CN112156077B - N-acetylglucosamine tablet and preparation method thereof - Google Patents
N-acetylglucosamine tablet and preparation method thereof Download PDFInfo
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- CN112156077B CN112156077B CN202011154982.1A CN202011154982A CN112156077B CN 112156077 B CN112156077 B CN 112156077B CN 202011154982 A CN202011154982 A CN 202011154982A CN 112156077 B CN112156077 B CN 112156077B
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7008—Compounds having an amino group directly attached to a carbon atom of the saccharide radical, e.g. D-galactosamine, ranimustine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
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Abstract
The invention relates to the field of pharmaceutical preparations, in particular to an N-acetylglucosamine tablet which comprises the following components in percentage by weight: 20-45% of N-acetylglucosamine, 35-65% of filler, 5-15% of disintegrating agent, 5-15% of adhesive and 0.5-5% of lubricant. The invention also provides a preparation method of the tablet. The invention not only improves the particle size of the N-acetylglucosamine, increases the dissolution rate of the tablet, but also solves the problems that the N-acetylglucosamine raw material drug has a needle-shaped structure, the friability is unqualified during tabletting and the difference of tablet weight is large. In addition, the direct powder tabletting process is used in the preparation process, so that the problem of color change after the compatibility of N-acetylglucosamine and water is avoided, the content and weight difference of the finally prepared tablets meet the quality requirement, the production efficiency is high, and the labor intensity is low.
Description
Technical Field
The invention relates to the technical field of pharmaceutical preparations, in particular to an N-acetylglucosamine tablet and a preparation method thereof.
Background
N-acetylglucosamine is the smallest constitutional unit of chitin component in exoskeletons of insects and crustaceans, and is also the basic constitutional unit of many important polysaccharides in biological cells, which have many important physiological functions in the organism. Pharmacodynamic tests, pharmacokinetic tests and the like show that the traditional Chinese medicine composition can be used for treating diarrhea-predominant irritable bowel syndrome, and has obvious effect and low toxic and side effects.
The tablet is a tablet preparation prepared from the medicine and appropriate auxiliary materials by a preparation technology. Generally comprises raw medicines, fillers, adsorbents, binders, lubricants, dispersants, wetting agents, disintegrants, flavors, pigments and the like. The tablet has the advantages of accurate content, small weight difference, disintegration time or dissolution meeting the specification, proper hardness, beautiful appearance, good color, meeting the sanitary inspection standard, stable property in the specified storage period, and the like. Accurate dosage, stable physicochemical property, long storage period, convenient use, transportation and carrying, low cost and high yield.
The general tablet processing technology is that the materials are firstly crushed, granulated, dried and then made into tablets by a tablet press. The N-acetylglucosamine raw material is white or white-like crystalline powder, is easy to dissolve in water, and has the problems of unqualified friability during tabletting and large difference of tablet weight due to the needle-shaped structure of the raw material medicine, so that the N-acetylglucosamine tablet is not available at present and mainly takes the form of the raw material medicine.
Chinese patent document CN107320456A discloses an N-acetyl-D-glucosamine capsule preparation and a preparation method thereof. However, no report is found about an N-acetylglucosamine tablet and a preparation method thereof.
Disclosure of Invention
The invention aims to provide an N-acetylglucosamine tablet and a preparation method thereof, and solves the problems of unqualified friability and large difference of tablet weights during tabletting because the raw material medicines are in a needle-shaped structure. The particle diameter D of the N-acetylglucosamine in the invention 90 60-115 mu m, and the dissolution rate of the tablet in water for 15min is more than 85 percent.
The invention provides an N-acetylglucosamine tablet, which consists of the following components in percentage by weight:
20-45% of N-acetylglucosamine;
35-65% of a filler;
5-15% of a disintegrating agent;
5-15% of adhesive;
0.5 to 5 percent of lubricant;
wherein, the N-acetylglucosamine is subjected to jet milling to obtain a milled particle diameter D 90 60 to 115 mu m.
