Preparation of peptide containing biodegradable microspheres by melt process
First Claim
1. A process for preparing microspheres of an admixture of a biodegradable low melting point block copolymer and a water soluble and heat resistant peptide/protein drug, which comprises:
- (a) preparing a molten mixture of an effective amount of peptide/protein drug microparticles and a biodegradable block copolymer at a temperature above the melting temperature of said block copolymer;
(b) dispersing said molten mixture into a continuous fluid medium in such a manner as to form microdroplets of said molten mixture in said fluid medium;
(c) lowering the temperature of said microdroplets in a cooling environment below the melting point of said block copolymer to form solid microspheres; and
(d) separating said microspheres from said continuous fluid medium.
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Abstract
Peptide/protein biodegradable drug delivery devices are prepared as microspheres without the use of solvents by a polymer melt process. A melt of thermostable polypeptides and an appropriate low melting block copolymer mixture is prepared and dispersed in an appropriate fluid medium such as air, water or an immiscible organic fluid without using any organic solvent to form microdroplets. The fluid medium is cooled to solidify the microdroplets into microspheres and then collected and purified or further processed as drug delivery devices. These biodegradable microspheres are suitable as implantable or injectable pharmaceutical formulations. Following administration as solid microspheres into the body of a warm blooded animal, the formulations absorb water from the body to form a hydrogel from which the polypeptide is released continuously over an extended period of time.
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Citations
24 Claims
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1. A process for preparing microspheres of an admixture of a biodegradable low melting point block copolymer and a water soluble and heat resistant peptide/protein drug, which comprises:
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(a) preparing a molten mixture of an effective amount of peptide/protein drug microparticles and a biodegradable block copolymer at a temperature above the melting temperature of said block copolymer; (b) dispersing said molten mixture into a continuous fluid medium in such a manner as to form microdroplets of said molten mixture in said fluid medium; (c) lowering the temperature of said microdroplets in a cooling environment below the melting point of said block copolymer to form solid microspheres; and (d) separating said microspheres from said continuous fluid medium. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24)
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Specification