CN101249081A - Administer orally controlled release drug administration pharmaceutical tablet - Google Patents
Administer orally controlled release drug administration pharmaceutical tablet Download PDFInfo
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- CN101249081A CN101249081A CNA2008100206136A CN200810020613A CN101249081A CN 101249081 A CN101249081 A CN 101249081A CN A2008100206136 A CNA2008100206136 A CN A2008100206136A CN 200810020613 A CN200810020613 A CN 200810020613A CN 101249081 A CN101249081 A CN 101249081A
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- hydroxypropyl emthylcellulose
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Abstract
The invention relates to an oral tablet for controlled-release drug delivery, which contains 5-40% of an active component by weight and 60-95% of a carrier by weight, wherein the carrier is composed of a disintegrating agent and hydroxypropyl methylcellulose, and the active component is one selected from resveratrol, beta-1-3.6-glucan, flavonoids, tea polyphenols, vitamins, minerals, norfloxacin and diltiazem. The invention solves the problems that the hydrolysis rate of fatty acid esters the prior corrosive skeleton sustained-release tablet are influenced by pH value and digestive enzymes; and the hydrolysis rate of hydrophilic gel skeleton sustained-release tablet are influenced by physiologic factors, pH value and peristalsis speed of the gastrointestinal tract. Additionally, the oral tablet has long retention time in stomach, strong bioactivity, wide application range, no influences from physiologic factors, pH value and peristalsis speed of the gastrointestinal tract, and good absorption in upper segment of the small intestine (maximal absorption in B2 site).
Description
Technical field
The present invention relates to a kind of controlled-release pharmaceutical tablet, particularly a kind of is carrier and the bonded controlled-release pharmaceutical tablet of active ingredient with microcrystalline Cellulose and hydroxypropyl emthylcellulose.
Background technology
Before this method invention, more about the research of controlled-release pharmaceutical tablet aspect, also applied in medicine and the nourishing healthy product simultaneously.At present, following several controlled release method is arranged.
Insoluble matrix sustained release tablet: common used material has ethyl cellulose, polyethylene kind, crylic acid resin, ethylene-vinyl acetate copolymer etc.Because the speed that insoluble drug disengages in the skeleton is too slow, thereby water soluble drug is fit to this kind matrix sustained release tablet
Erodible matrix sustained release tablet: this kind tablet is that framework material and medicine are made tablet with inert fat and wax class substrate, and the release of medicine is the corrosion gradually of borrowing fat or waxiness, pH value, and digestive enzyme has certain influence to the hydrolysis rate of fatty acid ester.
This kind of hydrogel matrix slow releasing tablet slow releasing tablet is framework material with the hydrophilic high molecular polymer, and with medicine, framework material and an amount of adjuvant mix homogeneously are granulated, and are pressed into tablet and get final product.Expand in pipe intestinal digesting liquid and form gel in the oral back of made slow releasing tablet, drug release time is prolonged, and this type drug release is subjected to the gastrointestinal physiologic factor, and pH value and peristaltic velocity influence are bigger.
Summary of the invention
Purpose of the present invention just is to overcome above-mentioned defective, works out a kind of tablet of new controlled release drug administration.
Technical scheme of the present invention is:
Administer orally controlled release drug administration pharmaceutical tablet, its major technique is characterised in that by active ingredient, carrier to be formed, it is 5%～40% that active ingredient accounts for percentage by weight, it is 60～95% that carrier accounts for percentage by weight, wherein carrier is made up of disintegrating agent and hydroxypropyl emthylcellulose, and active ingredient is any in resveratrol, β-1-3.6-glucosan, flavonoid, tea polyphenols, vitamin, mineral, norfloxacin, the diltiazem.
Advantage of the present invention and effect have been to provide a kind of method of new controlled-release pharmaceutical tablet, and raw material and equipment are conventional products, easily buying, and technology is simple, is suitable for mass industrialized production.
The present invention makes tablet be stranded in the stomach prolong drug release time, improves drug absorption, is beneficial to the raising bioavailability.Its tablet system belongs to a kind of preparation of fluid dynamic equilibrium by medicine and hydrophilic colloid and the prepared oral tablet of other auxiliary material.
Particularly, adopt microcrystalline Cellulose (or other disintegrating agents) and hydroxypropyl emthylcellulose (HPMC) to constitute carrier, mate with active ingredient; Microcrystalline Cellulose can quicken medicine dissolution velocity in vivo, and hydroxypropyl emthylcellulose can delay medicine dissolution velocity in vivo, by the synergism of the two, just can control medicine rate of release in vivo, make active ingredient in human body, obtain the most effective performance.
Advantage of the present invention and effect also are to provide a kind of method of new controlled-release pharmaceutical tablet, and raw material and equipment are conventional products, easily buying, and technology is simple, is suitable for mass industrialized production.
