Liquid propellant-free formulation comprising an antimuscarinic drug

A propellant and preparation technology, which is applied in the field of preparation of the preparation, can solve problems such as the chemical stability of amino ester derivatives

Inactive Publication Date: 2013-10-09
CHIESI FARM SPA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] However, amino ester derivatives may encounter chemical stability problems in aqueous solution

Method used

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  • Liquid propellant-free formulation comprising an antimuscarinic drug
  • Liquid propellant-free formulation comprising an antimuscarinic drug
  • Liquid propellant-free formulation comprising an antimuscarinic drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0114] Example 1 - Determination of the Solubility of Active Ingredient C1 in Water-Ethanol Mixtures

[0115] The solubility of C1 in water / ethanol mixtures was determined as follows. Prepare vials containing excess C1 with 0%, 2.5%, 5% and 25% ethanol in water.

[0116] After equilibration, the samples were filtered through a 0.2 μm filter.

[0117] Record the results in the attached picture of picture , from which the C1 solubility can be extrapolated.

Embodiment 2

[0118] Example 2 - Propellant-free liquid formulation comprising C1 as active ingredient and ethanol solvent agent

[0119] A 10 mM citrate buffer containing 5.0% (v / v) ethanol was prepared and the pH was adjusted to 4.5 using 1 N sodium hydroxide.

[0120] 7 mg of C1 was weighed into a vial and 2 ml of 10 mM citrate buffer, pH 4.0 containing 5.0% ethanol was added. The solution was stirred, vortexed for 30 s every 5 min for 45 min, and then filtered using a 0.2 μm filter. Osmolarity was shown to be approximately 290 mOsm / kg.

Embodiment 3

[0121] Example 3 - Inhibitors containing C1 as active ingredient and propylene glycol as co-solvent Injection liquid preparation

[0122] Three 10 mM citrate buffers containing 1.85% (v / v) propylene glycol (PG) were prepared and the pH was adjusted to 4.0, 5.0 and 6.0 using 1 N sodium hydroxide.

[0123] 2, 3 and 4 mg of Cl were weighed into separate vials and 1 ml of 10 mM citrate buffer, pH 4.0 containing 1.85% propylene glycol was added. Each solution was stirred, vortexed for 30 s every 5 min for 45 min, and then filtered using a 0.2 μm filter. pH and osmolarity were then tested.

[0124] Similar formulations containing C1 as the active ingredient were prepared but using starting solutions in which the pH was 5.0 and 6.0, respectively. All prepared formulations are reported in Table 1.

[0125] Table 1 - Composition of the formulations

[0126]

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Abstract

Liquid, propellant-free pharmaceutical formulation for administration by nebulization which comprising an antimuscarinic drug as active ingredient are useful for the prevention and / or treatment of a wide range of conditions including respiratory disorders.

Description

field of invention [0001] The present invention relates to a propellant-free liquid pharmaceutical formulation suitable for administration by nebulizer, comprising an antimuscarinic drug as active ingredient. [0002] The invention also relates to a process for the preparation of the formulation and its use in the prevention and / or treatment of various conditions including respiratory diseases. Background of the invention [0003] Airway obstruction characterizes a variety of serious respiratory diseases, including asthma and chronic obstructive pulmonary disease (COPD). Events leading to airway obstruction include airway wall edema, increased mucus production, and inflammation. [0004] Drugs used to treat respiratory diseases such as asthma and COPD are currently administered by inhalation. One advantage of the inhalation route over the systemic route is the possibility to deliver the drug directly to the site of action, avoiding any systemic side effects, thus providing...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/439A61K9/00
CPCA61K9/0078A61K31/439A61K45/06A61P11/00A61P11/06A61P29/00A61K2300/00A61K9/08
Inventor A·索里亚尼拉斯奇尼E·鲁特罗
Owner CHIESI FARM SPA
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