CN103432082A - Glucosamine composition and preparation method thereof - Google Patents
Glucosamine composition and preparation method thereof Download PDFInfo
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- CN103432082A CN103432082A CN2013103824761A CN201310382476A CN103432082A CN 103432082 A CN103432082 A CN 103432082A CN 2013103824761 A CN2013103824761 A CN 2013103824761A CN 201310382476 A CN201310382476 A CN 201310382476A CN 103432082 A CN103432082 A CN 103432082A
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- glucosamine
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Abstract
The invention relates to a pharmaceutical composition of glucosamine, and specifically relates to a pellet preparation suitable for oral administration and prepared from glucosamine or a pharmaceutically acceptable salt of the glucosamine, and a preparation method thereof. The glucosamine pellets contain the glucosamine or the pharmaceutically acceptable salt of the glucosamine, a diluent, a disintegrating agent, a binder and other pharmaceutic adjuvants; the grain size of the pellets is generally in the range from 0.1 to 10 mm, preferably from 0.1 to 5 mm and more preferably from 0.1 to 2 mm. The glucosamine pellets provided by the invention can be directly filled into capsules or pressed into tablets; as the pellet process is adopted, the wet granulation process of a common preparation is simplified, the probability of the glucosamine being wet is reduced and the stability of the product is improved; the glucosamine pellets are convenient to take, especially for gastric ulcer sufferers.
Description
Technical field
The present invention relates to medical technical field, exactly the present invention relates to a kind of pellet preparations that oral glucosamine or its pharmaceutically acceptable salt make and preparation method thereof that is applicable to.
Background technology
Glucosamine is a kind of natural amino monosaccharide, can stimulate chondrocyte to produce the proteoglycan with normal polymer structure, improve the repair ability of chondrocyte, suppress the release of the hydrolytic enzyme such as lysosomal enzyme, collagenase and phospholipase A2, minimizing destroys the hydrolysis of articular cartilage substrate, and can prevent the generation of the super oxyradical of damaging cells, promote the repair and reconstruction of cartilage matrix, thereby can delay the pathological process of osteoarthritis and the process of disease.Glucosamine is for prevention and the existing very long history for the treatment of osteoarthritis, in the U.S., be most popular articular cartilage nutrient drug at present, with health food supply market, in Europe, because thering is specific clinical efficacy, as ethical goods, manage and provide the patient required.
At present domestic commercially available glucosamine product forms is mainly tablet, and capsule all should be when meal or one after each meal, to reduce gastrointestinal upset, the patient of gastric ulcer is particularly arranged.The preparation technology of commercially available Glucosamine hydrochloride tablet (capsule) and glucosamine sulfate capsule (sheet) is wet granulation, and its preparation technology is respectively pulverizing-mixing-soft material processed-granulation-drying-granulate-total mix-tabletting-coating; Pulverizing-mixing-soft material processed-granulation-drying-granulate-total mix-fill.Both preparation sections are more loaded down with trivial details, and equipment needed thereby is many, need to strictly control each link well, just can guarantee that preparation has good repeatability and product quality.The stability of commercially available sample has problems equally, glucosamine has and certain draws moistly, and after product is placed the several months, the glucosamine formulations character easily changes, as principal agent composition (glucosamine) color is yellow, rather than white or off-white color; Simultaneously, the mobility of glucosamine is poor, and when making preparation, operation easier is large, when filling capsule or tabletting, easily causes the problems such as content uniformity or content is inhomogeneous, thereby affects the quality of product, has certain hidden danger of quality.
