82 results about "Diphosphonates" patented technology

The present invention provides methods of treating or preventing a medical condition that is responsive to a bisphosphonate compound in a subject. The methods comprise administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of the bisphosphonate no less frequently than a bi-weekly dosage schedule. In some embodiment, the bisphosphonate compound is zoledronic acid.

The invention relates to a pharmaceutical composition and oral dosage forms comprising a bisphosphonate in combination with an enhancer to enhance intestinal delivery of the bisphosphonate to the underlying circulation. Preferably, the enhancer is a medium chain fatty acid or a medium chain fatty acid derivative having a carbon chain length of from 6 to 20 carbon atoms, and the solid oral dosage form is a controlled release dosage form such as a delayed release dosage form.

Compositions and methods for treating osteoporosis using the compositions are disclosed where the compositions have reduced GI toxicity and improved bio-availability and include a bisphosphonate and zwitterionic phospholipid.

An implantable medical device has a medical unit, such as a pacemaker lead, and a casing at least partially enclosing the medical unit. The casing is formed of a base polymer such as a polyurethane, a polyurethane copolymer, a fluoropolymer and a polyolefin or a silicone rubber. The casing has biologically active agents covalently bonded to the base polymer. The biologically active agents can be attached to the base polymer as surface active end groups. As an alternative, the biologically active may be attached to a backbone the base polymer. As yet a further alternative, the biologically active agents may be attached to surface modifying end groups, which are in turn attached to the base polymer. Examples of suitable biologically active agents are microbial peptide agents, detergents, non-steroidal anti-inflammatory drugs, cations, amine-containing organosilicones, diphosphonates, fatty acids and fatty acid salts.

A method of inhibiting the activity or production of cytokines or growth factors associated with vascular restenosis, by administering to an individual an effective amount of an active ingredient comprising a bisphosphonate particle or a bisphosphonate particulate. The bisphosphonate may be encapsulated, embedded or adsorbed within the particle, dispersed uniformly in the polymer matrix, adsorbed on the particle surface, or in combination of any of these forms. The particles include liposomes or inert polymeric particles, such as microcapsules, nanocapsules, nanoparticles, nanospheres, or microparticles. The particulates include any suspended or dispersed form of the bisphosphonate which is not encapsulated, entrapped, or adsorbed within a polymeric particle. The particulates include suspended or dispersed colloids, aggregates, flocculates, insoluble salts and insoluble complexes of the active ingredient. The cytokines and growth factors include, but are not limited to interleukin 1-β, matrix metalloproteinase-2, and platelet-derived growth factor β (PDGFβ).

This invention provides pharmaceutical compositions and methods related to the prevention and treatment of primary tumors and metastatic, malignant or spreading cancers by selectively targeting cancer associated myeloid derived cells by the targeted delivery of a bisphosphonate formulated with a non-liposomal particle carrier. In some aspects, the bisphosphonate particles have one or more properties suitable for phagocytosis by cancer associated myeloid derived cells and release of the bisphosphonate within the macrophages. Advantageously, administering the particles to a subject reduces the level and/or activity of cancer associated myeloid derived cells in the subject.

Oral dosage forms of a risedronate comprised of a safe and effective amount of a pharmaceutical composition comprising risedronate, a chelating agent, and, means for effecting delayed release of the risedronate and the chelating agent in the small intestine provide immediate release of the pharmaceutical composition to the small intestine of the mammal subject and pharmaceutically effective absorption of the bisphosphonate with or without food or beverages. The present invention substantially alleviates the interaction between risedronate and food or beverages, which interaction results in the bisphosphonate active ingredient not being available for absorption. The resulting oral dosage form may thus be taken with or without food. Further, the present invention effects delivery of risedronate and the chelating agent to the small intestine, substantially alleviating the upper GI irritation associated with bisphosphonate therapies. These benefits simplify previously complex treatment regimens and can lead to increased patient compliance with bisphosphonate therapies.

The present invention provides novel solid pharmaceutical dosage forms for oral administration comprising a bisphosphonate, or a pharmaceutically acceptable salt thereof, which bisphosphonate is present in an amount not therapeutically effective when the bisphosphonate is orally administered alone; and a modified amino acid carrier, or a pharmaceutically acceptable salt thereof, which modified amino acid carrier is present in an amount effective to facilitate absorption of the bisphosphonate in the gastrointestinal tract such that the bisphosphonate is therapeutically effective. The ratio of bisphosphonate to modified amino acid carrier is from about 1:30 to about 1:1, respectively. These novel solid pharmaceutical dosage forms are useful in the treatment or control of bone diseases and particular disorders in calcium metabolism, including, for example, osteoporosis, hypercalcaemia of cancer, and the treatment of metastatic bone pain. The present invention also provides a method for treating these diseases employing the solid pharmaceutical dosage forms and a method for preparing the pharmaceutical dosage forms.

