CN110898025A - Acarbose sustained-release preparation and preparation method thereof - Google Patents
Acarbose sustained-release preparation and preparation method thereof Download PDFInfo
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Abstract
The invention relates to the field of pharmaceutical preparations, in particular to an acarbose sustained-release preparation and a preparation method thereof; it is a core-spun tablet formed by a slow-release inner core and a quick-release outer layer; the slow release inner core is an inner core, and the quick release outer layer forms a package on the outer layer of the slow release inner core; the slow release inner core and the quick release outer layer both contain acarbose; and the mass ratio of the acarbose in the slow-release inner core to the acarbose in the quick-release outer layer is 5: 1-25. The method comprises the steps of tabletting a slow-release inner core material to obtain a slow-release inner core, carrying out secondary tabletting on a quick-release outer layer material and the slow-release inner core, and forming a core-spun tablet by the slow-release inner core and the quick-release outer layer; the acarbose sustained release preparation is obtained. The sustained-release preparation has higher safety, can take effect quickly and has long drug effect. The preparation method of the sustained-release preparation mainly comprises granulation and tabletting processes, does not relate to operations such as laser drilling and the like, has low technical difficulty and is convenient for industrial production.
Description
Technical Field
The invention relates to the field of pharmaceutical preparations, in particular to an acarbose sustained-release preparation and a preparation method thereof.
Background
China has about 1.14 hundred million type 2 diabetic patients and nearly 1.5 hundred million pre-diabetic patients, and the patients become the countries with the largest number of diabetic patients. The type 2 diabetes patients are generally treated by oral hypoglycemic drugs, and from the data of market sales statistical analysis, the first three hypoglycemic drug varieties are acarbose, repaglinide and metformin respectively.
Acarbose is an α glucosidase inhibitor that competitively inhibits the glucoside hydrolase in the intestine, reduces the breakdown of polysaccharides and sucrose into glucose, and the absorption of sugar is correspondingly slowed, thus having the effect of lowering postprandial blood glucose.
The acarbose oral quick-release solid preparation on the market at present can be quickly disintegrated in gastric juice after being taken and can take effect after being absorbed into blood. However, because of the common preparation, the drug release is too fast, the immediate blood drug concentration is too high, and the blood drug concentration is too low after transient metabolism, the former is easy to generate toxic and side effects, such as gastrointestinal discomfort, liver and kidney function damage and the like, and the latter can cause the duration of the drug effect to be too short. In addition, the patient needs to take the medicine three times a day, which is inconvenient, easy to forget to take the medicine and neglect to take the medicine, and influences the treatment effect.
Aiming at the problems of the acarbose oral quick-release preparation, a research team improves the acarbose oral quick-release preparation and discloses an acarbose osmotic pump tablet and a preparation method thereof.
In addition, the osmotic pump has the obvious characteristic of time lag, which can cause the defect of untimely blood sugar reduction. The constant rate zero order release of a conventionally controlled release dosage form such as an osmotic pump tablet is not essential, and a patient is more in need of a drug which exerts its drug effect quickly after a meal and slowly after a quick onset.
Therefore, there is an urgent need to provide a novel acarbose sustained release preparation and a method for preparing the same to solve or partially solve the problems of the prior art.
Disclosure of Invention
The invention aims at overcoming the defects in the prior art and provides an acarbose sustained-release preparation which has high clinical safety, can quickly take effect and has long drug effect.
The second purpose of the invention is to provide a method for preparing the acarbose sustained-release preparation.
In order to realize the aim, the invention designs an acarbose sustained-release preparation which is a core-spun tablet formed by a sustained-release inner core and a quick-release outer layer; the slow release inner core is an inner core, and the quick release outer layer forms a package on the outer layer of the slow release inner core; the slow release inner core and the quick release outer layer both contain acarbose; and the mass ratio of the acarbose in the slow-release inner core to the acarbose in the quick-release outer layer is 5: 1-25.
