Biphasic controlled release delivery system for high solubility pharmaceuticals and method

STABLE PHARMACEUTICAL COMPOSITION FOR OPTIMIZED DELIVERY OF AN HIV ATTACHMENT INHIBITOR

A pharmaceutical composition contains the compound 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-c]pyridin-3-yl]-1,2-dioxoethyl]-piperazine, and hydroxypropyl methyl cellulose (HPMC) having a viscosity of at least about 100 cP, wherein the composition does not contain any enzyme inhibitors. 1. A pharmaceutical composition consisting essentially of the phosphate ester prodrug of an HIV attachment inhibitor , 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1 ,2 ,4-triazol-1-yl)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2 ,3-c]pyridin-3-yl]-1 ,2-dioxoethyl]-piperazine in the form of a tris salt , and hydroxypropyl methyl cellulose (HPMC) having a hydrated viscosity of at least about 100 cP , microcrystalline cellulose , silicon dioxide , and magnesium stearate , wherein said composition provides a desired extended absorption of the parent compound when administered to humans , provides for stability of the prodrug against alkaline phosphatase while still contained within the dosage form under post-administration conditions , and further wherein said composition does not contain any enzyme inhibitors.2. The composition of claim 1 , wherein said compound is present in said composition in an amount of about 20-90% by weight.3. The composition of claim 2 , wherein said compound is present in an amount of about 50-85% by weight.4. The composition of claim 3 , wherein said compound is present in an amount of about 60-75% by weight.5. The composition of claim 1 , wherein said HPMC is present is said composition in an amount of about 10-50% by weight.6. The composition of claim 5 , wherein said HPMC is present in an amount of about 15-40% by weight.7. The composition of claim 6 , wherein said HPMC is present in an amount of about 20-30% by weight.8. The composition of claim 1 , wherein said HPMC has a viscosity of at least about 2000 cP.9. The composition of claim 8 , wherein said HPMC has a viscosity of at least about 3000 cP.10. The ...

Biphasic controlled release delivery system for high solubility pharmaceuticals and method

Novel salts of metformin and method

Biphasic controlled release delivery system for high solubility pharmaceuticals and method

A biphasic controlled release delivery system for pharmaceuticals which have high water solubility, such as the antidiabetic metformin HCl salt, is provided which provides a dosage form that has prolonged gastric residence so that a dosing regimen of at least one gram metformin, once daily, may be achieved while providing effective control of plasma glucose. The delivery system includes (1) an inner solid particulate phase formed of substantially uniform granules containing a pharmaceutical having a high water solubility, and one or more hydrophilic polymers, one or more hydrophobic polymers and/or one or more hydrophobic materials such as one or more waxes, fatty alcohols and/or fatty acid esters, and (2) an outer solid continuous phase in which the above granules of inner solid particulate phase are embedded and dispersed throughout, the outer solid continuous phase including one or more hydrophilic polymers, one or more hydrophobic polymers and/or one or more hydrophobic materials such ...

Formule medicamenteuse a liberation controlee

La formule pharmaceutique a liberation controlee selon l'invention libere un produit pharmaceutique de nature basique a une vitesse controlee quel que soit le pH du milieu. La formule contient un produit pharmaceutique basique, jusqu'a environ 45 % en poids d'un polymere dependant du pH qui est un sel de l'acide alginique, tel que l'alginate de sodium, jusqu'a environ 35 % en poids d'un agent de gelification qui est un hydrocolloide independant du pH, ayant une viscosite de jusqu'a environ 100 000 centipoises en solution a 2 % a 20 °C, un liant et des excipients. Le produit pharmaceutique de nature basique peut etre un antagoniste du calcium.

Bilayer tablet formulations

The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations.

Multilayered tablet containing pravastatin and aspirin and method

A multilayered tablet having three or more layers is provided which is useful for cholesterol lowering and reducing the risk of a myocardial infarction, which includes a first layer containing aspirin, another layer containing pravastatin, and a middle barrier layer, which preferably contains a buffering agent, which separates the first layer containing aspirin from the other layer containing pravastatin, and prevents or minimizes interaction of aspirin with pravastatin. A method for lowering cholesterol and reducing risk of a myocardial infarction employing such composition is also provided.

