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Enteric extended-release tegafur-gimeracil-potassium oxonate preparation, and preparation method thereof

A technology for sustained-release preparations and sustained-release tablets, which is used in the field of tablets, capsules, and solid oral enteric-coated extended-release preparations to achieve stable blood drug concentrations and reduce adverse reactions.

Inactive Publication Date: 2018-03-27
江苏金甙生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This is contrary to the design of our invention patent to prepare tegafur for immediate release, and according to the general conditions for preparing sustained-release preparations, tegafur has a half-life of 13 hours, which is generally no longer suitable for preparation of sustained-release preparations

Method used

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  • Enteric extended-release tegafur-gimeracil-potassium oxonate preparation, and preparation method thereof
  • Enteric extended-release tegafur-gimeracil-potassium oxonate preparation, and preparation method thereof
  • Enteric extended-release tegafur-gimeracil-potassium oxonate preparation, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] Example 1: S-1 enteric-coated sustained-release tablets (skeleton type)

[0073] Material No.

1

2

3

Tegafur

20mg

40mg

80mg

Gimeracil

5.8mg

11.6mg

23.2mg

Oteracil Potassium

19.6mg

39.2mg

78.4mg

HPMC

20mg

80mg

150mg

MCC

20mg

80mg

200mg

EC

15mg

50mg

100mg

lactose

25mg

60mg

120mg

Calcium sulfate

10mg

30mg

60mg

Magnesium stearate

5mg

10mg

20mg

Acrylic resin No. Ⅱ

25mg

100mg

200mg

[0074] The preparation steps are:

[0075] ①Preparation of sustained-release tablet cores: Gymeracil, oteracil potassium and a certain amount of pharmaceutical excipients were crushed separately and passed through an 80-mesh standard sieve, weighed according to the prescription amount, fully mixed together, and then added a certain amount of 65% Ethanol solution is used as a binder to pre...

Embodiment 2

[0079] Example 2: S-1 enteric-coated sustained-release capsules (skeleton type)

[0080] Material No.

1

2

3

Tegafur

20mg

40mg

80mg

Gimeracil

5.8mg

11.6mg

23.2mg

Oteracil Potassium

19.6mg

39.2mg

78.4mg

HPMC

20mg

80mg

150mg

MCC

20mg

80mg

200mg

EC

15mg

50mg

100mg

lactose

25mg

60mg

120mg

Calcium sulfate

10mg

30mg

60mg

Magnesium stearate

5mg

10mg

20mg

[0081] ①Preparation of sustained-release capsule core: Gymeracil, oteracil potassium and a certain amount of pharmaceutical excipients were crushed separately and passed through an 80-mesh standard sieve, weighed according to the prescription amount, fully mixed together, and then added a certain amount of 65% Ethanol solution is used as a binder to prepare soft materials, passed through a 20-mesh standard sieve, dried at 60°C for 3 hours, and...

Embodiment 3

[0084] Example 3: S-1 enteric-coated sustained-release tablets (film-coated type)

[0085] Material No.

1

2

3

Tegafur

20mg

40mg

80mg

Gimeracil

5.8mg

11.6mg

23.2mg

Oteracil Potassium

19.6mg

39.2mg

78.4mg

HPMC

20mg

80mg

150mg

MCC

20mg

80mg

200mg

EC

15mg

50mg

100mg

MCC

25mg

60mg

120mg

pvp

10mg

30mg

60mg

Magnesium stearate

5mg

10mg

20mg

Acrylic resin No. Ⅱ

25mg

100mg

200mg

Acrylic resin No.Ⅲ

25mg

100mg

200mg

[0086] The preparation steps are:

[0087] ①Preparation of sustained-release tablet cores: Gymeracil, oteracil potassium and a certain amount of pharmaceutical excipients were crushed separately and passed through an 80-mesh standard sieve, weighed according to the prescription amount, fully mixed together, and then added a certain amount of 65% E...

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Abstract

The invention relates to an oral solid enteric extended-release tegafur-gimeracil-potassium oxonate medicinal preparation (a tablet or capsule) and a preparation method thereof, belonging to the technical field of extended-release preparations of drugs. The release form of drugs may be extended release, quick release or double release (extended release and quick release); the release effect enables plasma concentration to be stationary and avoids the phenomenon of peak-valley fluctuation of plasma concentration; and thus, the bioavailability and curative effect of drugs are improved, and administration frequency and total dose are reduced, which enables toxic and side effect on gastrointestinal tracts and the like to be reduced and medication compliance to be improved. The oral solid enteric extended-release tegafur-gimeracil-potassium oxonate medicinal preparation is applicable to treatment of locally advanced or metastatic (i.e., cases where tumor tissue cannot be surgically removed)gastric cancer, head and neck cancer, colorectal cancer, non-small cell lung cancer, breast cancer, pancreatic cancer, bile duct cancer, cervical cancer, prostate cancer, etc.

Description

technical field [0001] The invention relates to a solid oral enteric-coated sustained-release (extended release) preparation that provides a pharmaceutical composition of tegafur, gimeracil and oteracil potassium, which are tablets and capsules, and belongs to the technical field of drug sustained-release preparations. said [0002] Tablets and capsules are enteric-coated preparations, and their drug release form can be sustained release, quick release or double release. The drug sustained-release preparation is used for the treatment of unresectable locally advanced or metastatic gastric cancer, lung cancer, head and neck cancer, colorectal cancer, non-small cell lung cancer, breast cancer, pancreatic cancer, bile duct cancer, cervical cancer and prostate cancer, etc. . Background technique [0003] Japan Dapeng Pharmaceutical Industry Co., Ltd. has developed the compound Tegafur capsule of Tegafur: Gimeracil: Oteracil Potassium 1:0.4:1 since 1991, and the trade name is T...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/513A61K31/44A61K31/53A61K9/22A61K9/36A61K9/32A61K9/52A61K47/38A61K47/32A61K47/44A61K47/10A61P35/00
CPCA61K9/0002A61K9/167A61K9/2077A61K9/209A61K9/284A61K9/2866A61K31/44A61K31/513A61K31/53A61K2300/00
Inventor 温天文汪志友胡一桥
Owner 江苏金甙生物技术有限公司
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