Further, the sustained-release inner core comprises the following components in percentage by mass: 10-60% of acarbose, 10-60% of a framework material, 10-50% of a release regulator, 0-5% of a slow-release lubricant and 0-1% of a slow-release pigment.
Still further, the quick-release outer layer comprises the following components in percentage by mass: 10-60% of acarbose, 20-70% of a filler, 3-25% of an internal disintegrating agent, 3-25% of an external disintegrating agent, 0-5% of a quick-release lubricant and 0-2% of a quick-release pigment.
Still further, the sustained-release inner core comprises the following components in percentage by mass: 20-50% of acarbose, 20-50% of a framework material, 20-40% of a release regulator, 0.1-4.9% of a slow release lubricant and 0-0.5% of a slow release pigment;
the quick-release outer layer comprises the following components in percentage by mass: 20-50% of acarbose, 30-60% of a filler, 5-20% of an internal disintegrating agent, 5-20% of an external disintegrating agent, 0.1-5% of a quick-release lubricant and 0-1% of a quick-release pigment.
Furthermore, in the slow release inner core, the framework material is any one of hydroxypropyl methylcellulose, hydroxypropyl cellulose and povidone,
the release regulator comprises any one of ethyl cellulose, acrylic resin copolymer, polyethylene glycol and polyvidone,
the slow release lubricant is one of talcum powder, magnesium stearate, superfine silica gel powder, stearic acid, hydrogenated vegetable oil and sodium stearyl fumarate.
Furthermore, the framework material is hydroxypropyl methyl cellulose; the release regulator is ethyl cellulose; the lubricant is magnesium stearate.
Still further, in the quick-release outer layer, the filler is one of sucrose, microcrystalline cellulose, starch, mannitol, lactose and pregelatinized starch;
the internal disintegrating agent and the external disintegrating agent are one of crospovidone, sodium carboxymethyl starch, sodium hydroxymethyl starch, sodium carboxymethyl cellulose, calcium carboxymethyl cellulose, croscarmellose sodium and low-substituted hydroxypropyl cellulose,
the quick-release lubricant is one of talcum powder, magnesium stearate, superfine silica gel powder, stearic acid, hydrogenated vegetable oil and sodium stearyl fumarate.
Still further, the filler is microcrystalline cellulose or lactose;
the internal disintegrating agent is crospovidone, and the external disintegrating agent is sodium carboxymethyl starch; the weight ratio of the crospovidone to the sodium carboxymethyl starch is 1: 1-2; the lubricant is magnesium stearate.
Still further, the sustained-release inner core comprises the following components in percentage by mass: 25-50% of acarbose, 20-50% of hydroxypropyl methyl cellulose, 20-40% of ethyl cellulose, 0.1-4.9% of slow-release lubricant and 0-0.5% of slow-release pigment; the slow release lubricant is magnesium stearate or aerosil;
the quick-release outer layer comprises the following components in percentage by mass: 20-50% of acarbose, 30-60% of filler, 5-20% of crospovidone, 5-20% of sodium carboxymethyl starch, 0.1-5% of magnesium stearate and 0-1% of quick-release pigment, wherein the filler is microcrystalline cellulose or lactose.
The invention also provides a preparation method of the acarbose sustained-release preparation, which is characterized by comprising the following steps: the method comprises the following steps:
1) weighing 10-60% of acarbose, 10-60% of a framework material, 10-50% of a release regulator, 0-5% of a slow release lubricant and 0-1% of a slow release pigment in percentage by mass;
2) mixing acarbose, a framework material, a release regulator and a sustained-release pigment, granulating, and mixing the prepared granules with a sustained-release lubricant to obtain a sustained-release inner core material;
3) weighing 10-60% of acarbose, 20-70% of a filler, 3-25% of an internal disintegrating agent, 3-25% of an external disintegrating agent, 0-5% of a quick-release lubricant and 0-2% of a quick-release pigment in percentage by mass;
4) mixing acarbose, filler, internal disintegrating agent and quick-release pigment, granulating, and mixing the obtained granule, external disintegrating agent and quick-release lubricant to obtain quick-release outer layer material;
5) tabletting the sustained-release inner core material obtained in the step 2) to obtain a sustained-release inner core;
6) performing secondary tabletting on the quick-release outer layer material in the step 4) and the slow-release inner core in the step 5), and forming a core-spun tablet by the slow-release inner core and the quick-release outer layer; the acarbose sustained release preparation is obtained.
