Abstract: A pharmaceutical composition having improved solubility comprising a hydrophobic drug or pharmaceutically acceptable salt thereof and a compound having at least one carboxylic acid moiety, wherein the molar ratio of the compound having at least one carboxylic acid moiety to the hydrophobic drug or pharmaceutically acceptable salt thereof is from about 0.1:1 to about 25:1. The pharmaceutical composition exhibits rapid dissolution upon contact with physiological solvents, such as water, saliva or gastrointestinal fluids.

Abstract: A process for the preparation of polymorph Form I of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine, or olanzapine.

Abstract: This invention provides a process of preparation of novel polymorphic hemifumarate salts of 8-chloro-6,11-dihyfro-11-(4-piperidylidene)-5H-benzo[5,6]-cyclohepta[1,2-b]pyridine, hereinafter called “desloratadine”. These polymorphic salt forms show much higher solubility in water and also in protic organic solvents compare to the parent desloratadine. The process of preparing the polymorphic forms comprising: a) mixing the ethanolic solution of desloratadine and fumaric acid at a temperature of from about 55° C. to 70° C., and stirring for 30 to 45 minutes after mixing, and thereafter filtering the solid thereby prepared in hot condition; to yield the polymorphic form 2 having a DSC of 232° C.±2° C.; or b) mixing the ethanolic solution of desloratadine and fumaric acid at a temperature of form about 15° C. room temperature (25° C.) and stirring at this temperature for 30 to 45 minutes, then filtering at room temperature; to yield the polymorphic form 1 having a DSC of 224° C.±2° C.

Abstract: Thus, the present invention is directed toward an oral pharmaceutical composition in a solid dosage form comprising:

Abstract: This invention provides a process of preparation of novel polymorphic hemifumarate salts of 8-chloro-6,11-dihydro-11-(4-piperidylidene)-5H-benzo[5,6]-cyclohepta[1,2-b]pyridine, hereinafter called “desloratadine”. These polymorphic salt forms show much higher solubility in water and also in protic organic solvents compare to the parent desloratadine.

Abstract: A process for the preparation of polymorph Form I of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine, or olanzapine.

Abstract: This invention provides a process for preparing sodium ferric gluconate complex in sucrose using the following steps: a) combining a ferric salt solution with a weak alkali chosen from the group consisting of alkaline earth metal and ammonium salts, such as sodium carbonate, sodium bicarbonate, lithium carbonate, potassium carbonate, potassium bicarbonate, ammonium carbonate, ammonium bicarbonate and mixtures thereof, to form the ferric oxyhydroxide; b) combining ferric oxyhydroxide and sodium gluconate in solution to yield the sodium ferric gluconate complex; c) isolating the sodium ferric gluconate complex; and d) combining the sodium ferric gluconate with sucrose in solution to yield the desired sodium ferric gluconate complex in sucrose.

Abstract: An oral pharmaceutical composition in a solid dosage form comprising:

Abstract: Thus, the present invention is directed toward an oral pharmaceutical composition in the form of a tablet comprising:

Abstract: This invention provides a process for preparing sodium ferric gluconate complex in sucrose using the following steps:

Abstract: A process for preparing 5-methylisoxazole-4-carboxylic-(4′-trifluoromethyl)-anilide comprising: (a) reacting ethylacetoacetate, triethylorthoformate, and acetic anhydride at a temperature of from about 75° C. to about 150° C., to form ethyl ethoxymethyleneacetoacetic ester; (b) combining the ethyl ethoxymethyleneacetoacetic ester with sodium acetate or a salt of trifluoroacetic acid in the presence of hydroxylamine sulfate at a temperature of from about −20° C. to 10° C., to form ethyl-5-methylisoxazole-4-carboxylate; (c) reacting the ethyl-5-methylisoxazole-4-carboxylate with a strong acid to form 5-methylisoxazole-4-carboxylic acid; (d) reacting the crystallized 5-methylisoxazole-4-carboxylic acid with thionyl chloride to form 5-methylisoxazole-4-carbonyl chloride; and (e) reacting the 5-methylisoxazole-4-carbonyl chloride with trifluoromethyl aniline and an amine base at a temperature of from about 0° C. to about 50° C.