Micropill is that a kind of multiple-unit dosage disperses dosage form, and dose is composed of multiple units, and with single-dose type, compares, and has many advantages: (1) can improve medicine and gastrointestinal tract contact area, makes drug absorption complete, thereby improves bioavailability; (2) by the micropill combination of several different rate of releasing drug, can obtain desirable rate of releasing drug, avoid peak valley phenomenon, and can maintain longer action time, reduce untoward reaction; (3) medicine is dispersed in each piller, and gastrointestinal tract mucous stimulation is lowered even and disappears; (4) its release rule has repeatability; (5) can be distributed in whole gastrointestinal tract, medicine seldom is subject to the impact that gastric emptying changes in vivo, as pylorus is closed,, there is not the zest problem in the performance difference that can overcome gastrointestinal tract difference transfer time and irregular gastric emptying difference is produced; (6) make some character that micropill can change medicine, as good fluidity after the one-tenth ball, size evenly, non-friable etc., is easy to process (as coating, divided dose), and can be used as the basis for preparing tablet, capsule etc.; (7) improve medicine stability, cover disagreeable taste.
If glucosamine can be made to micropill, can take full advantage of the plurality of advantages of micropill, after the one-tenth ball, mobility is better, and size evenly, is easy to tabletting or loads capsule; Also simplify technique, reduce glucosamine and draw wet probability; Also can avoid the impact of clinical application food simultaneously, facilitate the patient to take, improve patient's compliance.After making micropill, medicine reduces even and disappears gastrointestinal tract mucous stimulation, is particularly useful for patients w ith peptic ulcer disease.
Summary of the invention
An object of the present invention is to provide the novel form that a kind of glucosamine or its pharmaceutically acceptable salt are made, i.e. the glucosamine micropill.Described glucosamine micropill, compare with commercial preparation, simplified technique, reduce the quality of the pharmaceutical preparations problem that in the preparation process, wet granulation causes, before the micropill molding, added one deck isolation coat layer, carry out again compress tablet coating or fill capsule, effectively guaranteed the glucosamine formulations quality.The product of making more convenient patient take, especially patients w ith peptic ulcer disease.
Another object of the present invention is to provide a kind of method for preparing the glucosamine pellet preparations.
The objective of the invention is to realize by the following technical solutions:
A kind of glucosamine micropill, by this micropill weighing scale, it comprises:
Glucosamine 50-90%
Diluent 1-15%
Disintegrating agent 1-10%
Binding agent 1-10%
Other adjuvants 1-5%
Described glucosamine micropill diameter is 0.1-10mm.
Preferably, glucosamine micropill of the present invention, by this micropill weighing scale, it comprises:
Glucosamine 65-85%
Diluent 5-15%
Disintegrating agent 2-8%
Binding agent 2-8%
Other adjuvants 1-5%
Described glucosamine micropill diameter is 0.1-5mm, more preferably 0.1-2mm.
Glucosamine micropill of the present invention, glucosamine is selected from glucosamine hydrochloride, glucosamine sulfate or other pharmaceutically acceptable salts, through pulverization process, preferred micronized glucosamine, the content of glucosamine in glucosamine micropill of the present invention, weighing scale by this micropill is generally 50-90%, is preferably 65-85%, more preferably 75-85%.
The diluent adopted in glucosamine micropill of the present invention can be any conventional diluent well known in the art, comprise and be selected from a kind of in microcrystalline Cellulose, lactose, mannitol, starch, glucide, its content in glucosamine micropill of the present invention, weighing scale by this micropill is generally 1-15%, be preferably 5-15%, more preferably 5-12%.
The disintegrating agent adopted in glucosamine micropill of the present invention comprises and is selected from a kind of in carboxymethyl starch sodium, crospolyvinylpyrrolidone, low-substituted hydroxypropyl cellulose (L-HPC), cross-linking sodium carboxymethyl cellulose, it is at the content of glucosamine micropill of the present invention, weighing scale by this micropill is generally 1-10%, be preferably 2-8%, more preferably 2-5%.
The binding agent adopted in glucosamine micropill of the present invention comprises and is selected from ethanol, starch, pregelatinized Starch, hypromellose sodium (HPMC), a kind of in zein, Lac, it is at the content of glucosamine micropill of the present invention, weighing scale by this micropill is generally 1-10%, be preferably 2-8%, more preferably 2-5%.
