CN112121024A - Mecobalamin orally disintegrating tablet and preparation process thereof - Google Patents
Mecobalamin orally disintegrating tablet and preparation process thereof Download PDFInfo
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- CN112121024A CN112121024A CN202011209370.8A CN202011209370A CN112121024A CN 112121024 A CN112121024 A CN 112121024A CN 202011209370 A CN202011209370 A CN 202011209370A CN 112121024 A CN112121024 A CN 112121024A
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- Prior art keywords
- mecobalamin
- orally disintegrating
- disintegrating tablet
- parts
- glidant
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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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
-
- 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
- A61K31/7135—Compounds containing heavy metals
- A61K31/714—Cobalamins, e.g. cyanocobalamin, i.e. vitamin B12
-
- 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
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
-
- 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
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
Abstract
The invention provides a mecobalamin orally disintegrating tablet and a preparation process thereof, wherein the tablet comprises the following components: mecobalamin, excipient, disintegrant, glidant, flavoring agent, binder and magnesium stearate. The mecobalamin orally disintegrating tablet prepared by the preparation process provided by the invention can be rapidly disintegrated in the oral cavity, the medicine is rapidly dissolved, the effect is fast, the absorption is more rapid, the bioavailability is higher, and the tablet is particularly suitable for the old, the young and patients who have difficulty in swallowing solid tablets.
Description
Technical Field
The invention relates to the technical field of medicinal chemistry, in particular to a mecobalamin orally disintegrating tablet and a preparation process thereof.
Background
Methylcobalamin (methylcobalalamin), chemical name: cobalt-alpha- [ alpha-5, 6-dimethylbenzimidazolyl ] -cobalt-beta-methylcobalaminide, formula: C63H91CoN13O14P, molecular weight: 1344.38, it is a deep red crystal or crystalline powder, and has no odor and taste. Mecobalamin is a coenzyme type vitamin B12 developed by Euonymus japonicus K.K., is mainly used for treating peripheral nerve diseases and megaloblastic anemia caused by vitamin B12 deficiency in medicine, has good conductivity on nerve tissues compared with other coenzyme type vitamin B12 medicines, is easy to enter neuron organelles, promotes the synthesis of nucleic acid, protein and nerve myelin in nerve cells, and repairs damaged peripheral nerves by stimulating the regeneration of axons and sheaths, and is a relatively effective medicine for treating peripheral nerve diseases. Mecobalamin in the prior art is usually a solid tablet, has slow dissolution and effect, contains more impurities in the medicine and has poor stability.
Disclosure of Invention
The invention aims to disclose a mecobalamin orally disintegrating tablet which can be rapidly disintegrated in oral cavity, has the advantages of fast drug dissolution, fast effect, quicker absorption and higher bioavailability, and is especially suitable for the old, the young and patients who have difficulty in swallowing solid tablets.
In order to realize the aim, the invention provides a mecobalamin orally disintegrating tablet, which comprises the following components: mecobalamin, excipient, disintegrant, glidant, flavoring agent, binder and magnesium stearate.
In some embodiments, the weight parts of the components are 0.3-0.6 part of mecobalamin, 60-80 parts of excipient, 20-30 parts of disintegrant, 4-6 parts of glidant, 3-6 parts of flavoring agent, 51-103 parts of adhesive and 1-1.5 parts of magnesium stearate.
In some embodiments, the excipient is mannitol.
In some embodiments, the disintegrant is sodium carboxymethyl starch and low substituted-hydroxypropyl cellulose.
In some embodiments, the glidant is colloidal silicon dioxide.
In some embodiments, the flavoring agent is aspartame.
In some embodiments, the binder is povidone and a 50% ethanol solution.
The second purpose of the invention is to disclose a preparation process of mecobalamin orally disintegrating tablets, which is carried out under the dark condition that the illumination intensity is lower than 5LX, and the dry moisture of the product is reduced to be less than 2 percent, thereby effectively preventing the growth of related substances in the product and improving the stability of the product.
In order to achieve the purpose, the invention provides a preparation process of a mecobalamin orally disintegrating tablet, which comprises the following steps and is carried out under the condition of keeping out light with the illumination intensity lower than 5 LX:
the method comprises the following steps: sieving mecobalamin, excipient, disintegrant, glidant and correctant respectively;
step two: uniformly mixing mecobalamin, an excipient, a disintegrating agent, a glidant and a flavoring agent in a mixer;
step three: adding adhesive into the mixture to prepare wet granules in a wet granulator;
step four: drying the wet granules to reduce the dry water content to below 2%;
step five: sieving the dried granules with a rocking granulator, granulating, mixing the prepared granules with magnesium stearate, and tabletting to obtain mecobalamin orally disintegrating tablet.
In some embodiments, step four: the wet granules were dried in a fluid bed dryer at 60 ℃ and the moisture was measured after 1 hour of drying.
Compared with the prior art, the invention has the beneficial effects that: the mecobalamin orally disintegrating tablet prepared by the preparation process provided by the invention can be rapidly disintegrated in the oral cavity, the medicine is rapidly dissolved, the effect is fast, the absorption is more rapid, the bioavailability is higher, and the tablet is particularly suitable for the old, the young and patients who have difficulty in swallowing solid tablets.
