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

A technology of solid dispersion and pharmaceutical excipients, applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, drug combinations, etc., can solve the problems affecting drug bioavailability and low solubility, and achieve fast dispersion and dissolution, Good solubility and 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 CN102459198A discloses three crystal forms of Selesipah: Form I, Form II and Form III, wherein Form I is a thermodynamically stable crystal form with good stability, but the crystal form has low solubility in water , affecting the bioavailability of the drug

Method used

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

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Dissolve Selexipa (50 mg) in isopropanol (600 microliters) and water (900 microliters), heat to 60°C and stir to dissolve. The above solution was rapidly cooled to -10°C, and a white solid was precipitated, filtered, and dried to obtain amorphous seraxipa, and the X-ray powder diffraction pattern was as follows: figure 1 As shown, there is no characteristic peak of the crystal form of Selesipah in the X-ray powder diffraction pattern.

Embodiment 2

[0050] Dissolve Selexipah (50 mg) in ethanol (600 microliters) and water (600 microliters), and stir to mix evenly at 40°C. The above solution was slowly concentrated to dryness in a rotary evaporator to obtain a white solid, which gave amorphous selexipa, and the X-ray powder diffraction pattern was as follows: figure 2 As shown, there is no characteristic peak of the crystal form of Selesipah in the X-ray powder diffraction pattern.

Embodiment 3

[0052] Add Selexipa (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 a JISL micro-spray dryer LSD-48, and the inlet temperature was maintained at 60°C and the outlet temperature was 50°C. The outlet material was collected to obtain a white solid, which was further vacuum-dried to obtain a mixture of amorphous Selexipah and povidone-K30. Solid dispersion. X-ray powder diffraction pattern as image 3 As shown, in the X-ray powder diffraction pattern of the solid dispersion, there is no characteristic peak of the crystalline form of Selexipah after deducting the background peaks of the pharmaceutical excipients.

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Abstract

The invention discloses amorphous selexipag, which is characterized in that the characteristic peak of the selexipag does not exist in an X-ray powder diffraction spectrum. The invention discloses a preparation method of the amorphous selexipag, a solid dispersoid of the amorphous selexipag and a pharmaceutic adjuvant and a preparation method of the solid dispersoid. The solid dispersoid is prepared from the selexipag and the pharmaceutic adjuvant; the weight ratio of the selexipag to the pharmaceutic adjuvant is 1 to (0.1 to 100), wherein the selexipag is in an amorphous state; the X-ray powder diffraction spectrum of the solid dispersoid has no characteristic peak of a crystal of the selexipag after the background peak of the pharmaceutic adjuvant is deducted. The solid dispersoid of the selexipag 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 selexipag, 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 an amorphous seraxipa, and also relates to a solid dispersion of an amorphous seraxipa and pharmaceutical excipients and a preparation method thereof. Background technique [0002] Selexipag, the chemical name is 2-{4-[(5,6-diphenyl-2-pyrazinyl)(isopropyl)amino]butoxy}-N-(methylsulfonyl Acyl) acetamide, trade name Uptravi, its structure is as follows: [0003] [0004] The drug is a selective non-prostanoid IP prostacyclin receptor agonist developed by Nippon Shinyaku Co., Ltd. It is suitable for the treatment of pulmonary arterial hypertension (PAH, WHO group I) to delay disease progression and reduce the risk of hospitalization for PAH. Compared with existing drugs, Selexipah has a better safety profile and provides an additional treatment option for patients with pulmonary arterial hypertension. On December 21, 2015, the FDA approved Uptravi to be la...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D241/20A61K9/14A61K31/4965A61P9/12A61P11/00
CPCA61K9/145A61K9/146A61K31/4965C07D241/20
Inventor 张席妮熊志刚资春鹏王颖琦
Owner CHANGZHOU FANGNAN MEDICINE TECH CO LTD
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