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Chloroquine spray and preparation method thereof

A technology of chloroquine and spray, which is applied in the direction of pharmaceutical formulations, antiviral agents, local antibacterial agents, etc., can solve the problems affecting the quality and curative effect of drugs, the low bioavailability of tablets, and the difficulty of dividing doses or coatings, etc., to achieve Achieve long-term protection, promote absorption and residence time, and have less toxic and side effects

Pending Publication Date: 2020-07-17
广州康健医学科技有限公司 +2
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, the main forms of chloroquine drugs on the market are injections and tablets. However, injections are generally used in professional institutions such as hospitals, mainly for acute and severe patients; the bioavailability of tablets is not high, and the drug stability is not good. Disadvantages such as small distribution area in the gastrointestinal tract, large irritation, poor fluidity, uneven size, difficult to divide doses or coating, long disintegration time, slow dissolution rate, large dosage, etc., directly affect the quality and efficacy of the drug
Moreover, chloroquine is a small molecule drug with a bitter taste and is easy to penetrate the cell membrane and accumulate in the cells. Studies have shown that large doses and long-term use will cause certain side effects, which can lead to serious complications such as deafness, retinopathy, and leukopenia, and Dizziness, gastrointestinal discomfort, skin itching, arrhythmia and other adverse reactions

Method used

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  • Chloroquine spray and preparation method thereof
  • Chloroquine spray and preparation method thereof
  • Chloroquine spray and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Example 1 Preparation of chloroquine phosphate spray

[0056] The chloroquine phosphate spray is composed of powder A and solution B; the powder A contains chloroquine phosphate, carrageenan and a sweetener, and the solution B is a potassium chloride aqueous solution containing borneol and menthol, and the pH value is adjusted to 6.0.

[0057] In terms of mass volume percentage, the dosage of each component is: 8% carrageenan, 1% sweetener, 0.8%-0.9% potassium chloride.

[0058] The amounts of chloroquine phosphate, borneol, menthol, and ethanol are shown in Table 1. A series of chloroquine phosphate sprays were prepared according to different proportions of chloroquine phosphate, borneol, menthol, and ethanol (alcohol).

[0059] The preparation method of powder A of the spray is: formulating carrageenan into an aqueous solution with a mass concentration of 10%-20%, adding sweetener, heating to 30-100°C, adding chloroquine phosphate, cooling, drying, and powdering to obtain pow...

Embodiment 2

[0064] Example 2 Bacteriostatic test of chloroquine phosphate spray

[0065] 1. Test the antibacterial effect of each group of chloroquine phosphate sprays prepared in Example 1.

[0066] The antibacterial test method is as follows: take the nutrient agar medium (Sabao's agar medium) of the 3rd to 14th generation of the strain and wash the lawn with 5mL 0.03mol / L phosphate buffer solution (hereinafter referred to as PBS) to make the bacteria Mix the solution uniformly, use a standard bacterial turbidity tube, dilute with the above PBS to a bacterial concentration of 5.0×l0 5 ~4.5×10 6 / mL of bacterial suspension.

[0067] Take 5 mL of the sample solution (sample 1:1 dilution) and 4 tubes of the control sample solution (sample without antibacterial components), add 100 μL of the above bacterial suspension respectively, mix well, and start timing for 2 minutes. Mix thoroughly and dilute appropriately. Take 0.5 mL of each dilution and place it on the culture medium of the corresponding...

Embodiment 3

[0081] Example 3 Quality test of chloroquine phosphate spray

[0082] The sprays shown in Table 5 were prepared with reference to Example 1, and the sprays of different formulations were tested in a double-blind manner, and the irritation, bitterness, stickiness of spraying into the oral cavity, and acceptability were scored after the trial. The statistical results of trial use of its products are shown in Table 5.

[0083] Table 5 Quality test of chloroquine phosphate spray

[0084]

[0085]

[0086] In this trial, the score was irritation from 1 to 10 points, the higher the score, the stronger the irritation; the bitterness from 1 to 10 points, the higher the score, the stronger the bitterness; the viscosity from 1 to 10 points, the more the score High viscosity is stronger; acceptability ranges from 1 to 10 points, the higher the score, the stronger the acceptability. It can be seen from the results in Table 5 that the chloroquine phosphate spray of the present invention is mild...

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Abstract

The invention discloses a chloroquine spray and a preparation method thereof. The spray consists of a powder and a solution, wherein the powder contains chloroquine or a chloroquine derivative, a carrier macromolecular material and a sweetening agent, and the solution is a salt solution containing borneol and / or menthol. The spray containing a chloroquine medicament is developed for the first time, has small toxic and side effects, can be directly used for antibacterial and antiviral protection of the oral and nasopharynx, can be used for clearing the nose and cleaning the pharynx and throat,and has the original clinical treatment application. Meanwhile, the method utilizes the carrier macromolecular material to wrap the chloroquine, prolongs the retention time of the chloroquine spray in the oral mucosa or the nasal mucosa to achieve the effect of slow release and long-acting, and can obviously improve the bacteriostatic disinfection effect of the chloroquine by being supplemented with menthol, borneol and ethanol. The chloroquine spray is mild and non-irritating, has good taste and convenient use, and can provide normal care for healthy people and more effective prevention andtreatment measures for infected or latent people in the aspects of virus protection such as novel coronavirus and the like.

Description

Technical field [0001] The invention belongs to the field of medical and health technology. More specifically, it relates to a chloroquine spray and a preparation method thereof. Background technique [0002] In the study of SARS-related coronaviruses, it was found that chloroquine can effectively prevent the spread of SARS-related coronaviruses during cell culture. The mechanism of action is to inhibit the terminal glycosylation of ACE2. In addition, existing clinical studies have found that chloroquine phosphate has initially shown a good clinical effect on the new coronavirus, and it has been written into the "New Coronavirus Pneumonia Diagnosis and Treatment Plan (Trial Sixth Edition)". On the afternoon of February 17, 2020, Sun Yanrong, deputy director of the Biological Center of the Ministry of Science and Technology, also introduced chloroquine at a press conference. Chloroquine phosphate is an antimalarial drug that has been used clinically for more than 70 years. Past r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/4706A61K47/36A61P11/02A61P11/04A61P31/02A61P31/04A61P31/14A61K31/045
CPCA61K31/4706A61K31/045A61K9/006A61K9/0043A61K47/36A61P11/02A61P31/14A61P31/04A61P31/02A61P11/04A61K2300/00
Inventor 王建瑜李相玲刘琦卢梅芳袁曼莉
Owner 广州康健医学科技有限公司
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