Detailed Description
The present invention is described in detail below with reference to various embodiments, but it should be understood that these embodiments are not intended to limit the present invention, and those skilled in the art should be able to make modifications and substitutions on the functions, methods, or structures of these embodiments without departing from the scope of the present invention.
The embodiment discloses a mecobalamin orally disintegrating tablet, which comprises the following components: mecobalamin, excipient, disintegrant, glidant, flavoring agent, binder and magnesium stearate.
The weight portions of the components are 0.3 to 0.6 portion of mecobalamin, 60 to 80 portions of excipient, 20 to 30 portions of disintegrant, 4 to 6 portions of glidant, 3 to 6 portions of flavoring agent, 51 to 103 portions of adhesive and 1 to 1.5 portions of magnesium stearate.
The excipient is mannitol. The disintegrant is sodium carboxymethyl starch and low-substituted-hydroxypropyl cellulose. The glidant is colloidal silicon dioxide. The flavoring agent is aspartame. The binder is povidone and 50% ethanol solution.
Preparation of 1000 tablets of orally disintegrating tablets requires 0.5g of mecobalamin, 60 to 80g and preferably 70g of mannitol, 5 to 10g and preferably 8g of sodium carboxymethyl starch, 15 to 20g and preferably 18g of low-substituted-hydroxypropylcellulose, 4 to 6g and preferably 5g of colloidal silicon dioxide, 1 to 3g and preferably 2g of povidone, 5g of aspartame, 1 to 1.5g and preferably 1.2g of magnesium stearate, 50 to 100g and preferably 80g of 50% ethanol solution.
The embodiment also discloses a preparation process of the mecobalamin orally disintegrating tablet, which comprises the following steps and is carried out under the light-shielding condition that the illumination intensity is lower than 5 LX:
the method comprises the following steps: sieving mecobalamin, excipient, disintegrant, glidant, and correctant respectively.
Specifically, mannitol and low-substituted-hydroxypropyl cellulose are respectively sieved by a 40-mesh sieve, carboxymethyl starch sodium, colloidal silicon dioxide and aspartame are manually premixed, then crushed, granulated and sieved by a 80-mesh sieve, and mecobalamin, the sieved carboxymethyl starch sodium, colloidal silicon dioxide and aspartame are sieved by a 60-mesh sieve.
Step two: uniformly mixing mecobalamin, mannitol, low-substituted-hydroxypropyl cellulose, sodium carboxymethyl starch, colloidal silicon dioxide and aspartame in a mixer to obtain intermediate mixed powder;
step three: adding polyvidone and 50% ethanol solution, and making into wet granule in wet granulator;
step four: drying the wet granules in a fluidized bed dryer at 60 ℃, measuring the moisture after drying for 1 hour, reducing the dry moisture to below 2 percent, and improving the stability of the product to obtain dry granules;
step five: sieving the dried granules with a 20-mesh sieve by a swing granulator, granulating, mixing the prepared granules with magnesium stearate, measuring the content of the intermediate granules, and tabletting to obtain the mecobalamin orally disintegrating tablet, namely the plain tablet.
Testing and result analysis:
respectively filling the intermediate mixed powder, the dried granules and the plain tablets into a large-scale weighing bottle, flatly laying the powder with the thickness of less than 5mm, placing the powder in a dark place (the illumination intensity is less than 5LX), near red light (the illumination intensity is more than 5LX) and under white light for sampling and inspecting related substances at 2h, 8h and 24h, wherein the detection results are as follows:
TABLE 1
And (4) analyzing results: from Table 1, it can be seen that the substances of the samples have a tendency to grow under white light and near red light (with the illuminance of more than 5LX), and the substances do not grow when the samples are operated under the condition of avoiding light (with the illuminance of less than 5LX), so that the preparation process can increase the stability of the products when the samples are operated under the condition of avoiding light (with the illuminance of less than 5 LX).
Secondly, after the wet granules are dried on the fluidized bed, the moisture content is respectively controlled to be 1.97% (191118 batches) and 2.96% (191117 batches), and the obtained dried granules are respectively tableted to be used for detecting related substances, and the detection results are as follows:
TABLE 2
TABLE 3
TABLE 4
And (4) analyzing results: as can be seen from tables 2, 3 and 4, the substances involved in the sample with 2.96% moisture (191117 lot) all showed a tendency to increase, and the substances involved in the sample with 1.97% moisture (191118 lot) did not increase, so that the sample with 1.97% moisture (191118 lot) showed better stability than the sample with 2.96% moisture (191117 lot).
The above-listed detailed description is only a specific description of a possible embodiment of the present invention, and they are not intended to limit the scope of the present invention, and equivalent embodiments or modifications made without departing from the technical spirit of the present invention should be included in the scope of the present invention.
Furthermore, it should be understood that although the present description refers to embodiments, not every embodiment may contain only a single embodiment, and such description is for clarity only, and those skilled in the art should integrate the description, and the embodiments may be combined as appropriate to form other embodiments understood by those skilled in the art.