Glucosamine pellet preparations of the present invention is compared with commercially available glucosamine ordinary preparation, has the following advantages: (1) medicine is dispersed in each piller, and gastrointestinal tract mucous stimulation is lowered even and disappears; (2) can be distributed in whole gastrointestinal tract, medicine seldom is subject to the impact that gastric emptying changes in vivo, facilitates the patient to take at any time, especially patients w ith peptic ulcer disease; (3) make some character that micropill can change medicine, as good fluidity after the one-tenth ball, size evenly, non-friable etc., is easy to coating, and can be used as the basis for preparing tablet, capsule etc.; (4) simplified technological process, reduce the quality of the pharmaceutical preparations problem that in the preparation process, wet granulation causes, before the micropill molding, added one deck isolation coat layer, carry out again after compress tablet coating or fill capsule tabletting again coating or load capsule, improving medicine stability.
The invention provides a kind of method for preparing the glucosamine pellet preparations, described method comprises the steps:
(1) glucosamine, diluent and/or disintegrating agent are crossed respectively to 80 mesh sieves, fully mix homogeneously; Add suitable amount of adhesive to make soft material; Then spheronization is extruded in employing, fluid bed pill legal system obtains micropill; By after the dry screening of the micropill made, obtain the glucosamine micropill.
(2) the glucosamine micropill made is become to capsule or tabletting with the filling machine fill after coating make tablet.
Wherein, described glucosamine is selected from glucosamine hydrochloride, glucosamine sulfate or other pharmaceutically acceptable salts;
Wherein, described diluent is selected from a kind of in microcrystalline Cellulose, lactose, mannitol, starch, glucide;
Wherein, described disintegrating agent is selected from a kind of in carboxymethyl starch sodium, crospolyvinylpyrrolidone, low-substituted hydroxypropyl cellulose (L-HPC), cross-linking sodium carboxymethyl cellulose;
Wherein, described binding agent is selected from ethanol, starch, pregelatinized Starch, hypromellose sodium (HPMC), a kind of in zein, Lac.
Form is described in further detail content of the present invention more by the following examples, but should not be interpreted as in the above-mentioned subject area of the present invention at this point and only limit to following examples.Do not breaking away under the above-mentioned technology prerequisite of the present invention, the corresponding replacement of making according to ordinary skill knowledge and customary means or the modification of change, include within the scope of the invention
.
[embodiment 1]
(1) prescription 1(1000 sheet)
The micropill prescription
Amino glucosamine 240g (by giving money as a gift)
Microcrystalline Cellulose 40g
Carboxymethyl starch sodium 15g
5% hypromellose sodium (5cps) ethanol-water solution 240ml
Pulvis Talci 30g
Coating fluid prescription
Stomach dissolved film coating pre-mix dose 6g
50% ethanol-water solution 240ml
(2) preparation method
The glucosamine hydrochloride of above-mentioned recipe quantity, microcrystalline Cellulose and carboxymethylstach sodium are crossed respectively to 80 mesh sieves, fully mix homogeneously; Add the alcohol-water liquid of 5% hypromellose sodium appropriate the material mixed, make soft material; Then add extruder, be squeezed into bar; Bar is placed in spheronizator round as a ball, adds 5% hypromellose sodium simultaneously and reach in right amount Pulvis Talci 30g, the round as a ball time is 5min, and 55-60 ℃ of dry 8h sieves and collect the micropill of 18-32 order particle diameter, obtains the glucosamine micropill.Then carry out compaction of pellet, then drop in the high-efficiency coating pot, spray into above-mentioned coating solution and carry out coating, drying, obtain the glucosamine hydrochloride pellet preparations.
