CN100560135C - The application of gellan gum in slow releasing preparation - Google Patents
The application of gellan gum in slow releasing preparation Download PDFInfo
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- CN100560135C CN100560135C CNB2007100692888A CN200710069288A CN100560135C CN 100560135 C CN100560135 C CN 100560135C CN B2007100692888 A CNB2007100692888 A CN B2007100692888A CN 200710069288 A CN200710069288 A CN 200710069288A CN 100560135 C CN100560135 C CN 100560135C
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- gellan gum
- slow releasing
- application
- adjuvant
- medicine
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Abstract
The invention discloses the application of a kind of gellan gum in delaying drug release and a kind of slow releasing preparation of medicine, comprise effective ingredient and adjuvant, comprise gellan gum in the described adjuvant, active ingredient slowly discharges to medicine by forming the gel barrier after the gellan gum aquation.The extensive use of gellan gum in food industry shows, itself is safe, and this is very important to pharmaceutic adjuvant; Simultaneously, research of the present invention shows that also the application potential of gellan gum in the oral sustained release sheet is huge.
Description
Technical field
The present invention relates to a kind of new purposes of gellan gum, especially in slow releasing preparation, delay the application of drug release.
Background technology
The long period continues to discharge medicine in vivo after the slow releasing preparation medication, thereby keep drug disposition valid density in a long time, reduce the medication number of times, alleviate the peak valley phenomenon of blood drug level, help reducing the untoward reaction of medicine, improve the compliance that the patient takes medicine greatly, by wide clinical application.Wherein oral administration is to use most convenient, and is the most extensive, also is to hold route of administration easily accepted by people most, so the research and development of oral sustained release dosage form has become an important directions of current medicine development.At present the hydrogel matrix tablet in the oral sustained release dosage form simple because of preparation process, produce easily and go, properties of product are stable and be subjected to the favor of enterprise deeply.Hydrophilic gel matrix material commonly used at present has hypromellose, sodium alginate, chitosan and polyvinyl alcohol etc.Because factors such as performances, price, using maximum is hypromellose, and available adjuvant kind is single relatively, has restricted the research and development and the application of such dosage form.
Gellan gum (Gellan Gum) is the another food microorganisms polysaccharide of the U.S. Kelco company eighties in 20th century after the exploitation xanthan gum, it is to belong to (pseu--domonaseloden) under neutrallty condition by false pseudomonas bacillus waterweed, with the glucose is carbon source, ammonium nitrate is a nitrogenous source, and in the culture medium formed of some inorganic salts, after fermentation produces the extracellular polysaccharide colloid, through the isopropyl alcohol extraction, dry, pulverize and the bright food additive of a kind of novel full impregnated that obtains.At present many enterprises such as domestic existing Zhejiang Zhongken Biotechnology Co., Ltd., the Xinhe River, Hebei biochemical industry company limited produce, mainly in food industry as thickening agent, stabilizing agent, can be used for beverage, bread, milk product, meat products, noodles, cake, cookies, instant coffee, fish product, popsicle, in the food such as ice cream, can be used as the gellant of producing impact at lower dosage of solids fruit jam and fruit jelly, also be used for soft sweet and sweet food.
Summary of the invention
The invention provides a kind of new purposes of gellan gum.
The application of a kind of gellan gum in delaying drug release, described medicine are oral drugs, can be water soluble drugs, also can be insoluble drugs.
The present invention also provides a kind of slow releasing preparation of medicine, includes effective constituent and adjuvant, comprises gellan gum in the described adjuvant, by forming the gel barrier after the gellan gum aquation, delays the release of medicine active ingredient.
The quality percentage composition of gellan gum in slow releasing preparation is 1%~30%, preferred 5%~20%.
Slow releasing preparation of the present invention is by directly being pressed into tablet with active ingredient and adjuvant mix homogeneously; Or after granulating, be pressed into tablet.
As preferably, described slow releasing preparation is the hydrogel matrix slow releasing tablet.
The slow releasing tablet that the application gellan gum is made belongs to hydrogel matrix tablet, it is a kind of water erodible matrix, tablet is met aqueous medium (as Digestive system in the human body), gellan gum is because hydration forms gel, then slowly diffuse to tablet surface behind the medicine dissolution, be discharged in the medium by the gel barrier.Simultaneously, the gel skeleton after the aquation disperses insoluble drug wherein also to disperse thereupon, be discharged in the medium also in continuous corrosion.
Wherein water soluble drug has the bulk erosion effect concurrently based on diffusion mechanism; Insoluble drug is then based on bulk erosion.Therefore water soluble drug and insoluble drug all can delay drug release with gellan gum.
