Controlled-release of an active substance into a high fat environment

A technology for active substances and controlled release, applied in the direction of organic active ingredients, medical preparations containing active ingredients, drug delivery, etc., can solve the problem of no indication, no method of teaching controlled release or delivery system usage, no indication of oil digestion Problems such as the huge impact of the product, to achieve the effect of reducing side effects

Inactive Publication Date: 2006-01-25
PFIZER PRODS ETAT DE CONNECTICUT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is not indicated how to choose the polymer to avoid these effects, and there is no indication of the potentially large impact of oil digestion products on the coating material
[0012] Thus, while the prior art has described numerous dosage forms and coating materials for the controlled release of active substances, none of them teach the use of controlled release or delivery systems that are particularly suitable for the use of beneficial substances in the system. Controlled release while remaining in high-fat environments such as gastrointestinal fluids following a high-fat meal

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0132]In order to determine suitability for use in a high fat environment, several polymers intended to be tested to determine their suitability as asymmetric membrane coating materials for a wide range of dosage forms of the present invention were examined. GI fluid intake of a high fat diet was simulated by using 0.5 wt% "50% hydrolyzed model oil" mixed in 0.01 M aqueous HCL. The polymers were obtained as commercial films or by casting polymer solutions onto glass plates with a Gardner knife (Gardner labs, Inc., Bethesda, MD) to form dense films. Table I lists the polymers tested, the polymer solution composition used to cast the films, and the final thickness of each type of film. After casting, the solvent was evaporated overnight at ambient conditions (22°C). The films were then soaked in water for 30 seconds to 5 minutes, removed from the glass plates, and then dried in a 37°C oven for at least 16 hours to remove all coating solvent prior to evaluation.

[0133] First ...

Embodiment 2

[0137] Polymers used as cladding materials to make asymmetric films in the broad formulations of the present invention were cast into films, as described in Example 1 . The film is contacted with each component of the dietary fat mixture and with a model mixture containing sufficient amounts of dietary fat and / or dietary fat digested products to simulate the environment of use. Thick films of this material were cast from acetone solutions. Three ethyl celluloses (Ethocel(R); S100, Ethocel M70 and Ethocel M50) and one cellulose acetate (CA398-10) were tested. Films of polymer blends (Ethocel S100 and CA398-10) were also used. The resulting film pellets (10-20 mg dry weight) were placed in 0.05% MFD containing 3 wt% of the fat component tested. The solution was shaken at 37°C for at least 20 hours. The film pieces were recovered, wiped dry and weighed.

[0138] The results are tabulated in Tables III and IV below; the formulations used in the mixtures are given in Table V. ...

Embodiment 3

[0146] Controlled release tablets containing pseudoephedrine and coated with ethyl cellulose are manufactured as follows. First, a mixture was prepared containing 75.4 wt% pseudoephedrine HCl, 3.4 wt% hydroxypropyl cellulose, and 21.2 wt% microcrystalline cellulose. The blend was wet granulated and dried in a P-K processor. The dried granules were milled with a Fitzpatrick mill and then mixed in a V-blender. The dried granules (59.8 wt%) were blended with microcrystalline cellulose (40.2 wt%), milled with a Fitzpatrick mill, and reblended. The final mixture was prepared by adding 0.5 wt% magnesium stearate and mixing. Tablets containing 240 mg of pseudoephedrine HCl were prepared from this blend on a rotary tablet press with a 7 / 16" process and the target tablet weight was 537 mg.

[0147] The drug core is then coated with an asymmetric ethyl cellulose film formed by the following phase inversion method disclosed in US Patents 5,612,059 and 5,698,220. A solution containing...

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Abstract

The present invention provides a controlled release delivery composition which can be administered to a high fat use environment such as the human gastrointestinal tract following a high fat meal. The delivery composition is embodied as a core surrounded by an asymmetric polymeric membrane. In a preferred embodiment, the asymmetric polymeric membrane is cellulose acetate.

Description

Field of Invention [0001] The present invention relates to a controlled release of an active substance in a high-fat environment provided, for example, by the consumption of high-fat foods, and more particularly, to compositions and delivery devices for such controlled release. Background of the Invention [0002] The pharmaceutical literature is full of delivery systems for the administration of beneficial substances. The different designs of these delivery systems are reflected in, for example, differences in desired absorption, bioavailability, and route of administration of beneficial substances (also referred to herein as "pharmaceutical" or "active" substances or simply "drugs"), and Attempts are made to increase patient acceptability, increase the efficacy of actives delivered to the site of action, and minimize side effects by, for example, limiting peak blood levels. [0003] As will be appreciated by those skilled in the art of pharmacy and medicine, oral inhalati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K31/135A61K31/495A61K31/00A61K9/00A61K9/20A61K9/28A61K31/137A61K31/4985
CPCA61K9/2866A61K31/137A61K9/0004A61K9/209A61K31/4985A61K9/28
Inventor 马克·B·奇德劳德韦恩·T·弗里森斯科特·M·赫比格詹姆斯·A·S·奈廷格尔辛西娅·A·奥克萨南詹姆斯·B·韦斯特
Owner PFIZER PRODS ETAT DE CONNECTICUT
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