[embodiment 2]
(1) prescription 2(1000 grain)
The micropill prescription
Amino glucosamine 240g(is by giving money as a gift)
Microcrystalline Cellulose 40g
Carboxymethyl starch sodium 15g
5% hypromellose sodium (5cps) ethanol-water solution 240ml
Pulvis Talci 30g
(2) preparation method
The glucosamine hydrochloride of above-mentioned recipe quantity, microcrystalline Cellulose and carboxymethylstach sodium are crossed respectively to 80 mesh sieves, fully mix homogeneously; Add the alcohol-water liquid of 5% hypromellose sodium appropriate the material mixed, make soft material; Then add extruder, be squeezed into bar; Bar is placed in spheronizator round as a ball, adds 5% hypromellose sodium simultaneously and reach in right amount Pulvis Talci 30g, the round as a ball time is 5min, and 55-60 ℃ of dry 8h sieves and collect the micropill of 18-32 order particle diameter, obtains the glucosamine micropill.Obtain the glucosamine hydrochloride pellet preparations with capsule-filling agent fill capsule.
[embodiment 3]
(1) prescription 3(1000 grain)
Glucosamine sulfate 240g(is by giving money as a gift)
Lactose 40g
Low-substituted hydroxypropyl cellulose 10g
10% zein alcoholic solution 200ml
Silicone oil is appropriate
(2) preparation method
The glucosamine sulfate of above-mentioned recipe quantity, lactose and low-substituted hydroxypropyl cellulose are crossed respectively to 80 mesh sieves; abundant mix homogeneously; make the glucosamine suspension with purified water; with the spray of fluidized bed coating granulator, be wrapped on 20-30 purpose celphere; after oven dry, add again 10% zein ethanol and the silicone oil of recipe quantity to carry out in right amount coating; get 18-24 order micropill after oven dry, obtain the glucosamine sulfate micropill.Obtain the glucosamine sulfate pellet preparations with capsule-filling agent fill capsule again.
[embodiment 4]
The glucosamine pellet preparations of embodiment 1,2,3 is placed in respectively to uncovered culture dish, is placed in 60 ℃ of calorstats, dissolution (pH6.8 phosphate buffer) and content when within 10 days, sampling detects 35min, testing result is in Table 1.
Table 1 hot test (60 ℃).
[embodiment 5]
The glucosamine pellet preparations of embodiment 1,2,3 is placed in respectively to uncovered culture dish, tiling one deck, be placed in 25 ℃, in the vessel of RH92.5% sealing, dissolution (pH6.8 phosphate buffer) and content when within the 10th day, sampling detects 35min, testing result is in Table 2.
The high wet test of table 2 (5 ℃, RH92.5%).
[embodiment 6]
The glucosamine pellet preparations of embodiment 1,2,3 is placed in respectively to uncovered culture dish, tiling one deck, adjustable range, make intensity of illumination be about 4500Lux, dissolution (pH6.8 phosphate buffer) and content when within the 10th day, sampling detects 35min, testing result is in Table 3.
Table 3 exposure experiments to light (500 ± 500Lux).
The result of the test of embodiment 4-6 shows, glucosamine pellet preparations of the present invention dissolution and the content of sample under various conditions has no significant change, and glucosamine pellet preparations steady quality of the present invention, controlled is described, can effectively guarantee drug safety.
[embodiment 7]
Oar method according to Chinese Pharmacopoeia version appendix XC dissolution method in 2010 is measured dissolubility, the results are shown in Table 4 and table 5.
Table 4: glucosamine pellet preparations and the commercially available ordinary tablet dissolution contrast in pure water.
Table 5: glucosamine pellet preparations and the commercially available ordinary tablet dissolution contrast in the pH6.8 phosphate buffer.
Claims (6)
1. a glucosamine micropill, press this micropill weighing scale, and it comprises:
Glucosamine 50-90%
Diluent 1-15%
Disintegrating agent 1-10%
Binding agent 1-10%
Other adjuvants 1-5%
Wherein, described glucosamine is selected from glucosamine hydrochloride, glucosamine sulfate or other pharmaceutically acceptable salts;
Described diluent is selected from a kind of in microcrystalline Cellulose, lactose, mannitol, starch, glucide;
Described disintegrating agent is selected from a kind of in carboxymethyl starch sodium, crospolyvinylpyrrolidone, low-substituted hydroxypropyl cellulose (L-HPC), cross-linking sodium carboxymethyl cellulose;
Described binding agent is selected from a kind of in ethanol, starch, pregelatinized Starch, hypromellose sodium (HPMC), zein, Lac;
Described micropill diameter is 0.1-10mm.
