Pharmaceutical compositions and dosage forms of thalidomide

A thalidomide and dosage form technology, applied in the field of thalidomide pharmaceutical composition and dosage form, can solve problems such as unacceptable thalidomide, inability to ingest diseases, etc.

Inactive Publication Date: 2006-02-22
CELGENE CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In particular, certain patients may not be able to accept thalidomide in the usual existing oral dosage forms, or be unable to take in the large amounts of thalidomide necessary to effectively treat their disease

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] 5.1. Example 1: 200MG Thalidomide Dosage Capsules

[0078] Table 2 illustrates the batch and single dose formulations for 200 mg, i.e. about 40% by weight thalidomide single dose unit #0 capsules

[0079] Material

[0080] The pregelatinized starch (SPRESS B-820) and thalidomide components were passed through a 710 micron screen and then charged to a diffusion mixer with a baffle insert and mixed for 15 minutes. Magnesium stearate was passed through a 210 micron sieve and added to a diffusion blender and the mixture was then encapsulated in #0 capsules using a Dosator type capsule filling machine weighing 500 mg per capsule (8400 capsules per batch).

Embodiment 2

[0081] 5.2. Example 2: 100MG Thalidomide Dosage Tablets

[0082] Table 3 illustrates the batch and single dose unit formulations for 100 mg, 40% by weight thalidomide single dose unit tablets.

[0083] Material

[0084] The microcrystalline cellulose, croscarmellose sodium, and thalidomide components were passed through a 30 mesh screen (about 430[mu] to about 655[mu]). Pluronic F-68(R) (manufactured by JRH Biosciences, Inc. of Lenexa, KS) was passed through a 20 mesh screen (about 457[mu] to about 1041[mu]). Add Pluronic F-68 surfactant and 0.5 kg of croscarmellose sodium to a 16 qt. double-barrel tank mixer and mix for approximately 5 minutes, transferring the mixture to a 3 cubic foot double-shell tumbler mixer , add microcrystalline cellulose and mix for about 5 minutes. Thalidomide was then added and mixed for an additional 25 minutes. The premix was passed through a roller compactor with a hammer mill at the blowdown of the roller compactor and returned t...

Embodiment 3

[0085] 5.3. Example 3: Dosage Units of Thalidomide of the Prior Art

[0086] Table 4 illustrates the prior art batch formulation and single dose unit formulation for 50 mg, 12.5% ​​by weight thalidomide single dose unit #0 capsules.

[0087] Material

weight%

Quantity (mg / tablet)

Quantity (kg / batch)

Thalidomide

12.5％

50.0

7.50

microcrystalline cellulose

15.0％

60.0

9.00

Kollidon 90F

USP 1

3.0％

12.0

1.80

Stearic acid NF

1.0％

4.0

0.60

colloidal silica

0.2％

0.8

0.12

Crospovidone NF

4.0％

16.0

2.40

Anhydrous Lactose NF

64.3％

257.3

38.58

total

100.0％

400.0mg

60.00kg

[0088] 1 Also produced by BASF as Povidone 90F USP

[0089] Microcrystalline cellulose, KOLLIDON 90F, stearic acid, colloidal silicon dioxide, crospovidone and anhydrous lactose w...

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PUM

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Abstract

Pharmaceutical compositions and single unit dosage forms of thalidomide and pharmaceutically acceptable prodrugs, salts, solvates, hydrates, or clathrates are disclosed. Also disclosed are methods of treating and preventing diseases and conditions such as, but not limited to, leprosy, chronic graft-vs-host disease, rheumatoid arthritis, sarcoidosis, an inflammatory condition, inflammatory bowel disease, and cancer using the novel dosage forms disclosed herein.

Description

[0001] This application claims priority to provisional application 60 / 426,016, filed November 14, 2002, which is hereby incorporated by reference in its entirety. technical field [0002] The present invention relates in part to pharmaceutical compositions and dosage forms comprising thalidomide and pharmaceutically acceptable prodrugs, salts, solvates, hydrates and clathrates thereof. Background technique [0003] Thalidomide is a racemic compound commercially available under the trade name THALOMID®, and its chemical name is α-(N-phthalimide) glutarimide or 2-(2,6-dioxo- 3-piperidinyl)-1H-isoindole-1,3-(2H)-dione. Thalidomide was originally developed for the treatment of morning sickness, but it was withdrawn due to tetragenic effects. Thalidomide is currently approved in the United States for the treatment of human erythema nodosum leprosy. Physician's Desk Reftrence(R), 1081-1085 (edition 55, 2001). [0004] Thalidomide has been reported to be used in patients with le...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K9/20A61K31/454
CPCA61K9/2054A61K9/4866A61K9/4858A61K9/2031A61K31/454A61P1/00A61P1/04A61P19/02A61P19/04A61P29/00A61P31/08A61P35/00A61P35/02A61P37/02A61P37/06A61K9/48
Inventor P·德安吉奥
Owner CELGENE CORP
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