Mecobalamin tablet and preparation method thereof

Abstract

The invention discloses a mecobalamin tablet and a preparation method thereof. The mecobalamin tablet comprises a plain tablet and a film coating layer; the mass ratio of the plain tablet to the filmcoating layer is 100:510; the plain tablet comprises the following components in percentage by weight: 0.5% of mecobalamin, 40% to 70% of directly-compressed lactose, 15% to 45% of micro-crystalline fiber, 0 to 15% of corn starch, 0 to 15% of pregelatinized starch, 0 to 2% of stearic acid and 0 to 2% of a lubricant; the film coating layer comprises the following components in percentage by weight:20% to 40% of hydroxypropyl methyl cellulose, 20% to 50% of polyethylene glycol; 10% to 35% of titanium dioxide; 1% to 15% of yellow iron oxide; and 1% to 15% of red iron oxide. The preparation method of the mecobalamin tablet disclosed by the invention is simple; a mecobalamin raw material medicine can be uniformly dispersed in a manner of sieving and mixing the mecobalamin raw material medicineand proper auxiliary materials; the phenomenon of aggregation of the raw material medicine is prevented by a mechanical force, the raw material medicine is fully adsorbed on the auxiliary materials,and then the raw material medicine is mixed with other auxiliary materials step by step to improve the content uniformity; The preparation method disclosed by the invention reduces the stability riskby adopting a powder direct-compression process, and further improves the stability of the preparation by adopting a high-shading-performance film coating material for coating.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a methylcobalamin tablet and a preparation method thereof. Background technique [0002] Methylcobalamin is a vitamin B12 whose structure is a macrocyclic complex centered on cobalt ion. Methylcobalamin is a kind of vitamin B12. There are many forms of vitamin B12. The common ones are cyanocobalamin, methylcobalamin, adenosylcobalamin and hydroxocobalamin; among them, methylcobalamin and adenosylcobalamin are coenzyme types Vitamin B12, only these two types of vitamin B12 can be directly used by the human body, other forms of vitamin B12 need to be converted into two forms of methylcobalamin and adenosylcobalamin in the cells before they can be utilized. [0003] Methylcobalamin is a methylation active preparation of vitamin B12. There is a methyl group on the central cobalt molecule, which can participate in the methyl conversion of substances, so it is easy to transp...

AI Technical Summary

Problems solved by technology

Wetting agents are used in the process, but the active ingredient is a highly soluble drug and the size is small, which will lead to the dissolution of part of the active ingredient; while wet granulation will cause large differences in particle size distribution between particles, and the aqueous solution of the soluble active ingredient in the granules during the drying process Vaporization towards the surface, thereby migrating soluble active ingredients to the surface of the particles, resulting in differences in content between particles

This preparation method is not only cumbersome, but it is easy to cause content differences between particles for small-sized and highly soluble drugs, and the addition of wetting agent increases the risk of methylcobalamin degradation; therefore, small-sized drugs in the marketed preparations usually choose the powder direct mixing process

However, methylcobalamin tablets adopt the method of conventional powder direct pressure and incremental mixing. Even if the methylcobalamin raw material is pulverized and the particle size distribution is controlled, the methylcobalamin raw material still gathers into agglomerates after pulverization, and cannot be mixed with incremental excipients. Uniform dispersion, leading to the inability to effectively control the content uniformity of the final product

[0005] CN102716102B discloses a method for controlling the production of related substances under light, which uses a fluidized bed to coat the methylcobalamin raw material under the LED red light source to isolate the light, thereby improving the light stability of methylcobalamin, but the technology The plan obviously ignores a key indicator. In the fluidized bed granulation process, the methylcobalamin raw material is coated with coating powder and inevitably sticks into granules. When the particle size is too large, the content uniformity of methylcobalamin in the preparation cannot be guaranteed, thereby affecting the effectiveness and safety of the preparation

However, it is obvious that this technical solution can only guarantee the stability of the storage period in the unremoved packaging process, and cannot guarantee the degradation risk that may not be taken in time after the patient unpacks during the production process or during use.

It can be seen that the prior art does not have a simple and reliable method that can solve the content uniformity and stability of methylcobalamin tablets

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