The principle of the invention is as follows:
1) the quick-release outer layer and the slow-release inner core both contain the acarbose, the release speeds of the quick-release outer layer and the slow-release inner core are different, and the effective medicinal ingredients are released in a time-selected and quantity-selected manner according to the metabolic rule or the medication period of a human body, so that the design can realize the administration as required and the medicinal effect is durable; in addition, the outermost layer is provided with a quick-release outer layer, so that the quick-release outer layer can ensure quick effect after medicine taking and is convenient to take medicine.
2) The quick-release outer layer or the slow-release inner core of the medicine can extend to form a closed space, namely the core-spun tablet. Can be set into a multi-layer core-spun product according to specific requirements, and the slow-release inner core and the quick-release outer layer are arranged at intervals. Combining various influencing factors in the production process, firstly forming a double-layer core-spun tablet, namely, the inner core is a slow-release inner chip, and the drug effect is durable; the outer part is a quick-release outer layer which can quickly take effect; the industrial production process of the preparation mainly comprises granulation and tabletting processes, does not relate to operations such as laser drilling and the like, has low technical difficulty and is convenient for industrial production.
3) The mass ratio of the acarbose in the slow-release inner core material to the acarbose in the quick-release outer layer material is 1: 2-2: 1, preferably 2:1, so that the effective dose can be quickly reached after the medicine is taken, and in the medicine metabolism process, the effective medicine components in the slow-release inner core chip are used for compensation, so that the medicine effect is more durable.
4) At least one of the quick-release outer layer material or the slow-release inner core material contains pigment, the pigment accounts for 0.01-1% of the mass content of the material, the pigment is added, so that the two material components can be distinguished in the production process, the forming quality of the medicine can be visually checked, and natural pigment or artificially synthesized pigment can be selected.
5) The slow release inner core comprises acarbose, a framework material, a release regulator and a lubricant. The matrix material is a gel matrix material and plays a role in sustained and controlled release, if the matrix material is determined according to clinical requirements, too little matrix material can not play a role in sustained release, and if the matrix material is too much, the matrix material is released too slowly; the release regulator regulates the release rate of the drug to meet the administration requirement, and is determined according to the release rate of the drug.
The invention has the beneficial effects that:
1. the acarbose sustained-release preparation provided by the invention is provided with the quick-release outer layer on the outermost layer, so that the rapid effect can be ensured after the medicine is taken; the sustained-release inner core contained in the sustained-release preparation can make the duration of the drug effect longer. And no organic solvent is used in the preparation process;
2. the sustained-release preparation has higher safety, can take effect quickly and has long drug effect.
3. The preparation method of the sustained-release preparation mainly comprises granulation and tabletting processes, does not relate to operations such as laser drilling and the like, has low technical difficulty and is convenient for industrial production.
4. The granulation mode of the slow release inner core and the quick release outer layer is dry granulation, organic solvent is not needed, and the prepared slow release preparation has better safety.
Drawings
FIG. 1 is a schematic structural diagram of an acarbose sustained release formulation;
in the figure, a quick-release outer layer 1 and a slow-release inner core 2
Figure 2 is a graph of the dissolution profile of acarbose tablets.
Detailed Description
The present invention is described in further detail below with reference to specific examples so as to be understood by those skilled in the art.
