Injectable depot formulations and methods for providing sustained release of nanoparticle compositions

A nanoparticle and pharmaceutical preparation technology, applied in the field of ziprasidone for the treatment of mental illness, can solve the problems of poor water solubility of ziprasidone and difficulty in storage of ziprasidone

Inactive Publication Date: 2008-04-23
PFIZER PRODS ETAT DE CONNECTICUT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, ziprasidone is poorly soluble in water
Although depot antipsychotics reduce the risk of relapse and thus have the potential to lead to greater success rates in the treatment of schizophrenia, conventional depot technology can be used to formulate ziprasidone capable of delivering effective plasma levels of ziprasidone Ketone storage has always been difficult

Method used

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  • Injectable depot formulations and methods for providing sustained release of nanoparticle compositions
  • Injectable depot formulations and methods for providing sustained release of nanoparticle compositions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0148] Preparation of Formulation A

[0149] A crude suspension was prepared by placing 8.86 grams of ziprasidone free base and 48.90 grams of milling media (500 micron polystyrene beads) in a 100 ml milling chamber.

[0150] To this suspension, 4.2 ml each of 10% Pluronic(R) F108 solution and Tween(R) 80 solution were added. In addition, 27.8 ml of water for injection was added to the milling chamber. The above mixture is stirred until a homogeneous suspension is obtained. The suspension was then milled in Nanomill-1 (manufacturer: Elan Drug Delivery, Inc.) at 2100 RPM for 30 minutes, and the temperature was maintained at 4°C during the milling. The resulting suspension was filtered under vacuum to remove the milling media, and the suspension was characterized by microscopy and light scattering (Brookhaven). For microscopic observation, place a drop of the diluted suspension between the cover glass and the glass slide and observe in bright and dark fields. For light scattering p...

Embodiment 2

[0153] Preparation of Formulation B

[0154] A crude suspension was prepared by placing 8.84 grams of ziprasidone free base and 48.90 grams of milling media (500 micron polystyrene beads) in a 100 ml milling chamber.

[0155] To this suspension, 4.2 ml of a 10% solution of Pluronic(R) F108 was added. In addition, 32 ml of water for injection was added to the milling chamber. The above mixture was milled under the same conditions as in Example 1.

[0156] The milling was stopped at 30 minutes, at which time the above suspension became a paste, so a uniform, non-aggregated, free-flowing nano suspension was not obtained. Because the paste cannot be filtered to separate the milling media, no additional characterization can be performed.

Embodiment 3

[0158] Preparation of Formulation C

[0159] A crude suspension was prepared by placing 8.82 grams of ziprasidone free base and 48.87 grams of milling media (500 micron polystyrene beads) in a 100 ml milling chamber.

[0160] To this suspension, add 4.2 ml of a 10% solution of PVP-K30. In addition, 32 ml of water for injection was added to the milling chamber. The above mixture was milled under the same conditions as in Example 1.

[0161] The milling was stopped at 30 minutes, at which time the above suspension became a paste, so a uniform, non-aggregated, free-flowing nano suspension was not obtained. Because the paste cannot be filtered to separate the milling media, no additional characterization can be performed.

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Abstract

Pharmaceutical formulations comprising: a compound selected from the group consisting of ziprasidone, having a maximum average particle size; a carrier; and preferably at least two surface stabilizers are disclosed. The present invention also comprises methods of treating psychosis with such a formulation and processes for making such a formulation.

Description

Invention field [0001] The present invention relates to pharmaceutical active compounds. The present invention particularly relates to ziprasidone (including nanoparticles of ziprasidone, especially nanoparticles containing one or more surface stabilizers), and formulations containing ziprasidone nanoparticles. The present invention includes a pharmaceutical preparation comprising: a compound selected from the group consisting of ziprasidone having the largest average particle diameter; a carrier; and optionally a surface stabilizer (for example, at least two surface stabilizers). The present invention also includes a method of treating psychosis with the preparation and a method of preparing the preparation. Background of the invention [0002] Ziprasidone is a known compound with the following structure: [0003] [0004] It is disclosed in U.S. Patent Nos. 4,831,031 and 5,312,925. Ziprasidone has utility as a neuroleptic, so it is especially suitable as an antipsychotic. In ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/14A61K31/496
CPCA61K9/145A61K9/146A61K9/0024A61K31/496A61P25/14A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28A61K9/107B82B1/00B82Y5/00
Inventor J·C·沙P·S·沙D·R·瓦格纳P·维斯尼基
Owner PFIZER PRODS ETAT DE CONNECTICUT
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