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Inhalation drug composition with budesonide and nitric oxide synthase (NOS) inhibitor

A technology for inhaling drugs and compositions, which is applied in the direction of drug combinations, medical preparations containing active ingredients, drug delivery, etc. It can solve problems such as severe irritation, biological cough, and poor inhalation effects, and achieve good therapeutic effects and improve Effects of airway remodeling

Inactive Publication Date: 2013-06-05
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, we also found that drugs such as S-methylisothiourea and aminoguanidine, on the one hand, due to their own chemical properties, have greater irritation when used for inhalation therapy, which has caused biological coughing and inhalation effects. Poor, on the other hand, combined with glucocorticoids can not play a synergistic effect, which may be due to the inability of hormones and drugs such as S-methylisothiourea and aminoguanidine to form a "permissive action" (Permissive action) in the lungs

Method used

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  • Inhalation drug composition with budesonide and nitric oxide synthase (NOS) inhibitor
  • Inhalation drug composition with budesonide and nitric oxide synthase (NOS) inhibitor
  • Inhalation drug composition with budesonide and nitric oxide synthase (NOS) inhibitor

Examples

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Effect test

Embodiment 1

[0038] Budesonide 80mg, L-N 6 -(1-Iminoethyl)-lysine 600mg dissolved in ethanol, after filtration, the filtrate was spray-dried and micronized to make the average particle size reach 2μm, and 10g of anhydrous lactose was micronized to an average particle size of 20μm by a flow energy mill , after mixing, pass through a 200-mesh sieve for 3 times, mix evenly, and pack in No. 3 capsules. Budesonide 80 μg per capsule, L-N 6 -(1-iminoethyl)-lysine 600 μg.

[0039] The process conditions are: the inlet temperature is 105°C, the outlet temperature is 68°C, the air flow rate is 90%, the inner diameter of the nozzle outlet is 0.1cm, the air flow rate of the nozzle is 800ml / min, and the injection speed is 50mL / h

Embodiment 2-1

[0041] Dissolve 250 mg of budesonide and 25 mg of N-nitro-L-arginine in ethanol. After filtration, the filtrate is spray-dried and micronized to make the average particle size reach 4 μm. 40 g of anhydrous lactose is micronized to The average particle size is 40 μm, mixed evenly, mixed 3 times with a 200 mesh sieve, and then packed into No. 3 capsules. Each capsule contains budesonide 250μg and N-nitro-L-arginine 25μg.

[0042] The process conditions are as follows: inlet temperature is 105°C, outlet temperature is 68°C, air flow rate is 90%, nozzle outlet inner diameter is 0.1cm, nozzle air flow rate is 800ml / min, and sample injection speed is 50mL / h.

Embodiment 2-2

[0044] According to the formulation of Example 2-1, the carrier was changed to octaacetate-D-cellobiose octaacetate with an average particle size of 35 μm, and the powder spray was prepared according to the process of Example 2-1.

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Abstract

An inhalation drug composition with budesonide and a nitric oxide synthase (NOS) inhibitor comprises the budesonide which serves as an active ingredient, an amino acid derivative which serves as the NOS inhibitor, and one or more types of drug auxiliary materials applicable to inhalation.

Description

technical field [0001] The invention relates to a pharmaceutical composition, which is an inhalation pharmaceutical composition containing corticosteroids and NOS inhibitors. Background technique [0002] Glucocorticoids have anti-inflammatory, anti-allergic, anti-rheumatic, and immunosuppressive effects, and are widely used in the treatment of allergic and autoimmune inflammatory diseases. Such as connective tissue disease, active rheumatism, rheumatoid arthritis, lupus erythematosus, severe bronchial asthma, severe dermatitis, ulcerative colitis, acute leukemia, etc. It is also used for some serious infections, poisoning, and malignant lymphoma. treat. [0003] Asthma is a chronic airway inflammation characterized by reversible airway obstruction and increased airway responsiveness. Airway obstruction is caused by two factors: increased secretions caused by bronchial mucosal inflammation, mucosal edema, and smooth muscle spasm stimulated by inflammation; while asthma Inc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/58A61K31/198A61K9/72A61P11/06
Inventor 孙亮陈松赵琳
Owner TIANJIN JINYAO GRP
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