Example 1
As shown in figure 1, the acarbose sustained-release preparation 1 comprises an acarbose sustained-release inner core, a framework material 20%, a release regulator 35%, a release lubricant 4.9% and a release pigment 0.1%. The quick-release outer layer contains 20% of acarbose, 39.9% of filler, 20% of internal disintegrating agent, 20% of external disintegrating agent and 0.1% of quick-release lubricant.
Example 1
The preparation method comprises the following steps:
(1) mixing acarbose, a framework material, a release regulator and a release pigment, then performing dry granulation, and mixing the prepared granules with a release lubricant to obtain a slow-release inner core material;
(2) mixing acarbose, filler and internal disintegrating agent, performing dry granulation, and mixing the obtained granules with external disintegrating agent and quick-release lubricant to obtain quick-release outer material;
(3) tabletting the slow release inner core material to obtain a slow release inner core tablet core;
(4) and carrying out secondary tabletting on the quick-release outer layer material and the sustained-release inner core tablet core to obtain a sustained-release preparation 1.
Example 2
The acarbose sustained-release preparation 2 comprises 50% of acarbose, 20% of framework material, 27% of release regulator, 2.5% of release lubricant and 0.5% of release pigment in a sustained-release inner core. The quick-release outer layer contains 50% of acarbose, 30% of filler, 12% of internal disintegrating agent, 5% of external disintegrating agent and 3% of quick-release lubricant.
Example 2
The preparation method comprises the following steps:
(1) mixing acarbose, a framework material, a release regulator and a release pigment, then performing dry granulation, and mixing the prepared granules with a release lubricant to obtain a slow-release inner core material;
(2) tabletting the sustained-release inner core material to obtain a sustained-release tablet core;
(3) mixing acarbose, filler and internal disintegrating agent, performing dry granulation, and mixing the obtained granules with external disintegrating agent and quick-release lubricant to obtain quick-release outer material;
(4) and carrying out secondary tabletting on the quick-release outer layer material and the sustained-release tablet core to obtain a sustained-release preparation 2.
Example 3
The acarbose sustained-release preparation 3 comprises 29.9 percent of acarbose, 50 percent of framework material, 20 percent of release regulator and 0.1 percent of release lubricant in a sustained-release inner core. The quick-release outer layer contains acarbose 40%, filler 43%, internal disintegrating agent 5%, external disintegrating agent 10%, quick-release lubricant 1%, and quick-release pigment 1%.
Example 3
The preparation method comprises the following steps:
(1) mixing acarbose, a framework material and a release regulator, then performing dry granulation, and mixing the prepared granules with a release lubricant to obtain a slow-release inner core material;
(2) mixing acarbose, filler, internal disintegrating agent and quick-release pigment, performing dry granulation, and mixing the obtained granules with external disintegrating agent and quick-release lubricant to obtain quick-release outer layer material;
(3) tabletting the slow release inner core material to obtain a slow release inner core tablet core;
(4) and performing secondary tabletting on the quick-release outer layer material and the sustained-release inner core tablet core to obtain a sustained-release preparation 3.
Example 4
The acarbose sustained release preparation 4, the sustained release inner chip contains 30% of acarbose, 30% of framework material, 39% of release regulator and 1% of release lubricant. The quick-release outer layer contains 35% of acarbose, 49.99% of filler, 5% of internal disintegrating agent, 5% of external disintegrating agent, 5% of quick-release lubricant and 0.01% of quick-release pigment.
Example 4
The preparation method comprises the following steps:
(1) mixing acarbose, a framework material and a release regulator, then performing dry granulation, and mixing the prepared granules with a release lubricant to obtain a slow-release inner core material;
(2) tabletting the slow release inner core material to obtain a slow release inner core tablet core;
(3) mixing acarbose, filler, internal disintegrating agent and quick-release pigment, performing dry granulation, and mixing the obtained granules with external disintegrating agent and quick-release lubricant to obtain quick-release outer layer material;
(4) and performing secondary tabletting on the quick-release outer layer material and the sustained-release inner core tablet core to obtain a sustained-release preparation 4.
