Non-polymeric lipophilic pharmaceutical implant compositions for intraocular use
AssigneeAlcon Inc.
InventorsBhagwati P. Kabra, Janet D. Howie
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Abstract
Solid or semi-solid intraocular implant compositions are disclosed. The compositions contain a lipophilic compound but lack a polymeric ingredient.
Claims23
An implant composition comprising a blend mixture of a lipophilic compound having a molecular weight of 150-4000 and a pharmaceutically effective amount of a drug, wherein the implant composition contains neither a polymeric ingredient nor an organic solvent that is miscible with or dispersible in water, wherein the implant composition is solid at a temperature of 37° C. and becomes a liquid above 37° C., and said implant composition is solidifiable in a human, and the lipophilic compound is of the formula
- wherein
- R1 is —H, —OH, —COOH, —CnH2n+1-2m, —COOCnH2n+1-2m,
- —COO(CH2CH2O)nCH2CH2OH, —CH2R3, or
- R2, R3 and R4 are independently —H, —OH, —COOH, —CnH2n+1-2m,
- —OOCCnH2n+1-2m, —COOCnH2n+1-2m, —COO(CH2CH2O)nCH2CH2OH, —Cn—H2n+1-2mCOO(CH2CH2O)nCH2CH2OH,
- —OOCCnH2n+1-2mCOOCn′H2n′+1-2m′, —COO−Na+, —COO−K+, —SO3H,
- —SO3−Na+, —SO3−K+, —NH2, —Cl,
- n, n′ and n″ are independently 0-50;
- and
- m and m′ are independently 0-10, wherein said lipophilic compound is present is an amount of at least 30 wt % based on the weight of the intraocular implant composition.
An intraocular implant composition comprising a blend mixture of a lipophilic compound having a molecular weight of 150-4000 and a pharmaceutically effective amount of a drug, wherein the implant composition contains neither a polymeric ingredient nor an organic solvent that is miscible with or dispersible in water, wherein the composition is solid at a temperature of 37° C. and becomes a liquid above 37° C., and said composition is solidifiable in a human eye, and the lipophilic compound is of the formula
- wherein
- R1 is —H, —OH, —COOH, —CnH2n+1-2m, —COOCnH2n+1-2m,
- —COO(CH2CH2O)nCH2CH2OH, —CH2R3, or
- R2, R3 and R4 are independently —H, —OH, —COOH, —CnH2n+1-2m,
- —OOCCnH2n+1-2m, —COOCnH2n+1-2m, —COO(CH2CH2O)nCH2CH2OH, —Cn—H2n+1-2mCOO(CH2CH2O)nCH2CH2OH,
- —OOCCnH2n+1-2mCOOCn′H2n′+1-2m′, —COO−Na+, —COO−K+, —SO3H,
- —SO3−Na+, —SO3−K+, —NH2, —Cl,
- n, n′ and n″ are independently 0-50;
- and
- m and m′ are independently 0-10, wherein said lipophilic compound is present in an amount of at least 50 wt % based on the weight of the intraocular implant composition, and wherein the lipophilic compound of formula (I) is selected from the group consisting of diethylene glycol mono stearate;
- propylene glycol mono stearate;
- glyceryl monostearate;
- glyceryl monolinoleate;
- glyceryl monooleate;
- glyceryl monopalmitate;
- and mixtures thereof.
An intraocular implant composition comprising a blend mixture of a lipophilic compound having a molecular weight of 150-4000 and a pharmaceutically effective amount of a drug, wherein the implant composition contains neither a polymeric ingredient nor an organic solvent that is miscible with or dispersible in water, wherein the composition is solid at a temperature of 37° C. and becomes a liquid above 37° C., and said composition is solidifiable in a human eye, and the lipophilic compound is of the formula
- wherein
- R1 is —H, —OH, —COOH, —CnH2n+1-2m, —COOCnH2n+1-2m,
- —COO(CH2CH2O)nCH2CH2OH, —CH2R3, or
- R2, R3 and R4 are independently —H, —OH, —COOH, —CnH2n+1-2m,
- —OOCCnH2n+1-2m, —COOCnH2n+1-2m, —COO(CH2CH2O)nCH2CH2OH, —CnH2n+1-2mCOO(CH2CH2O)nCH2CH2OH,
- —OOCCnH2n+1-2mCOOCn′H2n′+1-2m′, —COO−Na+, —COO−K+, —SO3H,
- —SO3−Na+, —SO3−K+, —NH2, —Cl,
- n, n′ and n″ are independently 0-50;
- and
- m and m′ are independently 0-10, wherein said lipophilic compound is present in an amount of at least 50 wt % based on the weight of the intraocular implant composition, and wherein the lipophilic compound of formula (I) is selected from the group consisting of:
- glyceryl monolaurate;
- glyceryl dilaurate;
- glyceryl monomyristate;
- glyceryl dimyristate;
- glyceryl monopalmitate;
- glyceryl dipalmitate;
- glyceryl monostearate;
- glyceryl distearate;
- glyceryl monooleate;
- glyceryl dioleate;
- glyceryl monolinoleate;
- glyceryl dilinoleate;
- glyceryl monoarachidate;
- glyceryl diarachidate;
- glyceryl monobehenate;
- and glyceryl dibehenate.
Dependencies are inferred from the claim text.