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Sustained-release pharmaceutical compositions comprising an antipsychotic drug and uses thereof

A technology of antipsychotic drugs and compositions, which is applied in the direction of drug combinations, medical preparations containing active ingredients, medical preparations with non-active ingredients, etc., and can solve the problem of reducing the frequency of antipsychotic drug administration and slow-release drugs with high characteristics Embedding rate and other issues

Active Publication Date: 2021-03-23
TAIWAN LIPOSOME CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these antipsychotic liposome formulations failed to simultaneously exhibit significant sustained-release drug properties or high drug entrapment in liposomes
[0006] There remains an unmet need for sustained release formulations with high drug entrapment efficiency to reduce dosing frequency and improve therapeutic efficacy of antipsychotic drugs used in the treatment of schizophrenia and / or bipolar disorder

Method used

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  • Sustained-release pharmaceutical compositions comprising an antipsychotic drug and uses thereof
  • Sustained-release pharmaceutical compositions comprising an antipsychotic drug and uses thereof
  • Sustained-release pharmaceutical compositions comprising an antipsychotic drug and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0048] Example 1, the preparation of aripiprazole liposome formulation

[0049]Empty liposomes were prepared by the lipid film hydration-extrusion method. HSPC, cholesterol and DSPE-PEG2000 (59.5 / 39.6 / 0.9 mole percent) were dissolved in chloroform, and the organic solvent was removed under vacuum by a rotary evaporator to form a thin lipid film. The dried lipid film was hydrated with 75 mM triethylammonium sucrose octasulfate (pH 6.0) at 60° C. for 30 minutes to form liposomes with aqueous core entrapped with triethylammonium sucrose octasulfate. After six freeze-thaw cycles between liquid nitrogen and 60°C water, liposomes were squeezed 10 times through a polycarbonate filter with a pore size of 0.2 μm. Unentrapped triethylammonium sucrose octasulfate was removed by dialysis against a 9.4% sucrose solution.

[0050] Containing 1.0 mg / mL aripiprazole (Abblis Chemicals LLC, USA), empty liposomes (containing 2.5 mM lipid) prepared according to the previous paragraph, 100 mM ci...

example 2

[0053] Example 2, the preparation of olanzapine liposome formulation

[0054] Empty liposomes were prepared according to Example 1. The bilayer membrane contains HSPC, cholesterol and DPPG (59.5 / 39.6 / 0.9 mole percent) and the capture agent is 300 mM ammonium sulfate.

[0055] A reaction mixture containing 6.1 mg / mL olanzapine (TCI America, US), empty liposomes of 21.3 mM lipid, and 35 mM histidine buffer (pH 7.35) was incubated at 60° C. for 15 minutes, and then passed through Sephadex TM Unentrapped olanzapine was isolated with G-50 fine gel (GE Healthcare) or dialysis bags (Spectrum Labs) in 9.4% sucrose solution. The olanzapine (drug) concentration and lipid concentration of the reaction mixture and olanzapine-embedded liposomes were measured using an ultraviolet / visible (UV / Vis) spectrometer. D / L and entrapment efficiency of olanzapine liposome formulation are calculated according to example 1. The particle size distribution was measured by a dynamic light scattering i...

example 3

[0057] Example 3, the preparation of risperidone liposome formulation

[0058] Empty liposomes were prepared according to Example 1. The bilayer membrane contains HSPC, cholesterol and DSPE-PEG2000 (59.5 / 39.6 / 0.9 mole percent) and the capture agent is 300 mM ammonium sulfate.

[0059] A reaction mixture containing 5.4 mg / mL risperidone (TCI America, US), empty liposomes of 24.4 mM lipid, and 20 mM histidine buffer (pH 6.5) was incubated at 60° C. for 15 minutes, and then passed through Sephadex TM Unentrapped risperidone was isolated with G-50 fine gel (GE Healthcare) or dialysis bags (Spectrum Labs) in 9.4% sucrose solution. The risperidone (drug) concentration and lipid concentration of the reaction mixture and risperidone-embedded liposomes were measured using an ultraviolet / visible (UV / Vis) spectrometer. The D / L and embedding efficiency of risperidone liposome formulation are calculated according to example 1.

[0060] Using 300 mM ammonium sulfate as capture agent, th...

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Abstract

The present invention relates to a pharmaceutical composition comprising at least one liposome and an antipsychotic drug with a high drug to lipid ratio and encapsulation efficiency. The pharmaceutical composition improves the pharmacokinetic profile and sustains the release of the antipsychotic drug. Also provided is the method for treating schizophrenia or bipolar disorder using the pharmaceutical composition disclosed herein.

Description

[0001] This application claims the benefit of U.S. Patent Application No. 62 / 715,979, filed August 8, 2018, the entire contents of which are incorporated herein by reference. technical field [0002] The present invention is directed to a sustained-release pharmaceutical composition comprising antipsychotic drugs and using at least one trapping agent with high drug to lipid ratio and high encapsulation efficiency. The high drug-to-lipid ratio, high embedding efficiency and sustained release profile of the pharmaceutical composition reduce the frequency of administration, increase patient compliance and improve therapeutic outcome. Background technique [0003] Schizophrenia and bipolar disorder are complex mental health disorders with debilitating symptoms. Aripiprazole, olanzapine, quetiapine, and risperidone are approved antipsychotic drugs for the treatment of schizophrenia and bipolar disorder. These drugs can be administered orally in the form of lozenges, capsules or ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/10A61K9/00
CPCA61K9/1271A61K9/1278A61P25/18A61K31/551A61K31/519A61K31/496A61K31/554A61K31/5513A61K9/0019A61K47/02A61K47/26
Inventor 洪基隆方元成高颢文林宜谕沃尔特.高特尼
Owner TAIWAN LIPOSOME CO LTD
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