Abstract: The present invention provides a hard gelatine capsule containing a pharmaceutical composition comprising cyclosporin A in a mixture with a surfactant of HLB value at least 10, substantially free of any oil and when a hydrophilic phase is present, the hydrophilic phase being a polyethylene glycol and/or a lower alkanol provided that any lower alkanol present is present in less than 12% of the total weight of the composition absent the hard gelatine capsule.

Abstract: A process for making enantiomerically enriched 4-piperidinylglycine having the formula (I), said process comprising (a) combining N-protected glycine ester with 4-piperidone to form didehydroamino acid ester; (b) reducing the didehydroamino acid ester with hydrogen gas in the presence of a rhodium catalyst selected from the group consisting of (R,R)-BPE-Rh; (S,S)-BPE-Rh; (R,R)-DuPHOS-Rh; (S,S)-DuPHOS-Rh; and combinations thereof; whereby a protected compound is formed; and (c) removing the protecting groups from the protected compound, whereby the 4-piperidinylglyeine having the formula (I) is formed, wherein X− is an anion wherein X is independently a halogen; and “*” designates an asymmetric carbon having (R)- or (S)-configuration. The process of the invention yields an enantiomerically enriched (R)-4-piperidineglycine or (S)-4-piperidineglycine.

Abstract: An accelerated process for preparing a methyl ester having formula (III) said process comprising reacting a carboxylic acid or salt thereof having formula (I) with dimethyl carbonate having formula (II) in the presence of a catalyst selected from the group consisting of 1,8-diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; 4-dimethylaminopyridine; and combinations thereof, wherein R1 is selected from the group consisting of an alkyl, aryl, alkoxy, alkenyl, cycloalkyl, benzocycloalkyl, cycloalkylalkyl, aralkyl, heterocyclic, heteroaralkyl, alkoxyalkyl, carboxyalkyl, alkylcarbonyl, alkoxycarbonyl, alkoxycarbonylalkyl, and haloalkyl; and M is selected from the group consisting of hydrogen, a monovalent metal, and a monovalent fractional part of a polyvalent metal, wherein said process is conducted under microwave irradiation at a frequency from 300 MHz to 30 GHz, and at a temperature of from about 120° C. to 300° C.

Abstract: This invention provides pharmaceutical compositions comprising TGF-&bgr;.

Abstract: A mixture comprising a poly-ene macrolide and an antioxidant. Preferably, the poly-ene macrolide is rapamycin and the antioxidant is 2,6-di-tert.-butyl-4-methylphenol. The presence of the antioxidant improves the stability of the poly-ene macrolide to oxidation.

Abstract: A pharmaceutical composition in the form of a solid dispersion comprising a macrolide, e.g. a rapamycin or an ascomycin, and a carrier medium.

Abstract: An accelerated process for preparing an O-methyl phenol comprising reacting a phenol with dimethyl carbonate in the presence of a catalyst selected from 1,8-diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; and dimethylaminopyridine. According to another aspect, the invention provides an accelerated process for preparing an N-methyl heteroaromatic compound comprising reacting an NH-containing heteroaromatic compound with dimethyl carbonate in the presence of a catalyst selected from 1,8-diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; and dimethylaminopyridine. According to an additional aspect, the invention provides an accelerated process for preparing a methylated aminophenol comprising reacting an aminophenol having at least one N—H with dimethyl carbonate in the presence of a catalyst selected from 1,8-diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; and dimethylaminopyridine.

Abstract: The invention relates to an aerosol container for pharmaceutically active aerosols that are to be administered in predetermined amounts and that are supplied in the container in the form of a suspension, the suspension also comprising, in addition to a pharmaceutically active substance, at least a propellant gas. The aerosol container has a metering valve that comprises a metering chamber and a valve stem. In a first position of the valve stem, the metering chamber is in communication with the interior of the container and has been filled with a predetermined amount of the aerosol. In a second position of the valve stem, the amount of aerosol disposed in the metering chamber is released. The propellant gas is an alternative propellant gas that is free of fluorochlorohydrocarbons, preferably a propellant gas that comprises only fluorohydrocarbons, and the inner wall of the container is coated with a plastics coating.

