Atomization method of treprostinil aerosol inhalant for treating pulmonary arterial hypertension

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...

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 storage process, it is easy to agglomerate, which will cause the particle size to change and affect the efficacy of the drug. Therefore, it is usually necessary to use carrier particles to prevent the agglomeration of the drug powder. The drug powder is mixed so that the drug powder is adsorbed on the surface of the carrier particles. When in use, the drug powder is separated from the carrier particles during inhalation by the patient, enters the lungs of the human body and deposits, as described in the patent US Patent 10076505. The prescription is "1.06% treprostinil Sodium disulfide, 92.44% trehalose dihydrate, 2% polysorbate 80, 4% L leucine, 0.27% sodium citrate dihydrate and 0.23% sodium chloride", using macromolecular polysaccharides with large particle size The compound trehalose is mixed with treprostinil sodium micropowder as a carrier to make treprostinil inhalation, but in the process of inhalation and use of patients, large particle excipients are very easy to attach to the throat, resulting in foreign body sensation and affecting the patient's Inhalation experience, for patients with sensitive pharynx, it is more likely to cause stress cough, cough up the drug inhaled into the lungs, and then reduce the efficacy of the drug

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