BILAYER TABLET FORMULATIONS

The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations. 1. A bilayer tablet comprising: (1) a first layer wherein the first layer is a metformin hydrochloride extended release formulation; (2) a second layer wherein the second layer is a sodium dependent glucose transporter-2 inhibitor (SGLT2 inhibitor) formulation comprising dapagliflozin , dapagliflozin (S) propylene glycol hydrate , dapagliflozin (R) propylene glycol hydrate or canagliflozin; and (3) optionally a film coating comprising polyvinyl alcohol , titanium dioxide , polyethylene glycol , and talc that covers the first layer and the second layer.232-. (canceled) This application is a continuation of U.S. patent application Ser. No. 14/706,077, filed May 7, 2015; said application Ser. No. 14/706,077 is a continuation of U.S. patent application Ser. No. 13/965,879, filed Aug. 13, 2013, now U.S. Pat. No. 9,050,258, issued Jun. 9, 2015; said application Ser. No. 13/965,879 is a divisional of U.S. patent application Ser. No. 13/509,210, filed Jul. 25, 2012, now U.S. Pat. No. 8,535,715, issued Sep. 17, 2013; said application Ser. No. 13/509,210 is a national stage filing under 35 U.S.C. §371 of International Patent Application no. PCT/US10/56529, filed Nov. 12, 2010, which claims benefit under 35 U.S.C. §119(e) of the following U.S. Provisional Patent Application No. 61/261,087, filed Nov. 13, 2009. Each of the above listed applications is incorporated by reference herein in its entirety for all purposes.The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) formulations or ...

Bilayer Tablet Formulations

The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations. 1. A bilayer tablet comprising: (1) a first layer wherein the first layer is a metformin hydrochloride extended release formulation; (2) a second layer wherein the second layer is a sodium dependent glucose transporter-2 inhibitor (SGLT2 inhibitor) formulation comprising dapagliflozin , dapagliflozin (S) propylene glycol hydrate , dapagliflozin (R) propylene glycol hydrate or canagliflozin; and (3) optionally a film coating comprising polyvinyl alcohol , titanium dioxide , polyethylene glycol , and talc that covers the first layer and the second layer.2. The bilayer tablet according to wherein the total weight of the second layer is 300 mgs to 400 mgs.3. The bilayer tablet according to wherein the (1) first layer comprises metformin hydrochloride claim 1 , a binder claim 1 , a release modifier claim 1 , a lubricant claim 1 , and optionally a glidant; and (2) the second layer comprises dapagliflozin or dapagliflozin (S) propylene glycol hydrate claim 1 , two or three fillers claim 1 , a disintegrant claim 1 , a glidant claim 1 , and a lubricant.4. A bilayer tablet comprising: (1) a first layer wherein the first layer is a metformin hydrochloride extended release formulation comprising metformin hydrochloride claim 1 , sodium carboxymethyl cellulose; hydroxypropyl methylcellulose; magnesium stearate; and optionally silicon dioxide or colloidal silicon dioxide; (2) a second layer wherein the second layer is a sodium dependent glucose transporter-2 inhibitor (SGLT2 inhibitor) formulation comprising dapagliflozin or ...

Bilayer tablet formulations

The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations.

Method of use of a biphasic controlled release delivery system for high solubility pharmaceuticals and method

A biphasic controlled release delivery system for pharmaceuticals which have high water solubility, such as the antidiabetic metformin HCl salt, is provided which provides a dosage form that has prolonged gastric residence so that a dosing regimen of at least one gram metformin, once daily, may be achieved while providing effective control of plasma glucose. The delivery system includes (1) an inner solid particulate phase formed of substantially uniform granules containing a pharmaceutical having a high water solubility, and one or more hydrophilic polymers, one or more hydrophobic polymers and/or one or more hydrophobic materials such as one or more waxes, fatty alcohols and/or fatty acid esters, and (2) an outer solid continuous phase in which the above granules of inner solid particulate phase are embedded and dispersed throughout, the outer solid continuous phase including one or more hydrophobic polymers, one or more hydrophobic polymers and/or one or more hydrophobic materials such as one or more waxes, fatty alcohols and/or fatty acid esters, which may be compressed into tablets or filled into capsules. Methods for forming the so-described biphasic controlled release delivery system and using such biphasic controlled release delivery system for treating diabetes are also provided.

