Naloxone monopreparation and multi-layer tablet

A multi-layer tablet and naloxone technology, applied in pill delivery, medical preparations of non-active ingredients, digestive system, etc., can solve problems such as impossible to obtain therapeutic effect

Inactive Publication Date: 2017-09-26
德威洛克制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This formulation relies on the ambient pH of the GI tract for targeted release of naloxone, providing local and uniform supply of naloxone across the entire GI tract, making optimal therapeutic effect impossible

Method used

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  • Naloxone monopreparation and multi-layer tablet
  • Naloxone monopreparation and multi-layer tablet
  • Naloxone monopreparation and multi-layer tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0121] Tablets of the following compositions are manufactured:

[0122]

[0123] The components naloxone hydrochloride and glycerol-2-behenate were screened and mixed with each other. To obtain the final mixture, the colloidal silicon dioxide in sieved form is mixed first, and then the magnesium stearate. The mixture thus obtained is compressed into tablets by means of a conventional tablet press.

Embodiment 2

[0125] Tablets of the following compositions are manufactured similarly to Example 1:

[0126]

[0127]

[0128] SR consists of 80% by weight polyvinyl acetate, 19% by weight polyvinylpyrrolidone, 0.8% by weight sodium lauryl sulfate and 0.2% by weight colloidal silicon dioxide.

Embodiment 3

[0130] Coated bilayer tablets of the following compositions were manufactured:

[0131]

[0132]

[0133] The component of the naloxone layer, namely naloxone hydrochloride, SR, glyceryl-2-behenate, colloidal silicon dioxide and magnesium stearate were sieved and mixed with each other to form a first powder mixture. The other components of the placebo layer, ie, sugar granules, hypromellose, microcrystalline cellulose, colloidal silicon dioxide, and magnesium stearate, were sieved and mixed with each other to form a second powder mixture.

[0134] The first and second blends are compressed into bilayer tablet cores by means of a conventional bilayer tablet press. The bilayer tablet core thus obtained is Coating is carried out in a coater at a temperature between 30°C and 50°C, so that bilayer tablets are obtained.

[0135] release curve

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PUM

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Abstract

The present invention relates to a solid, oral pharmaceutical composition comprising naloxone, or a pharmaceutically acceptable salt thereof as the active ingredient, the composition having a delayed release of said active ingredient. The composition can comprise a matrix containing glycerol di-behenic acid esters as matrix formers, with a mass ratio of naloxone to matrix former(s) of between 1:1 and 1:10, whereby the active ingredient naloxone has a delayed release. According to the invention, in order to provide a composition suitable for a dosage covering at least twelve hours for treating opioid-induced obstipation, the composition has an in-vitro release rate of the active ingredient, measured using a vane stirrer method according to Eur. Ph. at 75 U/min in 500 ml of 0.1 N hydrochloric acid at 37 DEG C, of 0 % to 75 % in 2 h, 3 % to 95 % in 4 h, 20 % to 100 % in 10 h, 30 % to 100 % in 16 h, 50 % to 100 % in 24 h and more than 80 % in 36 h, said composition having an IC50/Cmax value of at least 40. Preferably, the composition comprises a value for tmax (naloxone) / tmax (naloxone-3-glucuronoid) of at least 5. In an alternative embodiment, the composition can take the form of a multi-layer tablet.

Description

Background technique [0001] Constipation is a significant side effect of opioid analgesic regimens. It is considered to be one of the most common side effects and an undesirable complication especially in long-term opioid treatment, occurring in about 85% of patients. In contrast to other opioid-induced side effects, opioid-induced constipation is a chronic condition that does not lose intensity over the course of treatment. The effect of opioids on bowel motility may be based on the binding of opioids to opioid receptors in the gastrointestinal tract, where they occur in greater density. [0002] Corresponding treatments are aimed at eliminating this peripheral side effect of opiates. Because opioid-induced constipation is uncomfortable and can be painful, it often leads to discontinuation of opioid therapy, and thus compromises the therapeutic effect of opioids. One can conclude from opioid-induced constipation that opioids directly and locally affect the entire intestine...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/24A61K47/14A61K31/485A61P25/04
CPCA61K9/0002A61K9/2013A61K9/2086A61K9/209A61K31/485A61K2300/00A61P1/10A61P25/04
Inventor 伊莲娜·雷尔奥拉夫·蒙得辛格尔伊莎贝尔·戈尔菲耶尔西尔维亚·雅各布奥利尔·鲁施
Owner 德威洛克制药有限公司
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