Claims (9)
1. A mecobalamin orally disintegrating tablet is characterized by comprising the following components: mecobalamin, excipient, disintegrant, glidant, flavoring agent, binder and magnesium stearate.
2. The mecobalamin orally disintegrating tablet of claim 1, wherein the components comprise, by weight, 0.3-0.6 parts of mecobalamin, 60-80 parts of an excipient, 20-30 parts of a disintegrant, 4-6 parts of a glidant, 3-6 parts of a flavoring agent, 51-103 parts of an adhesive and 1-1.5 parts of magnesium stearate.
3. The mecobalamin orally disintegrating tablet of claim 2, wherein said excipient is mannitol.
4. The mecobalamin orally disintegrating tablet of claim 2, wherein said disintegrant is sodium carboxymethyl starch and low substituted-hydroxypropyl cellulose.
5. The mecobalamin orally disintegrating tablet of claim 2, wherein said glidant is colloidal silicon dioxide.
6. The mecobalamin orally disintegrating tablet of claim 2, wherein said flavoring agent is aspartame.
7. The mecobalamin orally disintegrating tablet of claim 2, wherein said binder is povidone and 50% ethanol solution.
8. The process for preparing a mecobalamin orally disintegrating tablet according to any one of claims 1 to 7, comprising the steps of:
the method comprises the following steps: sieving mecobalamin, excipient, disintegrant, glidant and correctant respectively;
step two: uniformly mixing mecobalamin, an excipient, a disintegrating agent, a glidant and a flavoring agent in a mixer;
step three: adding adhesive into the mixture to prepare wet granules in a wet granulator;
step four: drying the wet granules to reduce the dry water content to below 2%;
step five: sieving the dried granules with a rocking granulator, granulating, mixing the prepared granules with magnesium stearate, and tabletting to obtain mecobalamin orally disintegrating tablet.
9. The process for preparing a mecobalamin orally disintegrating tablet according to claim 8, wherein the fourth step: the wet granules were dried in a fluid bed dryer at 60 ℃ and the moisture was measured after 1 hour of drying.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202011209370.8A CN112121024A (en) | 2020-11-03 | 2020-11-03 | Mecobalamin orally disintegrating tablet and preparation process thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202011209370.8A CN112121024A (en) | 2020-11-03 | 2020-11-03 | Mecobalamin orally disintegrating tablet and preparation process thereof |
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| Publication Number | Publication Date |
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| CN112121024A true CN112121024A (en) | 2020-12-25 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN202011209370.8A Pending CN112121024A (en) | 2020-11-03 | 2020-11-03 | Mecobalamin orally disintegrating tablet and preparation process thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114515278A (en) * | 2022-03-08 | 2022-05-20 | 北京斯利安药业有限公司 | Mecobalamin oral sustained-release film agent and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1742748A (en) * | 2005-09-29 | 2006-03-08 | 周卓和 | Methy cobalamine dispersion tablet and preparing method |
| EP2384742A1 (en) * | 2010-05-03 | 2011-11-09 | The Jordanian Pharmaceutical Manufacturing Co. | Pharmaceutical excipient, method for its preparation and use thereof |
| CN104784049A (en) * | 2014-01-17 | 2015-07-22 | 南京瑞尔医药有限公司 | Preparation method for mecobalamin tablets |
-
2020
- 2020-11-03 CN CN202011209370.8A patent/CN112121024A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1742748A (en) * | 2005-09-29 | 2006-03-08 | 周卓和 | Methy cobalamine dispersion tablet and preparing method |
| EP2384742A1 (en) * | 2010-05-03 | 2011-11-09 | The Jordanian Pharmaceutical Manufacturing Co. | Pharmaceutical excipient, method for its preparation and use thereof |
| CN104784049A (en) * | 2014-01-17 | 2015-07-22 | 南京瑞尔医药有限公司 | Preparation method for mecobalamin tablets |
Non-Patent Citations (1)
| Title |
|---|
| 国家药典委员会编: "《中华人民共和国药典二部注释》", 31 October 2019, 中国医药科技出版社 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114515278A (en) * | 2022-03-08 | 2022-05-20 | 北京斯利安药业有限公司 | Mecobalamin oral sustained-release film agent and preparation method thereof |
| CN114515278B (en) * | 2022-03-08 | 2023-11-14 | 北京斯利安药业有限公司 | Mecobalamin oral sustained-release film and preparation method thereof |
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| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| CB02 | Change of applicant information |
Address after: 219 Furong Zhongsi Road, Xishan Economic and Technological Development Zone, Wuxi City, Jiangsu Province, 214000 Applicant after: Zhuohe Pharmaceutical Group Co.,Ltd. Address before: 219 Furong Zhongsi Road, Xishan Economic and Technological Development Zone, Wuxi City, Jiangsu Province, 214000 Applicant before: Zhuohe Pharmaceutical Group Co.,Ltd. |
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| CB02 | Change of applicant information | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20201225 |
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| RJ01 | Rejection of invention patent application after publication |