STABLE PHARMACEUTICAL COMPOSITION FOR OPTIMIZED DELIVERY OF AN HIV ATTACHMENT INHIBITOR

A pharmaceutical composition contains the compound 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-c]pyridin-3-yl]-1,2-dioxoethyl]-piperazine, and hydroxypropyl methyl cellulose (HPMC) having a viscosity of at least about 100 cP, wherein the composition does not contain any enzyme inhibitors.

Bilayer tablet formulations

The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations.

Reduced Mass Metformin Formulations

The present invention relates to metformin extended release (XR) formulations with improved compactability to provide reduced mass tablets, granulations, and capsules. 1. A metformin pharmaceutical formulation comprising (1) metformin; (2) one or more binders; (3) one or more release modifiers; (4) , one or more glidants; (5) one or more lubricants; and (6) optionally a coating; wherein the pharmaceutical formulation is an extended release formulation in the form of a reduced mass tablet , stock granulation , or capsule.2. The pharmaceutical formulation according to comprising (1) metformin hydrochloride; (2) sodium carboxymethyl cellulose; (3) hydroxypropyl methylcellulose; (4) silicon dioxide or colloidal silicon dioxide; (5) magnesium stearate; and (6) optionally Opadry® II.3. The pharmaceutical formulation according to comprising (1) about 72-82% metformin hydrochloride; (2) about 3-5% sodium carboxymethyl cellulose; (3) about 15-22% hydroxypropyl methylcellulose 2208; (4) about 0.75-1.25% silicon dioxide or about 0.25-0.75% colloidal silicon dioxide; and (5) about 0.1-0.5% magnesium stearate.4. The pharmaceutical formulation according to comprising (1) about 76.6% metformin hydrochloride; (2) about 3.84% sodium carboxymethyl cellulose; (3) about 18% hydroxypropyl methylcellulose 2208; (4) about 1% silicon dioxide; and (5) about 0.53% magnesium stearate.5. The pharmaceutical formulation according to wherein there is a coating and the coating is Opadry® II.6. The pharmaceutical formulation according to comprising (1) about 1000 mgs of metformin hydrochloride; (2) about 50 mgs of sodium carboxymethyl cellulose; (3) about 235 mgs of hydroxypropyl methylcellulose 2208; (4) about 13 mgs of silicon dioxide; and (5) about 7 mgs of magnesium stearate.7. The pharmaceutical formulation according to wherein there is a coating and the coating is Opadry® II.8. A pharmaceutical formulation comprising (1) about 76.6% metformin hydrochloride; (2) about 3.84% sodium ...

REDUCED MASS METFORMIN FORMULATIONS

The present invention relates to metformin extended release (XR) formulations with improved compactability to provide reduced mass tablets, granulations, and capsules.

SOLID TABLET DOSAGE FORM OF RIDINILAZOLE

The present invention relates to solid tablet oral dosage forms of 2,2′-di(pyridin-4-yl)-1H,1′H-5,5′-bibenzo[d]imidazole (which may also be known as 2,2′-di-4-pyridinyl-6,6′-bi-1H-benzimidazole; 5,5′-bis[2-(4-pyridinyl)-1H-benzimidazole]; 2,2′-bis(4-pyridyl)-3H,3′H-5,5′-bibenzimidazole; or 2-pyridin-4-yl-6-(2-pyridin-4-yl-3H-benzimidazol-5-yl)-1H-benzimidazole), referenced herein by the INN name ridinilazole, and pharmaceutically acceptable derivatives, salts, hydrates, solvates, complexes, bioisosteres, metabolites or prodrugs thereof.

