Treatment of pulmonary hypertension by inhaled iloprost with a microparticle formulation

A technology of iloprost and medicament, which is applied in the field of treatment of pulmonary arterial hypertension, and can solve problems such as side effects and limited effects

Inactive Publication Date: 2007-12-19
BAYER SCHERING PHARMA AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, each treatment has limited efficacy and side effects

Method used

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  • Treatment of pulmonary hypertension by inhaled iloprost with a microparticle formulation
  • Treatment of pulmonary hypertension by inhaled iloprost with a microparticle formulation
  • Treatment of pulmonary hypertension by inhaled iloprost with a microparticle formulation

Examples

Experimental program
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preparation example Construction

[0236] If one surfactant is used during the preparation of the matrix, various surfactants can be added to the continuous phase such as emulsifiers. Exemplary emulsifiers or surfactants used can be (0.1-5% by weight), including most physiologically acceptable emulsifiers. Examples include bile salts or bile acids, conjugated amino acids and non-conjugated ones such as bezoar deoxycholic acid, and natural and synthetic forms of cholic acid. In contrast to the method described here, these surfactants will coat the microparticles and facilitate the dispersion of the administration.

[0237] Pore ​​former

[0238] An amount between 0.01% and 90% weight / volume can be included to increase matrix porosity and pore generation during matrix preparation. The pore-forming agent can be added to, for example, solid particles or an aqueous solvent to the polymer solution, emulsified with the polymer solution or co-dissolved in the polymer solution. For example, in spray drying, solvent evapora...

Embodiment 1

[0598] Microparticle porosity and iloprost or another drug other than iloprost that need to be given release In vitro analysis of effects

[0599] To prepare microspheres containing iloprost and / or another drug that needs to be administered in addition to iloprost, the raw materials used are obtained by the following method: iloprost is obtained from Schering AG or another suitable supplier Obtained; Phospholipids (DPPQ from Avanti Polar Lipids (Alabaster, AL) or another suitable supplier; Polymer (PLGA) from BI Chemicals (Petersburg VA) or another suitable supplier; Ammonium bicarbonate from Spectrum Chemicals (Gardena CA); and dichloromethane from EMScience (Gibbstown NJ) or another suitable supplier.

[0600]Use any of the above-mentioned different combinations of particle components to prepare microparticles containing iloprost and / or another drug other than iloprost that need to be administered and having different porosities, so that the resulting microparticles have diffe...

Embodiment 2

[0603] Containing iloprost for in vivo analysis and / or another drug that needs to be administered in addition to iloprost Preparation of radiolabeled microparticles

[0604] The microparticles containing iloprost and / or another drug to be administered in addition to iloprost were prepared as in the method of the above-mentioned Example 1.

[0605] The dried microspheres are then labeled with technetium or another suitable isotope. In addition, other suitable detectable labels can also be used. The labeled particles are transferred to a stainless steel mixing container and artificially mixed with lactose. The mixed raw materials are then mixed with a turbulent vibration-mixer, and the mixed materials are manually filled into capsules, such as No. 3 Coni-Snap capsules obtained from Capsugel, Greenwood, S.C. or other suitable capsules.

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Abstract

The present invention discloses microparticles comprising iloprost. In some embodiments, the microparticles are used to treat pulmonary hypertension. Also disclosed are devices comprising microparticles. Conjugation therapy using microparticles is also provided.

Description

Technical field [0001] This application is a non-provisional application under the title of U.S. Provisional Application No. 60 / 591,253 for the treatment of pulmonary hypertension by inhalation of iloprost and microparticle preparations filed on July 26, 2004, which is incorporated herein by reference in its entirety. [0002] The preferred embodiment of the present invention relates to microparticles containing iloprost, and to a method of treatment of pulmonary hypertension by delivering these microparticles through the lungs. Background technique [0003] Pulmonary hypertension is a debilitating condition characterized by increased lung resistance causing right ventricular failure and death. Pulmonary hypertension (PH) that has no obvious cause is called primary pulmonary hypertension. Pulmonary hypertension includes high arterial pressure in the lungs and other conditions. Recently, various physiological changes in cases related to these disorders have been characterized. The...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K31/5578A61P11/00
CPCA61K9/1647A61K31/7024A61K9/145A61K31/5578A61K9/1641A61K9/1617A61K9/0073A61K9/0075A61K31/557A61P11/00A61P3/14A61P43/00A61P9/08A61P9/12A61K9/00A61K9/14
Inventor 克蒂斯·鲁格朱立安·A·布莱尔
Owner BAYER SCHERING PHARMA AG
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