# US 5,705,194 A · Pharmaceutical compositions containing polyalkylene block copolymers which gel at physiological temperature

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- Number: US 5,705,194 A
- Document ID: US5705194A
- Status: Granted
- Kind: A
- Application number: 08/727,863
- Filed: 1996-10-08
- Granted: 1998-01-06
- Earliest claimed: 1995-02-24
- Assignees: NanoSystems L.L.C.
- Inventors: Sui-Ming Wong; Eugene R. Cooper; Shuqian Xu
- Web page: https://patentgrep.com/patent/US5705194A

## CPC

- A61K 9/146: {with organic macromolecular compounds}
- Y10S 977/745: having a modified surface
- Y10S 977/773: Nanoparticle, i.e. structure having three dimensions of 100 nm or less
- Y10S 977/775: Nanosized powder or flake, e.g. nanosized catalyst
- Y10S 977/788: Of specified organic or carbon-based composition
- Y10S 977/927: Diagnostic contrast agent
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- Y10S: TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS

## Abstract

There is disclosed a pharmaceutical composition which gels at physiological temperature. The composition is comprised of a block copolymer containing one or more polyoxyethylene blocks and one or more polyoxy (higher alkylene) blocks wherein at least some of the blocks are linked together by a linking group characterised in that the linking group is an oxymethylene group, and a therapeutic agent. The therapeutic agent is present as (i) nanoparticles of the therapeutic agent having the block copolymer adsorbed on the surface thereof, (ii) a suspension in a solution of the block copolymer, or (iii) as an aqueous solution in a solution of the block copolymer.

## Claims

### Claim 1

A pharmaceutical composition comprised of
a) a triblock copolymer having the following repeating units in random order
--((E.sub.r P.sub.s E.sub.r)CH.sub.2 O).sub.z --
wherein
P is oxypropylene,
E is oxyethylene,
r is an integer from 2 to 160,
s is an integer from 15 to 65, and
z is an integer from 2 to 50, wherein the triblock copolymer gels at physiological temperature, and
b) a therapeutic agent, wherein the therapeutic agent is present as
(I) nanoparticles of the therapeutic agent having the block copolymer adsorbed on the surface thereof,
(II) a suspension in a solution of the block copolymer, or
(III) an aqueous solution in a solution of the block copolymer.

### Claim 2 (depends on 1)

A composition according to claim 1 wherein said block copolymer has the following repeating units in random order
--›(E.sub.r P.sub.s E.sub.r)CH.sub.2 O!.sub.z --
wherein
P is oxypropylene;
E is oxyethylene;
r is an integer from 75 to 150;
s is an integer from 30 to 50; and,
z is an integer from 2 to 10.

### Claim 3 (depends on 1)

A composition according to claim 1 wherein said block copolymer has the formula: ##STR2## wherein r is 114; s is 44 and z is 3 to 4.

### Claim 4 (depends on 1)

A composition according to claim 1 wherein said block copolymer has the formula:
--›(E.sub.r P.sub.s E.sub.r)CH.sub.2 O!.sub.z --›(E.sub.t)CH.sub.2 O!.sub.w
wherein
P is oxypropylene;
E is oxyethylene;
r is an integer from 2 to 160;
s is an integer from 15 to 65;
z is an integer from 2 to 50;
t is an integer from 1 to 10; and
w is an integer from 2 to 50.

### Claim 5 (depends on 1)

A composition according to claim 1 wherein said therapeutic agent is an agent for ophthalmic application.

### Claim 6 (depends on 1)

A composition according to claim 1 wherein said therapeutic agent is an agent for nasal application.

### Claim 7 (depends on 1)

A composition according to claim 1 wherein said therapeutic agent is an agent for oral application.