Polymer, and pharmaceutical composition employing the same

Patent metadata

Field	Value
Publication number	US-9737607-B2
Application number	US-201514757563-A
Country	US
Kind code	B2
Filing date	Dec 24, 2015
Priority date	Dec 24, 2014
Publication date	Aug 22, 2017
Grant date	Aug 22, 2017

Abstract

A polymer and a pharmaceutical composition employing the same are disclosed. The polymer includes a first repeating unit, a second repeating unit, and a third repeating unit. In particular, the first repeating unit is

the second repeating unit is

wherein R 1 is C 1-6 alkyl group; and the third repeating unit is

wherein X is

and Y is a hydrophilic polymeric moiety.

First claim

What is claimed is:

1. A polymer, comprising a first repeating unit, a second repeating unit, and a third repeating unit, wherein the first repeating unit is

the second repeating unit is

wherein R 1 is C 1-6 alkyl group; and, the third repeating unit is

wherein X is

and Y is hydrophilic polymeric moiety, wherein the hydrophilic polymeric moiety is polyethylene glycol moiety, methoxy polyethylene glycol moiety, polyvinylpyrrolidone moiety, polyacrylic acid moiety, or polymethacrylic acid moiety, wherein the first repeating unit has a weight percentage of 5-50 wt %, the second repeating unit has a weight percentage between 10-55 wt %, and the third repeating unit has a weight percentage between 25-75 wt %, based on the total weight of the first repeating unit, the second repeating unit, and the third repeating unit, wherein the hydrophilic polymeric moiety has a grafting ratio between 0.1% and 10%.

2. The polymer as claimed in claim 1 , wherein the hydrophilic polymeric moiety has a weight average molecular weight between 500 and 100,000.

3. The polymer as claimed in claim 1 , wherein the third repeating unit is

wherein n>1.

4. The polymer as claimed in claim 1 , wherein the third repeating unit is

wherein n>1.

5. The polymer as claimed in claim 1 , wherein R 1 is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, tert-butyl group, pentyl group, or hexyl group.

6. The polymer as claimed in claim 1 , wherein the polymer has a weight average molecular weight between 5,000 and 500,000.

7. The polymer as claimed in claim 1 , wherein the second repeating unit is

8. The polymer as claimed in claim 7 , wherein the polymer has an esterification degree between 10% and 85%.

9. The polymer as claimed in claim 1 , further comprising: a fourth repeating unit, wherein the fourth repeating unit is

wherein Z is a hydrophobic moiety.

10. The polymer as claimed in claim 9 , wherein the hydrophobic moiety is phenyl group, naphthyl group, or C 4-20 alkyl group.

11. The polymer as claimed in claim 9 , wherein the hydrophobic moiety is a polyester moiety.

12. The polymer as claimed in claim 11 , wherein the polyester moiety has a weight average molecular weight between 500 and 5,000.

13. The polymer as claimed in claim 11 , wherein the polyester moiety is polycaprolactone moiety, polylactic acid moiety, polyglycolic acid moiety, or poly(lactic-co-glycolic) acid moiety.

14. The polymer as claimed in claim 9 , wherein the first repeating unit has a weight percentage of 5-40 wt %, the second repeating unit has a weight percentage of 10-50 wt %, the third repeating unit has a weight percentage of 25-70 wt %, and the fourth repeating unit has a weight percentage of 5-50 wt %, based on the total weight of the first repeating unit, the second repeating unit, and the third repeating unit.

15. The polymer as claimed in claim 12 , wherein the hydrophobic moiety has a grafting ratio between 0.1% and 10%.

16. A pharmaceutical composition, comprising:
a bioactive component; and
an excipient, wherein the excipient comprises the polymer as claimed in claim 1 .

17. The pharmaceutical composition as claimed in claim 16 , wherein the bioactive component is lipophilic drug.

18. The pharmaceutical composition as claimed in claim 17 , wherein the bioactive component is non-steroid anti-inflammatory drug, psychotropic drug, antilipemic drug, antiemetic drug, or a combination thereof.

19. The pharmaceutical composition as claimed in claim 17 , wherein the bioactive component is ibuprofen, naproxen, ketoprofen, flurbiprofen, fenoprofen, suprofen, fluprofen, fenbufen, tolmetin sodium, zomepirac, sulindac, indomethacin, mefenamic acid, meclofenamate, diflunisal, flufenisal, piroxicam, sudoxicam, isoxicam, chlorpheniramine, brompheniramine, dexchlorpheniramine, dexbrompheniramine, triprolidine, chlorcyclizine, diphenhydramine, doxylamine, tripelennamine, cyproheptadine, bromodiphenhydramine, phenindamine, pyrilamine, azatadine, acrivastine, astemizole, azelastine, cetirizine, ebastine, fexofenadine, ketotifen, carbinoxamine, desloratadine, loratadine, pheniramine, thonzylamine, mizolastine, terfenadine, chlophendianol, caramiphen, dextromethorphan, codeine, hydrocodone, pseudoephedrine, ephedrine, phenylephrine, guaifenesin, guaiacotsulfonate, celecoxib, rofecoxib, valdecoxib, acetaminophen, phenacetin, acteylsalicylic acid, aripiprazole, fenofibrate, aprepitant, nevirapine, glyburide, sorafenib, vemurafenib, telaprevir, or a combination thereof.

Assignees

• Ind Tech Res Inst

Inventors

• Chen Jui-Hsiang
• Chen Yu-Hua
• Tsai Chia-Chen
• Teng Tse-Min
• Shih Ting-Yu
• Wang Chia-Chun
• Hong Chia-Wei
• Sheu Jennline
• Cheng hui-ling
• Chen shu-feng
• Huang Hung-Jui
• Wang Shu-Ling

Classifications

• C08G81/027

  containing polyester or polycarbonate sequences · CPC title

• C08G18/7671

  containing only one alkylene bisphenyl group · CPC title

• A61K9/2027

  obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates · CPC title

• C08G18/6212

  Polymers of alkenylalcohols; Acetals thereof; Oxyalkylation products thereof · CPC title

• C08G18/283

  Compounds containing ether groups, e.g. oxyalkylated monohydroxy compounds · CPC title