Bilayer Tablet Formulations

The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations.

BILAYER TABLET FORMULATIONS

The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations.

Amorphous form of 5-bromopyridin-3-yl 3-deoxy-3-[4-(3,4,5-trifluorophenyl)-1h-1,2,3-triazol-1-yl]-1-thio-alpha-d-galactopyranoside

A stabilized amorphous form of a compound of formula I as well as compositions for oral administration including the compound of formula I in a therapeutically effective amount. Also, methods for treatment of a disease or disorder in which therapeutically effective amount of a composition including a compound of formula I is administered to a subject in need thereof.

Phosphonosulfonate squalene synthetase inhibitor salts and method

New salt forms of the phosphonosulfonate squalene synthetase inhibitor are provided which include the calcium, the t-butylamine salt, t-octylamine salt and the dehydroabietylamine salt. These salts inhibit cholesterol biosynthesis and therefore are used in lowering serum cholesterol and in treating atherosclerosis.

Biphasic controlled release delivery system for high solubility pharmaceuticals and method

A biphasic controlled release delivery system for pharmaceuticals which have high water solubility, such as the antidiabetic metformin HCl salt, is provided which provides a dosage form that has prolonged gastric residence and includes (1) an inner solid particulate phase formed of substantially uniform granules containing a pharmaceutical having a high water solubility, and one or more hydrophilic polymers, one or more hydrophobic polymers and/or one or more hydrophobic materials such as one or more waxes, fatty alcohols and/or fatty acid esters, and (2) an outer solid continuous phase in which the above granules of inner solid particulate phase are embedded and dispersed throughout, the outer solid continuous phase including one or more hydrophilic polymers, one or more hydrophobic polymers and/or one or more hydrophobic materials such as one or more waxes, fatty alcohols and/or fatty acid esters, which may be compressed into tablets or filled into capsules. Methods for forming the so-described biphasic controlled release delivery system and using such biphasic controlled release delivery system for treating diabetes are also provided.

Biphasic controlled release delivery system for high solubility pharmaceuticals and method.

A biphasic controlled release delivery system for pharmaceuticals which have high water solubility, such as the antidiabetic metformin HC1 salt, is provided which provides a dosage form that has prolonged gastric residence and includes (1) an inner solid particulate phase formed of substantially uniform granules containing a pharmaceutical having a high water solubility, and one or more hydrophilic polymers, one or more hydrophobic polymers and/or one or more hydrophobic materials such as one or more waxes, fatty alcohols and/or fatty acid esters, and (2)an outer solid continuous phase in which the above granules of inner solid particulate phase are embedded and dispersed throughout, the outer solid continuous phase including one or more hydrophilic polymers, one or more hydrophobic polymers and/or one or more hydrophobic materials such as one or more waxes, fatty alcohols and/or fatty acid esters, which may be compressed into tablets or filled into capsules. Methods for informing the so-described biphasic controlled release delivery system and using such biphasic controlled release delivery system and using such biphasic controlled release delivery system for treating diabetes are also provided.

Biphasic controlled release delivery system for high solubility pharmaceuticals and method

A biphasic controlled release delivery system for pharmaceuticals which have high water solubility, such as the antidiabetic metformin HCl salt, is provided which provides a dosage form that has prolonged gastric residence and includes (1) an inner solid particulate phase formed of substantially uniform granules containing a pharmaceutical having a high water solubility, and one or more hydrophilic polymers, one or more hydrophobic polymers and/or one or more hydrophobic materials such as one or more waxes, fatty alcohols and/or fatty acid esters, and (2) an outer solid continuous phase in which the above granules of inner solid particulate phase are embedded and dispersed troughout, the outer solid continuous phase including one or more hydrophilic polymers, one or more hydrophobic polymers and/or one or more hydrophobic materials such as one or more waxes, fatty alcohols and/or fatty acid esters, which may be compressed into tablets or filled into capsules. Methods for forming the so-described biphasic controlled release delivery system and using such biphasic controlled release delivery system for treating diabetes are also provided.

