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Methylnaltrexone compound, oral tablet and preparation methods of two

A technology of methylnaltrexone and oral tablets, which is applied in the field of medicine, can solve the problems of low oil-water partition coefficient and low absorption of methylnaltrexone bromide, achieve good oral absorption and improve fat solubility

Active Publication Date: 2015-01-14
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Because methylnaltrexone bromide has strong hydrophilicity, it is easily soluble in aqueous solution, and the oil-water partition coefficient is too low, which leads to little absorption of methylnaltrexone bromide in the gastrointestinal tract

Method used

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  • Methylnaltrexone compound, oral tablet and preparation methods of two
  • Methylnaltrexone compound, oral tablet and preparation methods of two
  • Methylnaltrexone compound, oral tablet and preparation methods of two

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] This example is used to illustrate brominated methylnaltrexone phospholipid complex and its preparation method.

[0067] Weigh 100mg of methylnaltrexone bromide, dissolve it in 50ml of methanol at 25°C, add hydrogenated soybean lecithin (HSPC) equivalent to 1 times the molar amount of bromide methylnaltrexone, and disperse evenly. After oscillating at a constant temperature for 5 hours under the same conditions, stop the reaction to obtain a colorless to light yellow clear solution, then evaporate the methanol under reduced pressure at 50°C, dry it in vacuum at 50°C for 48 hours, crush the dried product and sieve it to obtain methyl bromide Naltrexone Phospholipid Complex.

[0068] Take brominated methylnaltrexone, hydrogenated soybean lecithin, brominated methylnaltrexone phospholipid complex, and a physical mixture of brominated methylnaltrexone and hydrogenated soybean lecithin (mixed at a molar ratio of 1:1) Carried out X-ray diffraction analysis, the results are a...

Embodiment 2

[0071] This example is used to illustrate brominated methylnaltrexone phospholipid complex and its preparation method.

[0072] Weigh 50mg of methylnaltrexone bromide, dissolve it in 30ml of ethanol at 30°C, add HSPC equivalent to 2 times the molar amount of bromide methylnaltrexone, disperse evenly, shake at 30°C for 3 hours , to stop the reaction, to obtain a colorless to light yellow clear solution, then evaporate the methanol under reduced pressure at 45°C, dry in vacuum at 50°C for 40h, crush and sieve the dried product to obtain brominated methylnaltrexone phospholipid complex .

Embodiment 3

[0074] This example is used to illustrate brominated methylnaltrexone phospholipid complex and its preparation method.

[0075] Weigh 200mg of methylnaltrexone bromide, dissolve it in 30ml of ethanol at 40°C, add DSPG equivalent to 0.5 times the molar amount of methylnaltrexone bromide, disperse evenly, shake at 40°C for 2 hours , to stop the reaction, to obtain a colorless to pale yellow clear solution, then evaporate methanol under reduced pressure at 55°C, dry in vacuum at 50°C for 36h, crush and sieve the dried product to obtain brominated methylnaltrexone phospholipid complex .

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PUM

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Abstract

The invention provides a methylnaltrexone compound. The compound comprises methylnaltrexone or pharmaceutically-acceptable salts and phosphatide, wherein the molar ratio of methylnaltrexone or the pharmaceutically-acceptable salts to phosphatide is 1:0.5-2, and the compound is prepared by dissolving methylnaltrexone or the pharmaceutically-acceptable salts and phosphatide in a solvent and performing evaporation to remove the solvent. The invention also provides a methylnaltrexone oral tablet. The oral table contains the above methylnaltrexone compound and additives, and the additives are one or more selected from fillers, disintegrating agents, adhesives, chelating agents, stabilizing agents and lubricants. A preparation method of the oral tablet comprises the following steps: mixing the methylnaltrexone compound with the additives and tabletting to prepare the methylnaltrexone oral tablet.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a methylnaltrexone complex, an oral tablet and a preparation method thereof. Background technique [0002] Opioids are widely used to alleviate the suffering of patients with advanced cancer and other terminal illnesses. Opioids are narcotic drugs that activate opioid receptors in the central nervous system to relieve pain. However, opioids can also interact with receptors outside the central nervous system, leading to side effects including constipation, nausea, emesis, urinary retention, and severe itching. Even more noteworthy is the effect of opioids on the gastrointestinal tract. Among them, opioids inhibit gastric emptying and intestinal propulsive motor activity, thereby reducing the rate of intestinal transit, which can lead to constipation. The efficacy of opioids for pain is often limited due to the side effects caused by them. [0003] The chemical nam...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/28A61K31/485A61K47/24A61P1/10
Inventor 靳文仙孙歆慧李艳贞邹美香王成港刘钫阎卉刘欢郭振华
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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