WATER-SOLUBLE SUPRAMOLECULAR COMPLEXES

摘要

Water-soluble supramolecular complexes formed from a water soluble block copolymer and at least one associative gelling adjuvant. The copolymer includes at least two blocks of polyethylene oxide and at least one block of polypropylene oxide. The adjuvant has a water solubility less than 0.5 g/100 ml at 20° C. When combined with water, the complexes form a transparent reversely thermo-reversible hydrogel or solution that may be repeatedly hydrated and dehydrated. The hydrogel exhibits improved gelling efficiency and enhanced solubility and/or stability for sparely soluble and insoluble pharmaceutical agents. The complexes are useful in a variety of pharmaceutical and cosmetic products and applications and may be combined with an effective amount of a cosmetic, medicament, or diagnostic in a solid dosage form.

主权项

1. A composition comprising a water-soluble supramolecular complex, wherein the water-soluble supra-molecular complex includes:
(a) a water soluble block copolymer comprising at least two blocks of polyethylene oxide and at least one block of polypropylene oxide, wherein the copolymer is selected from the group consisting of:
(i) a tri-block copolymer having the general formula of HO-(EO)a(PO)b(EO)a-H, wherein 50≦a≦150 and 35≦b≦70;(ii) a linear multi-block copolymer, having the general formula of HO—[(PO)b(EO)a]m(PO)c[(EO)a(PO)b]m-H, wherein 50≦a≦150, 35≦b≦70, 35≦c≦70, and m>0;(iii) a chain extended, hyper-branched, or star-shaped block copolymer of the formula {[An(EO)a(PO)b(EO)aAn]E}m, wherein A is a monomer selected from the group consisting of esters, hydroxyl acid esters, carbonates, ethers, siloxanes, and amides, and E is a chain extender or crosslinking agent, 50≦a≦150, 35≦b≦70, 0≦n≦50, and m≧2;(iv) an end-modified block copolymer of the formula R-G-(EO)a(PO)b(EO)a-G-R, wherein G is selected from the group consisting of C—C, C—O, C(O)NH, S—C, C(O)—O, or Si—O, R is alkyl or arylalkyl having an alkyl chain length in the range of C8-C36, 50≦a≦150, 35≦b≦70; and(v) a grafted block copolymer, comprising a grafted side chain, comprising at least two blocks of polyethylene oxide, and at least one block of polypropylene oxide, and having the formula [A(EO)a(PO)b(EO)a]m, 50≦a≦150, 50≦b≦150, A is selected from the group consisting of vinyl, ester, amide, Imide, ether, and siloxane linkages, m≧2;wherein (EO) is a polyethylene oxide block and (PO) is a polypropylene oxide block; and (b) at least one associative gelling adjuvant having a water solubility less than 0.5 g/100 ml at 20° C.; wherein the complex is capable of being repeatedly hydrated and dehydrated with water to form a solution or a transparent reversely thermo-reversible hydrogel, and wherein the composition is provided in solid form.