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Fast release composition including melt granules of a moisture sensitive drug and process for manufacturing thereof

A composition and sensitive technology, applied in the direction of drug combination, active ingredients of heterocyclic compounds, metabolic diseases, etc., can solve problems such as chemical instability and difficulty in making pharmaceutically acceptable oral compositions

Active Publication Date: 2007-08-01
NOVARTIS AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moisture-sensitive therapeutic compounds may be difficult to formulate into pharmaceutically acceptable oral compositions due to their chemical instability

Method used

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  • Fast release composition including melt granules of a moisture sensitive drug and process for manufacturing thereof
  • Fast release composition including melt granules of a moisture sensitive drug and process for manufacturing thereof
  • Fast release composition including melt granules of a moisture sensitive drug and process for manufacturing thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0095] Solid oral dosage forms prepared by dry mixing

[0096] Compound I was first passed through a 25 mesh screen and 11.2 g were obtained. Compound I and 100 g of lactose were placed in a 1 quart V-blender and tumbled for 5 minutes. Transfer the mixture to a 25 mesh screen and return to the V-blender. The talc, crospovidone and remaining lactose were then added to the V-blender and the mixer was inverted for an additional 10 minutes. Separately, pass the hydrogenated castor oil through a 60 mesh screen. The hydrogenated castor oil was then added to the V-blender and tumbled for 5 minutes. The blend was then compressed on a Manesty B3B tablet press using round, standard concave and beveled edge dies. To prevent sticking, polish the mold beforehand. The obtained 150 mg tablet contains about 5 mg of Compound I and is designated herein as "Sample 1". Sample 1 contained no Compound I particles coated or substantially coated with hydrogenated castor oil.

Embodiment 2

[0098] Solid oral dosage form prepared from melt-granulated granules using hydrogenated castor oil

[0099] As a comparison with Sample 1, a solid oral dosage form was prepared from melt-granulated Compound I. Compound I and the hydrophobic melt component, hydrogenated castor oil, were passed through 25 mesh and 60 mesh sieves, respectively. These ingredients were then added to the 1 L pan of a Key International (Englishtown, NJ) Model KG5 high shear granulator.

[0100] A heating mantle surrounds the pan and sets the rheostat at 80°C. This granulator is equipped with an impeller and no chips. Turn on the impeller to mix the therapeutic compound and hydrophobic melt components.

[0101] After mixing, the granules were removed from the pan and spread onto aluminum foil to cool. These granules were then sieved with a Frewitt shaker.

[0102] These granules were then transferred to a V-blender filled with microcrystalline cellulose and crospovidone. The V-blender was turned...

Embodiment 3

[0106] Solid oral dosage form prepared from melt-granulated granules using stearic acid

[0107] As a comparison with Sample 1 and Sample 2, another solid oral dosage form was prepared from melt-granulated granules of Compound I. The same procedure as disclosed in Example 2 was used; however, all of the hydrogenated castor oil was replaced with stearic acid. Thus, stearic acid is a hydrophobic melt component in the melt-granulated granules and a lubricant for the tablet itself. These tablets are designated herein as "Sample 3".

[0108] Table 1 summarizes the compositions of samples prepared in Examples 1, 2, and 3.

[0109] Table 1

[0110]

sample

sample 1

(mg)

sample 2

(mg)

sample 3

(mg)

Compound I

Hydrogenated castor oil as melt component

Stearic acid as molten component

Spray-dried lactose as a bulking agent

Crospovidone as a disintegrant

Talc as an anti-sticking agent

Hydrogenated castor oil as a lubr...

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PUM

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Abstract

Solid oral dosage forms that include melt granules of a moisture-sensitive therapeutic compound and a hydrophobic melt component. The melt granules better protect the therapeutic compound from hydrolytic degradation. Such solid oral dosage forms also possess immediate-release characteristics rather than that associated with extended-release or controlled-release drug products.

Description

field of invention [0001] The present invention relates to immediate-release pharmaceutical compositions comprising a moisture-sensitive therapeutic compound and a hydrophobic melt component. The present invention also relates to methods of preparing such immediate release pharmaceutical compositions. Background of the invention [0002] A factor that can limit the commercial prospects of therapeutic compounds is the compound's susceptibility to moisture. Moisture sensitive therapeutic compounds can be difficult to formulate into pharmaceutically acceptable oral compositions due to their chemical instability. This chemical instability may be particularly pronounced when the moisture sensitive therapeutic compound is used in dosage forms containing excipients with high equilibrium water content. Moisture can migrate from such excipients and cause hydrolytic degradation of the moisture sensitive therapeutic compound. [0003] One method used to minimize chemical instability...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/20
CPCA61K9/1617A61K9/2095A61P3/00A61P3/10A61K31/40A61K9/2081
Inventor J·科瓦尔斯基O·卡尔布A·T·M·塞拉尤迪恩Y·乔希
Owner NOVARTIS AG
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