Methods of treating acromegaly in a subject are described herein. Exemplary methods include orally administering to the subject at least once daily at least one dosage form comprising octreotide, wherein the octreotide in each dosage form is 20 mg, and wherein the administering occurs at least 1 hour before a meal or at least 2 hours after a meal.

Novel microsphere compositions for use in parenteral formulations are provided. The microspheres comprise a biodegradable polymer of a molecular weight greater than 10,000 daltons, an active therapeutic agent, and a cellulose-derived material such as ethyl cellulose, carboxymethyl cellulose, hydroxypropylmethyl cellulose, or sodium carboxymethyl cellulose. The microsphere compositions decreased deviation in mean microsphere diameter, improved drug entrapment, and improved microsphere stability.

Novel microsphere compositions for use in parenteral formulations are provided. The microspheres comprise a biodegradable polymer of a molecular weight greater than 10,000 daltons, an active therapeutic agent, and a cellulose-derived material such as ethyl cellulose, carboxymethyl cellulose, hydroxypropylmethyl cellulose, or sodium carboxymethyl cellulose. The microsphere compositions decreased deviation in mean microsphere diameter, improved drug entrapment, and improved microsphere stability.

Provided is a sustained-release lipid pre-concentrate in the form of a lipid solution, including an unsaturated fatty acid having 14 to 20 carbon atoms (C14˜C20); a phospholipid; and α-tocopherol acetate, wherein the sustained-release lipid pre-concentrate is free of diacyl glycerol and sorbitan unsaturated fatty acid ester; and forms a liquid crystal in an aqueous medium. Further provided is a sustained-release injectable pharmaceutical composition in the form of a lipid solution, including the pre-concentrate and a pharmacologically active substance, wherein the sustained-release injectable pharmaceutical composition is free of diacyl glycerol and sorbitan unsaturated fatty acid ester.

Provided is a sustained-release lipid pre-concentrate in the form of a lipid solution, including an unsaturated fatty acid having 14 to 20 carbon atoms (C14˜C20); a phospholipid; and α-tocopherol acetate, wherein the sustained-release lipid pre-concentrate is free of diacyl glycerol and sorbitan unsaturated fatty acid ester; and forms a liquid crystal in an aqueous medium. Further provided is a sustained-release injectable pharmaceutical composition in the form of a lipid solution, including the pre-concentrate and a pharmacologically active substance, wherein the sustained-release injectable pharmaceutical composition is free of diacyl glycerol and sorbitan unsaturated fatty acid ester.

The invention relates to oral pharmaceutical compositions of an active agent and a lipid conjugate of a cell penetrating peptide conjugated to a lipid molecule. The conjugated lipid acts as a permeation enhancer for the active agent in the composition. In other words, oral bioavailability of the active agent increases when co-administered together with the lipid conjugate described herein.

The present invention relates to methods of preparing peptide-based prodrugs having enhanced oral bioavailability and intestinal penetration. Said prodrugs are characterized in improved lipophilicity, reduced electric charge and tendency to undergo biotransformation through enzymatic reaction (e.g. in the blood stream) to form biologically active peptides.

The present invention relates to methods of preparing peptide-based prodrugs having enhanced oral bioavailability and intestinal penetration. Said prodrugs are characterized in improved lipophilicity, reduced electric charge and tendency to undergo biotransformation through enzymatic reaction (e.g. in the blood stream) to form biologically active peptides.

This application describes modified amino acids and polypeptides comprising a SO.sub.2F or CH.sub.2CH.sub.2SO.sub.2F group bound to the side chain of an amono acid or amino acid residue of a polypeptide in place of a hydrogen of a hydroxyl or amino substituent thereof. Methods of covalently binding the polypeptides to receptot sites of receptor proteins are also described herein.

This application describes modified amino acids and polypeptides comprising a SO.sub.2F or CH.sub.2CH.sub.2SO.sub.2F group bound to the side chain of an amono acid or amino acid residue of a polypeptide in place of a hydrogen of a hydroxyl or amino substituent thereof. Methods of covalently binding the polypeptides to receptot sites of receptor proteins are also described herein.