Sugar-coated tablet

A preparation and sugar coating technology, applied in sugar-coated pills, pill delivery, medical preparations of inactive ingredients, etc., to achieve the effect of oxidation inhibition

Inactive Publication Date: 2008-06-04
TAKEDA PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Also, from a safety standpoint, there are not many orally administered antioxidants

Method used

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  • Sugar-coated tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0075] Hereinafter, the present invention will be described in more detail by examples and the like, but they are not meant to limit the present invention.

[0076] In addition, the storage conditions in the following evaluation examples refer to storage in air, unless otherwise specified in the specification, such as "the oxygen concentration is 95% or higher". Further, in the storage conditions of the evaluation examples described below, no humidity adjustment was performed unless otherwise described about the humidity adjustment.

reference example 1

[0078] Compound A and sodium ascorbate were placed in the air at 40° C. and 75% RH for 1 month, respectively, and then their residual rates were measured. As a result, the residual rate of Compound A was 89.7% (W / W), and the residual rate of sodium ascorbate was 99.0% (W / W).

[0079]Quantification of Compound A was performed by the HPLC method under the following conditions.

[0080] Solvent: Acetonitrile

[0081] Measurement wavelength: 287nm

[0082] Column: CHIRALCEL OJ-R 4.6 mm×150 mm (manufactured by Daicel Chemical Industries, Ltd.)

[0083] Mobile phase: mixed solution of acetonitrile / 10mM ammonium acetate aqueous solution (16:9)

[0084] Column oven temperature: about 25°C

[0085] Sodium ascorbate was quantified by iodine titration (solvent: metaphosphoric acid solution (1→50), indicator: starch test solution).

Embodiment 1

[0095] Formulations were prepared according to the recipe shown in Table 3. Sugar-coated tablets were obtained by spraying the sugar-coating solution to the tablets (330 g) obtained in Comparative Example 2 by using a pan coater (Hicoater 20, Freund Industrial Co., Ltd.) so as to obtain a coating of 170 mg per tablet , the sugar coating solution comprises erythritol (221g), talc (68g), gum arabic powder (34g) and microcrystalline cellulose (17g). At this time, adjust the product temperature to 35°C to 55°C for coating.

[0096] [table 3]

[0097] 25mg tablet

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Abstract

Disclosed is a pharmaceutical preparation wherein an active ingredient unstable to oxygen is stabilized by coating a portion containing the active ingredient unstable to oxygen with a sugar-coating layer containing (1) a sugar alcohol as a sugar-coating base and (2) a binder.

Description

technical field [0001] The invention relates to a sugar-coated preparation. Background technique [0002] Among the pharmaceutically effective compounds, there are compounds that are unstable to oxygen (ie, compounds that are easily oxidized). Because it is difficult to provide stable formulations containing such compounds as active ingredients by conventional manufacturing techniques, said compounds are usually initially excluded from drug candidates. In developing formulations of this compound, certain means for said formulations are required, such as storing said formulations in containers made of substances with low oxygen permeability and also replacing said containers with gases other than oxygen An internal gap, optionally an oxygen absorber or scavenger is sealed within the container to remove oxygen from the container. As a technique for solving such problems, a stable film-coated tablet comprising a nitrogen-labile nitrogen-containing fused heterocyclic compound ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K9/16A61K9/20A61K31/4035A61K47/10A61K47/26A61P25/16A61P25/28
CPCA61K9/2013A61K9/2054A61K9/2866A61K9/2018A61K31/4035A61K9/2826A61K9/286A61P25/16A61P25/26A61P25/28A61K9/20A61K47/10A61K9/28
Inventor 内山善博仲野庆则
Owner TAKEDA PHARMA CO LTD
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