Thermoreversible gel as a liquid pharmaceutical carrier for...

A - Human Necessities – 61 – K

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A61K 47/34 (2006.01) A61K 9/00 (2006.01) A61K 9/06 (2006.01) A61K 47/10 (2006.01) A61K 47/32 (2006.01) A61L 26/00 (2006.01) A61L 29/08 (2006.01) A61K 7/42 (1990.01)

Patent

CA 2085690

ABSTRACT Thermoreversible gel as a liquid pharmaceutical carrier for a galenic formulation There is disclosed a thermoreversible gel as a liquid pharmaceutical carrier for a galenic formulation having improved thermo-rheological properties and with a gel- ling temperature interval between about 25 °C and 37 °C, which comprises a) 10 to 30 wt.% of block copolymers of a-hydro-.omega.-hydroxypoly(oxyethylene)/ poly(oxypropylene)/poly(oxy-ethylene) (Poloxamer) of the formula H(OCH2CH2)a (OCHCH2)b (OCH2CH2)aOH CH3 wherein a is at least 2 and b is at least 15 and the total portion of hydrophilic polyethylene units amounts to from 20 to 90 wt.% of the copolymer having a molecular weight from 1000 to above 16000; b) 0.01 to 5 wt.% of carboxyvinyl polymer (carbomer) having a molecular weight from l x 106 to 4 x 106; c) such an amount of a pharmaceutically acceptable base as necessary for adjusting the pH to a value between 4 and 8; d) 20 to about 85 wt.% of water, and e) optionally usual auxiliary agents. There is also disclosed a liquid galenic formulation containing a therapeutically active amount of an active substance and a thermoreversible gel as a liquid pharmaceutical carrier, the active substance being selected from the group consisting of .beta.-lactamic antibiotics and other antibacterial agents, chemotherapeutics, antiinfectives, topical anesthetics, anti-inflammatory and analgesic agents, antifungal agents, coronaryvasodilators, antiviral agents, miotics and anticholinergics, mydriatic agents, an- tiglaucoma agents, antihistaminics, biogenic peptides and cosmetic agents At room temperature, such a formulation is in the sol form, which is converted into a gel form at a temperature about the body temperature and thus the application onto eye, skin and mucous membranes of the body cavities as well as the improved biopharmaceutical usefulness are made possible.

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