Hydroxychloroquine liposome inhalant and preparation method thereof

A technology for hydroxychloroquine lipid and inhalant, applied in the field of hydroxychloroquine liposome inhalation and preparation thereof, can solve the problems of inability to reach the lesion, slow absorption, adverse reactions, etc., and achieves reduction of adverse reactions, improvement of compliance, and improvement of drugs. therapeutic effect

Pending Publication Date: 2022-05-03
珠海润都制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method of administration not only absorbs slowly and cannot directly reach the lesion, but also causes the drug to accumulate in the non-lesion site along with the blood circulation, which in turn leads to the occurrence of adverse reactions

Method used

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  • Hydroxychloroquine liposome inhalant and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1: Its preparation method of a kind of hydroxychloroquine liposome inhalation

[0028] (1) Weigh an appropriate amount of phospholipids and cholesterol in an eggplant-shaped bottle according to the mass ratio of 4:1, add 10mL of ethanol and ultrasonically dissolve it completely. The eggplant-shaped flask was installed on a rotary evaporator, and the organic solvent was evaporated at 40°C. After the ethanol is completely volatilized, add 5 mL of ammonium sulfate solution (200 mmol / L) to the eggplant-shaped bottle, hydrate at 40 °C for 40 min, and after fully hydrated, sonicate for 5 min, and filter with a 0.22 μm filter membrane.

[0029] (2) Transfer the liquid in step 1 into a dialysis bag, place it in 250 mL of 1% glucose solution, dialyze in an air bath shaker at 37°C and 100 rpm / min, and replace the dialysis medium every 1 h. The dialysis medium needs to be changed 6 times during the whole dialysis process.

[0030] (3) After the dialysis, pour out the ...

Embodiment 2

[0032] Embodiment 2. The preparation of hydroxychloroquine liposome freeze-dried powder

[0033] (1) Weigh an appropriate amount of phospholipids and cholesterol, 100 mg in total, in an eggplant-shaped bottle according to a mass ratio of 4:1, add 10 mL of ethanol and ultrasonically dissolve it completely. The eggplant-shaped flask was installed on a rotary evaporator, and the organic solvent was evaporated at 40°C. After the ethanol was completely volatilized, 5 mL of ammonium sulfate solution (300 mmol / L) was added to the eggplant-shaped bottle, and hydrated at 40 °C for 40 min. After fully hydrating, it was sonicated for 5 min, and filtered with a 0.22 μm filter membrane.

[0034] (2) Transfer the liquid in step 1 into a dialysis bag, place it in 250 mL of 1% glucose solution, dialyze in an air bath shaker at 37°C and 100 rpm / min, and replace the dialysis medium every 1 h. The dialysis medium needs to be changed 6 times during the whole dialysis process.

[0035] (3) After...

Embodiment 3

[0037] Embodiment 3. The preparation of hydroxychloroquine liposome freeze-dried powder

[0038] (1) Weigh an appropriate amount of phospholipids and cholesterol (100 mg) in an eggplant-shaped bottle according to the mass ratio of 5:1, add 10 mL of ethanol and ultrasonically dissolve it completely. The eggplant-shaped flask was installed on a rotary evaporator, and the organic solvent was evaporated at 40°C. After the ethanol was completely volatilized, 5 mL of ammonium sulfate solution (400 mmol / L) was added to the eggplant-shaped bottle, hydrated at 40 °C for 40 min, and then ultrasonicated for 5 min after fully hydrating, and filtered with a 0.22 μm filter membrane.

[0039] (2) Transfer the liquid in step 1 into a dialysis bag, place it in 250 mL of 1% glucose solution, dialyze in an air bath shaker at 37°C and 100 rpm / min, and replace the dialysis medium every 1 h. The dialysis medium needs to be changed 6 times during the whole dialysis process.

[0040](3) After the d...

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Abstract

The invention provides a hydroxychloroquine lipidosome inhalant, the hydroxychloroquine lipidosome inhalant comprises hydroxychloroquine, phospholipid and cholesterol, and the dosage form of the hydroxychloroquine lipidosome inhalant is aerosol. According to the invention, the hydroxychloroquine is prepared into the liposome preparation, the medicine is wrapped in the liposome, so that the adverse taste stimulation can be reduced, the compliance of a patient is improved, and the medicine can directly reach the lung to exert the efficacy in a pulmonary administration mode of the hydroxychloroquine aiming at pneumonia, so that the curative effect of the medicine is improved, and the adverse reaction is reduced; the final preparation form is a freeze-dried product and is filled with nitrogen, the instability phenomenon of the liposome preparation in the storage and transportation process can be avoided, the stability of the preparation is improved, the novel hydroxychloroquine liposome preparation is used as a novel hydroxychloroquine preparation, the blank of the preparation is made up, and a better choice is provided for patients taking drugs for different diseases.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a hydroxychloroquine liposome inhalation and a preparation method thereof. Background technique [0002] The main problem of oral hydroxychloroquine treatment may be serious side effects and toxicity, which is mainly caused by the inconsistent accumulation concentration of the drug on alveolar target cells, depending on intestinal absorption, hepatic first-pass metabolism, etc. By preparing it into an inhalation, the drug can be targeted to act on the patient's lungs, thereby reducing the dosage, thereby reducing systemic adverse reactions and improving patient compliance. [0003] Hydroxychloroquine is a crystalline powder with a bitter taste. Bad smells such as bitterness of drugs are important constraints to improving patients' medication compliance. Appropriate and effective taste masking methods can improve patients' compliance, increase curative effect, and imp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K9/127A61K9/12A61K47/28A61K47/24A61K31/4706A61P11/00A61P31/14
CPCA61K9/127A61K9/0078A61K47/28A61K47/24A61K31/4706A61P11/00A61P31/14
Inventor 张诚诚刘杰谢斌关东张贵明兰柳琴
Owner 珠海润都制药股份有限公司
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