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Formulations of (s)-3-(4-((4-(morpholinomethyl)benzyloxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione

A technology of dosage and excipients, applied in (S)-3-(4-((4-(morpholinylmethyl)benzyloxy)-1-oxoisoindoline-2-yl ) Preparation field of piperidine-2,6-dione

Active Publication Date: 2016-08-24
CELGENE CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, Compound A is prone to hydrolysis and has chemical stability issues

Method used

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  • Formulations of (s)-3-(4-((4-(morpholinomethyl)benzyloxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione
  • Formulations of (s)-3-(4-((4-(morpholinomethyl)benzyloxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione
  • Formulations of (s)-3-(4-((4-(morpholinomethyl)benzyloxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0283] 5.1 Example 1: Compound A Dosage Capsules

[0284] Table 1 illustrates the batch formulation and single dose formulation of a single dosage unit of Compound A at 0.3 mg strength in #4 capsules.

[0285] Table 1. Formulation of 0.3 mg Strength Compound A Capsules

[0286]

[0287] *Denotes the amount of the salt form of Compound A that provides the potency of 0.3 mg of the free base of Compound A (ie, the amount that provides 0.3 mg of 100% pure Compound A).

[0288] Compound A was premixed with a portion of anhydrous lactose and pregelatinized starch. Pass the premix through a 0.032 inch / 20 mesh screen. Grind the remaining lactose through a 0.032 inch / 20 mesh screen. Combine premix with remaining lactose. To this mixture was further blended stearic acid which passed through a 0.0232 inch / 30 mesh screen. The final blend was enclosed in #4 capsules.

[0289] Table 2 illustrates batch and single dose formulations of single dosage units of 0.1 mg strength Compound...

Embodiment 2

[0304] 5.2 Example 2: Stability of formulations

[0305] The accelerated stability of the 0.3 mg strength PD01-082 formulation (described in Table 1 above) and the other 0.3 mg strength formulations described in Tables 5-7 below were evaluated at 40°C / 75% RH and determined initial , 1-month, 3-month and 6-month time periods impurity levels. To determine impurity levels, the HPLC gradient method was employed using the following conditions:

[0306] Column: XBridge C18 column, 4.6×150mm, 3.5μm particle size

[0307] Temperature: autosampler: ambient temperature; column: 40°C

[0308] Mobile phase: A: 20mM ammonium acetate: acetonitrile (95:5, v / v)

[0309] B: 20mM ammonium acetate: acetonitrile (10:90, v / v)

[0310]

[0311] Flow rate: 1.0mL / min

[0312] Injection volume: 50μL

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Abstract

Pharmaceutical compositions and single unit dosage forms of (S)-3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a pharmaceutically acceptable stereoisomer, prodrug, salt, solvate, hydrate, or clathrate, are provided herein. Also provided are methods of treating, managing, or preventing various disorders, such as cancer, an inflammatory disease and / or an immune-related disorder.

Description

[0001] This patent application claims priority to US Provisional Patent Application Serial No. 61 / 888,419, filed October 8, 2013, which is incorporated herein by reference in its entirety. 1. Technical field [0002] Provided herein is (S)-3-(4-((4-(morpholinylmethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6- Formulations and dosage forms of diketone or CC-220. Also provided herein are methods of using the formulations and dosage forms. 2. Background of the invention [0003] Drug substances are usually administered as part of a formulation in combination with one or more other agents that serve different or specialized drug functions. By the selective use of pharmaceutical excipients different types of dosage forms can be prepared. Since pharmaceutical excipients have multiple functions and contribute to pharmaceutical formulations in many different ways, for example, dissolving, diluting, thickening, stabilizing, preserving, coloring, flavoring, etc. Properties th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48
CPCA61K9/4858A61K9/4866A61K31/5377A61K47/26Y02A50/30A61P1/04A61P1/16A61P11/06A61P13/08A61P13/12A61P15/00A61P17/00A61P17/14A61P19/02A61P19/08A61P21/02A61P21/04A61P25/00A61P27/16A61P29/00A61P3/00A61P35/00A61P37/00A61P37/02A61P5/14A61P9/14A61K47/14A61K47/36A61K9/0053
Inventor 达尔尚·帕瑞克阿尼尔·门诺
Owner CELGENE CORP
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