectin solution mix homogeneously, in indomethacin crude drug 0.1g adding pectin solution, ultrasonic it is uniformly dispersed;
⑶ slowly splash into this suspension in 6% calcium chloride solution, carries out the gelling curing reaction, and placement after dripping is finished, sucking filtration form gel ball;
⑷ above-mentioned gel ball distilled water wash 2 ~ 3 times, drying obtains finished product.
Embodiment 2:
The preparation method of a kind of lecithin that contains indomethacin/calcium pectinate micropill: step is:
⑴ pectin 0.4g adds the 8ml distilled water, forms colloidal solution, adds the NaOH solution saponification of 2ml 2%, stirs and is made into pectin solution;
⑵ add 0.3g lecithin, stirs to make itself and pectin solution mix homogeneously, in indomethacin crude drug 0.15g adding pectin solution, ultrasonic it is uniformly dispersed;
⑶ slowly splash into this suspension in 6% calcium chloride solution, carries out the gelling curing reaction, and placement after dripping is finished, sucking filtration form gel ball;
⑷ above-mentioned gel ball distilled water wash 2 ~ 3 times, drying obtains finished product.
Embodiment 3:
The preparation method of a kind of lecithin that contains indomethacin/pectin zinc micropill, step is:
⑴ pectin 0.4g adds the 8ml distilled water, forms colloidal solution, adds the NaOH solution saponification of 2ml 2%, stirs and is made into pectin solution;
⑵ add 0.3g lecithin, treats itself and pectin solution mix homogeneously, in indomethacin crude drug 0.1g adding pectin solution, ultrasonic it is uniformly dispersed;
⑶ slowly splash into suspension in 5% liquor zinci chloridi, carries out the gelling curing reaction, and placement after dripping is finished, sucking filtration form gel ball;
⑷ above-mentioned gel ball distilled water wash 2 ~ 3 times, drying obtains finished product.
Embodiment 4:
The preparation method of a kind of lecithin that contains indomethacin/pectin zinc micropill, step is:
⑴ pectin 0.4g adds the 8ml distilled water, forms colloidal solution, adds the NaOH solution saponification of 2ml2%, stirs and is made into pectin solution.
⑵ add 0.5g lecithin, treats itself and pectin solution mix homogeneously, in indomethacin crude drug 0.1g adding pectin solution, ultrasonic it is uniformly dispersed;
⑶ slowly splash into suspension in 6% liquor zinci chloridi, carries out the gelling curing reaction, and placement after dripping is finished, sucking filtration form gel ball;
⑷ above-mentioned gel ball distilled water wash 2 ~ 3 times, drying obtains finished product.
Claims (5)
1. pectin colon targeting drug administration method that contains lecithin, it is characterized in that: step is:
⑴ add the distilled water stirring and dissolving with pectin, forms colloidal solution, adds aqueous slkali and carry out saponification, stirs and be made into pectin solution;
⑵ add lecithin in pectin solution, mix homogeneously adds the medicine that needs carrier band again, and ultra-sonic dispersion forms uniform suspension;
⑶ slowly splash into mass concentration with above-mentioned suspension is in 1% ~ 6% bivalent metal ion saline solution, carries out gel solidification reaction, places afterwards after dripping, sucking filtration, forms gel ball;
⑷ distilled water wash gel ball, the gained gel ball at room temperature obtains finished product after the drying.
2. the pectin colon targeting drug administration method that contains lecithin according to claim 1, it is characterized in that: described pectin comprises hypo-methoxy pectin and hyper-methoxy pectin, high methoxyl carries out saponification by alkali in advance to be processed, alkali comprises sodium hydroxide, potassium hydroxide, sodium carbonate etc., and the addition of alkali is 2% ~ 20% of pectin quality.
3. the pectin colon targeting drug administration method that contains lecithin that relates to according to claim 1, it is characterized in that: the mass ratio of described lecithin and pectin is 1:4 ~ 8:4.
4. the pectin colon targeting drug administration method that contains lecithin according to claim 1, it is characterized in that: the medicine of described carrier band comprises indomethacin, ketoprofen, acemetacin, mesalazine, budesonide, diclofenac sodium, and the mass ratio of itself and pectin is 1:1-1:8.
5. the pectin colon targeting drug administration method that contains lecithin according to claim 1, it is characterized in that: described bivalent metal ion salt comprises 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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| CN201210448390.XA CN102940888B (en) | 2012-11-12 | 2012-11-12 | Targeted drug delivery method of pectin colon containing lecithin |
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| CN102940888A true CN102940888A (en) | 2013-02-27 |
| CN102940888B CN102940888B (en) | 2014-09-24 |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104367588A (en) * | 2014-11-29 | 2015-02-25 | 山西医科大学 | Dexamethasone, pectin and zinc combined gel oral colon-specific drug delivery pellet |
| CN108851084A (en) * | 2018-06-06 | 2018-11-23 | 福建省农业科学院农业工程技术研究所 | A kind of site specific DDS for colon micella of load Quercetin and preparation method thereof |
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| 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 |
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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 |
|---|
| 《pharmazie》 20001231 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" 第55卷, 第1期 * |
| 《现代化工》 20110228 刘健等 "果胶基口服结肠靶向给药系统的研究进展" 第31卷, 第2期 * |
| 《生物医学工程学杂志》 20091031 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" 第26卷, 第5期 * |
| 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》, vol. 55, no. 1, 31 December 2000 (2000-12-31) * |
| 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》, vol. 31, no. 2, 28 February 2011 (2011-02-28) * |
| 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》, vol. 26, no. 5, 31 October 2009 (2009-10-31) * |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104367588A (en) * | 2014-11-29 | 2015-02-25 | 山西医科大学 | Dexamethasone, pectin and zinc combined gel oral colon-specific drug delivery pellet |
| 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 |
| CN108851084A (en) * | 2018-06-06 | 2018-11-23 | 福建省农业科学院农业工程技术研究所 | A kind of site specific DDS for colon micella of load Quercetin and preparation method thereof |
| 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 |
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| CN102940888B (en) | 2014-09-24 |
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