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Colchicines gastric floating sustained-release tablet and method for preparing same

A technology of colchicine and gastric floating, which is applied in the direction of medical formula, medical preparations containing active ingredients, etc., and can solve the problem of high toxicity of colchicine, small gout therapeutic index, and bioavailability Low-level problems, to achieve the effect of improving bioavailability, reducing the number of medications, and stabilizing blood drug concentration

Inactive Publication Date: 2009-09-23
普尔药物科技开发(深圳)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] But there is such shortcoming in prior art: promptly the toxicity of colchicine is bigger, and the therapeutic index that is clinically used for the treatment of gout is little (therapeutic window plasma drug concentration is 0.5~3ng / ml)
In order to overcome the disadvantages of common tablets and capsules with large toxic and side effects, it is necessary to make them into sustained and controlled release preparations; the present invention discloses gastric retention type sustained release preparations, which solves the problems of narrow oral absorption window and low bioavailability. To achieve the purpose of controlling drug release and obtaining a more stable blood drug concentration, reducing gastrointestinal adverse reactions, improving drug bioavailability, and facilitating drug use

Method used

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  • Colchicines gastric floating sustained-release tablet and method for preparing same
  • Colchicines gastric floating sustained-release tablet and method for preparing same
  • Colchicines gastric floating sustained-release tablet and method for preparing same

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0074] The preparation process of colchicine gastric floating sustained-release tablets is detailed in figure 1 shown.

[0075] With reference to relevant bibliographical reports and preliminary experimental results, the present invention adopts similarity factor method (f 2 ) as an evaluation index to investigate the effects of prescription components and preparation process on the release behavior of colchicine matrix controlled-release tablets.

[0076] The basic prescriptions used in the experiment are as follows:

[0077] Colchicine

example 1

[0079] During the experiment, unless otherwise specified, the fixed process parameters were as follows: the raw and auxiliary materials were mixed evenly by the method of equal increment, and the powder was directly compressed into tablets. The die of the tablet press is shallow concave (Φ=7mm); the hardness of the tablet core is 35-45N, and the tablet weight is 150mg±2%.

[0080] In vitro drug release conditions: small cup method, with 200mL of 0.1mol L -1 HCl is the drug release medium, the paddle speed is 100r min -1 , medium temperature 37 ℃.

[0081] 2.1 Prescription single factor investigation

[0082] 2.1.1 The effect of the amount of effervescent agent on drug release behavior

[0083] Fix the dosage of other components in the prescription and the dosage ratio of effervescent agent sodium bicarbonate and citric acid, adjust the ratio of effervescent agent in the prescription, and replace it with the same amount of microcrystalline cellulose, and investigate the eff...

Embodiment 1

[0145] Preparation:

[0146] a. Mix colchicine with polyoxyethylene WSR303, sodium bicarbonate, Eudragit L100-55, microcrystalline cellulose, citric acid, red iron oxide, and magnesium stearate in equal increments;

[0147] b. Carry out direct powder compression, the die of the tablet machine is shallow concave, Φ=7mm; tablet core hardness 35-45N, tablet weight 150mg±2%.

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Abstract

The invention discloses a colchicines gastric floating sustained-release tablet, which comprises active components of colchicines and pharmaceutic adjuvant according to the weight ratio of 1:24-1,999, wherein the pharmaceutic adjuvant comprises a hydrophilic gel framework material, a effervescing agent, a floating assistant material, a filler, a pH value regulator and a lubricant. The colchicines gastric floating sustained-release tablet can swell quickly in gastric juice or a similar gastric juice medium and can float on the gastric juice for at least 4 hours. The invention also relates to a method for preparing the colchicines gastric floating sustained-release tablet. The colchicines gastric floating sustained-release tablet can reach the effective blood-drug concentration quickly after being taken and then release drugs slowly, and can maintain the balanced blood-drug concentration so as to reduce the dose times, relieve the toxic side effect and improve the bioavailability.

Description

technical field [0001] The invention relates to a medicine containing colchicine and a preparation method thereof, in particular to a colchicine gastric floating preparation and a preparation method thereof. Background technique [0002] Colchicine is a tropolone alkaloid, which was first isolated from the corm of Colchicum autumnale L., a plant of the Liliaceae family in Europe. Colchicine has significant biological activity, mainly anti-inflammatory, anti-tumor, anti-fibrosis and other pharmacological effects. Recurrent pericarditis, Bechet's disease, etc. also have good curative effect. Among them, colchicine is a specific drug for the treatment of acute attacks of gout. It was used to treat the attacks of gout as early as 1763, and it is still the main drug for treatment. [0003] However, the prior art has the disadvantages that colchicine is highly toxic and has a small therapeutic index for clinical treatment of gout (the therapeutic window blood drug concentration ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/165A61K47/32A61K47/34A61K47/38A61P19/06A61P35/00A61K47/10
Inventor 王文苹刘姹杨大坚陈新滋
Owner 普尔药物科技开发(深圳)有限公司
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