Further, the particle diameter D of the crushed N-acetylglucosamine 90 75 to 95 μm.
Further, the filler is microcrystalline cellulose.
Further, the disintegrating agent is sodium carboxymethyl cellulose.
Further, the adhesive is povidone.
Furthermore, the lubricant is silica gel micropowder.
Further, the N-acetylglucosamine tablet comprises the following components in percentage by weight:
25-40% of N-acetylglucosamine;
40-60% of a filler;
5-10% of a disintegrating agent;
8-12% of adhesive;
1-3% of lubricant.
In a second aspect of the present invention, there is provided a method for preparing the N-acetylglucosamine tablet as described above, comprising the steps of:
a. pulverizing N-acetylglucosamine with air flow, and pulverizing to obtain D 90 60-115 μm;
b. mixing the crushed N-acetylglucosamine, a filler, a disintegrating agent and an adhesive in a mixer to obtain premixed powder;
c. putting the premixed powder and the lubricant into a mixer for mixing to obtain total mixed powder;
d. and tabletting the total mixed powder to obtain the N-acetylglucosamine tablet.
The invention has the advantages that:
1. the raw material of the N-acetylglucosamine tablet prepared by the invention passes through the air flowAfter grinding, D 90 Is 60-115 mu m, not only improves the particle size of the N-acetylglucosamine, increases the dissolution rate of the tablet, but also solves the problems that the N-acetylglucosamine raw material drug has a needle-shaped structure, the friability is unqualified during tabletting and the difference of tablet weight is large;
2. in addition, the direct powder tabletting process is used in the preparation process, so that the problem of color change after the compatibility of N-acetylglucosamine and water is avoided, the content, weight difference and related substances of the finally prepared tablet meet the quality requirements, and other indexes can meet the pharmacopoeia standards.
Detailed Description
The following examples are provided to illustrate specific embodiments of the present invention.
Example 1:
an N-acetylglucosamine tablet comprises the following components in percentage by weight:
20% of N-acetylglucosamine;
65% of microcrystalline cellulose;
5% of sodium carboxymethyl cellulose;
5% of polyvidone;
5% of micropowder silica gel;
the preparation method comprises the following steps:
a. pulverizing N-acetylglucosamine with air flow to obtain powder with particle diameter D 90 Is 60 μm;
b. mixing the crushed N-acetylglucosamine, the filler, the disintegrating agent and the adhesive in a mixer to obtain premixed powder;
c. placing the premixed powder and the lubricant into a mixer for mixing to obtain total mixed powder;
d. and tabletting the total mixed powder to obtain the N-acetylglucosamine tablet.
Example 2:
an N-acetylglucosamine tablet comprises the following components in percentage by weight:
25% of N-acetylglucosamine;
60% of microcrystalline cellulose;
5% of sodium carboxymethyl cellulose;
5% of polyvidone;
5% of micropowder silica gel;
the preparation method comprises the following steps:
a. pulverizing N-acetylglucosamine with air flow to obtain powder with particle diameter D 90 Is 75 μm;
b. mixing the crushed N-acetylglucosamine, the filler, the disintegrating agent and the adhesive in a mixer to obtain premixed powder;
c. placing the premixed powder and the lubricant into a mixer for mixing to obtain total mixed powder;
d. and tabletting the total mixed powder to obtain the N-acetylglucosamine tablet.
Example 3:
an N-acetylglucosamine tablet comprises the following components in percentage by weight:
40% of N-acetylglucosamine;
40% of microcrystalline cellulose;
10% of sodium carboxymethyl cellulose;
5% of polyvidone;
5% of micropowder silica gel;
the preparation method comprises the following steps:
a. pulverizing N-acetylglucosamine with air flow to obtain powder with particle diameter D 90 Is 95 μm;
b. mixing the crushed N-acetylglucosamine, a filler, a disintegrating agent and an adhesive in a mixer to obtain premixed powder;
c. placing the premixed powder and the lubricant into a mixer for mixing to obtain total mixed powder;
d. and tabletting the total mixed powder to obtain the N-acetylglucosamine tablet.
