Oral film-form base and preparation

Patent metadata

Field	Value
Publication number	US-10092505-B2
Application number	US-201313737255-A
Country	US
Kind code	B2
Filing date	Jan 9, 2013
Priority date	Jan 11, 2012
Publication date	Oct 9, 2018
Grant date	Oct 9, 2018

Abstract

The present invention provides an oral film-form base which has a rapid dissolution profile in the mouth and sufficient film strength, and gives an improved taking property by foaming in the mouth. The oral film-form base includes an edible polymer soluble both in water and in an organic solvent having a solubility parameter of 9.7 or higher, a foaming agent, and an auxiliary foaming agent, wherein the foaming agent is foamable in the presence of water, and the foaming agent and the auxiliary foaming agent each are insoluble in the organic solvent, have an average particle size of 0.1 to 60 μm, and are included in particle states.

First claim

The invention claimed is:

1. An oral film-form preparation comprising an oral film-form base and a drug in the oral film-form base, wherein the oral film-form base comprises
an edible polymer soluble both in water and in an organic solvent having a solubility parameter of 9.7 or higher, wherein the edible polymer is at least one of polyvinylpyrrolidone or hydroxypropyl cellulose,
a foaming agent particle, and
an auxiliary foaming agent particle,
wherein the foaming agent particle is foamable in the presence of water,
the foaming agent particle and the auxiliary foaming agent particle each are insoluble in the organic solvent, have an average particle size of 0.1 to 60 μm, and are included in particle states,
the foaming agent particle and the auxiliary foaming agent particle are dispersed uniformly in a film containing the edible polymer and the drug,
the foaming agent particle is at least one selected from the group consisting of sodium hydrogen carbonate, sodium carbonate, magnesium carbonate, ammonium hydrogen carbonate, ammonium carbonate, potassium carbonate, and calcium carbonate, and
the auxiliary foaming agent particle is at least one selected from the group consisting of L-ascorbic acid, potassium L-bitartrate, calcium dihydrogen pyrophosphate, disodium dihydrogen pyrophosphate, galacturonic acid, glucuronic acid, monosodium fumarate, potassium aluminum sulfate, sodium DL-malate, potassium dihydrogen phosphate, and dipotassium hydrogen phosphate.

2. The oral film-form preparation according to claim 1 , wherein the foaming agent particle and the auxiliary foaming agent particle each have an average particle size of 0.1 μm to 30 μm.

3. The oral film-form preparation according to claim 1 , wherein the polyvinylpyrrolidone has a weight-average molecular weight of 2,500 to 3,000,000.

4. The oral film-form preparation according to claim 1 , wherein the hydroxypropyl cellulose has a weight-average molecular weight of 10,000 to 1,200,000.

5. The oral film-form preparation according to claim 1 , wherein the hydroxypropyl cellulose has a hydroxypropoxy substitution degree of 50 to 100%.

6. The oral film-form preparation according to claim 1 , further comprising particles of at least one selected from the group consisting of mono- to hexasaccharide sugars and sugar alcohols thereof each having an average particle size of 0.1 to 60 μm.

7. An oral film-form preparation comprising an oral film-form base and a drug in the oral film-form base, wherein the oral film-form base comprises
an edible polymer soluble both in water and in an organic solvent having a solubility parameter of 9.7 or higher,
a foaming agent particle, and
an auxiliary foaming agent particle,
wherein the foaming agent particle is foamable in the presence of water,
the foaming agent particle and the auxiliary foaming agent particle each are insoluble in the organic solvent, have an average particle size of 0.1 to 60 μm, and are included in particle states,
the foaming agent particle and the auxiliary foaming agent particle are uniformly dispersed in a film containing the edible polymer and the drug, wherein the film is a dried film,
the foaming agent particle is at least one selected from the group consisting of sodium hydrogen carbonate, sodium carbonate, magnesium carbonate, ammonium hydrogen carbonate, ammonium carbonate, potassium carbonate, and calcium carbonate, and
the auxiliary foaming agent particle is at least one selected from the group consisting of L-ascorbic acid, potassium L-bitartrate, calcium dihydrogen pyrophosphate, disodium dihydrogen pyrophosphate, galacturonic acid, glucuronic acid, monosodium fumarate, potassium aluminum sulfate, sodium DL-malate, potassium dihydrogen phosphate, and dipotassium hydrogen phosphate.

Assignees

• Nitto Denko Corp

Inventors

• Asari Daisuke
• Hori Mitsuhiko
• Shishido takuya

Classifications

• A61K9/0007 Primary

  Effervescent (A61K9/0065 takes precedence) · CPC title

• A61K9/006

  Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays · CPC title

• A61K47/02

  Inorganic compounds · CPC title

• A61K9/70 Primary

  Web, sheet or filament bases {; Films; Fibres of the matrix type containing drug (hollow drug-filled fibres A61K9/0092)} · CPC title

• A61K47/38

  Cellulose; Derivatives thereof · CPC title