Example 5
The acarbose sustained release preparation 5 comprises 20 percent of acarbose, 39 percent of framework material, 40 percent of release regulator and 1 percent of release lubricant in a sustained release inner core. The quick-release outer layer contains 20% of acarbose, 60% of filler, 6.8% of internal disintegrating agent, 10% of external disintegrating agent, 3% of quick-release lubricant and 0.2% of quick-release pigment.
Example 5
The preparation method comprises the following steps:
(1) mixing acarbose, a framework material and a release regulator, then performing dry granulation, and mixing the prepared granules with a release lubricant to obtain a slow-release inner core material;
(2) mixing acarbose, filler, internal disintegrating agent and quick-release pigment, performing dry granulation, and mixing the obtained granules with external disintegrating agent and quick-release lubricant to obtain quick-release outer layer material;
(3) tabletting the slow release inner core material to obtain a slow release inner core tablet core;
(4) and performing secondary tabletting on the quick-release outer layer material and the sustained-release inner core tablet core to obtain a sustained-release preparation 5.
Comparative example 1 ordinary acarbose tablet
The cumulative dissolution rates of the acarbose sustained release formulations prepared in the comparative example conventional tablet and examples 1 to 5 were measured at different time periods, respectively, and the results are shown in fig. 2: the common tablet is completely released in about 15 min; the prepared sustained release preparation can release 40-50% in about 1h, and can take effect quickly after being taken, and the later period of complete release needs about 11h, namely the drug effect is maintained for a long time, and the sustained release can be carried out for 12 h.
Other parts not described in detail are prior art. Although the present invention has been described in detail with reference to the above embodiments, it is only a part of the embodiments of the present invention, not all of the embodiments, and other embodiments can be obtained without inventive step according to the embodiments, and the embodiments are within the scope of the present invention.
Claims (10)
1. An acarbose sustained release preparation, which is characterized in that: it is a core-spun tablet formed by a slow-release inner core and a quick-release outer layer; the slow release inner core is an inner core, and the quick release outer layer forms a package on the outer layer of the slow release inner core; the slow release inner core and the quick release outer layer both contain acarbose; and the mass ratio of the acarbose in the slow-release inner core to the acarbose in the quick-release outer layer is 5: 1-25.
2. The acarbose sustained release formulation according to claim 1, wherein: the sustained-release inner core comprises the following components in percentage by mass: 10-60% of acarbose, 10-60% of a framework material, 10-50% of a release regulator, 0-5% of a slow-release lubricant and 0-1% of a slow-release pigment.
3. The acarbose sustained release formulation according to claim 2, wherein: the quick-release outer layer comprises the following components in percentage by mass: 10-60% of acarbose, 20-70% of a filler, 3-25% of an internal disintegrating agent, 3-25% of an external disintegrating agent, 0-5% of a quick-release lubricant and 0-2% of a quick-release pigment.
4. The acarbose sustained release formulation according to claim 3, wherein: the sustained-release inner core comprises the following components in percentage by mass: 20-50% of acarbose, 20-50% of a framework material, 20-40% of a release regulator, 0.1-4.9% of a slow release lubricant and 0-0.5% of a slow release pigment;
the quick-release outer layer comprises the following components in percentage by mass: 20-50% of acarbose, 30-60% of a filler, 5-20% of an internal disintegrating agent, 5-20% of an external disintegrating agent, 0.1-5% of a quick-release lubricant and 0-1% of a quick-release pigment.
5. The acarbose sustained release formulation according to claim 2 or 4, characterized in that: in the sustained-release inner core, the skeleton material is any one of hydroxypropyl methylcellulose, hydroxypropyl cellulose and polyvidone, the release regulator comprises any one of ethyl cellulose, acrylic resin copolymer, polyethylene glycol and polyvidone,
the slow release lubricant is one of talcum powder, magnesium stearate, superfine silica gel powder, stearic acid, hydrogenated vegetable oil and sodium stearyl fumarate.