2. according to the glucosamine micropill of claim 1, by this micropill weighing scale, glucosamine (by giving money as a gift) content is 50%-90%, is preferably 65-85%, more preferably 75-85%.
3. according to the glucosamine micropill of claim 1, by this micropill weighing scale, amount of diluent is 1%-15%, is preferably 5-15%, more preferably 5-12%.
4. according to the glucosamine micropill of claim 1, by this micropill weighing scale, disintegrant content is 1%-10%, is preferably 2-8%, more preferably 2-5%.
5. according to the glucosamine micropill of claim 1, by this micropill weighing scale, binder content is 1%-10%, is preferably 2-8%, more preferably 2-5%.
6. according to the described glucosamine micropill of claim 1-5 any one claim, it makes capsule or tablet directly or after carrying out coating.
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| CN2013103824761A CN103432082A (en) | 2013-08-29 | 2013-08-29 | Glucosamine composition and preparation method thereof |
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| CN2013103824761A CN103432082A (en) | 2013-08-29 | 2013-08-29 | Glucosamine composition and preparation method thereof |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018165930A1 (en) * | 2017-03-16 | 2018-09-20 | 北京科信必成医药科技发展有限公司 | Glucose pellet, and preparation method therefor and uses thereof |
| CN112587499A (en) * | 2020-12-29 | 2021-04-02 | 成都锦华药业有限责任公司 | Berberine hydrochloride pellet and preparation method thereof |
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| US20050181044A1 (en) * | 2004-02-18 | 2005-08-18 | Jaime Romero | Compositions and methods for timed release of water-soluble nutritional supplements, green coffee extract |
| US20080220079A1 (en) * | 2007-03-02 | 2008-09-11 | Farnam Companies, Inc. | Sustained release compositions using wax-like materials |
| CN101642461A (en) * | 2008-08-07 | 2010-02-10 | 杨喜鸿 | Drug composition of iguratimod and glucosamine, preparation method and drug application thereof |
| US20100209572A1 (en) * | 2007-08-08 | 2010-08-19 | Sanypet S.P.A | Process for producing a product for feeding animals |
| US20110027357A1 (en) * | 2004-02-18 | 2011-02-03 | Isaac Gilinski | Compositions and methods for timed release of water-soluble nutritional supplements |
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2013
- 2013-08-29 CN CN2013103824761A patent/CN103432082A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050181044A1 (en) * | 2004-02-18 | 2005-08-18 | Jaime Romero | Compositions and methods for timed release of water-soluble nutritional supplements, green coffee extract |
| US20110027357A1 (en) * | 2004-02-18 | 2011-02-03 | Isaac Gilinski | Compositions and methods for timed release of water-soluble nutritional supplements |
| US20080220079A1 (en) * | 2007-03-02 | 2008-09-11 | Farnam Companies, Inc. | Sustained release compositions using wax-like materials |
| US20100209572A1 (en) * | 2007-08-08 | 2010-08-19 | Sanypet S.P.A | Process for producing a product for feeding animals |
| CN101642461A (en) * | 2008-08-07 | 2010-02-10 | 杨喜鸿 | Drug composition of iguratimod and glucosamine, preparation method and drug application thereof |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018165930A1 (en) * | 2017-03-16 | 2018-09-20 | 北京科信必成医药科技发展有限公司 | Glucose pellet, and preparation method therefor and uses thereof |
| US11278557B2 (en) | 2017-03-16 | 2022-03-22 | Cosci Med-Tech Co. Ltd. | Glucose pellets, preparation method and use thereof |
| CN112587499A (en) * | 2020-12-29 | 2021-04-02 | 成都锦华药业有限责任公司 | Berberine hydrochloride pellet and preparation method thereof |
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Application publication date: 20131211 |