Be in particular in:
1. under body temperature, form the gel barrier film and expand the original figure of tablet of maintenance behind the tablet contact gastric juice at surface hydration:
2. the composition of tablet is beneficial at Entogastric lingering;
3. the selection of carrier and consumption can both meet the inside and outside drug release feature that tablet requires, and can slowly dissolve diffusion, keep the long period at gastric, generally can reach 20～24 hours;
4. pharmaceutically active is strong, and dosage range is big, can less than 40%;
5. applied widely, be not subjected to the gastrointestinal physiologic factor, the influence of pH value and peristaltic velocity.(as medicine stable under the acid condition and be easy to the medicine that dissolving absorbs under acid condition, as norfloxacin, diltiazem etc.; Gastric acid secretion inhibitor is as ranitidine etc.; The stomach medicine is brought into play the effect of treatment gastroenteritis by the helicobacter pylori that suppresses gastric mucosa as some drugs);
6. continue to absorb at gastrointestinal tract, as at upper part of small intestine, absorb best B2 etc. and locate to absorb.
Other advantages of the present invention and effect will continue to describe below.
Description of drawings
The analytical data figure of Fig. 1--tablet of the present invention under the condition of simulated gastric fluid.
Releasing curve diagram at the uniform velocity in 24 hours inherent simulated gastric fluids of Fig. 2--active ingredient resveratrol.
The specific embodiment
Embodiment 1:
Get the active ingredient resveratrol, accounting for percentage by weight is 30%; Microcrystalline Cellulose is 25% in the carrier, and hydroxypropyl emthylcellulose (HPMC) is 45%, and sum of the two is 70%; Add water high speed shear mixer mix homogeneously; Can be made into tablet.
Embodiment 2:
Get active ingredient β-1-3.6-glucosan 20%; Microcrystalline Cellulose is 30% in the carrier, and hydroxypropyl emthylcellulose (HPMC) is 50%, and sum of the two is 80%; Add water high speed shear mixer mix homogeneously; Can be made into tablet.
Embodiment 3:
Getting any in active ingredient flavonoid, tea polyphenols, vitamin, mineral, norfloxacin, the diltiazem is 10%; Microcrystalline Cellulose is 30% in the carrier, and hydroxypropyl emthylcellulose (HPMC) is 60%, adds water high speed shear mixer mix homogeneously; Can be made into tablet.
Embodiment 4:
Getting any in active ingredient norfloxacin, the diltiazem is 5%; Microcrystalline Cellulose replaces with other disintegrating agents in the carrier, any as in Powderd cellulose, dried starch, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, cross linked polyvinyl pyrrolidone, the cross-linking sodium carboxymethyl cellulose, be 45%, hydroxypropyl emthylcellulose (HPMC) is 50%, adds water high speed shear mixer mix homogeneously; Can be made into tablet.
According to experimental results show that, in different active component by after adding above-mentioned composition and making up in flakes, discovery can effectively be controlled active component at the intravital rate of release of people, and after finding that active component is through this combination tabletting, alleviate the toxic action that active component concentrates release to bring, and, reduced the dose of medicine by continual slow release, increased the effect of medicine.
Detect effect:
1. our employed microcrystalline Cellulose and hydroxypropyl emthylcellulose are the adjuvants that uses in medicine and health product and food through for many years, we can say that it is a safety non-toxic.
2. microcrystalline Cellulose (or other disintegrating agents) can quicken medicine dissolution velocity in vivo, and hydroxypropyl emthylcellulose (HPMC) can delay medicine dissolution velocity in vivo, by both suitable collocation and generation synergism, just can effectively control medicine rate of release in vivo.
3. if there is not controlled-release technology, medicine can be concentrated rapid release in vivo, discharges if there is the medicine of side effect once to concentrate, and will produce very strong toxic and side effects to human body.And through behind the controlled-release technology, drug slow discharges, and the medication amount that at every turn discharges is lower, just can not produce toxic and side effects.Medicine all has only certain action time, after finishing action time, just must take medicine once more, and the controlled-release technology continual release medicine of energy just, does not need to take once more just to reach same effect, so can reduce dose.The medicine of same dosage, after concentrated the release, because the cause that absorbs, unnecessary amount will be discharged; And controlled-release technology, same dosage can reach the purpose of whole absorptions by slowly discharging, thereby strengthens the effect of medicine.
4. the present invention is according to the difference of active component, carry out different combinations after, can play cooperative effect, rather than simple stack, through relevant experimental study, the present invention can bring into play the speed of obvious control drug release, and safe without toxic side effect.
Experimental results show that as shown in Figure 1: is example with resveratrol as functional component:
Prescription: resveratrol 13.6%, microcrystalline Cellulose 26.4%, hydroxypropyl emthylcellulose (HPMC) 60% adds the tablet that water is made with high speed shear mixer mix homogeneously.
As shown in Figure 2, resveratrol at the uniform velocity discharged in simulated gastric fluid in 24 hours, and release profiles and release reach in the Chinese Pharmacopoeia requirement to slow release tablet.