6. The acarbose sustained release formulation according to claim 5, wherein: the framework material is hydroxypropyl methyl cellulose; the release regulator is ethyl cellulose; the lubricant is magnesium stearate.
7. The acarbose sustained release formulation according to claim 3 or 4, characterized in that: in the quick-release outer layer, the filler is one of sucrose, microcrystalline cellulose, starch, mannitol, lactose and pregelatinized starch;
the internal disintegrating agent and the external disintegrating agent are one of crospovidone, sodium carboxymethyl starch, sodium hydroxymethyl starch, sodium carboxymethyl cellulose, calcium carboxymethyl cellulose, croscarmellose sodium and low substituted hydroxypropyl cellulose,
the quick-release lubricant is one of pulvis Talci, magnesium stearate, silica gel micropowder, stearic acid, hydrogenated vegetable oil, and sodium stearyl fumarate.
8. The acarbose sustained release formulation according to claim 7, wherein: the filler is microcrystalline cellulose or lactose; the internal disintegrating agent is crospovidone, and the external disintegrating agent is sodium carboxymethyl starch; the weight ratio of the crospovidone to the sodium carboxymethyl starch is 1: 1-2; the lubricant is magnesium stearate.
9. The acarbose sustained release formulation according to claim 4, wherein: the sustained-release inner core comprises the following components in percentage by mass: 25-50% of acarbose, 20-50% of hydroxypropyl methyl cellulose, 20-40% of ethyl cellulose, 0.1-4.9% of slow-release lubricant and 0-0.5% of slow-release pigment; the slow release lubricant is magnesium stearate or aerosil;
the quick-release outer layer comprises the following components in percentage by mass: 20-50% of acarbose, 30-60% of filler, 5-20% of crospovidone, 5-20% of sodium carboxymethyl starch, 0.1-5% of magnesium stearate and 0-1% of quick-release pigment, wherein the filler is microcrystalline cellulose or lactose.
10. A preparation method of an acarbose sustained-release preparation is characterized by comprising the following steps: the method comprises the following steps:
1) weighing 10-60% of acarbose, 10-60% of a framework material, 10-50% of a release regulator, 0-5% of a slow release lubricant and 0-1% of a slow release pigment in percentage by mass;
2) mixing acarbose, a framework material, a release regulator and a sustained-release pigment, granulating, and mixing the prepared granules with a sustained-release lubricant to obtain a sustained-release inner core material;
3) weighing 10-60% of acarbose, 20-70% of a filler, 3-25% of an internal disintegrating agent, 3-25% of an external disintegrating agent, 0-5% of a quick-release lubricant and 0-2% of a quick-release pigment in percentage by mass;
4) mixing acarbose, filler, internal disintegrating agent and quick-release pigment, granulating, and mixing the obtained granule, external disintegrating agent and quick-release lubricant to obtain quick-release outer layer material;
5) tabletting the sustained-release inner core material obtained in the step 2) to obtain a sustained-release inner core;
6) performing secondary tabletting on the quick-release outer layer material in the step 4) and the slow-release inner core in the step 5), and forming a core-spun tablet by the slow-release inner core and the quick-release outer layer; the acarbose sustained release preparation is obtained.
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| CN201911273829.8A CN110898025A (en) | 2019-12-12 | 2019-12-12 | Acarbose sustained-release preparation and preparation method thereof |
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| CN111991363A (en) * | 2020-09-22 | 2020-11-27 | 北京诺康达医药科技股份有限公司 | Compound sustained-release preparation and preparation method and application thereof |
| CN112080264A (en) * | 2020-08-11 | 2020-12-15 | 中国石油天然气股份有限公司 | Scale inhibition particle and preparation method and application thereof |
| CN114159400A (en) * | 2021-11-22 | 2022-03-11 | 山东省药学科学院 | Favipiravir core-wrapped tablet |
| CN116763752A (en) * | 2023-08-24 | 2023-09-19 | 北京福元医药股份有限公司 | Acarbose tablet and preparation method thereof |
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