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Inhalant containing chloroquine therapeutic agent and preparation method of inhalant

A technology for a therapeutic agent and an inhalant, which is applied to the field of inhalants containing chloroquine therapeutic agents and the preparation thereof, can solve the problems of heavy reaction, low utilization rate, long course of treatment, etc., and achieves enhanced stability and improved use efficiency. , strong targeting effect

Inactive Publication Date: 2021-10-29
DISCOVERY SHENZHEN NEW MEDICINES DEV CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Chloroquine phosphate is currently sold at home and abroad as oral preparations. Oral preparations are more convenient to use, but the onset is slow and the utilization rate is low, accompanied by dizziness, headache, vertigo, loss of appetite, nausea, vomiting, abdominal pain, diarrhea, skin itching, rash, Even exfoliative dermatitis, tinnitus, irritability and other adverse reactions, the course of treatment is long, there may be serious reactions when the dosage is large, and the common one is the toxicity to the eyes

Method used

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  • Inhalant containing chloroquine therapeutic agent and preparation method of inhalant
  • Inhalant containing chloroquine therapeutic agent and preparation method of inhalant
  • Inhalant containing chloroquine therapeutic agent and preparation method of inhalant

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] A kind of chloroquine phosphate powder spray for inhalation, its prescription consists of

[0040]

[0041] Preparation Process:

[0042] (1) dissolving leucine in water for injection, adding chloroquine phosphate and mannitol, stirring to form a uniform solution;

[0043] (2) adopt spray drying technology to carry out spray drying to above-mentioned solution, obtain chloroquine phosphate inhalation powder spray;

[0044] The spray drying process conditions are: air inlet temperature: 118°C±2°C; material temperature: 60°C, atomization pressure: 170kPa, liquid feed rate: 12.0mL / min, solid-liquid content of the mixture: 15mg / mL.

[0045] (3) Fill the dried chloroquine phosphate dry powder in 3#HPMC vegetable capsules, and then seal them with a capsule encapsulation machine.

Embodiment 2

[0047] A kind of hydroxychloroquine sulfate powder spray for inhalation, its prescription consists of

[0048]

[0049]

[0050] Preparation Process:

[0051] (1) dissolving leucine in water for injection, adding hydroxychloroquine sulfate and mannitol, stirring to form a uniform solution;

[0052] (2) adopt spray drying technology to carry out spray drying to above-mentioned solution, obtain hydroxychloroquine sulfate powder mist inhalation;

[0053] The spray drying process conditions are: air inlet temperature: 118°C±2°C; material temperature: 60°C, atomization pressure: 170kPa, liquid feed rate: 12.0mL / min, solid-liquid content of the mixture: 15mg / mL.

[0054] (3) Fill the dried hydroxychloroquine sulfate dry powder in 3#HPMC vegetable capsules, and then seal them with a capsule encapsulation machine.

Embodiment 3

[0056] A kind of hydroxychloroquine sulfate powder spray for inhalation, its prescription consists of

[0057]

[0058] Preparation Process:

[0059] (1) dissolving leucine in water for injection, adding hydroxychloroquine sulfate and lactose, stirring to form a uniform solution;

[0060] (2) adopt spray drying technology to carry out spray drying to above-mentioned solution, obtain hydroxychloroquine sulfate powder mist inhalation;

[0061] The spray drying process conditions are: air inlet temperature: 118°C±2°C; material temperature: 60°C, atomization pressure: 170kPa, liquid feed rate: 12.0mL / min, solid-liquid content of the mixture: 15mg / mL.

[0062] (3) Fill the dried hydroxychloroquine sulfate dry powder in 3#HPMC vegetable capsules, and then seal them with a capsule encapsulation machine.

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Abstract

The invention provides a chloroquine inhalant and a preparation method thereof, and belongs to the field of medicine preparations. The inhalant comprises chloroquine phosphate or hydroxychloroquine sulfate, a stabilizer and a diluent, can improve use efficiency, has a preventive effect, such as a new epidemic situation-COVID-19, and can take effect quickly. The powder inhalation has better stability, has the effects of masking taste, enhancing stability and protecting organism biological membranes on chloroquine phosphate or hydroxychloroquine sulfate after being wrapped by the stabilizer, is absorbed through the lungs, has a high targeting effect, also can effectively avoid the first-pass effect caused by the liver during oral administration, and improves bioavailability.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an inhalant containing chloroquine therapeutic agents and a preparation method thereof. Background technique [0002] Chloroquine Phosphate (Chloroquine Phosphate) is an antimalarial drug, which is obtained by optimizing the structure of the oldest antimalarial drug quinine (Cinchona Cream), and its chemical name is 7-chloro-4-[[[4-( Diethylamino)-1-methylbutyl]amino]quinoline phosphate (1:2), the molecular formula is C 18 h 26 ClN 3 2H 3 PO 4 , the molecular weight is 515.87. [0003] [0004] Hydroxychloroquine sulfate (hydroxychloroquine sulfate) is an antimalarial drug. Like chloroquine, hydroxychloroquine is a weak base, which can exert its effect by concentrating the acidic vesicles of parasites and inhibiting the polymerization of heme. interact to inhibit certain enzymes. The chemical name is 2-[[[4-[(7-chloro-4-quinolyl)amino]pentyl]ethylamino]ethanol...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K31/4706A61K47/18A61P31/14A61P11/00
CPCA61K9/12A61K9/0073A61K31/4706A61K47/183A61P31/14A61P11/00
Inventor 张哲峰侯雯徐彬彬张爱琴
Owner DISCOVERY SHENZHEN NEW MEDICINES DEV CO LTD
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