Nanoparticulate formulations and methods for the making and use therof

Inactive Publication Date: 2009-01-01
MARINUS PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0078]A “therapeutically effective amount” or “effective amount” is that amount of a pharmaceutical agent to achieve a pharmacological effect. The term “therapeutically effective amount” includes, for example, a prophylactically effective amount. An “effective amount” of drug is an amount needed to achieve a desired pharmacologic effect or therapeutic improvement without undue adverse side effects. The effective amount of a drug will be selected by those skilled in the art depending on the particular patient and the disease. It is understood that “an effective amount” or “a therapeutically effective amount” can vary from subject to subject, due to variation in metabolism of drug, age, weight, gene

Problems solved by technology

The drugs that would benefit from this approach are l

Method used

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  • Nanoparticulate formulations and methods for the making and use therof
  • Nanoparticulate formulations and methods for the making and use therof
  • Nanoparticulate formulations and methods for the making and use therof

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of USP Simulated Gastric and Intestinal Fluid

Simulated Intestinal Fluid (SIF)

[0352]Monobasic potassium phosphate (6.8 g) and sodium hydroxide (0.616 g) are added into 250 ml of distilled water in a 1000 ml volumetric flask and swirled until dissolved. 700 ml distilled water is added and the pH checked. The pH is adjusted to pH 6.8+ / −0.1 by adding either 0.2N sodium hydroxide or 0.2N hydrochloric acid and the volume is brought to 1000 ml.

Simulated Gastric Fluid (SGF)

[0353]Sodium chloride (2 g), 750 ml distilled water, and 7.0 ml of concentrated hydrochloric acid are added into a 1000 ml volumetric flask. The flask is swirled to mix and the volume brought to 1000 ml with distilled water. The pH should be approx. 1.2.

example 2

Particle Size Measurement Method

[0354]The following methods and settings for particle size measurement were used for all D50 values for ganaxolone and phenyloin.

Particle Size Method Using Horiba Laser Scattering Particle Size Distribution Analyzer LA-910

[0355]Particle size measurement using Horiba laser scattering particle size distribution analyzer is generally well known for those skilled in the art. It is important that the parameters be kept constant when measuring different samples if they are used for comparison purposes. For ganaxolone and phenyloin nanoparticulate compositions, instrument settings and sample preparation method are described below:

Instrument Settings and Parameters:

[0356]Measure Conditions: Circulation=4; ultrasonic time=1; agitation=1; sampling times: red laser=10, blue lamp=2; preferred % transmittance: blue lamp=75-80%; blank: red laser=10, blue lamp=2. For D50 values after sonication, the sonication power is set to low and the sonication time is 1 minute....

example 2a

Sample Preparation and Particle Size (D50) Determination

[0359]For concentrated nanoparticle drug suspensions, dilute the nanoparticulate composition with deionized water to approximately 5 mg / mL API concentration. Shake well for 15-30 seconds. Add 120 mL of deionized water to the chamber, turn agitation and recirculation settings on. Transfer the nanoparticulate suspension via a pipette to the sample chamber in sufficient quantity to reach the transmittance range of 75-80% blue lamp. If a suspension or stability indicating dispersion is at a concentration of approximately 0.5 mg / ml do not further dilute if not necessary and use directly for particle size measurement. Transfer the sample to be measured via a pipette to up to the desired transmittance range (75-80% blue lamp). Take a measurement and collect the D50 value. This will be the unsonicated particles size. Sonicate for 1 min and take a measurement again to collect D50 value. This will be the particle size after 1 minute soni...

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Abstract

The present invention is directed to size-stabilized drug nanoparticulate compositions and methods of preparation thereof.

Description

[0001]This application claims the benefit of U.S. Provisional Patent Application No. 60 / 861,616, filed on Nov. 28, 2006, the disclosure of which is hereby incorporated by reference in its entirety.FIELD OF THE INVENTION[0002]Described herein are nanoparticulate formulations of drugs having an aqueous solubility of less than 1 mg / ml in a pH of about 7.4 which provide enhanced stability, physical and chemical properties and can provide enhanced pharmacokinetic properties to achieve an optimal balance between pharmacodynamic and side effect profiles in mammals, and dosage forms containing the same, as well as methods of making nanoparticulate drug formulations and their use in the treatment of various disorders.BACKGROUND OF THE INVENTION[0003]It has been very difficult to formulate therapeutically effective dosage forms specific for drugs having an aqueous solubility of less than 1 mg / ml in a pH of about 7.4, across a broad range of therapeutic agents (e.g. medroxyprogesterone acetate...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K9/14A61K9/20
CPCA61K9/1623A61K9/0075A61K9/2886A61K9/5078A61K47/48961B82Y5/00A61K31/58A61K8/63A61K9/145A61K47/14C07J71/00Y10S977/906Y10S977/773A61K9/007A61K9/0073A61K9/008A61K9/0078A61K9/1652A61K47/6949A61P11/00A61P17/04A61P27/02A61K47/50A61K9/10A61K9/16
Inventor SHAW, KENNETHZHANG, MINGBAO
Owner MARINUS PHARMA
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