Abstract: This disclosure relates to the use of &agr;,&agr;-dibromo-&agr;-chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-&agr;,&agr;-dibromo-&agr;-chloroacetophenone is especially useful as an intermediate for the preparation of flecainide, a known pharmaceutical.

Abstract: A quick dissolving, high loading ribavirin composition which is essentially free of ribavirin polymorphic forms, said composition is prepared by a process comprising: (a) mixing ribavirin, at least one disintegrant and/or at least one filler to form an homogenous mixture; (b) granulating the mixture in the presence of water to form a granulation; (c) drying the granulation; and (d) mixing at least one disintegrant and/or at least one lubricant with the granulation to produce a ribavirin composition, wherein said ribavirin composition comprises at least 80 weight percent of ribavirin, based on the total weight of the composition. The ribavirin compositions prepared by the wet granulation process of the invention are free flowing and have adequate bulk density for processing into capsules. In addition, the ribavirin compositions contain at least 80 weight percent of ribavirin. Furthermore, the ribavirin compositions are substantially free of polymorphic forms of ribavirin, i.e.

Abstract: The present invention relates to a process for preparing tablet dosage forms of poorly-compressible pharmaceutical agents and to tablet dosage forms prepared according to the inventive process. The inventive process is especially useful for preparing tablets of the poorly-compressible drug metformin HCl.

Abstract: This disclosure relates to the use of &agr;,&agr;-dibromo-&agr;-chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-&agr;,&agr;-dibromo-&agr;-chloro-acetophenone is especially useful as an intermediate for the preparation of flecainide, a known pharmaceutical.

Abstract: This disclosure relates to the use of &agr;,&agr;-dibromo-&agr;-chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-&agr;,&agr;-dibromo-&agr;-chloroacetophenone is especially useful as an intermediate for the preparation of flecainide, a known pharmaceutical.

Abstract: Midodrine hydrochloride, ±1-(2′,5′-dimethoxyphenyl)-2-glycineamido-ethanol-(1)-HCl, is prepared from a novel intermediate, 1-(2′,5′-dimethoxyphenyl)-2-azidoethanone.

Abstract: A solid pharmaceutical tablet having a predetermined dosage that can be divided into a plurality of sub-dosage units by applying a minimal amount of force to the tablet. The tablet comprises a solid body having a top surface, a bottom surface, an outer surface, and an inner surface. The inner surface defines an aperture having a shape corresponding to the shape of the tablet. The area of the aperture is at least 15% of the area of the tablet. Impressed within the top surface of the tablet are a first plurality of symmetrical score lines and impressed within the bottom surface of the tablet are a second plurality of symmetrical score lines. The score lines extend from the aperture to the outer surface of the tablet. Finally, each of the sub-dosage units has a dosage that is a fraction of the predetermined dosage of the tablet.

Abstract: The present invention relates to the discovery of novel polymorph form of an active pharmaceutical agent and the process for its preparation. More specifically, the present invention relates to the preparation of a novel polymorph form of terazosin hydrochloride, a well known anti-hypertensive agent.

Abstract: A controlled release pharmaceutical formulation which undergoes substantially zero order release of active drug is provided, preferably in the form of a coated tablet, containing a core portion from which the angiotensin converting enzyme inhibitor (S)-1-[3-(benzoylthio)-2-methyl-1-oxopropyl]-L-proline is slowly released over a controlled length of time. The core also includes one or more hydrocolloid gelling agents having a viscosity of within the range of from about 8000 to about 100,00 centipoises in 2% solution at 20.degree. C., such as hydroxypropylmethyl cellulose and/or methyl cellulose, one or more inert fillers or excipients, one or more lubricants, and optionally one or more anti-adherents such as silicon dioxide and water. The above-described core is coated with a conventional pharmaceutical coating composition. A method of using such controlled release formulations in treating hypertension is also provided.