Anthelmintic gel composition and a method for their preparation at ambient temperatures
AssigneeAmerican Cyanamid Company
InventorJames M. Quinlan
Life of this patent
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Abstract
This invention relates to aqueous gels, which remain gelatinous in a temperature range as low as -27.degree. C. containing dl- or 1-6-phenyl-2,3,5,6-tetrahydro(-)imidazo[2,1-b]thiazole, acylamino derivatives, thereof and pharmaceutically acceptable salts thereof, characterized by gelation and preparation at ambient temperatures (20.degree.-60.degree. C.), under vacuum, without additional heating or cooling in their preparation.
Claims19
A method for the preparation, at ambient temperatures, of clear aqueous homogeneous gels characterized by subzero gelation points, comprising, mixing about 15-50% by weight of the gellant .alpha.-hydro-.OMEGA.-hydroxy-poly(oxyethylene)poly(oxypropylene)poly(oxye thylene) block copolymer, average molecular weight 12,500;
- mp 56.degree. C., Brookfield viscosity of 3100 at 77.degree. C.;
- surface tension of a 0.1% aqueous solution:
- 40.6 dynes/cm (measured with a du Nouy tensiometer) with 14-31% by weight of propylene glycol, 0-41% by weight of one or more active ingredients, and admixing the thus formed mixture with about 30-50% by weight of water and stirring the resulting mixture at ambient temperatures (20.degree.-60.degree. C.) without additional heating or cooling, until it is homogeneous at atmospheric pressure or under reduced pressure of from 10-100 mm Hg.
A aqueous composition comprising:
- 3-25% by weight of a pharmaceutically acceptable salt of the anthelmintic compound of the formula:
- ##STR3## wherein X is hydrogen or --NH--R;
- R is C.sub.2 -C.sub.5 alkanoyl or benzoyl;
- or the optical isomers thereof;
- 30-50% by weight of water;
- 14-31% by weight of propylene glycol;
- and greater than 30% by weight of the gellant .alpha.-hydro-.OMEGA.-hydroxy-poly(oxyethylene)poly(oxypropylene)poly(oxye thylene) block copolymer, average molecular weight 12,500, specific gravity 1.05;
- mp 56.degree. C., viscosity 3100 at 77.degree. C.;
- wherein said compositions are gels in the temperature range of from -20.degree. to +60.degree. C.;
- with the proviso that the water/gellant ratio is from 0.54/1.0 to 2.0/1.0;
- and that the components of said composition add up to a total of 100% by weight.
A method for the preparation of an aqueous composition, comprising;
- dissolving 3-25% by weight of a pharmaceutically acceptable salt of the anthelmintic compound of formula:
- ##STR5## wherein X is hydrogen or --NH--R;
- R is C.sub.2 -C.sub.5 alkanoyl or benzoyl;
- or the optical isomers thereof;
- 1.5% by weight of citric acid and 1.0% by weight of trisodium citrate;
- 0.5% by weight of benzyl alcohol;
- 0.01-0.03% by weight of C.I. Acid yellow No. 5;
- 0.001-0.02% by weight of an antifoaming agent comprising a mixture of dimethylpolysiloxanes of formula:
- ##STR6## silica gel wherein the calculated average value of m is 200-350, the mixture is a viscous liquid, d=0.965-0.970, n.sub.D.sup.25 about 1.404, viscosity about 60,000 centistokes, in 15-50% by weight of water and preferably 20-30% by weight of the gellant .alpha.-hydro-.OMEGA.-hydroxy-poly(oxyethylene)poly(oxypropylene)poly(oxye thylene) block copolymer, average molecular weight 12,500;
- specific gravity 1.05;
- mp 56.degree. C.;
- viscosity 3100 at 77.degree. C. dissolved or slurried in 14-31% by weight of propylene glycol at from 60.degree.-80.degree. C.;
- and stirring said mixture at ambient temperatures of from 20.degree.-60.degree. C., under reduced pressure of from 25-50 mm Hg until a clear solution occurs;
- with the provisos that the water/gellant ratio is from 0.94/1.0 to 2.5/1 and that the components of said composition add up to a total of 100%.
An aqueous composition comprising:
- 3-25% by weight of a pharmaceutically acceptable salt of the anthelmintic compound of the formula:
- ##STR7## wherein X is hydrogen or --NH--R;
- R is C.sub.2 -C.sub.5 alkanoyl or benzoyl;
- or the optical isomers thereof;
- 30-50% by weight of water;
- 14-31% by weight of propylene glycol;
- and 15-30% by weight of the gellant .alpha.-hydro-.OMEGA.-hydroxy-poly(oxyethylene)poly(oxypropylene)poly(oxye thylene) block copolymer, average molecular weight 12,500, specific gravity 1.05;
- mp 56.degree. C., viscosity 3100 at 77.degree. C.;
- wherein the compositions are gels in the temperature range of from -20.degree. to +60.degree. C.;
- with the proviso that the water/gellant ratio is from 0.54/1.0 to 1.39/1.0;
- and that the components of the composition add up to a total of 100% by weight.
Dependencies are inferred from the claim text.