Atomization method of treprostinil aerosol inhalant for treating pulmonary arterial hypertension

A technology for treprostinil and pulmonary arterial hypertension, which is applied in nebulizers for treatment, aerosol delivery, spray delivery, etc. It can solve the problems of affecting patients' inhalation experience, affecting drug efficacy, and equipment cannot be placed flat or dumped. , to achieve the effect of convenient daily carrying and use, increasing medication compliance, and less medication dosage

Pending Publication Date: 2022-01-04
ZHAOKE PHARMA GUANGZHOU
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Since pulmonary arterial hypertension is a chronic disease, the high-incidence period is generally between 20 and 40 years old. Moderate and mild patients receiving treatment can still go out and work normally. The aerosol inhalation Tyvaso needs to use a specific product that is large in size and inconvenient to carry according to the product requirements. The atomization device, because the atomization device needs to be used four times a day when it is awake after adding the liquid medicine, and it needs to be used once every four hours. When using it, an external power supply is required, and the device must not be placed flat or dumped during the day's use or standby. It is necessary to replace the atomized water every day and carry out regular cleaning and sterilization operations. Therefore, it is very inconvenient for patients to use the aerosol inhalation Tyvaso daily, which affects their quality of life and work.
[0007] The particle size of the drug particles in the dry powder inhaler and inhalation powder aerosol is small (1-5 μm), and because of the strong interaction force (van der Waals force, electrostatic force and capillary force) between the particles, the aggregation of the particles is strong, During the stor

Method used

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  • Atomization method of treprostinil aerosol inhalant for treating pulmonary arterial hypertension
  • Atomization method of treprostinil aerosol inhalant for treating pulmonary arterial hypertension
  • Atomization method of treprostinil aerosol inhalant for treating pulmonary arterial hypertension

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Accurately weigh 120 mg of treprostinil and put it in a volumetric flask, add 10 ml of methanol, and shake to dissolve. Using a high-precision ultrasonic atomization coating machine, the drug solution is coated on the foil array of the drug inhaler, and the coating amount is 30 μg / cm 2 ,dry. When in use, the patient inhales air, and the heating controller in the inhalation system will give the foil a pulse current of 3 volts for 0.3 seconds to rapidly heat the foil to 300°C and vaporize treprostinil to form an aerosol, which can be inhaled The airflow diversion controller in the device controls the airflow above the foil to be 2-7L / min, and about 6 μg of treprostinil aerosol is brought into the human body.

Embodiment 2

[0039] Accurately weigh 300 mg of treprostinil diethanolamine salt, put it in a volumetric flask, add 10 ml of absolute ethanol, and shake to dissolve. Using a high-precision ultrasonic atomization coating machine, the drug solution is coated on the foil array of the drug inhaler, and the coating amount is 90 μg / cm 2 ,dry. When in use, the patient inhales air, and the heating controller in the inhalation system will give the foil a pulse current of 4.5 volts for 0.5 seconds to rapidly heat the foil to 250°C and vaporize treprostinil diethanolamine salt to form gas. For the aerosol, the airflow diversion controller in the inhaler controls the airflow above the foil to be 2-7L / min, and about 15 μg of treprostinil diethanolamine salt aerosol is brought into the human body.

Embodiment 3

[0040] Example 3 Delivery Dose Determination

[0041] According to Chinese Pharmacopoeia delivery dose uniformity requirement, adopt DUSA tube (dosage unit sampling apparatus, unit dose sampling device) method, the treprostinil aerosol made in embodiment 1 and the treprostinil diethanolamine made in embodiment 2 The delivered dose of the aerosol was determined.

[0042] Connect the suction port of the aerosol system to the DUSA tube, turn on the vacuum pump, and adjust the throttle valve of the flow meter to make the flow rate reach 28.3L / min (±5%). The aerosol system uses a suitable rubber interface to connect with the DUSA tube equipped with a filter membrane to ensure that the connection is sealed. Spray the sample into the DUSA tube once, add methanol and sodium hydroxide solution with a pipette gun, vortex for 30s, and sonicate for 10min. The supernatant was taken as the test solution, and the operation was repeated 10 times. It was measured by high performance liquid ch...

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PUM

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Abstract

The invention discloses an atomization method of a treprostinil aerosol inhalant for treating pulmonary arterial hypertension. According to the principle that aerosol is formed in a high-temperature state of medicine, treprostinil is coated on a heating plate of a medicine inhaler, gaseous treprostinil is formed through heating and is quickly condensed to form aerosol, and the aerosol is inhaled into the lung through a gas path and directly acts on a receptor in a pulmonary artery blood vessel, so that the treprostinil aerosol takes effect quickly, directly acts on a target spot, and is small in dosage and quick in metabolism, and the dose distributed to other organs of a human body is low. The treprostinil aerosol inhalant is convenient for a patient to carry and use in daily life, increases the medication compliance of the patient, and has a good application prospect.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to an atomization method of treprostinil aerosol inhalation used for treating pulmonary hypertension. Background technique [0002] Pulmonary hypertension is a type of malignant pulmonary vascular disease characterized by vascular remodeling of small pulmonary arteries, often due to progressive increase in pulmonary vascular resistance, which eventually leads to right heart failure and death in patients. Treprostinil is a targeted therapeutic drug for pulmonary arterial hypertension. It belongs to prostacyclin analogs. Its pharmacological effects are similar to those of endogenous prostacyclin. It has direct vasodilation and platelet aggregation inhibitory effects on the pulmonary and systemic arterial vascular beds. . [0003] Treprostinil currently developed and marketed preparations include subcutaneous or intravenous injections (Remodulin, 20ml: 20mg), slow-release ta...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K31/192A61M11/04A61P9/12A61P11/00
CPCA61K31/192A61K9/0073A61P9/12A61P11/00A61M11/041
Inventor 李小羿戴向荣殷雷
Owner ZHAOKE PHARMA GUANGZHOU
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