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Controlled release of highly soluble agents

A drug and sustained-release technology, applied in the field of delivering sustained-release preparations and treating glaucoma, can solve problems such as inappropriate preparations and administration

Inactive Publication Date: 2006-03-01
控释给药系统公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Many therapeutic drugs are most readily available as salts that are highly soluble in water and, therefore, are generally not suitable for formulation and administration by commonly used sustained-release systems

Method used

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  • Controlled release of highly soluble agents
  • Controlled release of highly soluble agents

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0080] Particles (1.5 mm in diameter, 2.0 mg) comprising D,L-lactide-co-glycolide (PLGA) and bovine albumin (1:1, w:w) were manually compressed. The particles were then dip-coated in a solution of PLGA / PEG (polyethylene glycol) in acetone and air dried. The dried coated particles were then embedded in a silicone array and covered by silicone, leaving 0.59mm diameter pores uncovered by silicone to allow albumin to diffuse.

[0081] The particles were placed in 1.0 ml of phosphate buffer (pH 7.4) and tested for release at 37°C. Samples were taken periodically and analyzed for albumin by HPLC.

[0082] figure 1 Cumulative release profile of particles coated with PLGA / PEG(8 / 2) is shown.

Embodiment 2

[0084]Particles (1.5 mm in diameter, 2.0 mg) comprising D,L-lactide-co-glycolide (PLGA) and bovine albumin (1:1, w:w) were manually compressed. The particles were then dip-coated in a solution of PLGA in acetone and air-dried. The dried coated particles were then embedded in a silicone array and covered by silicone, leaving 0.59mm diameter pores uncovered by silicone to allow albumin to diffuse.

[0085] The particles were placed in 1.0 ml of phosphate buffer (pH 7.4) and tested for release at 37°C. Samples were taken periodically and analyzed for albumin by HPLC.

[0086] figure 2 Cumulative release graph representing PLGA-coated particles.

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Abstract

The invention provides a device and method for treating and / or preventing raised intraocular pressure, such as that associated with glaucoma or the use of corticosteroids with adrenergic agents. The invention provides insertable sustained-release devices adapted to maintain a therapeutically effective concentration of one or more adrenergic agents for an extended period of time, and a method of use thereof.

Description

Background of the invention [0001] Various devices have been developed for the prolonged local release of drugs in living organisms. The advantage of such a device is that it provides high concentrations of the active compound at the location where it is required for activity, while maintaining low systemic concentrations of the same drug. In cases where the active compound is toxic, such as when the drug is a steroid or an antineoplastic compound, it is very important to keep systemic concentrations low. Likewise, maintaining high local concentrations of drugs is important in situations where effective treatment of disease states is at or near safe dosage ranges. [0002] Implantable pharmaceutical compositions have been developed that deliver compounds in a single dose and provide controlled delivery of such compounds. Specifically, in U.S. Patent 6,051,576, Ashton et al. describe the covalent linking of two or more drug compounds (parent drugs) to form drug compounds that...

Claims

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Application Information

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IPC IPC(8): A61K9/32A61K9/00A61K9/50A61K31/382A61K31/542A61L27/34A61L27/54A61L31/10A61L31/16
CPCA61L27/34A61K9/5031A61L2300/602A61L2300/21A61K9/0092A61L31/16A61K31/382A61L31/10A61K31/542A61L27/54A61L2300/436A61K9/0051A61P27/06A61K9/209A61K9/28
Inventor 保罗·阿什顿
Owner 控释给药系统公司
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