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Water insoluble polymer: starch-based film coatings for colon targeting

a technology of starch-based film and insoluble polymer, which is applied in the direction of biocide, colloidal chemistry, drug compositions, etc., can solve the problems of premature drug release through water-filled channels, and achieve the effect of sufficient mechanical stability

Inactive Publication Date: 2011-08-18
ROQUETTE FRERES SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides a delivery system for controlled release of active ingredients in a polymeric film coating that can be used for patients with inflammatory bowel diseases and other colon-related disorders. The coating is designed to withstand the harsh conditions of the gastrointestinal tract and is adjustable to the specific needs of different drugs. The coating is a mixture of a water insoluble polymer and a starch composition that does not form particulate in the polymer. The starch composition can be a native starch or a modified starch, such as hydroxypropylated or acetylated starch. The coating is a solid dispersion and can be in the form of a liquid, semi-liquid, or solid form. The starch composition can contain at least one legume or cereal starch, such as pea or horse bean starch. The starch composition has a high swollen ability improving its surface area and digestibility in the colon. The modified starch is stabilized to prevent cracking and has a low degree of substitution. The invention also provides new polymeric film coatings that allow for site-specific drug targeting to the colon.

Problems solved by technology

Indeed, with known polymer coatings, the problem of accidental crack formation can result in premature drug release through water-filled channels.

Method used

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  • Water insoluble polymer: starch-based film coatings for colon targeting
  • Water insoluble polymer: starch-based film coatings for colon targeting
  • Water insoluble polymer: starch-based film coatings for colon targeting

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0095]A. Materials and Methods

[0096]A.1. Materials

[0097]Branched maltodextrin (BMD) [a branched maltodextrin with non digestible glycoside linkages: α-1,2 and α-1,3, NUTRIOSE® FB 06 Roquette Fréres], Peas starch (granular pea starch N-735) (35% amylose), a pregelatinized hydroxypropyl pea starch (PS HP-PG)(LYCOAT® RS 780), a maltodextrin (MD)(GLUCIDEX® 1, Roquette Freres), EURYLON® 7 A-PG (an acetylated and pregelatinized high amylose maize starch (70% amylose) (Roquette Freres, Lestrem, France), EURYLON® 6 A-PG (an acetylated and pregelatinized high amylose maize starch) (60% amylose) (Roquette Freres, Lestrem, France) and EURYLON® 6 HP-PG (a hydroxypropylated and pregelatinized high amylose maize starch (60% amylose) (Roquette Freres, Lestrem, France); aqueous ethylcellulose dispersion (Aquacoat® ECD 30; FMC Biopolymer, Philadelphia, USA); triethylcitrate (TEC; Morflex®, Greensboro, USA); pancreatin (from mammalian pancreas=mixture containing amylase, protease and lipase; Fisher B...

example 2

[0120]A. Materials and Methods

[0121]A.1. Materials

[0122]Pregelatinized hydroxypropyl pea starch (PS HP-PG) (LYCOAT® RS 780, Roquette Freres), EURYLON® 7 A-PG (an acetylated and pregelatinized high amylose maize starch (70% amylose)) (Roquette Freres, Lestrem, France), EURYLON® 6 A-PG (an acetylated and pregelatinized high amylose maize starch (60% amylose)) (Roquette Freres, Lestrem, France) and EURYLON® 6 HP-PG (a hydroxypropylated and pregelatinized high amylose maize starch (60% amylose)) (Roquette Freres, Lestrem, France); aqueous ethylcellulose dispersion (Aquacoat ECD 30; FMC Biopolymer, Philadelphia, USA); triethylcitrate (TEC; Morflex, Greensboro, USA).

[0123]A.2. Preparation of thin, polymeric films

[0124]Thin polymeric films were prepared by casting blends of different types of polysaccharides and aqueous ethylcellulose dispersion into Teflon moulds and subsequent drying for 1 d at 60° C. The water soluble polysaccharide was dissolved in purified water (5% w / w, in the case o...

example 3

[0140]A. Materials and methods

[0141]A.1. Materials

[0142]Peas starch N-735 (peas starch; Roquette Freres, Lestrem, France); Aquacoat ECD 30 (aqueous ethylcellulose dispersion; FMC Biopolymer, Brussels, Belgium); triethylcitrat (TEC; Morflex, Greensboro, N.C., USA); 5-aminosalicylic acid (5-ASA; Sigma-Aldrich, Isle d'Abeau Chesnes, France); microcrystalline cellulose (Avicel PH 101; FMC Biopolymer); bentonite and polyvinylpyrrolidone (PVP, Povidone K 30) (Coopertation Pharmaceutique Francaise, Melun, France); pancreatin (from mammalian pancreas=mixture of amylase, protease and lipase) and pepsin (Fisher Bioblock, Illkirch, France); extracts from beef and yeast as well as tryptone (=pancreatic digest of casein) (Becton, Dickinson and Company, Franklin Lakes, N.J., USA); L-cysteine hydrochloride hydrate (Acros Organics, Geel, Belgium); cysteinated Ringer solution (Merck, Darmstadt, Germany).

[0143]A.2. Preparation of Free Films

[0144]Thin, free films were prepared by casting blends of pea...

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Abstract

A controlled release delivery dosage form for controlled release of an active ingredient, includes an active ingredient coated in a polymeric mixture of: at least a water insoluble polymer and a starch composition including at least one component selected from the group consisting of a starch having an amylose content of between 20 and 45%, a modified starch having an amylose content of between 50 and 80% and a legume starch. The present invention also relates to the use and method for making the same.

Description

FIELD OF THE INVENTION[0001]The present invention relates to a dosage form for the controlled delivery of active ingredient(s). The present invention also relates to the use and method for making the same.BACKGROUND OF THE INVENTION[0002]Colon targeting can be very helpful for many pharmaco-therapies, including the treatment of inflammatory bowel diseases, such as Crohn's Disease (CD) and Ulcerative Colitis (UC).[0003]If a locally acting drug is orally administered using a conventional pharmaceutical dosage form, the latter rapidly dissolves in the contents of the stomach, the drug is released and likely to be absorbed into the blood stream. This leads to elevated systemic drug concentrations and, thus, an increased risk of undesired side effects and at the same time to low drug concentrations at the site of action in the colon, resulting in poor therapeutic efficiency. These restrictions can be overcome if drug release is suppressed in the stomach and small intestine and time-contr...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/14A61K9/00A61K47/26A61K47/32A61P1/00B05D5/00B05D7/24
CPCA61K9/0053A61K9/2846A61K9/2826A61P1/00A61P1/04A61K47/36
Inventor HAEUSLER, OLAFWILS, DANIELSIEPMANN, JUERGENKARROUT, YOUNESS
Owner ROQUETTE FRERES SA