Mutual Pharmaceutical Company, Inc.

Other

Sigmapharm Laboratories, LLC

Sigmapharm, Inc.

Spireas, Spiridon

Bolton, Sanford M.

Spiridon Spireas

Sanford M Bolton

Ishari Piya

Rakesh Grover

Sunil Sagi

Ram K Kallur

Disclosed are highly stable compositions having outstanding storage stability and/or demonstrating exceptional resistance to aqueous solution degradation, the composition including an orally active nucleotide analog or an orally active nucleotide analog prodrug, which is orally bioavailable, such as adefovir dipivoxil and tenofovir disoproxil. For example, when a composition of the invention is stored for 1 month or for 18 months at 25&#xb0; C. and 60% relative humidity, its orally active nucleotide analog or orally active nucleotide analog prodrug degrades to provide a composition containing no more than 0.2% or no more than 0.7% by weight of a less orally bioavailable impurity, respectively. Also disclosed are a container/closure package system including the composition and a package insert and methods of manufacturing the composition and treating a patient for a disease or condition, for example, a viral disease or cancer, with the use of the composition.

Highly stable compositions of orally active nucleotide analogues or orally active nucleotide analogue prodrugs

Pharmaceutical formulations, and processes for making same, comprising an amino acid which is liable to formation of an undesirable lactam, and a stabilizer comprising a volatile alcohol; a non-volatile alcohol; a water immiscible liquid or solid; a liquid with a relatively low dielectric constant; a liquid surface active agent; a solid surface active agent; an antioxidant; a ketone; an aldehyde; a solid polyethylene glycol of high molecular weight; polyvinylpyrrolidone; a derived cellulose; silicon dioxide; or a combination thereof.

Stable solid dosage forms of amino acids and processes for producing same

Pharmaceutical formulations and dosage forms are provided having improved stability to moisture-induced degradation when compared with conventional dosage forms, especially tablets. The invention features low compression forms of drugs known to be susceptible to moisture-induced degradation together with excipients, preferably in encapsulated forms. In other embodiments, relatively non-volatile oils can be admixed with the drug and/or the excipients to stabilize the formulations toward moisture-induced degradation. Hydrophobic powders are also optionally added to the formulations.

Stabilization of solid drug formulations

Pharmaceutical formulations and dosage forms are provided having improved stability to moisture-induced degradation when compared with conventional dosage forms, especially tablets. The invention features low compression forms of thyroid drugs together with excipients, preferably in encapsulated forms. In other embodiments, relatively non-volatile oils can be admixed with the drug and/or the excipients to stabilize the formulation toward moisture-induced degradation. Hydrophobic powders are also optionally added to the formulations.

Stabilization of solid thyroid drug formulations

The present invention provides stable formulations of ACE inhibitors, especially enalapril maleate, that can be manufactured in a time efficient, cost effective manner. Such formulations can be prepared simply and on a large industrial scale. The present invention also provides methods for the preparation of stable formulations of ACE inhibitors, especially enalapril maleate.

Stable formulations of ACE inhibitors, and methods for preparation thereof

A method of producing a free flowing and compressible liquid/power admixture of an active drug substance, by converting the active substance into a liquisolid system. This is accomplished by introducing by the drug into a non-volatile liquid or a mixture of non-volatile and volatile liquids to from a mixture, selecting at least one solid carrier material and admixing these components to produce a non-adherent, free-flowing and compressible liquid/power mass admixture, the amounts of drug and carrier being selected to optimize flow and compressibility.

Liquisolid systems and methods of preparing same

Liquisolid systems are acceptably flowing and compressible powdered forms of liquid medications. According to the concept of liquisolid systems, liduid lipophilic drugs, or water-insoluble solid drugs dissolved in suitable non-volatile solvents, may be converted into free-flowing and readily compressible powders by a simple admixture with selected powder excipients referred to as the carrier and coating materials. Various grades of microcrystalline or amorphous cellulose may be used as carriers, whereas very fine particle size silica powders may be used as coating materials.

Liquisolid systems are acceptably flowing and compressible powdered forms of liquid medications. According to the concept of liquisolid systems, liquid lipophilic drugs, or water-insoluble solid drugs dissolved in suitable non-volatile solvents, may be converted into free-flowing and readily compressible powders by a simple admixture with selected powder excipients referred to as the carrier and coating materials. Various grades of microcrystalline or amorphous cellulose may be used as carriers, whereas very fine particle size silica powders may be used as coating materials. Based on the theory that the carrier and coating materials can retain only certain amounts of liquid and at the same time maintain acceptable flow and compression properties, a new formulation-mathematical model is provided to calculate the optimum quantities of carrier and coating materials required to yield acceptably flowing and compressible liquid/powder admixtures.

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Newtown, PA, United States of America

Spiridon Spireas