Eureka AIR delivers breakthrough ideas for toughest innovation challenges, trusted by R&D personnel around the world.

Taste-masked pharmaceutical compositions with gastrosoluble pore-formers

a technology of poreformers and pharmaceutical compositions, which is applied in the direction of microcapsules, capsule delivery, organic active ingredients, etc., can solve the problems of poor taste, negative impact on the efficacy of treatment, and even non-compliance with treatment, so as to enhance the probability of achieving bioequivalence, taste-masking effect, and rapid/complete releas

Inactive Publication Date: 2006-05-18
ADARE PHARM INC
View PDF98 Cites 99 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0010] The present invention provides pharmaceutical compositions and methods for making taste-masked microparticles and orally disintegrating tablets. In accordance with particular embodiments, the compositions provide effective taste-masking, smooth mouthfeel (little or no aftertaste) and rapid / complete release upon reaching the stomach, thereby enhancing the probability of achieving bioequivalence to the reference product.

Problems solved by technology

However, such dosage forms have several disadvantages.
This leads to poor, even non-compliance with the treatment and thus has a negative impact on the efficacy of the treatment.
The conventional capsule or tablet dosage form is also inconvenient for the ‘people on the move’ who often do not have access to drinking water or fluids.
Consequently, substantially complete release of the drug from such chewable tablets in the gastrointestinal tract takes 2 hours or longer.
However, coating with water-insoluble polymers such as ethylcellulose (EC), cellulose acetate (CA), cellulose acetate phthalate, polyvinyl acetate, Eudragit® RS, RL, L, S and NE30D polymers, results in slower dissolution profiles and not-too-infrequently results in imparting sustained-release properties.
An undesirable consequence of taste-masking using a water-insoluble polymer alone or in combination with a water-soluble polymer is in general the slower release of the drug in the gastrointestinal tract.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Taste-masked pharmaceutical compositions with gastrosoluble pore-formers
  • Taste-masked pharmaceutical compositions with gastrosoluble pore-formers
  • Taste-masked pharmaceutical compositions with gastrosoluble pore-formers

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0086] Drug-layered Diphenhydramine hydrochloride Beads (drug load: 15%): Diphenhydramine hydrochloride (375 g) was slowly added to an aqueous solution of 41.8 g polyvinylpyrrolidone (binder) and 1667 g of purified water and mixed well. 60-80 mesh sugar spheres (1470 g) were coated with the drug-layering formulation in a Glatt GPCG 3. The drug containing pellets were dried, and a seal coat of Opadry Clear for a weight gain of 4% was applied on the drug-layered beads.

[0087] Taste-masked Beads with Ethylcellulose (EC-10) / Calcium Carbonate: 1000 g of drug-layered beads produced above were coated in the Glatt GPCG 3 with a membrane comprising 227.3 g of EC-10, 22.7 g of Myvacet 9-45 (diacetylated monoglyceride) and 68.2 g of calcium carbonate dissolved / suspended in 3916.6 g of 95 / 5 acetone / water. The coated beads were dried in the Glatt GPCG-3. The dissolution profiles in 0.1N HCl of the beads with a membrane thickness of up to 20% by weight are shown in FIG. 1.

example 2 (

Reference)

[0088] Taste-masked Beads with Ethylcellulose (EC-10) alone: IR beads were coated with a solution of EC-10 / Myvacet 9-45 at a ratio of 90 / 10 dissolved in 95 / 5 acetone / water for a weight gain of up to 20%. The coated beads were dried in the Glatt GPCG-3. The taste-masked beads coated at 20% typically release less than about 10% in 5 minutes when dissolution tested using the USP Apparatus 2 (paddles @ 50 rpm) in a phosphate buffer at pH 6.8. The dissolution profiles in 0.1N HCl of the beads with a membrane thickness of up to 20% by weight are shown in FIG. 2 suggesting that both taste-masking and rapid release can be achieved when coated with ethylcellulose alone from a solvent mixture although the dissolution profiles from the beads thus coated at acceptable taste-masking levels do not meet the desired dissolution profile for a corresponding immediate release product.

[0089] Rapidly Dispersing Microgranules: The rapidly dispersing microgranules may comprise a sugar alcohol s...

example 3

[0091] Taste-masked Beads with Polyvinyl acetate / Calcium Carbonate: 1000 g of drug-layered beads were coated in the Glatt GPCG 3 with a membrane comprising 550 g of Kollicoat SR30D (30% polyvinyl acetate aqueous dispersion), 5.8 g of Myvacet, 49.5 g of micronized calcium carbonate and 30 g of magnesium stearate dissolved / suspended in 2760.9 g of ethanol (final ratio of ethanol / water: 87 / 13). The coated beads were dried in the Glatt GPCG-3. The dissolution profiles in 0.1N HCl of the beads with a membrane thickness of up to 20% by weight are shown in FIG. 3.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Lengthaaaaaaaaaa
Fractionaaaaaaaaaa
Fractionaaaaaaaaaa
Login to View More

Abstract

There is provided a method for preparing an orally disintegrating tablet (ODT) composition comprising microparticles of one or more taste-masked active pharmaceutical ingredient(s), rapidly-dispersing microgranules, and other optional, pharmaceutically acceptable excipients wherein the ODT disintegrates on contact with saliva in the buccal cavity forming a smooth, easy-to-swallow suspension. Furthermore, the microparticles (crystals, granules, beads or pellets containing the active), coated with a taste-masking membrane comprising a water-insoluble polymer and one or more gastrosoluble inorganic or organic pore-formers (practically insoluble in water and saliva, but soluble in an acidic buffer), exhibit acceptable taste-masking when placed in the oral cavity and provide rapid, substantially-complete release of the dose on entry into the stomach.

Description

CROSS REFERENCE TO RELATED APPLICATION [0001] This application claims the benefit of U.S. Provisional Application No. 60 / 621,144, filed Oct. 21, 2004, which is hereby incorporated by reference.TECHNICAL FIELD [0002] This invention relates to an orally disintegrating tablet (ODT) composition comprising taste-masked microparticles of one or more active pharmaceutical ingredients suitable for oral administration for the treatment of diseases and rapidly-dispersing microgranules comprising a disintegrant and a sugar alcohol or a saccharide, or a mixture thereof, each of which having an average particle diameter of not more than 30 μm. The multi-particulate ODT composition contains rapidly-dispersing microgranules and drug-containing core particles (crystals or granules, beads or pellets of one or more active pharmaceutical ingredients) coated with a taste-masking membrane comprising a water-insoluble polymer in combination with one or more pore-formers such as inorganic or organic salts...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K9/26
CPCA61K9/0056A61K9/2081A61K9/501A61K9/5026A61K9/5047A61K9/5078A61K31/135A61K31/4045A61K31/495
Inventor LAI, JIN-WANGVENKATESH, GOPI M.QIAN, KEN KANGYI
Owner ADARE PHARM INC
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com