The adjuvant commonly used that belongs to hydrophilic gel matrix material is a hypromellose.Through contrast test, prepare the diclofenac sodium hydrogel matrix tablet of similar release characteristics, the consumption of framework material hypromellose accounts for 35% of prescription total amount in the prescription, and gellan gum only accounts for 5% of prescription total amount.Show that gellan gum delays the with better function of drug release in matrix tablet, in other words, the consumption that reaches identical slow release effect gellan gum still less.
The extensive use of gellan gum in food industry shows, itself is safe, and this is very important to pharmaceutic adjuvant; Simultaneously, research of the present invention shows that also the application potential of gellan gum in the oral sustained release sheet is huge.
Description of drawings
Fig. 1 is that the Dicolfanac Sodium Sustained Release Tablets drug accumulation of different gellan gum consumptions discharges percentage rate and time relation figure;
Fig. 2 discharges percentage rate and time relation figure for the trimebutine maleate sustained-release tablet drug accumulation;
Fig. 3 is that tartaric acid toterodine slow released drug accumulation discharges percentage rate and time relation figure.
The specific embodiment
The preparation of embodiment 1 Dicolfanac Sodium Sustained Release Tablets
Prescription 1: diclofenac sodium 75g, dextrin 105g and gellan gum 20g
Prescription 2: diclofenac sodium 75g, dextrin 110g and gellan gum 15g
Prescription 3: diclofenac sodium 75g, dextrin 115g and gellan gum 10g
With the dextrin is filler, and the fixing sheet of respectively writing out a prescription is heavy, regulates the gellan gum consumption and drafts above-mentioned prescription 1~3 (per 1000 amounts).Make binding agent with 75% ethanol 30ml, 0.3% magnesium stearate is made lubricant, and conventional wet granule compression tablet prepared promptly.
Slow releasing tablet to 3 prescriptions is carried out drug release determination by pharmacopeia, the result shows that the gellan gum consumption has tangible influence to drug release: along with the increase of gellan gum consumption, drug releasing rate reduces, also can regulate the release of slow releasing tablet, to adhere to specification by gellan gum consumption in the adjustment tablet.Referring to Fig. 1, vertical coordinate among Fig. 1 " Ft/% " represents that the drug accumulation of each time point slow releasing tablet discharges percentage rate by 1~3 Dicolfanac Sodium Sustained Release Tablets release profiles for preparing of writing out a prescription, and abscissa " t/h " is represented release time, and unit is hour (h).
The preparation of embodiment 2 trimebutine maleate sustained-release tablets
Prescription:
Trimebutine Maleate 300.0g
Gellan gum 50.0g
8% polyvinylpyrrolidonesolution solution 40.0ml
Fatty acid magnesium 1.0g
Make 1000
With conventional wet granule compression tablet prepared promptly, release profiles is referring to Fig. 2.
The preparation that embodiment is 3 tartaric acid toterodine slow released
Prescription:
Tolterodine tartrate 4.0g
Dextrin 135.0g
Gellan gum 9.0g
75% ethanol 22.0ml
Magnesium stearate 0.5g
Make 1000
With conventional wet granule compression tablet prepared promptly, release profiles is referring to Fig. 3.
Claims (2)
1, a kind of hydrogel matrix slow releasing tablet of Trimebutine Maleate, its raw material is formed as follows in 1000 amounts:
The polyvinylpyrrolidonesolution solution of Trimebutine Maleate 300g, gellan gum 50g, 40ml 8% and 1g magnesium stearate;
Wherein, described gellan gum is a hydrophilic gel matrix material.
2, a kind of hydrogel matrix slow releasing tablet of Tolterodine tartrate, its raw material is formed as follows in 1000 amounts:
The ethanol of Tolterodine tartrate 4g, dextrin 135g, gellan gum 9g, 22ml 75% and 0.5g magnesium stearate;
Wherein, described gellan gum is a hydrophilic gel matrix material.
Priority Applications (1)
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CNB2007100692888A CN100560135C (en) | 2007-06-18 | 2007-06-18 | The application of gellan gum in slow releasing preparation |
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CNB2007100692888A CN100560135C (en) | 2007-06-18 | 2007-06-18 | The application of gellan gum in slow releasing preparation |
Publications (2)
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CN101085361A CN101085361A (en) | 2007-12-12 |
CN100560135C true CN100560135C (en) | 2009-11-18 |
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Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
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CN107260693A (en) * | 2016-10-12 | 2017-10-20 | 钟术光 | Delay the composition of insoluble drug release |
CN107929747A (en) * | 2016-10-12 | 2018-04-20 | 钟术光 | The composition of hydrophilic polymer |
CN107198680A (en) * | 2016-10-12 | 2017-09-26 | 钟术光 | Sustained release preparation |
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2007
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Granted publication date: 20091118 Termination date: 20120618 |