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Fast-acting preparations for targeted therapy in pulmonary arterial hypertension

A technology for pulmonary arterial hypertension and targeted therapy, which is used in medical preparations, drug combinations, and cardiovascular system diseases with non-active ingredients. The effect of retention, storage and transport convenience

Active Publication Date: 2022-04-05
WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, nitric oxide molecules are in gaseous form, and nitric oxide gas (NO) is slightly soluble in water, and its solubility in water at 20°C is only 5.6×10-3g / L (equivalent to 0.186μmol / L), unable to be directly made into common pharmaceutical preparations
[0007] Therefore, although nitric oxide has good therapeutic potential for pulmonary arterial hypertension, nitric oxide is used as a gas, and there is no research report on how to efficiently carry nitric oxide gas in pharmaceutical preparations for the treatment of pulmonary arterial hypertension.

Method used

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  • Fast-acting preparations for targeted therapy in pulmonary arterial hypertension
  • Fast-acting preparations for targeted therapy in pulmonary arterial hypertension

Examples

Experimental program
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Effect test

Embodiment 1

[0024] The preparation of the quick-acting preparation of embodiment 1 pulmonary arterial hypertension targeted therapy

[0025] Preparation of quick-acting preparations for the treatment of pulmonary arterial hypertension in the experimental group: according to the component ratios in Table 1, the specific steps are as follows:

[0026] (1) Preparation of nitric oxide microbubbles: Take egg yolk phospholipids and poloxamer with a mass ratio of 1:20, mix them, dissolve them in anhydrous tert-butanol at 65°C with 10 times the mass, and slowly cool down until the solution solidifies, - Stand overnight at 10°C, freeze-dry to obtain a loose freeze-dried powder, transfer it into a stoppered bottle, fill it with nitric oxide gas to saturation, add 5 times the quality of the freeze-dried powder into water for injection, and mix well to get monoxide nitrogen microbubbles.

[0027] (2) Take polyglutamic acid and hydroxyethyl starch 130 / 0.4 with a mass ratio of 1:10, and dissolve it in...

Embodiment 2

[0033] The application effect of each group of quick-acting preparations of embodiment 2 for pulmonary hypertension model animals

[0034] (1) Establishment of pulmonary hypertension model animals

[0035] Taking Wistar rats as objects, referring to [Monocrotaline-induced experimental pulmonary hypertension morbid observation. Journal of Electronic Microscopy. 2002, 21(1): 45-54], using monocrotaline injection method to establish pulmonary hypertension model animals, The method is briefly described as follows: Monocrotaline is mixed with ethanol and normal saline (volume ratio 2:8) to make a 1% to 2% solution, and the rat is injected intraperitoneally at a time of 60 mg / kg, and is measured 2 to 3 weeks after administration. Pulmonary arterial pressure, to determine the success of the pulmonary arterial hypertension model.

[0036] (2) The effect of each group of preparations on the treatment of pulmonary hypertension model animals

[0037] The pulmonary hypertension rats suc...

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Abstract

The quick-acting preparation for targeted therapy of pulmonary hypertension of the present invention is composed of basic solution and nitric oxide microbubbles. The components of the basic solution include polyglutamic acid, hydroxyethyl starch and vasoactive intestinal peptide, the mass ratio of polyglutamic acid and hydroxyethyl starch is 1:10, and the vasoactive intestinal peptide is 6 mg / L. The nitric oxide microbubbles are composed of egg yolk phospholipids and poloxamers as bubble membrane materials to wrap nitric oxide gas into vesicles. The mass ratio of egg yolk phospholipids and poloxamers is 1:20, and the particle size ranges from 6 to 10 μm. The quick-acting preparation of the present invention is used for the treatment of pulmonary arterial hypertension.

Description

technical field [0001] The invention relates to a preparation for treating pulmonary hypertension, in particular to a quick-acting preparation for targeted therapy of pulmonary hypertension. Background technique [0002] Pulmonary arterial hypertension (PAH) is a hemodynamic abnormal state, which refers to pulmonary artery pressure exceeding a certain limit value, mainly manifested by pulmonary vascular intimal hyperplasia and fibrosis, adventitia thickening with moderate inflammatory infiltration, in situ thrombus and plexus Lesions are characteristic. Pulmonary hypertension is defined as the average pulmonary artery pressure ≥ 25mmHg (1mmHg = 0.133kPa) measured by right heart catheterization in a resting state. Multicellular and vascular injury remodels the pulmonary artery, restricts pulmonary artery blood flow, increases pulmonary vascular resistance progressively, increases right ventricular afterload, causes right ventricular hypertrophy, and eventually leads to right...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K47/34A61K47/36A61K47/24A61K47/10A61P9/12A61P11/00
CPCA61K9/08A61K47/34A61K47/36A61K47/24A61K47/10A61P9/12A61P11/00
Inventor 赵应征鲁翠涛姚情徐荷林李欣泽余润洁
Owner WENZHOU MEDICAL UNIV
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