Example 4:
an N-acetylglucosamine tablet comprises the following components in percentage by weight:
45% of N-acetylglucosamine;
35% of microcrystalline cellulose;
5% of sodium carboxymethyl cellulose;
12% of polyvidone;
3% of micropowder silica gel;
the preparation method comprises the following steps:
a. pulverizing N-acetylglucosamine with air flow to obtain powder with particle diameter D 90 115 μm;
b. mixing the crushed N-acetylglucosamine, a filler, a disintegrating agent and an adhesive in a mixer to obtain premixed powder;
c. putting the premixed powder and the lubricant into a mixer for mixing to obtain total mixed powder;
d. and tabletting the total mixed powder to obtain the N-acetylglucosamine tablet.
Example 5:
in this example, compared with the total powder mixing performance of Active Pharmaceutical Ingredient (API for short) prepared by airflow pulverization under the same conditions of other prescription processes, the results are shown in table 1.
TABLE 1
The results in table 1 show that the API produced in different states in the same formulation process had different flowability of the total blended powder, different content uniformity, and different tablet hardness and friability. The invention firstly carries out jet milling on N-acetylglucosamine, and the grain diameter D after the milling is 90 The total mixed powder prepared by the method has good fluidity and uniformity, and the hardness and friability of the tablets can meet the requirements, and particularly has obvious advantages in weight difference compared with other raw materials with particle size ranges, wherein the particle size ranges are 60-115 mu m.
Example 6:
this example compares the dissolution rates of tablets prepared from API in different states under the same conditions of other formulation processes, and the results are shown in table 2.
TABLE 2 dissolution rate (Paddle method, 50rpm, dissolution Medium: 900ml water, n = 12)
The results in Table 2 show that, under the same recipe, when D is 90 =75 μm and 95 μm, 15min dissolution is greater than 95%, and D 90 And (5) =170 mu m, the dissolution rate is lower than 85%. Especially when D 90 If the particle size is not less than 75 μm and not more than 90 μm, the dissolution RSD is small and the tablet quality is more uniform.
Example 7
This example compares the effect of different states of API on tableting speed during production under otherwise identical formulation processes, and the results are shown in table 3.
TABLE 3 Effect of different states of API on tabletting speed
* Indicating that the tablets could not be pressed.
From the above experimental results, it can be seen that, under the same other recipes and processes:
(1) Containing jet milling API (D) 90 =165 μm), tablets are susceptible to breaking when the tabletting speed is 50000 tablets/hour; the tabletting speed is higher than 50000 tablets per hour, the tablets are seriously cracked, and the tablets can not be formed.
(2) Containing jet milling API (D) 90 =75 μm), the tablet quality is not changed significantly when the tabletting speed is up to 150000 tablets/hour, and the production efficiency is high;
(3) Containing jet milling API (D) 90 =40 μm), when the tabletting speed is higher than 100000 tablets/hour, the total mixed powder can not be fed in time due to poor fluidity, and the tabletting can not be carried out.
While the preferred embodiments of the present invention have been described in detail, it will be understood by those skilled in the art that the invention is not limited thereto, and that various changes and modifications may be made without departing from the spirit of the invention, and the scope of the appended claims is to be accorded the full range of equivalents.
Claims (4)
1. The N-acetylglucosamine tablet is characterized by comprising the following components in percentage by weight:
20-45% of N-acetylglucosamine;
35-65% of a filler;
5-15% of a disintegrating agent;
5-15% of adhesive;
0.5 to 5 percent of lubricant;
wherein, the N-acetylglucosamine needs to be pulverized by airflow, and the particle diameter D after pulverization is 90 60-115 μm; the filler is microcrystalline cellulose; the disintegrating agent is sodium carboxymethyl cellulose; the adhesive is povidone; the lubricant is micro silica gel.
