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A kind of roflumilast solid dispersion and preparation method thereof and roflumilast preparation

A technology of solid dispersion and roflumilast, which is applied in the directions of non-active ingredients such as medical preparations, pharmaceutical formulations, and active ingredients of heterocyclic compounds, can solve the problems of low bioavailability and slow dissolution rate, and achieve bioavailability. high degree of effect

Active Publication Date: 2017-09-29
BEIJING COLLAB PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Since roflumilast is a BCS2 drug, it is an extremely difficult to dissolve drug, so there are problems such as slow dissolution rate and low bioavailability

Method used

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  • A kind of roflumilast solid dispersion and preparation method thereof and roflumilast preparation
  • A kind of roflumilast solid dispersion and preparation method thereof and roflumilast preparation
  • A kind of roflumilast solid dispersion and preparation method thereof and roflumilast preparation

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preparation example Construction

[0040] The invention provides a preparation method of roflumilast solid dispersion, comprising the following steps:

[0041] a), the carrier is heated and melted to obtain a carrier melt;

[0042] The carrier is copovidone, poloxamer or polyethylene glycol;

[0043] b), the carrier melt is mixed with Roflumilast;

[0044] c), mixing the obtained mixture, cooling and crushing to obtain a solid dispersion of roflumilast.

[0045] In the present invention, the carrier is first heated and melted to obtain a carrier melt. The carrier is copovidone, poloxamer or polyethylene glycol.

[0046] The carrier melt and roflumilast are then mixed. The mass ratio of the carrier to roflumilast is preferably 3-10:1. The mixing method of the carrier melt and roflumilast is preferably stirring.

[0047] In some embodiments of the present invention, the solubilizer is preferably added during the mixing process of the carrier melt and roflumilast, and the process is: mixing the carrier melt,...

Embodiment 1

[0072] Preparation of Roflumilast Solid Dispersion

[0073] 5g copovidone (S-630) was heated and melted to obtain a melt. Add 1 g of roflumilast to the melt, stir to dissolve. The copovidone melt dissolved with roflumilast was poured on an iron plate at -20°C and cooled rapidly. The obtained solid was cooled and pulverized and passed through an 80-mesh sieve to obtain a solid dispersion of roflumilast.

[0074] Carry out DSC scanning and X-ray powder diffraction analysis to the above-mentioned obtained roflumilast solid dispersion, get copovidone-roflumilast physical mixture, pure copovidone and pure roflumilast parallel determination simultaneously, the result Such as figure 1 and figure 2 as shown, figure 1 It is the DSC scanning figure of the roflumilast solid dispersion prepared in Example 1 of the present invention, wherein A is pure copovidone, B is pure roflumilast, C is roflumilast solid dispersion, and D is copolymerization Vitone-roflumilast physical mixture; ...

Embodiment 2

[0077] Preparation of Roflumilast Solid Dispersion

[0078] 5g copovidone (S-630) was heated and melted to obtain a melt. Add 100 mg of polyoxyethylene hydrogenated castor oil (RH-40) to the melt, stir to dissolve, then add 1 g of roflumilast, and stir to dissolve. The copovidone melt dissolved with polyoxyethylene hydrogenated castor oil and roflumilast was poured on an iron plate at -20°C, and cooled rapidly. The obtained solid was cooled and pulverized and passed through an 80-mesh sieve to obtain a solid dispersion of roflumilast.

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Abstract

The application belongs to the field of medicines, and in particular relates to a solid dispersion of roflumilast, a preparation method thereof and a preparation of roflumilast. The solid dispersion of roflumilast provided by this application, in parts by weight, includes: 1 part of roflumilast; 3 to 10 parts of carrier; the carrier is copovidone, poloxamer or polyethylene glycol diol. The roflumilast preparation provided by the present application includes, in parts by weight: 0.4-12 parts of the above-mentioned solid dispersion; 5-95 parts of filler. Experimental results show that the 30-minute dissolution rate of the roflumilast solid dispersion provided by the application is higher than 96%; the 30-minute dissolution rate of the roflumilast preparation provided by the application is higher than 98%, and the bioavailability is higher than 75%. %.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to a roflumilast solid dispersion, a preparation method thereof and a roflumilast preparation. Background technique [0002] Chronic obstructive pulmonary disease (COPD) is a chronic bronchitis or emphysema characterized by airflow obstruction, which can further develop into a common chronic disease of pulmonary heart disease and respiratory failure, with high morbidity and mortality. [0003] The exact etiology of COPD is unclear, but it is generally believed that factors related to the occurrence of chronic bronchitis and obstructive emphysema may be involved in the pathogenesis of COPD. The pathogenic factors that have been found can be roughly divided into two categories: environmental factors and individual susceptibility factors. Environmental factors include smoking, inhalation of dust and chemicals, air pollution, respiratory infections, etc. Individual predisposing fa...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K31/44A61K47/32A61K47/10A61P11/00
Inventor 张永强王珂赵大龙邹德超
Owner BEIJING COLLAB PHARMA
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