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Controlled-release drug composition

A pharmaceutical composition and the technology of the composition are applied in the field of controlled-release pharmaceutical compositions, and can solve the problems of inconsistent time periods of active ingredients and the like

Inactive Publication Date: 2007-07-11
KOWA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since cholesterol is synthesized in the body from midnight to morning, there is a high possibility that the blood concentration of the active ingredient does not coincide with the time period of cholesterol biosynthesis.

Method used

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  • Controlled-release drug composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] Table 2

[0072] Element

Addition amount (mg)

intestines

dissolve

sex

grain

Grain

A

grain

Grain

A

Refined white sugar spherical granules

114.00

pitavastatin calcium salt

12.00

sucrose

30.75

Hydroxypropyl methylcellulose (trade name: TC-5R)

18.00

Magnesium Aluminosilicate Metasilicate

2.40

Talc powder

0.60

Triethyl citrate

2.25

Subtotal

180.00

Methacrylic acid-methyl methacrylate copolymer (trade name: Eudragit L)

41.58

Talc

8.28

triethyl citrate

4.14

Subtotal

234.00

pitavastatin calcium salt

4.00

sucrose

10.25

Hydroxypropyl methylcellulose (trade name: TC-5R)

6.00

Magnesium Aluminosilicate Metasilicate

...

Embodiment 2

[0080] table 3

[0081] Element

Amount added (mg)

intestine

dissolve

sex

grain

grain

grain

grain

Granule A

30.00

Ethyl acrylate · methyl methacrylate · ethyl methacrylate chlorination

Trimethylammonium copolymer (trade name: Eudragit RS)

12.40

Hydroxypropyl cellulose

3.10

Talc powder

0.95

Triethyl citrate

1.55

Subtotal

48.00

pitavastatin calcium salt

4.00

sucrose

10.25

Hydroxypropyl methylcellulose (trade name: TC-5R)

6.00

Magnesium Aluminosilicate Metasilicate

0.80

Talc

0.20

triethyl citrate

0.75

Hydroxymethylpropylcellulose Phthalate

16.17

Talc

3.22

triethyl citrate

1.61

Subtotal

91.00

pitavastatin calcium s...

Embodiment 3

[0092] Table 4

[0093] Element

Amount added (mg)

grain

Grain

Granule A

180.00

Ethyl cellulose

10.00

Hydroxypropylmethylcellulose (trade name: TC-5R)

32.50

Talc powder

8.25

Triethyl citrate

3.25

Subtotal

234.00

intestine

dissolve

sex

grain

grain

Granule A

60.00

Methacrylic acid-methyl methacrylate copolymer (trade name: Eudragit S)

13.86

Talc powder

2.76

Triethyl citrate

1.38

Subtotal

78.00

total

312.00

[0094] In the same manner as in Example 1, 2400.0 g of Granule A was prepared.

[0095] Add 325.0 g of hydroxypropyl methylcellulose (trade name: TC-5R) to 1500 g of purified water and dissolve it with a disperser, and add 100.0 g of ethyl cellulose and tricitric acid to 4000.0 g of ethanol. 7.5 g of ethyl ester and 82.5 g of talc were m...

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PUM

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Abstract

A controlled-release drug composition characterized by comprising a composition (A) that contains pitavastatin or its salt or ester and initiates release thereof at least in the stomach and an enteric composition (B) that contains pitavastatin or its salt or ester. The use of this controlled-release drug composition leads to prolonged appropriate maintenance, starting just after administration, of the blood level of pitavastatin, so that safe and highly effective reduction of the blood cholesterol level can be realized.

Description

technical field [0001] The present invention relates to a controlled-release pharmaceutical composition containing HMG-CoA reductase inhibitor pitavastatin, its salt or its ester. Background technique [0002] Pitavastatin, its salt or its ester is known to have excellent HMG-CoA reductase inhibitory activity and is useful as a therapeutic drug for hypercholesterolemia (US Patent No. 5,856,336 and European Patent No. 0,304,063). Drugs for treating hypercholesterolemia, such as medicines containing pitavastatin, are used in oral preparations such as tablets, granules, and capsules (US Patent No. 6,465,477 and WO97 / 23200). Moreover, oral preparations are usually designed so that the concentration of the active ingredient in the blood reaches a peak value within 0.5-3 hours after taking it, and then disappears rapidly. However, since the biosynthesis of cholesterol proceeds from midnight to early morning, there is a high possibility that the blood concentration of the active i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/47A61K9/22A61K9/52A61P3/06A61P43/00A61K9/20A61K9/24A61K9/50
CPCA61K9/5078A61K9/2081A61K31/47A61K9/5026A61K9/209A61K9/5084A61K9/5036A61P3/06A61P43/00
Inventor 谷泽良夫下川达张小川广忠渡边真由美大箸千裕川岛弘行條田泰雄稲木敏男
Owner KOWA CO LTD