Oral dosage forms comprising risedronate or a salt thereof, a chelating agent, and means for effecting delayed release of the risedronate (or salt) immediate release of the oral dosage form to the small intestine of the mammal subject and pharmaceutically effective absorption of the bisphosphonate with or without food or beverages. The present invention substantially alleviates the interaction between the risedronate (or salt) and food or beverages, which interaction results in the active ingredient not being available for absorption. The resulting oral dosage form may thus be taken with or without food. Further, disclosed is delivery of risedronate and the chelating agent to the small intestine, substantially alleviating the upper GI irritation associated with bisphosphonate therapies. These benefits simplify previously complex treatment regimens and can lead to increased patient compliance with bisphosphonate therapies.

Compositions and methods for the treatment of arthritis, particularly rheumatoid arthritis and osteoarthritis. These compositions include at least one antifolate and at least one bisphosphonate, or pharmaceutically acceptable salts thereof

The present invention provides a method of treating or preventing osteoporosis comprising administering to a patient in need thereof an effective amount of pharmaceutical composition comprising benzamidine derivative or its salt, and bisphosphonate for the purpose of using simultaneously, separately, or sequentially as active ingredients. As a prophylactic or therapeutic composition for osteoporosis, the combination treatment of the benzamidine derivative and the bisphosphonate compound exhibits excellent inhibitory effect on osteoclast differentiation than the total effect of each individual treatment, thereby being used for the prevention or treatment of osteoporosis.

A biomedical polymer has a substantially linear base polymer; and branched polyethylene oxide covalently bonded to the base polymer as surface active end groups. The branched polyethylene oxide has at least two, more particularly at least four, and still more particularly at least six branches. Suitable base polymers include epoxies, polyurethanes, polyurethane copolymers, fluoropolymers, polyolefins and silicone rubbers. Biologically active agents may be attached to the branched polyethylene oxide. Suitable biologically active agents include microbial peptide agents, detergents, non-steroidal anti-inflammatory drugs, cations, amine-containing organosilicones, diphosphonates, fatty acids, fatty acid salts, heparin and glucocorticosteroids. The biological polymer may be used as a casing for a medical unit of an implantable medical device, such as a pacemaker. In this case, the casing at least partially encloses the medical unit.

The invention provides a binuclear platinum (II)-diphosphonic acid coordination compound, a preparation method and an application thereof, and belongs to the field of anti-cancer drugs. The binuclear platinum (II)-diphosphonic acid coordination compound has the structural formula shown in the description, wherein n is 2, 3, 4 or 5. The preparation method of the binuclear platinum (II)-diphosphonic acid coordination compound comprises the following steps: diphosphonic acid derivative and Pt(en)(OSO3)(H2O) are reacted under the function of Ba(OH)2 to obtain the binuclear platinum (II)-diphosphonic acid coordination compound. According to the compound, a link arm of C between diphosphonates is expanded; quinary aromatic amine (namely imidazole) is introduced in, so that at the initial usage stage of the coordination compound, the coordination compound has high intake in tumour cells and long residence time; and the aggregation concentration of the coordination compound in other non-targeted tissues is greatly reduced.

The present invention provides for methods and compositions for treating and/or preventing cardiac dysfunction by administering to subject a therapeutically effective amount of a bisphosphonate, functional analogue or a pharmaceutically effective salt thereof.

The present invention relates to depot formulations comprising a poorly water soluble salt of a bisphosphonate forming together with one or more biocompatible polymers, to poorly water-soluble salts of such bisphosphonates, to crystalline forms of the free compounds and the salts and to other related aspects, where the compounds are of the Formula (I), where R₁ and R₂ are as described in the specification. Compounds of the Formula (I) and their forms mentioned in the disclosure are useful for the treatment of bone-related disorders and cancer.

Conjugates of polymers or copolymers having attached thereto an anti-angiogenesis agent and a bisphosphonate bone targeting agent, and processes of preparing same, are disclosed.

Pharmaceutical compositions containing these conjugates and uses thereof in the treatment of bone related disorders are also disclosed.

The invention relates to devices, methods and formulation for subcutaneous administration of a bisphosphonate. In such a device, a drug core, comprising a bisphosphonate, is disposed in a tube. The devices may be administered to a patient in need of subcutaneously wherein the release of the bisphosphonate is desired to provide sustained release of a therapeutically effective dose of the bisphosphonate.

Provided is a solid dispersion comprising vitamin D or a derivative thereof and a cyclodextrin; a complex formulation for the prevention or treatment of osteophorosis, which includes the solid dispersion and a bisphosphonate; and a method for preparing said complex formulation. The complex formulation can maintain a constant therapeutic level of vitamin D or a derivative thereof through its improved drug stability, while enhancing the patient compliance by minimizing inconvenience and adverse effects when administered to patients.

The present invention provides for the administration of aryl-substituted 1,1-diphosphonate compounds to increase the dermal collagen content of skin and effect improvement in photoaged skin, chronologically aged skin and in skin of postmenopusal women and patients suffering from osteoporosis.