2. The N-acetylglucosamine tablet according to claim 1, wherein the particle size D of the N-acetylglucosamine after pulverization is D 90 75 to 95 μm.
3. The N-acetylglucosamine tablet of claim 1, which consists of the following components in percentage by weight:
25-40% of N-acetylglucosamine;
40-60% of a filling agent;
5-10% of a disintegrating agent;
8-12% of an adhesive;
1-3% of lubricant.
4. A process for the preparation of N-acetylglucosamine tablets according to any one of claims 1 to 3, comprising the steps of:
a. crushing N-acetylglucosamine by airflow;
b. mixing the crushed N-acetylglucosamine, the filler, the disintegrating agent and the adhesive in a mixer to obtain premixed powder;
c. placing the premixed powder and the lubricant into a mixer for mixing to obtain total mixed powder;
d. and tabletting the total mixed powder to obtain the N-acetylglucosamine tablet.
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| CN202011154982.1A CN112156077B (en) | 2020-10-26 | 2020-10-26 | N-acetylglucosamine tablet and preparation method thereof |
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Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1156027A (en) * | 1996-12-27 | 1997-08-06 | 中国人民解放军第三军医大学 | Application of N-aceto-D-aminoglucose in medicinal preparation for curing intestinal diseases |
| CN1283413A (en) * | 1999-08-09 | 2001-02-14 | 烧津水产化学工业株式会社 | Skin-care agent, health and face-care foodstuff |
| JP2009269929A (en) * | 2004-12-27 | 2009-11-19 | Yaizu Suisankagaku Industry Co Ltd | Intraorally disintegrable type n-acetylglucosamine tablet |
| CN101926808A (en) * | 2009-06-25 | 2010-12-29 | 积华药业有限公司 | Glucosamine formulations |
| WO2011111027A2 (en) * | 2010-03-11 | 2011-09-15 | Dexcel Pharma Technologies Ltd. | Oral dispersible delayed release tablet formulation |
| CN107320456A (en) * | 2016-04-29 | 2017-11-07 | 上海玉曜生物医药科技有限公司 | 2-acetylamino-2-deoxy-D-glucose capsule preparations and preparation method thereof |
| JP2019123686A (en) * | 2018-01-15 | 2019-07-25 | 株式会社ファンケル | Tablet containing proteoglycan-containing cartilage extract and glucosamine |
-
2020
- 2020-10-26 CN CN202011154982.1A patent/CN112156077B/en active Active
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1156027A (en) * | 1996-12-27 | 1997-08-06 | 中国人民解放军第三军医大学 | Application of N-aceto-D-aminoglucose in medicinal preparation for curing intestinal diseases |
| CN1283413A (en) * | 1999-08-09 | 2001-02-14 | 烧津水产化学工业株式会社 | Skin-care agent, health and face-care foodstuff |
| JP2009269929A (en) * | 2004-12-27 | 2009-11-19 | Yaizu Suisankagaku Industry Co Ltd | Intraorally disintegrable type n-acetylglucosamine tablet |
| CN101926808A (en) * | 2009-06-25 | 2010-12-29 | 积华药业有限公司 | Glucosamine formulations |
| WO2011111027A2 (en) * | 2010-03-11 | 2011-09-15 | Dexcel Pharma Technologies Ltd. | Oral dispersible delayed release tablet formulation |
| CN107320456A (en) * | 2016-04-29 | 2017-11-07 | 上海玉曜生物医药科技有限公司 | 2-acetylamino-2-deoxy-D-glucose capsule preparations and preparation method thereof |
| JP2019123686A (en) * | 2018-01-15 | 2019-07-25 | 株式会社ファンケル | Tablet containing proteoglycan-containing cartilage extract and glucosamine |
Non-Patent Citations (1)
| Title |
|---|
| 盐酸氨基葡萄糖片的研制及不同含量测定方法的评价;杨岚;《中国优秀硕士学位论文全文数据库工程科技I辑》;20070315(第3期);第一部分2.1片剂制备方法的选择 * |
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