Solid preparation and preparation method thereof

A technology for solid preparations and adhesives, which is used in pharmaceutical formulations, medical preparations with inactive ingredients, and inorganic inactive ingredients. Wet stability of formulations, etc.

Active Publication Date: 2011-03-23
北京中关科城科技股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the solid preparations containing these substances prepared by conventional methods, some of the above-mentioned shortcomings also often exist between the particles, such as the preparations often have more pores or gaps communicating with the outside world (the mechanical strength is not enough in the process of production, transportation, etc.) Also produce pores or gaps), moisture can enter the interior of the preparation through the pores or gaps to connect with the environment, make the moisture-unstable substances absorb moisture or lose water, and then cause the moisture-unstable substances inside the preparation to undergo physical and / or chemical changes, Affect the wet stability of the formulation

Method used

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  • Solid preparation and preparation method thereof
  • Solid preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0100] Embodiment 1 Nystatin vaginal effervescent tablet

[0101] Component mg / tablet

[0102] Nystatin (anhydrous substance) 33.3 (100,000u)

[0103] Isomalt GalenIQ 721 320

[0104] Polyethylene glycol 6000 96

[0105] Croscarmellose Sodium 17.7

[0106] Aspartan 1

[0107] Sodium bicarbonate 8.4

[0108] Monosodium citrate 19.6

[0109] Silica 4

[0110]

[0111] Total 500

[0112] Nystatin, Isomalt GalenIQ 721, polyethylene glycol 6000, and croscarmellose were fully dried (the residual moisture in the raw and auxiliary materials does not affect the stability of the preparation and the detection of moisture-unstable substances, the same below). Grind plain sodium, aspartame, sodium bicarbonate, monosodium citrate, and silicon dioxide separately, pass through a 60-mesh sieve, and mix uniformly by equal-volume incremental method. Pack 500 mg of the above-mentioned mixture into each vesicle in the punched packaging film m...

example 1

[0114] Reference Example 1: Replace the Isomalt GalenIQ 721 and two-thirds of the polyethylene glycol 6000 in the prescription with the same weight of α-lactose and microcrystalline cellulose, and prepare the reference product 1 by the above method.

example 2

[0115] Reference example 2: replace two-thirds of Isomalt GalenIQ 721 and four-fifths of polyethylene glycol 6000 in the prescription with α-lactose and microcrystalline cellulose of the same weight, and use the above method Preparation of reference product 2.

[0116] According to the method described in the instructions, detect the maximum change after the sodium bicarbonate in the above-mentioned embodiment and the reference example sampling sample react with monosodium citrate under the effect of moisture under the condition of relative humidity 75% and temperature 25 ℃ Amount (take a sample after a period of time during which the original content of the moisture-unstable substance therein can be reduced or changed by at least about 35% during the unhealed treatment, so that the sampling is repeated for a total of not less than 5 times, and the maximum amount of the moisture-labile substance The last 2 consecutive fluctuation range ratios of the amount of wet action variat...

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Abstract

The invention discloses a solid preparation. The solid preparation comprises a wet unstable substance, an enough amount of non-hygroscopic sugar alcohol (I) at the normal temperature, an enough amount of hydrophilic non-hygroscopic melt adhesive at the normal temperature and / or pharmaceutically acceptable additive and / or active component, wherein, the melting point of the melt adhesive is lower than that of the sugar alcohol (I); the melt adhesive melts, solidifies and adheres to the sugar alcohol (I) to form a bridging substance which leads the solid preparation to be completely or basicallycompletely insulated from the external environment. The invention also discloses a preparation method of the solid preparation; and the solid preparation has extremely high wet stability, higher hydrophilism, better disintegrating or releasing performance, and better mechanical performance, and insulates the external environment in a high degree, can insulate bad flavor or taste, and can be produced by a fully dry method.

Description

technical field [0001] The invention relates to a solid preparation. More specifically, the present invention relates to a solid formulation that is highly stable to humidity, has good mechanical properties and is hydrophilic. The invention also relates to a preparation method of the solid preparation. Background of the invention [0002] Some substances, including active ingredients, are easy to absorb moisture in the air, the surface is wetted, physical changes such as decomposing or agglomeration occur, and even chemical reactions such as discoloration and decomposition occur. This phenomenon is called hygroscopicity. There are also some active ingredients that are just the opposite, losing moisture themselves and showing weathering (sex). For example, some pharmaceutical powders with poor chemical stability, such as aspirin, penicillin G sodium (or potassium), acetylcholine chloride, tetracycline hydrochloride, etc., can decompose after the surface absorbs water; calc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/02A61K47/04A61K47/10A61K47/12A61K47/16A61K47/20A61K47/22A61K47/26A61K47/32A61K47/34A61K47/36A61K47/38A61K47/40A61K47/42
Inventor 钟术光
Owner 北京中关科城科技股份有限公司
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