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|Title:||Orally-disintegrating solid preparation|
|Abstract:||The present invention provides an orally-disintegrating solid preparation such as a tablet produced by tabletting fine granules showing controlled release of a pharmaceutically active ingredient and an additive, and the like, and the orally-disintegrating solid preparation containing fine granules coated with a coating layer containing a polymer affording a casting film having an elongation at break of about 100-about 700%. With the preparation, breakage of fine granules during tabletting can be suppressed in the production of an orally-disintegrating solid preparation containing fine granules showing controlled release of a pharmaceutically active ingredient.|
|Inventor(s):||Kurasawa; Takashi (Osaka, JP), Watanabe; Yasuko (Osaka, JP), Omachi; Yoshihiro (Osaka, JP)|
|Assignee:||Takeda Pharmaceutical Company Limited (Osaka, JP)|
1. An orally-disintegrating solid preparation comprising: (1) fine granules A, comprising core granules comprising R-lansoprazole or a salt thereof as a
pharmaceutically active ingredient; an intermediate coating layer on the core granules, the intermediate layer comprising at least one selected from the group consisting of low-substituted hydroxypropyl cellulose, hydroxypropyl cellulose, hypromellose,
polyvinylpyrrolidone, polyvinyl alcohol, methylcellulose and hydroxyethylmethylcellulose, the fine granules A comprising the intermediate coating layer in an amount of 0.02 part by weight-1.5 part by weight per 1 part by weight of the core granules; and
a controlled release film over the intermediate coating layer, wherein the controlled release film comprises a methacrylic acid-methyl acrylate-methyl methacrylate copolymer capable of affording a casting film having an elongation at break of 100%-700%,
wherein the amount of the pharmaceutically active ingredient dissolved from the fine granules A is not more than 10% in 2 hours as expressed by the dissolution rate in a pH 1.2 solution, and not more than 5% in 1 hour as expressed by the dissolution rate
in a pH 6.8 solution, and wherein the fine granules have an average particle size of 500 .mu.m or below; and (2) fine granules B comprising the same pharmaceutically active ingredient with a different release rate relative to the fine granules A,
wherein the fine granules B are enteric fine granules coated with a coating layer comprising an enteric polymer that is soluble at pH less than 6.0, but not at pH less than 5.0, wherein the enteric coating layer comprises an aqueous enteric polymer base
and a sustained-release substrate, wherein the aqueous enteric polymer base is at least one selected from the group consisting of, methacrylic acid ethyl acrylate copolymer, hydroxypropyl methylcellulose acetate succinate and carboxymethyl ethyl
cellulose, and the sustained-release substrate is at least one selected from the group consisting of methyl methacrylate-ethyl acrylate copolymer and ethylcellulose, wherein the preparation is in the form of a tablet.
2. The preparation of claim 1, wherein the fine granules B have an average particle size of 500 .mu.m or below.
3. The preparation of claim 1, wherein the fine granules A and the fine granules B comprise the pharmaceutically active ingredient at a weight ratio of 1:10-10:1.
4. The preparation of claim 1, further comprising an additive.
5. The preparation of claim 4, wherein the additive comprises a water-soluble sugar alcohol.
6. The preparation of claim 4, wherein the additive comprises a disintegrant.
7. The preparation of claim 4, comprising 10-50 wt % fine granules A, 10-30 wt % fine granules B, and 20-80 wt % additive.
8. The preparation of claim 1, wherein the total weight of the preparation is 1000 mg or below.
9. The preparation of claim 1, wherein the oral disintegration time is 90 seconds or less.
10. The preparation of claim 1, which is capable of achieving an average pH in the stomach of not less than 4 at 0.5 hours after oral administration and maintaining said pH or higher pH for 14 hours or longer.
11. The preparation of claim 1, wherein the pharmaceutically active ingredient is R-lansoprazole or a salt thereof, which reaches the maximum blood drug concentration in 5 hours and maintains the maximum blood drug concentration of not less than 100 ng/mL for 4 hours or longer, when 30 mg of the pharmaceutically active ingredient is administered orally.
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