Novel formulation of dehydrated lipid vesicles for controlled release of active pharmaceutical ingredient via inhalation

A pharmaceutically active, lipid-based technology for the treatment of asthma and other conditions

Inactive Publication Date: 2009-02-18
HONG KONG BAPTIST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These issues relate to the need for proper control over the rate of release

Method used

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  • Novel formulation of dehydrated lipid vesicles for controlled release of active pharmaceutical ingredient via inhalation
  • Novel formulation of dehydrated lipid vesicles for controlled release of active pharmaceutical ingredient via inhalation

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[0272] It has been found according to the present invention that when a high percentage of vesicle protector stabilizers and / or plasticizers are contained in liposomes, said vesicle protector stabilizers and / or plasticizers such as glycerol and fatty acid sucrose esters, which The molar percentage is generally between 0.1% and 40%. During or after freeze-drying or spray-drying and rehydration process, albuterol or other pharmaceutical active ingredients can successfully maintain the shape of lipid vesicles and remain in liposome vesicles. Medium delayed release.

[0273] According to the present invention, it is also found that the pharmaceutically active ingredient / lipid / stabilizer and / or plasticizer composition of the present invention has many improved properties, such as less leakage of the pharmaceutically active ingredient from liposomal vesicles, lower drug The toxicity and side effects of the drug can be controlled, the solubility and encapsulation rate of the drug can...

Embodiment 1

[0305] Aqueous multilamellar vesicles (MLVs) were prepared by conventional lipid membrane hydration methods, and small unilamellar vesicles (SUVs) were subsequently produced by extrusion. Lipids and albuterol were dissolved in chloroform and methanol, respectively, and the solutions were mixed with lipids and albuterol at the indicated molar ratios. The mixture was dried under a nitrogen stream to form a uniform lipid film, and then placed under vacuum overnight to remove residual organic solvents. The lipid film was hydrated in 10 mM Tris-isotonic saline buffer (10 mM Tris, 137 mM NaCl, and pH 7.4 at 25°C). The final concentration of lipid was controlled at 5-20mg / ml. The mixture was then kept at 80°C (above the transition temperature of all lipids) for 60 minutes to allow the liposomal structure to solidify. During curing, it was vortexed 3 times at the beginning, middle and end time points respectively and the stirring was continued for 5 minutes each time. The obtained ...

Embodiment 2

[0312] A mixture of part of DOPC or DOTAP and the active ingredient (albuterol, 0.04mmol) in a molar ratio of 1:2 was dissolved in 4ml of ethanol. Salbutamol liposome dispersions were formed by injecting the lipid / pharmaceutical active ingredient / ethanol solution into 50 ml of pH 7.4 phosphate buffer. Liposomes were extruded through 0.4 or 0.2 μm polycarbonate membranes to form liposome vesicles with uniform size distribution.

[0313] Determination of Encapsulation Efficiency

[0314] 150 μL of freshly prepared liposome samples were centrifuged with an AvantiJ-E centrifuge (JA-20, 17400×g, 6° C., and 20 min) through a MicroconY-10 centrifugal filter device (Millipore) with a molecular weight cut-off of 10 KD. The albuterol concentration in the centrifuged solution was determined spectrophotometrically at 276 nm. This concentration represents the albuterol concentration in the continuous phase of the liposomes (non-encapsulated albuterol). Spectrophotometry was also used to...

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Abstract

A new formulation of dehydrated lipid vesicles employs a vesicle preserver and permits the control of release and delivery of active pharmaceutical ingredients into the respiratory system for treatment in particular of asthma. The typical formulation provides controlled release of the active pharmaceutical ingredient from 0% to 100% from 0 to 72 hours after inhalation, changes the systemic administration to topical administration, allows prolonged therapeutic period for one administration, increased stability, with reduced dose, reduced systemic side effects, reduced toxicity.

Description

technical field [0001] The present invention relates to lipid vesicles, in particular to the treatment of asthma and other diseases. Background technique [0002] Asthma is a chronic disease of the respiratory system in which the airways are discontinuously constricted with associated inflammation. This causes symptoms such as coughing, wheezing, and shortness of breath with tightness in the chest. Asthma symptoms, which range from mild to life-threatening, are usually controlled with bronchodilators or combinations thereof. Asthma is of particular concern in developed countries because of its rapidly increasing prevalence, affecting up to a quarter of urban children. See LillyCM. Diversity of asthma: Evolving concepts of pathophysiology and lessons from genetics (diversity of asthma: evolutionary concepts of pathophysiology and lessons from genetics). JAllergyClinImmunol (Journal of Allergy Clinical Immunology). 2005;115(4 Suppl):S526-31. [0003] Animal models have de...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/12A61K45/00A61K47/18A61K47/24A61K47/26A61K47/34A61K47/36A61K47/38A61K47/40A61K47/42A61K47/44A61P11/06A61K31/137
CPCA61K9/127A61K31/137A61K9/0073A61P11/00A61P11/06
Inventor 杨智钧黄文华黄志新赵中振
Owner HONG KONG BAPTIST UNIV
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