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Modified release formulation and methods of use

一种调控释放、制剂的技术，应用在有效治疗神经系统过度兴奋的药物制剂领域，能够解决浓度水平波动等问题

Inactive Publication Date: 2014-03-05
VALEANT INT PHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, once released the active ingredient can still exhibit fluctuations in blood concentration levels

Method used

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  • Modified release formulation and methods of use
  • Modified release formulation and methods of use
  • Modified release formulation and methods of use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment I

[0086] Composition and ratio of modified release formulations

[0087] This example illustrates the composition and composition ratio of the formulation of the compound of formula I.

[0088] Table 1 provides the ingredients and their ratios used to formulate the pharmaceutical composition into a modified release dosage form. For all the following examples, the proportion of active ingredients used in the total dosage form varies from 35% to 65%, and the proportions of the remaining binders, disintegrants, surfactants, release modifiers, glidants or lubricants are shown in the table 1 range shown. Dry blending for direct compression or wet granulation of a portion of the formulation or wet granulation of the entire formulation can be used to produce granules and tablets.

[0089] Table 1. Exemplary Modified Release (MR) Formulations of Retigabine

[0090]

Embodiment II

[0092] Preparation of Modified Release Formulations

[0093] This example illustrates the method for preparing the modified release formulation of the present invention, and provides the constituent components and their respective ratios for formulating the modified release formulation of the present invention.

[0094] The methods described herein will be understood by those skilled in the art, since many such methods are well known in the art. Table 2 shows the ingredients and ratios used in the formulation of several embodiments of the claimed invention. It will be appreciated that the amounts and ratios of the constituents used in Tables 1 and 2 may be subdivided into smaller or larger amounts while maintaining the compositional ratios to produce different modified release formulations of the invention. It should be further understood that such ratios of constituents are also within the scope of the claims and the scope of the present invention.

[0095] Modified relea...

Embodiment III

[0108] Preparation of Modified Release Formulations Containing Different Amounts of Active Ingredient

[0109] This example describes the composition and ratios of several modified release formulations of the invention containing 200 mg retigabine.

[0110] Several modified release formulations were prepared with 200 mg retigabine and different proportions of the components of the present invention. Table 4 provides several modified release formulations containing 200 mg retigabine. In parentheses are the composition ratios per milligram tablet. For Formulation 9, additional granular SDS was used to prepare the composition. It will be appreciated that one skilled in the art can use larger or smaller partitioned components, as described in Table 4, while maintaining the ratios of the components, to produce similar modified release formulations. It is also understood that such allocations are within the scope of the present invention.

[0111] Modified release formulations...

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Abstract

A modified release pharmaceutical formulation includes about 30-70% N-(2-amino-4-(fluorobenzylamino)-phenyl)carbamic acid ethyl ester (retigabine), or a pharmaceutically acceptable salt, solvate or hydrate thereof, about 5-30% of a drug delivery matrix including hydroxypropylmethylcellulose (HPMC), about 1.0-10% of an anionic surfactant, and an enteric polymer. The pharmaceutical formulation produces a sustained plasma concentration of retigabine following administration to a subject for 4-20 hours longer than the time required for in vitro release of 80% of retigabine. A formulation includes about 30-70% N-(2-amino-4-(fluorobenzylamino)-phenyl)carbamic acid ethyl ester (retigabine), or a pharmaceutically acceptable salt, solvate or hydrate thereof, about 5-30% of a drug delivery matrix, and an agent for retarding release in the gastric environment. The plasma concentration vs. time profile of this formulation is substantially flat over an extended period lasting for about 4 hours to about 36 hours. A method of treating a disorder characterized by nervous system hyperexcitability includes administering to a subject an effective amount of these pharmaceutical formulations.

Description

Background of the invention [0001] This application claims priority to US Provisional Application No. 61 / 082,162, filed July 18, 2008, which is hereby incorporated by reference in its entirety. [0002] The present invention relates to a pharmaceutical composition, more particularly to a pharmaceutical preparation for effectively treating nervous system hyperexcitability. [0003] Many solid oral pharmaceuticals such as tablets or capsules are formulated to release the active ingredient immediately after ingestion. Generally, this immediate release (IR) dosage form results in very high initial plasma levels followed by a rapid decline. A possible consequence of an immediate-release dosage form is that patients experience fluctuations in different blood levels, which may result in a brief therapeutic overload followed by a period of therapeutic underdosing. These fluctuations or peaks and valleys in blood levels are difficult to regulate, reducing the overall therapeutic effe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/44
CPCA61K9/2013A61K9/2009A61K31/44A61K9/2054A61K9/2027A61P21/02A61P25/00A61P25/08A61P29/00A61P29/02A61K9/20A61K9/28
Inventor 比利安娜·纳吉松巴蒂
Owner VALEANT INT PHARM
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