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Anti-pulmonary fibrosis composition with improved dissolution property

A technology for pulmonary fibrosis and composition, which is applied in the field of anti-pulmonary fibrosis composition, can solve the problems of increasing drug dissolution, unexamined formation of dispersion stability, carrier interaction, recrystallization, etc., and achieves the effect of high solubility

Active Publication Date: 2020-11-24
NEOFORM BIOPHARMACEUTICAL LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The document International Journal of Nanomedicine 2018:13 8379–8393 introduced a solid dispersion of nintedanib prepared by electrospray technology, which can accelerate drug dispersion and dissolution under appropriate conditions, but did not examine the stability and Due to the interaction with the carrier, recrystallization may occur during the process and storage, which will affect the dissolution, and the method has high equipment costs and is not easy to scale up production
Some other patents also disclose nintedanib liposome, cyclodextrin inclusion complex, microemulsion preparation and its preparation technology, but only increase drug dissolution by physical means

Method used

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  • Anti-pulmonary fibrosis composition with improved dissolution property
  • Anti-pulmonary fibrosis composition with improved dissolution property
  • Anti-pulmonary fibrosis composition with improved dissolution property

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1: Nintedanib: Preparation of HPMCAS Salt

[0046] Add nintedanib free base and HPMCAS into a mixed solvent of methanol and dichloromethane (1:1 volume ratio) to form a solution, and an ionic bond is formed between the basic nintedanib and the acidic polymer HPMCAS.

[0047] Dissolve 1.2 g of HPMCAS in a certain volume of mixed solvent by magnetic stirring, then add 0.8 g of nintedanib free base and allow it to dissolve.

[0048] The resulting nintedanib containing 40% nintedanib (mass ratio):HPMCAS salt was passed through a Büchi micro spray dryer B290 equipped with an inert cycle B295 ( Labortechnik AG, Switzerland) spray-dried separation. A high-performance cyclone separator is used for separation, and the 50mL blue cap flask can be directly mounted to the cyclone separator for product collection. The parameter settings of the spray drying process are shown in Table 1.

[0049] Table 1

[0050] parameter Settings Suction 40kg / h In...

Embodiment 2

[0052] Embodiment 2: Nintedanib: Preparation of HPMCP salt

[0053] Add nintedanib free base and HPMCP into a mixed solvent of methanol and dichloromethane (1:1 volume ratio) to form a solution, and an ionic bond is formed between the basic nintedanib and the acidic polymer HPMCP.

[0054] 1.0 g of HPMCP was dissolved in a certain volume of mixed solvent by magnetic stirring, then 1.0 g of nintedanib free base was added and allowed to dissolve.

[0055] The resulting nintedanib containing 50% nintedanib (mass ratio): HPMCP salt was passed through a Büchi micro-spray dryer B290 equipped with an inert cycle B295 ( Labortechnik AG, Switzerland) spray-dried separation. A high-performance cyclone separator is used for separation, and the 50mL blue cap flask can be directly mounted to the cyclone separator for product collection. The parameter settings of the spray drying process are shown in Table 2.

[0056] Table 2

[0057] parameter Settings Suction 40kg / ...

Embodiment 3

[0059] Embodiment 3: Preparation of nintedanib amorphous

[0060] Nintedanib free base was added into a certain volume of dichloromethane to form a solution, which was then passed through a Büchi miniature spray dryer B290 equipped with an inert cycle B295 ( Labortechnik AG, Switzerland) spray-dried separation. A high-performance cyclone separator is used for separation, and the 50mL blue cap flask can be directly mounted to the cyclone separator for product collection. The parameter settings of the spray drying process are shown in Table 3.

[0061] table 3

[0062] parameter Settings Suction 40kg / h Inlet temperature 85℃ output temperature 60℃ Injection rate 5mL / min Atomizing airflow 0.5kg / h Inert loop cooling temperature -20℃

[0063] After spray drying, the product was placed in an oven at 50°C for 1 hour to remove excess solvent, and then XRPD was used to determine the physical state. The results were as follows: ...

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Abstract

The invention relates to an anti-pulmonary fibrosis composition with an improved dissolution property. The anti-pulmonary fibrosis composition comprises a salt formed by nintedanib and an acidic polymer. The salt formed by nintedanib and the acidic polymer has higher solubility and certain stability. The composition can be orally taken and is beneficial to dissolution and absorption of drugs in gastrointestinal tracts.

Description

technical field [0001] The present invention relates to the field of medicine, more specifically, to an anti-pulmonary fibrosis composition with improved dissolution properties. Background technique [0002] Idiopathic pulmonary fibrosis (IPF) is a progressive dyspnea and deterioration of lung function. Pulmonary fibrosis can be caused by a variety of factors, but the specific mechanism is still unclear. Their common characteristic is that the normal alveolar structure is damaged due to inflammation caused by various reasons at the beginning, resulting in alveolitis; the body repairs it with the accumulation of collagen scar tissue Inflammatory damage leads to fibrosis, leading to clinical symptoms such as dyspnea and hypoxia, and eventually respiratory failure. [0003] When the pulmonary fibrosis is mild, it is manifested as dyspnea and only occurs during strenuous activities; if the pulmonary fibrosis worsens, dyspnea may also occur at rest, and the entire course of the ...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61K9/14A61K47/38A61P11/00
CPCA61K31/496A61K9/146A61P11/00
Inventor 田芳高明张春良
Owner NEOFORM BIOPHARMACEUTICAL LTD
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