Solid dispersoid of lesinurad and pharmaceutic adjuvant and preparation method of solid dispersoid

A technology for solid dispersions and pharmaceutical excipients, which can be used in pharmaceutical formulations, medical preparations containing active ingredients, and pharmaceutical combinations, etc. It can solve problems such as poor stability and unsuitability for medicinal use, and achieve good dispersion, dispersion and dissolution. Fast, easy-to-achieve effects

Inactive Publication Date: 2017-10-24
CHANGZHOU FANGNAN MEDICINE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Patent CN101817793B reports the amorphous lecisnard free acid, but due to its extremely poor stability, it is not suitable for medicinal use

Method used

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  • Solid dispersoid of lesinurad and pharmaceutic adjuvant and preparation method of solid dispersoid
  • Solid dispersoid of lesinurad and pharmaceutic adjuvant and preparation method of solid dispersoid
  • Solid dispersoid of lesinurad and pharmaceutic adjuvant and preparation method of solid dispersoid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Add Lescinard (5 g) and povidone K30 (10 g) into water (300 ml), heat to 60° C. and stir to dissolve. The above solution was dried with JISL micro-spray dryer LSD-48, the inlet temperature was maintained at 60°C and the outlet temperature was 50°C, and the outlet material was collected to obtain a white solid, which was further vacuum-dried to obtain the mixture of amorphous Resinard and povidone-K30 Solid dispersion. X-ray powder diffraction pattern as figure 1 As shown, in the X-ray powder diffraction pattern of the solid dispersion, after deducting the background peaks of the pharmaceutical excipients, there is no characteristic peak of the Recinard crystal form.

Embodiment 2

[0042]Add Resinard (1 g) and hydroxypropylmethylcellulose E50 (0.2 g) into water (10 ml), heat to 40°C and stir to dissolve. The above solution was freeze-dried to obtain a white solid, that is, a solid dispersion of amorphous Recinad and hydroxypropylmethylcellulose E50. In the X-ray powder diffraction pattern of the solid dispersion, the background peaks of pharmaceutical excipients were deducted There is no characteristic peak of the Raysinard crystal form.

Embodiment 3

[0044] Heat Resinard (1 g) and polyethylene glycol 8000 (50 g) to melt, and rapidly cool to room temperature with stirring to obtain a white solid. Pulverize the above solid to obtain a white powdery solid, that is, a solid dispersion of amorphous Resinard and polyethylene glycol 8000. In the X-ray powder diffraction pattern of the solid dispersion, after deducting the background peaks of pharmaceutical excipients No characteristic peaks of the Raycinard crystal form.

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Abstract

The invention discloses solid dispersoid of amorphous lesinurad and a pharmaceutic adjuvant and a preparation method of the solid dispersoid. The solid dispersoid is prepared from the lesinurad and the pharmaceutic adjuvant; the weight ratio of the lesinurad to the pharmaceutic adjuvant is 1 to (0.1 to 100), wherein the lesinurad is in an amorphous state; the X-ray powder diffraction spectrum of the solid dispersoid has no the characteristic peak of a crystal of the lesinurad after the background peak of the pharmaceutic adjuvant is deducted. The solid dispersoid of the amorphous lesinurad and the pharmaceutic adjuvant, which is provided by the invention, is favorable in stability and dispersity, is used for increasing the dissolution rate of the lesinurad, is used for more beneficially improving the bioavailability of a medicinal preparation and the absorption of an organism to a medicine, and in an accelerated test condition, can be used for maintaining favorable physical stability and chemical stability. The preparation method of the amorphous solid dispersoid, which is provided by the invention, is simple to operate, low in cost, good in repeatability and easy to realize, and is suitable for industrialized production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a solid dispersion of amorphous Recinard and pharmaceutical excipients and a preparation method thereof. Background technique [0002] Selexipag, chemical name 2-[[5-bromo-4-(4-cyclopropyl-1-naphthalene)-4H-1,2,4-triazol-3-yl]thio ] Acetic acid, trade name Zurampic, is a new oral uric acid excretion drug developed by AstraZeneca, which treats gout patients with hyperuricemia by inhibiting the uric acid transporter URATI in the renal proximal convoluted tubule. Compared with existing drugs, Resinard has a better safety profile. On December 22, 2015, the FDA approved Zurampic to be used in combination with xanthine oxidase inhibitors (XOI) to treat gout-related blood uric acid levels Excessively high (hyperuricemia), it is predicted that by 2018, it is expected to become the dominant player in the gout drug market. The structure of the drug is shown below: ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/4196A61P19/06
CPCA61K9/145A61K9/146A61K31/4196
Inventor 张席妮熊志刚资春鹏涂福荣
Owner CHANGZHOU FANGNAN MEDICINE TECH CO LTD
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