Capecitabine rapidly disintegrating tablets

A technology of capecitabine and disintegrant, which is applied in the direction of pill delivery, coating, organic active ingredients, etc., and can solve problems such as capecitabine’s cohesiveness that cannot be overcome

Inactive Publication Date: 2012-03-07
F HOFFMANN LA ROCHE & CO AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Conventional excipients currently used in these tablets, such as lactose and croscarmellose sodium, cannot by themselves overcome the caking properties of capecitabine in the described tablets

Method used

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  • Capecitabine rapidly disintegrating tablets
  • Capecitabine rapidly disintegrating tablets
  • Capecitabine rapidly disintegrating tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-6

[0028] Preparation composition

[0029]

[0030]

[0031] 1 removed during processing

[0032] Manufacturing steps:

[0033] 1. Mix capecitabine with anhydrous lactose and a part of cross-linked polyvinylpyrrolidone

[0034] 2. Dissolve hypromellose in pure water

[0035] 3. Granulate the blend from step 1 with the granulation solution from step 2

[0036] 4. Wet milling of pellets from step 3

[0037] 5. Dry and grind the pellets from step 4

[0038] 6. Combine the pellet from step 5 with Ludiflash The remainder is a blend of crospovidone, mannitol, microcrystalline cellulose, aspartame, sodium saccharin, vanillin, bitter masking blend, and strawberry flavor

[0039] 7. Sift the magnesium stearate, add it to the blend from step 6 and mix

[0040] 8. Compress the tableting mixture from step 7 to nucleate

[0041] 9. Preparation of film coating suspension by dispersing the film coating mixture in purified water

[0042] 10 Film coat the cores from step 8 using ...

Embodiment 7-12

[0044] The following compositions represent preferred formulations in mg / tablet weight where lactose is replaced by mannitol.

[0045]

[0046] 1 removed during processing

[0047] Steps: Similar to the steps of Examples 1-6, except that anhydrous lactose is replaced by mannitol in step 1.

Embodiment 13

[0048] Example 13: Disintegration Characteristics of Dosage Forms

[0049]The following is a comparison of the disintegration times of the rapidly disintegrating tablets of the present invention and commercially available tablets at low and high tablet strengths.

[0050] Disintegration times were obtained using a USP disintegration apparatus without discs and 37°C water. The experimental test methods and resulting observed disintegration times were performed according to the USP disintegration test method (USP 29, General Chapters, Physical Tests, , which is hereby incorporated by reference .

[0051] For the purposes of this test, disintegration does not imply complete dissolution of the unit or even of its active ingredients. Complete disintegration is defined as the state in which, other than insoluble coating or fragments of the capsule shell, any residue of the unit remaining on the sieve of the test device is a soft mass without a distinct film core .

[0052] U...

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PUM

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Abstract

There is provided a film coated pharmaceutical composition comprising 5 '-deoxy-5-fluoro-N-[(pentyloxy)-carbonyl]-cytidine (capecitabine) and at least one disintegrant selected from the group comprising of crospovidone (particle size < 15-400 [mu]), croscarmellose sodium, sodium starch glycolate, low-substituted hydroxypropylcellulose, Ludiflash TM or any combination of these, together with other pharmaceutically acceptable excipients to form a rapidly disintegrating tablet.

Description

field of invention [0001] The present invention relates to a new rapidly disintegrating pharmaceutical dosage form having as active ingredient 5'-deoxy-5-fluoro-N-[(pentyloxy)-carbonyl]-cytidine (capecitabine ). The new dosage form is suitable for any patient, and is particularly suitable for patients who have difficulty swallowing solid oral dosage forms, including pediatric and geriatric populations. Background of the invention [0002] Capecitabine is a fluoropyrimidine carbamate with antineoplastic activity. It is a systemic prodrug of orally administered 5'-deoxy-5-fluorouridine (5'-DFUR), an antineoplastic agent. Capecitabine is marketed by Roche Laboratories as Xeloda The trade name is listed in the United States. Capecitabine has the chemical name 5'-deoxy-5-fluoro-N-[(pentyloxy)-carbonyl]-cytidine and has the following structural formula: [0003] [0004] Capecitabine is covered in US Patents (including US Patent Nos. 4,966,891 and 5,472,949) and USSN 60 / 6...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K31/7068A61K9/00
CPCA61K9/0095A61K9/2866A61K31/7068A61P35/00A61K9/28A61K9/20
Inventor 玛丽亚·奥克萨纳·巴钦斯基穆罕默德·拉希德保罗·安东尼·萨姆塔内夫尼特·哈尔戈文达斯·沙阿
Owner F HOFFMANN LA ROCHE & CO AG
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