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Methyldigoxin preparation capable of being rapidly absorbed in oral cavity and preparation method of methyldigoxin preparation

A digoxin and oral cavity technology, applied in the field of rapid absorption of digoxin oral preparations and its preparation, to achieve the effects of easy carrying and use, fast blood flow, and convenient clinical medication

Active Publication Date: 2017-01-11
南京斯泰尔医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order to solve the deficiencies of the prior art, the present invention provides a stable and fast-acting medigoxin oral rapid absorption preparation, which fundamentally solves the problem of medigoxin absorption in the tongue mucosa, and has stable quality and good uniformity

Method used

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  • Methyldigoxin preparation capable of being rapidly absorbed in oral cavity and preparation method of methyldigoxin preparation
  • Methyldigoxin preparation capable of being rapidly absorbed in oral cavity and preparation method of methyldigoxin preparation
  • Methyldigoxin preparation capable of being rapidly absorbed in oral cavity and preparation method of methyldigoxin preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Example 1 Medigoxin Sublingual Tablets (1000 Tablets)

[0055] Table 4 Prescription Composition of Medigoxin Sublingual Tablets

[0056] composition prescription Dosage (g) Weight fraction (%) active center Medigoxin 0.1 0.08 polyethylene glycol 6000 35.9 29.9 ethanol Appropriate amount / Compound Absorption System Methyl nonanoate 0.9 0.75 polyethylene glycol 400 2.7 2.25 citric acid Appropriate amount / Absolute ethanol Appropriate amount / Other accessories starch 12 10 lactose 67.2 56 Magnesium stearate 0.6 0.5 talcum powder 0.6 0.5

[0057] Weigh the prescribed amount of medigoxigenin and polyethylene glycol 6000, dissolve them completely in an appropriate amount of ethanol, dry them under normal pressure at a temperature of 45°C, and pulverize the dried solid until the particle size is 150~200μm, the obtained solid dispersion is the active cent...

Embodiment 2

[0058] Example 2 Medigoxin Orally Dissolving Tablets (1000 Tablets)

[0059] Table 5 The composition of the prescription of Medigoxin Oral Instant Dissolving Tablets

[0060] composition prescription Dosage (g) Weight fraction (%) active center Medigoxin 0.1 0.08 polyethylene glycol 6000 48 40.6 ethanol Appropriate amount / Compound Absorption System Methyl nonanoate 2 1.7 Propylene Glycol 4 3.4 Sodium dihydrogen phosphate Appropriate amount / Absolute ethanol Appropriate amount / purified water Appropriate amount / Other accessories Mannitol 19 16.1 lactose 38 32.1 Povidone K30 2.4 2.0 Sodium carboxymethyl starch 3.6 3.0 Magnesium stearate 0.6 0.5 silica 0.6 0.5

[0061] Weigh the prescribed amount of medicine and polyethylene glycol 6000, dissolve the two completely in the solvent, and crush the solid obtained by freeze-drying t...

Embodiment 3

[0062] Example 3 In Vitro Dissolution Study of Medigoxin Oral Rapid Absorption Preparation

[0063] (1) Sample:

[0064] Digoxin tablets (manufacturer: Chugai Pharmaceutical, batch number: 15J010D)

[0065] The Medigoxin sublingual tablet prepared in Example 1, batch number: 160217.

[0066] (2) Test method:

[0067] Take the sample piece, according to the dissolution rate and release rate determination method, respectively use 0.1 mol / L hydrochloric acid solution, water, pH4.5 acetate buffer solution, pH6.8 phosphate buffer solution 100ml as the dissolution medium, and the rotation speed is 1 minute 50 revolutions, operate according to the law, after 15 minutes, take a sample for measurement, and calculate the dissolution amount of each tablet.

[0068] (3) Experimental results:

[0069] Table 6 In vitro dissolution results of methyl digoxin oral rapid absorption preparation and ordinary tablets in different dissolution media

[0070]

[0071] The experimental results...

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Abstract

The invention relates to a methyldigoxin preparation capable of being rapidly absorbed in an oral cavity and a preparation method of the methyldigoxin preparation. The methyldigoxin preparation capable of being rapidly absorbed in the oral cavity comprises an active center, a compound absorption accelerating system and other pharmaceutically acceptable auxiliary materials. By utilizing characteristics that a sublingual mucosa has abundant blood vessels and a rapid blood flow, the methyldigoxin is prepared into the preparation capable of being rapidly absorbed in the oral cavity and is absorbed through the sublingual mucosa, and absorbed medicine directly enters systemic circulation. The technical difficulty that the methyldigoxin has a relatively small oil-water partition coefficient and low membrane permeability, is easy to degrade under an acidic condition and cannot be easily prepared into the preparation capable of being rapidly absorbed in the oral cavity in theory is overcome; the methyldigoxin is developed into the preparation which is high in membrane permeability, can rapidly have effect through the sublingual mucosa and has good compliance.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a medigoxin oral rapid absorption preparation and a preparation method thereof. Background technique [0002] Medigoxin is a derivative in which the β-hydroxyl group at the end of digoxin is substituted by methoxy. Its cardiotonic effect is stronger than that of digoxin. The cardiotonic effect of 0.3 mg of medigoxin is the same as that of 0.5 mg of digoxin. , and has the advantages of good oral absorption, rapid onset of action and high safety, and is clinically applicable to acute and chronic heart failure. Medigoxin is a medium-acting cardiac glycoside drug, which is white or off-white crystalline powder, odorless and bitter. Soluble in acetic acid, slightly soluble in methanol, slightly soluble in ethanol, very slightly soluble in water. [0003] In terms of dosage form design, the current dosage forms of medigoxin mainly include ordinary tablets, injections and drop...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K47/10A61K47/14A61K31/7048A61P9/04
CPCA61K9/006A61K9/2013A61K9/2031A61K31/7048
Inventor 姚静
Owner 南京斯泰尔医药科技有限公司
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