The present invention is raw materials used can both to buy from the market, the viscosity of used hydroxypropyl emthylcellulose (HPMC) is higher than or equals 4000cps, have only the HPMC of high viscosity (4000cps, 15000cps etc.) just to can be used as the skeleton of slow-release material, be used for the release of blocking medicine.
The claimed description that has scope to be not limited only to the foregoing description of the present invention.
Claims (4)
1. administer orally controlled release drug administration pharmaceutical tablet, it is characterized in that forming by active ingredient, carrier, it is 5%～40% that active ingredient accounts for percentage by weight, it is 60～95% that carrier accounts for percentage by weight, wherein carrier is made up of disintegrating agent and hydroxypropyl emthylcellulose, and active ingredient is any in resveratrol, β-1-3.6-glucosan, flavonoid, tea polyphenols, vitamin, mineral, norfloxacin, the diltiazem.
2. the tablet of oral controlled-release administration according to claim 1 is characterized in that it is 20% to 50% that disintegrating agent accounts for vehicle weight percentage ratio, and it is 50% to 80% that hydroxypropyl emthylcellulose accounts for vehicle weight percentage ratio.
3. the tablet of oral controlled-release administration according to claim 1 and 2 is characterized in that disintegrating agent is any in microcrystalline Cellulose, Powderd cellulose, dried starch, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, cross linked polyvinyl pyrrolidone, the cross-linking sodium carboxymethyl cellulose.
4. the tablet of oral controlled-release administration according to claim 1 and 2 is characterized in that hydroxypropyl emthylcellulose is the hydroxypropyl emthylcellulose of 4000cps viscosity.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008100206136A CN101249081A (en) | 2008-02-15 | 2008-02-15 | Administer orally controlled release drug administration pharmaceutical tablet |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008100206136A CN101249081A (en) | 2008-02-15 | 2008-02-15 | Administer orally controlled release drug administration pharmaceutical tablet |
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| CN101249081A true CN101249081A (en) | 2008-08-27 |
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| CNA2008100206136A Pending CN101249081A (en) | 2008-02-15 | 2008-02-15 | Administer orally controlled release drug administration pharmaceutical tablet |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101618021B (en) * | 2009-08-12 | 2011-04-06 | 河北科技大学 | Chitosan coating medicine slow release microsphere and preparation method thereof |
| CN101433329B (en) * | 2008-12-22 | 2012-06-27 | 南京大渊美容保健有限公司 | Nutritive composition with health-care function |
| CN103478732A (en) * | 2013-09-30 | 2014-01-01 | 杭州拜善晟生物科技有限公司 | Matrix sustained-release vitamin functional food and preparation method thereof |
| EP2818160B1 (en) | 2010-10-01 | 2017-11-08 | Aptalis Pharma Limited | Enteric coated, low-strength pancrelipase formulations |
| CN108968051A (en) * | 2018-08-06 | 2018-12-11 | 大连医诺生物股份有限公司 | Resveratrol sustained release preparation and preparation method thereof |
| US10993996B2 (en) | 2013-08-09 | 2021-05-04 | Allergan Pharmaceuticals International Limited | Digestive enzyme composition suitable for enteral administration |
-
2008
- 2008-02-15 CN CNA2008100206136A patent/CN101249081A/en active Pending
Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101433329B (en) * | 2008-12-22 | 2012-06-27 | 南京大渊美容保健有限公司 | Nutritive composition with health-care function |
| CN101618021B (en) * | 2009-08-12 | 2011-04-06 | 河北科技大学 | Chitosan coating medicine slow release microsphere and preparation method thereof |
| EP2818160B1 (en) | 2010-10-01 | 2017-11-08 | Aptalis Pharma Limited | Enteric coated, low-strength pancrelipase formulations |
| US11364205B2 (en) | 2010-10-01 | 2022-06-21 | Societe Des Produits Nestle S.A. | Stable low digestive enzyme content formulation |
| US10993996B2 (en) | 2013-08-09 | 2021-05-04 | Allergan Pharmaceuticals International Limited | Digestive enzyme composition suitable for enteral administration |
| CN103478732A (en) * | 2013-09-30 | 2014-01-01 | 杭州拜善晟生物科技有限公司 | Matrix sustained-release vitamin functional food and preparation method thereof |
| CN103478732B (en) * | 2013-09-30 | 2015-08-19 | 杭州拜善晟生物科技有限公司 | A kind of matrix sustained-release vitamin functional food and preparation method thereof |
| CN108968051A (en) * | 2018-08-06 | 2018-12-11 | 大连医诺生物股份有限公司 | Resveratrol sustained release preparation and preparation method thereof |
| CN108968051B (en) * | 2018-08-06 | 2022-07-12 | 大连医诺生物股份有限公司 | Resveratrol sustained-release preparation and preparation method thereof |
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Open date: 20080827 |