Abstract: Soft gelatin capsules having a capsule shell comprising gelatin, plasticizers and, if desired or required, further auxiliary agents, and a capsule filling containing a solvent including a migrateable solvent such as 1,2-propyleneglycol as a solvent in the capsule filling and in the capsule shell. The manufacture of said capsules is improved, if in the process for making the soft gelatin capsules the gelatin bands are cooled with a liquid, and preferably with water.

Abstract: The invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, which comprises nateglinide (I) or repaglinide and at least one other antidiabetic compound selected from the group consisting of thiazolidinedione derivatives (glitazones), sulfonyl urea derivatives and metformin for simultaneous, separate or sequential use in the prevention, delay of progression or treatment of diseases, especially metabolic disorders and in particular type 2 diabetes and diseases and conditions associated with diabetes; to a composition, respectively, which comprises nateglinide and a pharmaceutically acceptable carrier and to a process of making such composition; the use of such combination or composition for the preparation of a medicament for the prevention, delay of progression or treatment of metabolic disorders; a method of prevention, delay of progression or treatment of diseases in warm-blooded animals; the use of such combination or composition for

Abstract: Soft gelatin capsules having a capsule shell comprising gelatin, plasticizers and, if desired or required, further auxiliary agents, and a capsule filling containing a solvent including a migrateable solvent such as 1,2-propyleneglycol as a solvent in the capsule filling and in the capsule shell. The manufacture of said capsules is improved, if in the process for making the soft gelatin capsules the gelatin bands are cooled with a liquid, and preferably with water.

Abstract: A low temperature process for preparing a methyl ester having formula (III) said process comprising reacting a carboxylic acid or salt thereof having formula (I) with dimethyl carbonate having formula (II) in the presence of a catalyst selected from the group consisting of 1,8 diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; and combinations thereof, wherein said process is conducted at a temperature of about 10° C. to less than 120° C.; R1 is selected from the group consisting of an alkyl, aryl, alkoxy, alkenyl, cycloalkyl, benzocycloalkyl, cycloalkylalkyl, aralkyl, heterocyclic, heteroaralkyl, alkoxyalkyl, carboxyalkyl, alkylcarbonyl, alkoxycarbonyl, alkoxycarbonylalkyl and haloalkyl; and M is selected from the group consisting of hydrogen, a monovalent metal and a monovalent fractional part of a polyvalent metal.

Abstract: The invention relates to a pharmaceutical preparation, which contains an immunosuppressive active agent in dissolved form in a starch capsule, or hard or soft gelatin capsule which has been coated with one or several polymer films. The invention further relates to a process for the production of the pharmaceutical preparation.

Abstract: This invention relates to single dose dry powder inhalers in which medicament is stored in a capsule and is released by piercing the capsule wall with polymer-coated steel pins. Methods of preparation of polymer-coated piercing means and their use in releasing the medicament from the capsule are described.

Abstract: The present invention provides a hard gelatine capsule containing a pharmaceutical composition comprising cyclosporin A in a mixture with a surfactant of HLB value of at least 10, substantially free of any oil and when a hydrophilic phase is present, the hydrophilic phase being a polyethylene glycol and/or a lower alkanol provided that any lower alkanol, if present, is present in less than 12% of the total weight of the composition absent the hard gelatine capsule.

Abstract: Pharmaceutical compositions comprising a cyclosporin as active ingredient, a fatty acid triglyceride, a glycerol fatty acid partial ester or propylene glycol or sorbitol complete or partial ester, preferably, and a tenside having an HLB of at least 10.

Abstract: The invention is concerned with a parenteral formulation comprising a 5H-dibenz(b,f)azepine-5-carboxamide and an aqueous-based solvent. The parenteral formulation is useful in the treatment of seizures resulting from, e.g. epileptic attack.

Abstract: An oral dosage form comprising fluvastatin and HPMC, which oral dosage form is color-stable upon prolonged periods of storage.

Abstract: This invention provides composition comprising a cyclosporin and a carrier medium.