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Co-amorphous powder for treating asthmatic lung diseases and preparation method thereof

A lung disease, amorphous technology, applied in the field of crystal form and medicine, can solve problems such as side effects, high local concentration, hypokalemia, etc.

Active Publication Date: 2021-06-15
SHENZHEN NYCRIST TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

as beta 2 The adrenergic receptor agonist, albuterol, has been used in acute hyperkalemia, it stimulates the influx of potassium into the cells and thus lowers the potassium in the blood, however because of this effect, in the British NationalFormulary, it is stated High doses or prolonged use may cause hypokalemia, especially in some patients with renal failure
In addition, albuterol is soluble in water, and its solubility in 1mol / l hydrochloric acid solution is 50 mg / ml. When inhaled and administered, some drugs will enter the stomach, resulting in excessive local concentration and side effects.

Method used

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  • Co-amorphous powder for treating asthmatic lung diseases and preparation method thereof
  • Co-amorphous powder for treating asthmatic lung diseases and preparation method thereof
  • Co-amorphous powder for treating asthmatic lung diseases and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Salbutamol, various insoluble corticosteroids, and carriers were characterized by XRPD, DSC, and Raman, respectively.

[0063] 1. The ratio of albuterol to budesonide is 1:1, 1:2, 2:1. First, the co-crystal screening of the two active drugs was carried out, and the methods of suspension crystallization, cooling crystallization, and volatile crystallization were used respectively. The XRPD diffraction patterns showed a physical mixture of the two drugs, and it was difficult to obtain the co-crystal product of the two drugs.

[0064] 2. Using the ball milling method, ball milled albuterol and budesonide respectively. It was found that salbutamol could be milled for 40 minutes to obtain an amorphous form. However, crystal transformation occurred after 1.5 days at room temperature, indicating poor stability; budesonide still existed after ball milling for 60 minutes. Diffraction peaks of the crystal form of the starting material. Mix budesonide with different carriers resp...

Embodiment 2

[0108] Get 55.58mg salbutamol, 100mg budesonide, after being dissolved in 25ml 95% (v / v) ethanol, stir for 1 hour, then filter and get the clear liquid and spray dry, the condition is: inlet temperature 70 ℃, outlet temperature 50 ℃, cooling temperature : -17°C, injection speed 5%-7% (1.5ml / min-2.1ml / min), gas delivery rate 100%, constant temperature stirring at 37°C during the process until the liquid is sprayed out, and the obtained product is sealed and stored immediately.

Embodiment 3

[0110] Dissolve 30.24mg of serine in 3ml of purified water to prepare a serine solution. Weigh 60.11mg of albuterol and 109.82mg of budesonide, dissolve in 30ml of absolute ethanol, then add serine solution, stir for 60min to mix well, then ultrasonicate at 40KHz, 40℃ for 1 hour and then spray dry. The conditions are: inlet temperature 70°C, outlet temperature 48°C, cooling temperature: -17°C, sample injection speed 10%-12% (3ml / min-3.6ml / min), air supply 100%, and 37°C during the process Stir at constant temperature until the liquid is sprayed out, thereby obtaining a co-amorphous powder (ternary co-amorphous substance) for treating asthmatic lung diseases, which is immediately sealed and stored.

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Abstract

The invention discloses a co-amorphous powder for treating asthmatic pulmonary diseases and a preparation method thereof. Dissolving salbutamol, poorly soluble corticosteroid and carrier in a solvent, and then spray-drying to form a co-amorphous form among the three components to obtain a co-amorphous powder for treating asthmatic lung diseases. The present invention is based on the physical and chemical properties of salbutamol and the insoluble corticosteroid budesonide. A large number of experimental studies have been carried out, and a ternary co-amorphous substance containing three components of salbutamol, budesonide and serine has been found, which can not only significantly improve the Stability, but also effectively increase the solubility of the corticosteroid budesonide. In addition, serine is easily soluble in water and forms a colloid in 90%-95% (v / v) ethanol, which can evenly disperse salbutamol and insoluble corticosteroid budesonide, so that the final spray-dried amorphous powder has a uniform particle size.

Description

technical field [0001] The invention belongs to the field of crystal forms and medicine, and in particular relates to a co-amorphous powder for treating asthmatic lung diseases and a preparation method thereof. Background technique [0002] With the application of combinatorial chemistry and high-throughput screening in drug development, more than 40% of candidate drugs currently have poor solubility. This type of drug belongs to class II in the biopharmaceutical classification system. Therefore, it is necessary to seek to improve the solubility of this type of drug The method has become the key content of the pre-prescription research of pharmaceutical preparations. Compared with crystalline drugs, amorphous drugs are characterized by long-range disorder and short-range order, so their surface free energy is larger, and the particle surface is easy to hydrate. The deflocculation of the hydration film makes the drug easier to disperse, thereby improving the difficulty The s...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K9/72A61K47/18A61K31/137A61K31/58A61P11/06A61P11/00
CPCA61K9/0073A61K9/145A61K31/137A61K31/58A61P11/00A61P11/06A61K2300/00
Inventor 田芳安妮·齐默尔曼
Owner SHENZHEN NYCRIST TECH CO LTD
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