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Metaxalone co-crystal

A technology of metaxalone and co-crystal, applied in the field of new crystalline compounds, can solve the problems of poor human bioavailability, failure, low bioavailability of active pharmaceutical ingredients, etc.

Inactive Publication Date: 2015-10-07
NUFORMIX TECH LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Like metaxalone, active pharmaceutical ingredients (API's), which are generally less water soluble and less bioavailable, pose huge problems for the pharmaceutical industry
Some drug candidates fail in the clinical phase due to poor human bioavailability and formulation-related issues, studies show

Method used

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  • Metaxalone co-crystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 11

[0068] Embodiment 1.1:1 metaxalone adipic acid cocrystal

[0069] Preparation of 1.11:1 metaxalone adipic acid co-crystal

[0070] Metaxalone (500 mg) and adipic acid (330 mg) were weighed into glass vials. Isopropanol (IPA, 1.67ml) was added to the bottle. The resulting slurry was aged for 5 days (8 hour cycle of RT to 50°C, heating to 50°C over 4 hours and then cooling to RT with an additional 4 hours). The product was then vacuum filtered over about 1 hour. An additional 100 μl of IPA was added to the filter and the product was left to dry overnight at ambient conditions.

[0071] XRPD Characterization of 1.21:1 Metaxalone Adipic Acid Cocrystal

[0072] The XRPD experimental figure of 1:1 metaxalone adipic acid cocrystal is shown in figure 1 middle. Table 1 lists the figure 1 Angle °2θ±0.2°2θ, d-spacing and intensity of peaks identified in the XRPD pattern. The entire list of peaks or a subset thereof may be sufficient to characterize the co-crystal. Can be used ...

Embodiment 2

[0082] Embodiment 2.1: 0.5 metaxalone fumaric acid cocrystal

[0083] Preparation of 2.11:0.5 metaxalone fumaric acid co-crystal

[0084] Metaxalone (500 mg) and fumaric acid (262 mg) were weighed into glass vials. Isopropanol (IPAc, 1.67ml) was added to the bottle. The resulting slurry was aged for 5 days (RT to 50°C for 8 hours cycle, heating to 50°C over 4 hours and then cooling to RT with an additional 4 hours). The product was then vacuum filtered for about 1 hour. An additional 100 μl of IPAc was added to the filter and the product was left to dry overnight at ambient conditions.

[0085] XRPD characterization of 2.21:0.5 metaxalone fumaric acid co-crystal

[0086] The XRPD experimental figure of 1:0.5 metaxalone fumaric acid co-crystal is shown in Figure 5 middle. Table 2 lists the Figure 5 Angle °2θ±0.2°2θ, d-spacing and intensity of peaks identified in the XRPD pattern. The entire list of peaks or a subset thereof may be sufficient to characterize the co-cry...

Embodiment 3

[0103] Example 3. Metaxalone 1:1 salicylic acid co-crystal

[0104] 3. Preparation of 11:1 metaxalone salicylic acid co-crystal

[0105] Metaxalone (100 mg) and salicylic acid (62.4 mg) were placed in a stainless steel ball mill. Water (2 drops) was added. The two components were milled together for 60 minutes at 20 Hz. The product was removed from the ball mill and left to dry overnight at room temperature.

[0106] XRPD characterization of 3.21:1 metaxalone salicylic acid co-crystal

[0107] The XRPD experimental figure of 1:1 metaxalone salicylic acid co-crystal is shown in Figure 12 middle. Table 4 lists the Figure 12 Angle °2θ±0.2°2θ, d-spacing and intensity of peaks identified in the XRPD pattern. The entire list of peaks or a subset thereof may be sufficient to characterize the co-crystal. Can be used alone or in combination to characterize the source of 1:1 metaxalone salicylic acid cocrystal Figure 12 A subset of peaks includes 6.8, 16.1, 17.2, 22.6 and 24.6...

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Abstract

The invention relates to improvements of the physiochemical and / or the pharmaceutical properties of metaxalone. Disclosed herein are several new cocrystals of metaxalone, including: a 1:1 metaxalone adipic acid cocrystal, a 1:0.5 metaxalone fumaric acid cocrystal, a 1:1 metaxalone salicyclic acid cocrystal, a 1:0.5 metaxalone succinic acid cocrystal, and a 1:0.5 metaxalone maleic acid cocrystal. The therapeutic uses of these metaxalone cocrystals are described as well as therapeutic compositions containing them.

Description

[0001] References to related applications [0002] This application claims priority to US Provisional Application 61 / 289,766, filed December 23, 2009, and US Provisional Application 61 / 381,244, filed September 9, 2009. The disclosures of both provisional applications are incorporated herein by reference. technical field [0003] The present invention relates to novel crystalline compounds comprising metaxalone, and more particularly, the present invention relates to metaxalone cocrystals, their therapeutic use and medicaments comprising them combination. Background technique [0004] Metaxalone shown below, 5-[(3,5-dimethylphenoxy)methyl]-2-oxazolidinone is used to relax muscles and relieve musculoskeletal effects caused by strains, sprains, and other Painful muscle relaxants (musclerelaxant) for medical conditions, especially muscle cramps and back pain. [0005] [0006] Metaxalone is a white to almost white, odorless crystalline powder largely soluble in chloroform,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D263/24A61K31/421A61P21/02
CPCC07D263/24A61K31/421C07C55/10C07C55/14C07C57/145C07C57/15C07C65/10A61P21/02
Inventor 琼安·霍兰克里斯托弗·弗兰普顿艾伦·乔尔顿丹尼尔·古丁
Owner NUFORMIX TECH LTD
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