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Dry coated tablet

a tablet and coating technology, applied in the field of dry coating tablets, can solve the problems of difficult discontinuation of non-steroidal anti-inflammatory drugs, degrade life quality, etc., and achieve the effects of convenient administration, high stability of active ingredients, and convenient administration

Inactive Publication Date: 2016-01-26
TAKEDA PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0032]The dry coated tablet of the present invention can be administered for the treatment or suppression of the onset of gastric ulcer or duodenal ulcer while continuing administration of acetylsalicylic acid, since it contains (1) PPI having a strong acid secretion suppressive action and (2) acetylsalicylic acid useful as a prophylactic and / or therapeutic agent for diseases of cerebrovascular or circulatory, for example, a thrombus and / or embolization inhibitor for angina pectoris (chronic stable angina pectoris, unstable angina pectoris), myocardial infarction; a prophylactic and / or therapeutic agent for ischemic cerebrovascular disorder (transient ischemic attack (TIA), cerebral infarction); a thrombus and / or embolization inhibitor used after coronary-artery bypass surgery (CABG) or percutaneous transluminal coronary angioplasty (PTCA); or a prophylactic and / or therapeutic agent for Kawasaki disease (including cardiovascular sequelae due to Kawasaki disease).
[0033]Moreover, since acetylsalicylic acid can also be used as one kind of non-steroidal anti-inflammatory drug for the treatment of mainly pain, fever and inflammation, the dry coated tablet of the present invention can be administered for the treatment or suppression of the onset of gastric ulcer or duodenal ulcer while continuing administration of a non-steroidal anti-inflammatory drug.
[0034]The dry coated tablet of the present invention shows high stability of the active ingredients (acetylsalicylic acid and PPI), and expresses a pharmacological effect of the active ingredients stably and rapidly after administration.
[0035]The dry coated tablet of the present invention can be easily administered while maintaining the convenience of handling.
[0036]The dry coated tablet of the present invention and a dry coated tablet produced by the production method of the present invention are superior in tablet strength, dissolution property of active ingredients (acetylsalicylic acid and PPI), preservation stability and acid resistance.

Problems solved by technology

Particularly, in the treatment of rheumatoid arthritis, osteoarthritis and the like, discontinuation of administration of non-steroidal anti-inflammatory drug may be difficult, since it markedly degrades the quality of life (QOL).

Method used

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Examples

Experimental program
Comparison scheme
Effect test

reference example 1

Production of Lansoprazole Enteric Micro Granules Lansoprazole-Containing Micro Granules

[0272]Nonpareil 105 (trade name 41.6 kg) was charged in a tumbling fluid-bed coating granulator (POWREX CORPORATION, MP-400), and a lansoprazole-containing coating solution prepared in advance, which had the following composition, was sprayed for coating. Furthermore, an intermediate layer coating solution prepared in advance, which had the following composition, was sprayed for coating. After completion of the coating, the granules were dried to give lansoprazole-containing micro granules (132 kg).

[Lansoprazole-Containing Coating Solution]

[0273]

lansoprazole39.60kgmagnesium carbonate13.20kglow-substituted hydroxypropylcellulose6.60kghydroxypropylcellulose13.20kg(purified water)(185L)

[Intermediate Layer Coating Solution]

[0274]

hydroxypropylmethylcellulose9.24kglow-substituted hydroxypropylcellulose6.60kgsterile talc3.96kgtitanium oxide3.96kgmannitol9.24kg(purified water)(99.0L)

Lansoprazole Enteric ...

