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Metaxalone preparations

A technology of metaxalone and dosage form, applied in the field of metaxalone preparations

Inactive Publication Date: 2020-03-24
ICEUTICA PTY LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, these animal studies do not necessarily predict the pharmacokinetic properties of drug products in humans

Method used

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  • Metaxalone preparations
  • Metaxalone preparations
  • Metaxalone preparations

Examples

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[0076] (1) Surfactants and polymers, including but not limited to polyethylene glycol, polyvinylpyrrolidone (PVP), polyvinyl alcohol, crospovidone, polyvinylpyrrolidone-polyvinyl acrylate copolymer, cellulose derivatives , hydroxypropylmethylcellulose, hydroxypropylcellulose, carboxymethylethylcellulose, hydroxypropylmethylcellulose phthalate, polyacrylates and polymethacrylates, urea, sugar polyols, and their polymers, emulsifiers, sugar gums, starches, organic acids and their salts, vinylpyrrolidone and vinyl acetate; and / or

[0077] (2) Binders such as various celluloses and cross-linked polyvinylpyrrolidone, microcrystalline cellulose; and / or

[0078] (3) fillers such as lactose monohydrate, anhydrous lactose, microcrystalline cellulose, and various starches; and / or

[0079] (4) Lubricants such as agents that act on the fluidity of the powder to be compressed, including colloidal silicon dioxide, talc, stearic acid, magnesium stearate, calcium stearate, silica gel; and / or...

Embodiment 1

[0110] Embodiment 1: the dry grinding of metaxalone

[0111] Chemically, metaxalone is 5-[3,5-dimethylphenoxy)methyl]-2-oxazolidinone. The empirical formula is C12H15NO3, which corresponds to a molecular weight of 221.25 g / mol. Metaxalone is a white to almost white, odorless crystalline powder, readily soluble in chloroform, soluble in methanol and 96% ethanol, but practically insoluble in ether or water. The mechanism of action of metaxalone in humans has not been established, but may be due to general central nervous system depression.

[0112] Submicron sized metaxalone drug substance particles were prepared by dry milling metaxalone drug substance (40%) with lactose monohydrate and sodium lauryl sulfate in an attritor mill containing stainless steel grinding media. The total batch size is approximately 1 kg. The ground powder is discharged to the bottom of the mill and collected for analysis and further processing. The particle size distribution of the milled metaxalon...

Embodiment 2

[0116] Embodiment 2: the preparation and characterization of submicron metaxalone tablet

[0117] The milled powder is compressed into tablets using a dry granulation process. Briefly, milled powders were mixed with binders, disintegrants, and lubricants and then transformed into free-flowing granules using a roller compaction system (TFC-Lab Micro, Freund Vector). These granules are mixed with additional disintegrants, binders and lubricants and compressed to produce tablets with a potency of 300 mg. The tablets were tested for dissolution at the initial time point and at 2 and 4 weeks. Stability conditions were 25°C / 60%RH and 40°C / 75%RH. The results of this analysis are described in figure 2 middle. Dissolution was compared to 800 mg Skelaxin tablets. Dissolution was accomplished in a Sotax dissolution apparatus with 1000 ml of 0.01N HCl (pH = 2) at 37°C using a type 2 apparatus (paddle) set at a rotation speed of 100 rpm. An aliquot of the dissolution test solution w...

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Abstract

The invention describes a metaxalone dosage form containing metaxalone submicron particles and its application. The submicron dosage form has improved bioavailability relative to certain conventional metaxalone dosage forms.

Description

technical field [0001] The present disclosure relates to methods of producing metaxalone particles (e.g., nanoparticles) using dry milling, as well as compositions comprising metaxalone, medicaments (including unit dosage forms) produced using metaxalone in nanoparticle form, and and / or compositions, and methods of treatment using metaxalone compositions. Background technique [0002] Poor bioavailability is an important problem encountered in the development of therapeutic compositions. Many factors affect bioavailability, including the dosage form and the solubility and dissolution rate of the active substance (drug substance). However, due to complex interactions in the human body, the pharmacokinetic properties of a specific drug product (eg, a specific dosage form) cannot be predicted based on the solubility of a drug substance. [0003] Metaxalone known as (King Pharmaceuticals, Inc.) is marketed as an adjunct to rest, physical therapy, and other methods used to re...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00
CPCA61K9/145A61K9/20A61K31/421C07D263/24A61P21/00A61P21/02A61P29/00
Inventor H·W·伯士
Owner ICEUTICA PTY LTD
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