Pharmaceutical formulations comprising microcapsules
AssigneeInnovata Biomed Limited
InventorsRobert N. Boyes, Thomas R. Tice, Richard M. Gilley, Kenneth L. Pledger
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Abstract
Pharmaceutical formulations comprise (i) microcapsules which consist essentially of a biocompatible polymeric wall material encapsulating a drug, and (ii) a lipid soluble surfactant which is mixed with the microcapsules or is incorporated within or coats the wall material of the microcapsules. Such formulations may be presented as an aerosol or dry powder for inhalation. Microcapsules with surfactant incorporated in the wall material may be suspended in a pharmaceutically acceptable water-immiscible oil and the resulting suspension emulsified in an aqueous medium to obtain a formulation for oral administration.
Claims25
A pharmaceutical formulation suitable for inhalation, comprising:
- (i) microcapsules having an average diameter of from 0.1 to 10 .mu.m which consist essentially of a biodegradable, biocompatible wall-forming polymer encapsulating a drug, the polymer having a molecular weight of greater than 10,000 daltons, and
- (ii) a lipid-soluble surfactant which is selected from the group consisting of sorbitan trioleate, sorbitan monolaurate, sorbitan monooleate, sorbitan monopalmitate, sorbitan monostearate, a polyoxamer and a surface active fatty acid, which is present in an amount of from 1 to 25% by weight of the microcapsules and which is incorporated within the polymer forming the wall of the microcapsules.
A pharmaceutical formulation suitable for ingestion, comprising:
- (i) microcapsules having an average diameter of from 0.1 to 20 .mu.m which consist essentially of a biodegradable, biocompatible wall-forming polymer encapsulating a drug, the polymer having a molecular weight of greater than 10,000 daltons, and
- (ii) a lipid-soluble surfactant which is selected from the group consisting of sorbitan trioleate, sorbitan monolaurate, sorbitan monooleate, sorbitan monopalmitate, sorbitan monostearate, a polyoxamer and a surface active fatty acid, which is present in an amount of from 1 to 25% by weight of the microcapsules and which is incorporated within the polymer forming the wall of the microcapsules.
A process for the preparation of a pharmaceutical formulation which is suitable for inhalation and which comprises:
- (i) microcapsules having an average diameter of from 0.1 to 10 .mu.m which consist essentially of a biodegradable, biocompatible wall-forming polymer encapsulating a drug, and
- (ii) a lipid-soluble surfactant which is selected from the group consisting of sorbitan trioleate, sorbitan monolaurate, sorbitan monooleate, sorbitan monopalmitate, sorbitan monostearate, a polyoxamer and a surface active fatty acid, which is present in an amount of from 1 to 25% by weight of the microcapsules and which is incorporated within the polymer forming the wall of the microcapsules,
- the process comprising
- (a) forming a solution comprising a solvent, a biodegradable, biocompatible wall-forming polymer and a lipid soluble surfactant,
- (b) adding a drug to the solution thus formed, and
- (c) evaporating off the solvent to obtain microcapsules having an average diameter of from 0.1 to 10 .mu.m.
A process for the preparation of a pharmaceutical formulation which is suitable for ingestion and which comprises:
- (i) microcapsules having an average diameter of from 0.1 to 20 .mu.m which consist essentially of a biodegradable, biocompatible wall-forming polymer encapsulating a drug, and
- (ii) a lipid-soluble surfactant which is selected from the group consisting of sorbitan trioleate, sorbitan monolaurate, sorbitan monooleate, sorbitan monopalmitate, sorbitan monostearate, a polyoxamer and a surface active fatty acid, which is present in an amount of from 1 to 25% by weight of the microcapsules and which is incorporated within the polymer forming the wall of the microcapsules,
- the process comprising
- (a) forming a solution comprising a solvent, a biodegradable, biocompatible wall-forming polymer and a lipid soluble surfactant,
- (b) adding a drug to the solution thus formed, and
- (c) evaporating off the solvent to obtain microcapsules having an average diameter of from 0.1 to 20 .mu.m.
A pharmaceutical formulation suitable for inhalation, comprising
- (i) microcapsules having an average diameter of from 0.1 to 10 .mu.m which consist essentially of a biodegradable, biocompatible wall-forming polymer encapsulating a drug, the polymer having a molecular weight of greater than 10,000 daltons, and
- (ii) a lipid soluble surfactant which is a sorbitan fatty acid ester, which is present in an amount from 1 to 25% by weight of the microcapsules and which is incorporated within the polymer forming the wall of the microcapsules.
A pharmaceutical formulation suitable for ingestion, comprising
- (i) microcapsules having an average diameter of from 0.1 to 20 .mu.m which consist essentially of a biodegradable, biocompatible wall-forming polymer encapsulating a drug, the polymer having a molecular weight of greater than 10,000 daltons, and
- (ii) a lipid soluble surfactant which is a sorbitan fatty acid ester, which is present in an amount of from 1 to 25% by weight of the microcapsules and which is incorporated within the polymer forming the wall of the microcapsules.
Dependencies are inferred from the claim text.