example 1

[0280]Acetylsalicylic acid (granulation product: manufactured by Rhodia, Rhodine 3118, 57000 g), cornstarch (6270 g), microcrystalline cellulose (CEOLUS KG-1000 (trade name; manufactured by Asahi Kasei Chemicals Co., Ltd.), 3705 g) and carmellose (3705 g) were measured and mixed in a tumbler mixer. This was tableted using a rotary tableting machine (manufactured by Kikusui Seisakusho Ltd.) and φ7.0 mm R round punch to give a plain tablet (tablet weight 124 mg) of the inner core. 20% aqueous polysorbate 80 solution (960 g) was dissolved in water (21940 g), heated to 70° C., and glycerol monostearate (488 g) was dispersed in a dispersion machine to give a glycerol monostearate dispersion. Thereto were added methacrylic acid copolymer LD (Eudragit L30D-55 (trade name; manufactured by EVONIK INDUSTRIES), 24290 g (solid amount 7287 g)), ethyl acrylate-methyl methacrylate copolymer (Eudragit NE30D (trade name; manufactured by EVONIK INDUSTRIES), 2696 g (solid amount 808.8 g), citric anhyd...

example 2

[0283]Acetylsalicylic acid (granulation product: manufactured by Rhodia, Rhodine 3118, 57000 g), cornstarch (6270 g), microcrystalline cellulose (CEOLUS PH-101 (trade name; manufactured by Asahi Kasei Chemicals Co., Ltd.), 3705 g) and carmellose (3705 g) were measured and mixed in a tumbler mixer. This was tableted using a rotary tableting machine (manufactured by Kikusui Seisakusho Ltd.) and φ7.0 mm R round punch to give a plain tablet (tablet weight 124 mg) of the inner core. 20% aqueous polysorbate 80 solution (960 g) was dissolved in water (21940 g), heated to 70° C., and glycerol monostearate (488 g) was dispersed in a dispersion machine to give a glycerol monostearate dispersion. Thereto were added methacrylic acid copolymer LD (Eudragit L30D-55 (trade name; manufactured by EVONIK INDUSTRIES), 24290 g (solid amount 7287 g)), ethyl acrylate-methyl methacrylate copolymer (Eudragit NE30D (trade name; manufactured by EVONIK INDUSTRIES), 2696 g (solid amount 808.8 g), citric anhydr...

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Abstract

Provided is a dry coated tablet showing high stability of the active ingredient (proton pump inhibitor, acetylsalicylic acid), which stably and rapidly expresses the pharmacological effect of the active ingredient after administration. A dry coated tablet having an inner core and an outer layer, wherein the inner core is an enteric-coated tablet containing acetylsalicylic acid, and the outer layer contains enteric micro granules containing a proton pump inhibitor.

Description

TECHNICAL FIELD OF THE INVENTION[0001]The present invention relates to a dry coated tablet containing a proton pump inhibitor (hereinafter sometimes to be referred to as PPI) and acetylsalicylic acid. More particularly, the present invention relates to a dry coated tablet which is superior in the stability of the active ingredient and expresses a pharmacological effect stably and rapidly after administration.BACKGROUND OF THE INVENTION[0002]It sometimes happens that low dose acetylsalicylic acid administered to suppress thrombus and / or embolization (antiplatelet therapy) in cerebrovascular and circulatory diseases induces gastric ulcer or duodenal ulcer. Since discontinuation of administration of acetylsalicylic acid may result in thrombus and / or embolization, it is considered important to continue administration of low dose acetylsalicylic acid while suppressing the onset of ulcer.[0003]While acetylsalicylic acid is also known as a non-steroidal anti-inflammatory drug (NSAIDs), and...

Claims

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Application Information

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Patent Type & Authority Patents(United States)
IPC IPC(8): A61K9/16A61K9/28A61K9/32A01N43/00A61K31/616A61K9/24A61K31/4439A61K45/06A61K9/20A61K9/50
CPCA61K31/616A61K9/209A61K9/2054A61K9/2095A61K9/2846A61K9/2886A61K9/5078A61K31/4439A61K45/06A61K9/5026
Inventor KAWANO, TETSUYAMIMA, YASUSHIISHII, YUMIKO
Owner TAKEDA PHARMA CO LTD