Oral pharmaceutical formulation of BCS class III molecules
Inventors
Ailhas, Caroline • Herry, Catherine
Assignees
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Publication Number
US-10258692-B2
Publication Date
2019-04-16
Expiration Date
Abstract
The present invention concerns an oral pharmaceutical formulation made from a microemulsion between an aqueous solution comprising at least one BCS (Biopharmaceutics Classification System) class III active principle and one oily phase comprising an oily vehicle that is self-emulsifiable on contact with water.
Core Innovation
The invention concerns an oral pharmaceutical formulation in tablet form for baclofen, where baclofen is incorporated using an oil-in-water microemulsion. The microemulsion is formed between an aqueous solution comprising water and baclofen and an oil phase comprising an oil excipient self-emulsifiable in contact with water, and the tablet form includes residual moisture of less than 5%.
The formulation uses a neutral carrier impregnated with the oil-in-water microemulsion, with the impregnated carrier dried and compressed with compression excipients. The oil excipient self-emulsifiable in contact with water is defined as a mixture of mono-, bi- and triglycerides of PEG-8 esterified fatty acids, in the proportion of 50 to 80% caprylic acid and 20 to 50% capric acid.
The document links the microemulsion design to improved intestinal membrane permeability and bioavailability while maintaining non-toxicity. It also addresses converting the microemulsion into solid dosage forms via adsorption/granulation and characterizes particle size, stability, and flow properties, while maintaining residual moisture below 5%.
Claims Coverage
The independent claim is directed to an oral tablet formulation in which baclofen is delivered by a dried and compressed oil-in-water microemulsion impregnated into a neutral carrier, with specified microemulsion composition and tablet residual moisture. The claim set includes four inventive features, and dependent claims refine the oil excipient composition and narrow the therapeutic use to alcohol dependence or alcohol abstinence.
Dried and compressed microemulsion impregnated tablet with low residual moisture
An oral tablet formulation consisting of a neutral carrier impregnated with an oil-in-water microemulsion, dried and compressed with compression excipients, wherein the tablet form contains residual moisture of less than 5%.
Oil-in-water microemulsion composition defined by aqueous phase and oil phase percentages
The oil-in-water microemulsion is between an aqueous solution comprising water and baclofen and an oil phase comprising an oil excipient self-emulsifiable in contact with water, the microemulsion comprising from 2 to 30% oil phase and from 70% to 98% aqueous solution based on the total weight of the oil-in-water microemulsion.
PEG-8 esterified fatty acid mono-, bi- and triglyceride oil excipient with specified caprylic/capric proportions
The oil excipient self-emulsifiable in contact with water is a mixture of mono-, bi- and triglycerides of PEG-8 esterified fatty acids in the proportion of 50 to 80% caprylic acid and 20 to 50% capric acid.
Treatment purpose for alcohol dependence and maintaining alcohol abstinence
Treating alcohol dependence or maintaining alcohol abstinence by administering the formulation of the claim to a patient in need.
Overall, the claims focus on an oral baclofen tablet where a defined oil-in-water microemulsion is dried, impregnated into a neutral carrier, compressed, and kept at residual moisture below 5%, with an additional narrowing to treating alcohol dependence or maintaining alcohol abstinence.
Stated Advantages
Improved intestinal membrane permeability and bioavailability while maintaining non-toxicity.
Increased baclofen apparent permeability with Labrasol®-containing microemulsions.
Documented Applications
Treating alcohol dependence or maintaining alcohol abstinence by administering the formulation of the document to a patient in need.
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