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Ion exchange compositions with water-soluble mucosal adhesive polymers

A polymer, water-soluble technology, applied in the direction of organic active ingredients, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of low bioavailability of nicotine

Pending Publication Date: 2022-05-27
FERTIN PHARMA AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although this composition may generally cause fewer adverse effects, such as throat irritation, due to the prolonged release profile, a large amount of nicotine is swallowed by the user, and thus the bioavailability of the nicotine present in the formulation may be relatively low

Method used

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  • Ion exchange compositions with water-soluble mucosal adhesive polymers
  • Ion exchange compositions with water-soluble mucosal adhesive polymers
  • Ion exchange compositions with water-soluble mucosal adhesive polymers

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0196] Preparation of ion exchange composition particles with brilliant blue color

[0197] Purified water (10 ml) was placed in a plastic beaker with a screw cap. The water-soluble anionic mucoadhesive polymer was slowly added to the water and the plastic beaker was closed with a lid, then the dispersion was stirred at about 100°C for 6 hours. 1.5 ml of 1% Brilliant Blue stock solution was added and the gel mixture was stirred vigorously at 60°C to 80°C for 1 hour. Precipitation was performed by pipetting 2 ml of the polymer gel into 30 ml of isopropyl alcohol (IPA) with a positive displacement pipette under stirring. Discard the supernatant. The pellet was washed with fresh IPA until no solvent color was observed. Residual water and IPA were evaporated from the precipitate until the structure of the product was essentially solid. The product is comminuted to a given average particle size.

Embodiment 2

[0199] Preparation of ion exchange composition particles with brilliant blue color

[0200] Purified water (10 ml) was placed in a plastic beaker with a screw cap. The water-soluble anionic mucoadhesive polymer was slowly added to the water and the plastic beaker was closed with a lid, then the dispersion was stirred at about 100°C for 6 hours. 1.5 ml of 1% Brilliant Blue stock solution was added and the gel mixture was stirred vigorously at 60°C to 80°C for 1 hour. Precipitation was performed by pipetting 2 ml of the polymer gel into 30 ml of acetone with a positive displacement pipette under stirring. Discard the supernatant. The precipitate was washed with fresh acetone until no solvent color was observed. Residual water and acetone were evaporated from the precipitate until the structure of the product was essentially solid. The product is comminuted to a given average particle size.

Embodiment 3

[0202] Preparation of ion exchange composition particles with brilliant blue color

[0203] Isopropanol (30ml) was placed in a plastic beaker with a screw cap. 3 ml of brilliant blue aqueous solution (1%) was added. The water-soluble anionic mucoadhesive polymer was slowly added to the mixture, the plastic beaker was closed with a lid, and the dispersion was stirred for 1 hour. After a 1 hour standing time to allow the powder to settle, the supernatant was decanted and discarded. Evaporation of IPA from the residue gave a fine colored polymer powder.

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Abstract

The present invention relates to an oral tablet for transoral mucosal delivery of a bioactive compound, the tablet comprising: a sugar alcohol composition comprising one or more sugar alcohol particles in an amount of at least 20% by weight of the tablet; an ion exchange composition comprising a plurality of particles of at least one water-soluble anionic mucoadhesive polymer loaded with a cationic bioactive compound.

Description

technical field [0001] The present invention relates to the field of ion exchange compositions for loading with cationic bioactive compounds. In particular, the present invention relates to ion exchange compositions based on particles of water-soluble anionic mucoadhesive polymers. Background technique [0002] Ion exchange resins have traditionally been used in the field of oral delivery to achieve controlled release and delivery of bioactive compounds such as nicotine. The purpose of the ion exchange resin is to stabilize the bioactive compound and at the same time ensure a controlled release of the bioactive compound (eg nicotine) after oral administration. Adverse effects of the bioactive compound, such as throat irritation, can be mitigated in this way, while the bioactive compound can be delivered to the user in need thereof over an extended period of time for enhanced craving relief. [0003] Nicotine is a well known and highly characterized alkaloid which can be is...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/26A61K47/36A61K47/32A61K47/38A61K31/465
CPCA61K9/0056A61K9/006A61K9/2018A61K9/2027A61K9/205A61K9/2054A61K9/2081A61K31/465A61K9/5084A61K9/2086
Inventor 肯特·阿尔宾·涅尔森
Owner FERTIN PHARMA AS