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Pressurized metered dose inhalers and pharmaceutical aerosol formulations

A technology for inhalers and aerosols, which is applied in the field of pressure metered dose inhalers and aerosols, and can solve problems such as short shelf life

Inactive Publication Date: 2001-08-29
BAKER NORTON PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These preparations have a short shelf life and require refrigeration

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-3

[0044] Utilize the following steps to mix the components shown in Table 1 to make three kinds of suspension type aerosols according to the present invention:

[0045] 1. Weigh the solvent or surfactant into the plastic-coated glass bottle or aluminum can.

[0046]2. Add the weighed medicine.

[0047] 3. Install the valve on the bottle or jar.

[0048] 4. Add a known amount of propellant to the bottle or jar through the valve.

[0049] 5. Sonicate the preparation for about 5 minutes.

[0050] Unless otherwise stated, 19 ml aluminum metered dose inhaler canister Presspart with Bespak BK357, 63 μl metering valve was used.

[0051] The properties of the example aerosols were examined using one or more of the following:

[0052] Appearance (should show no outward signs of leakage or deformation);

[0053] The amount of leakage meets the standards of US Pharmacopoeia 23 and National Formulary 18;

[0054] Tank contents are within 10% on average;

[0055] Drugs per container a...

Embodiment 4-7

[0062] Using the method described in Example 1, the components shown in Table 2 were mixed to prepare four types of solution aerosols according to the present invention. In order to determine the stability of the solution aerosols, Examples 6 and 7 were kept at 40° C. and 75% relative humidity for 1 month (28 days), here considered accelerated conditions. The solution aerosol was equilibrated overnight at room temperature prior to testing. The properties of the solution-type aerosol were measured as in Example 1, and the results are shown in Table 2.

[0063] The data indicated that the released dose (measured per spray unit) after storage under accelerated conditions was lower than that obtained with the original sample due to drug adsorption on the valve gasket material. However, the solution aerosol showed no signs of chemical deterioration.

Embodiment 8 and 9

[0065] Using the method described in Example 1, the components shown in Table 3 were mixed to prepare two kinds of solution-type aerosols according to the present invention. In order to determine the stability of the solution-type aerosol, Example 9 was kept at 40° C. and 75% relative humidity for 1 month (28 days), which is regarded as an accelerated condition. The solution aerosol was equilibrated overnight at room temperature prior to testing. The properties of the solution-type aerosol were measured as in Example 1, and the results are shown in Table 3.

[0066] During the course of this study, drug could not be recovered from the spacer material, resulting in a 15% weight loss. However, the solution aerosol showed no signs of chemical deterioration.

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PUM

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Abstract

Provided are pressurized metered dose inhalers containing stable formulations of a beta-agonist drug in suspension or solution. Also provided are aerosol formulations suitable for inhalation therapy containing a beta-agonist drug in suspension or solution.

Description

field of invention [0001] The present invention relates to pressurized metered dose inhalers and aerosols for use in inhalation therapy. Background of the invention [0002] Due to environmental concerns, most of the chlorocarbon and chlorofluorocarbon propellants used in medical aerosols have been replaced by hydrofluoroalkanes such as 1,1,1,2-tetrafluoroethane (“HFA-134a ”) and 1,1,1,2,3,3,3-heptafluoropropane (“HFA-227ea”), which have been determined to be safe for use in pressurized metered dose inhalers. [0003] Such pharmaceutical aerosols are generally in the form of solutions or suspensions. Each type consists of at least drug and propellant. Some formulations also include one or more special purpose adjuvants such as cosolvents or surfactants (EP 0372777). Conventional solution aerosols contain low concentrations of co-solvents that are more polar than the propellant, and conventional suspension aerosols contain surfactants rather than co-solvents, the theory be...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/12A61K9/14A61K9/72A61K31/165A61K31/167A61K47/06A61K47/10A61M11/00A61M15/00
CPCA61K31/167A61K47/10A61K9/008A61K9/124
Inventor F·E·布隆迪诺M·布鲁卡托M·W·布恩纳非
Owner BAKER NORTON PHARMA INC
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