Biphasic controlled release delivery system for high solubility pharmaceuticals and method

A biphasic controlled release delivery system for pharmaceuticals which have high water solubility, such as the antidiabetic metformin HCl salt, is provided which provides a dosage form that has prolonged gastric residence and includes (1) an inner solid particulate phase formed of substantially uniform granules containing a pharmaceutical having a high water solubility, and one or more hydrophilic polymers, one or more hydrophobic polymers and/or one or more hydrophobic materials such as one or more waxes, fatty alcohols and/or fatty acid esters, and (2) an outer solid continuous phase in which the above granules of inner solid particulate phase are embedded and dispersed throughout, the outer solid continuous phase including one or more hydrophilic polymers, one or more hydrophobic polymers and/or one or more hydrophobic materials such as one or more waxes, fatty alcohols and/or fatty acid esters, which may be compressed into tablets or filled into capsules. Methods for forming the so-described biphasic controlled release delivery system and using such biphasic controlled release delivery system for treating diabetes are also provided.

Biphasic controlled release delivery system for high solubility pharmaceuticals and method

Bilayer tablet formulations

Salts of metformin and method

Novel salts of the antidiabetic agent metformin acre provided which are metformin salts of dibasic acids (2:1 molar ratio), preferably metformin (2:1) fumarate and metformin (2:1) succinate, which may be employed alone or in combination with another antihyperglycemic agent such as glyburide, for treating diabetes. A method for treating diabetes employing the novel metformin salt by itself or in combination with another antidiabetic agent is also provided.

PHARMACEUTICAL PREPARATIONS IN THE FORM OF BIOADHESIVE SUPPOSITORIES

COMPOSITION DE SUPPOSITOIRE BIOADHESIF COMPRENANT UN MEDICAMENT DANS UNE QUANTITE COMPRISE ENTRE ENVIRON 0,1 ET ENVIRON 25 DU POIDS DE LA COMPOSITION TOTALE, UN HYDROCOLLOIDE DANS UNE QUANTITE COMPRISE ENTRE ENVIRON 0,5 ET ENVIRON 20 DU POIDS DE LA COMPOSITION, DE L'EAU DANS UNE QUANTITE COMPRISE ENTRE ENVIRON 30 ET ENVIRON 65 DU POIDS DE LA COMPOSITION, ET UNE BASE DE SUPPOSITOIRE A BAS POINT DE FUSION, TELLE QUE, PEU APRES L'INSERTION DUDIT SUPPOSITOIRE A L'ENDROIT D'ACTION VOULU, LADITE BASE DE SUPPOSITOIRE FOND ET FORME UNE EMULSION PAR LAQUELLE LEDIT HYDROCOLLOIDE ET LEDIT MEDICAMENT SONT LIBERES POUR ADHERER A L'ENDROIT D'ACTION VOULU ET Y ETRE RETENUS. APPLICATION AUX SUPPOSITOIRES ANTIFONGIQUES ETOU ANTIBACTERIENS. BIOADHESIVE SUPPOSITORY COMPOSITION CONSISTING OF A MEDICINAL PRODUCT IN AN AMOUNT BETWEEN ABOUT 0.1 AND ABOUT 25 OF THE WEIGHT OF THE TOTAL COMPOSITION, A HYDROCOLLOID IN AN AMOUNT BETWEEN ABOUT 0.5 AND ABOUT 20 OF THE WEIGHT OF THE COMPOSITION, WATER IN AN AMOUNT BETWEEN ABOUT 30 AND ABOUT 65 OF THE WEIGHT OF THE COMPOSITION, AND A LOW MELTING-POINT SUPPOSITORY BASE, SUCH AS, SHORTLY AFTER THE INSERTION OF THE SAID SUPPOSITORY AT THE DESIRED PLACE OF ACTION, THE SAID SUPPOSITORY BASE SUBSTANCES AND SHAPES AN EMULSION BY WHICH THE HYDROCOLLOID AND THE MEDICINAL PRODUCT ARE RELEASED TO ADHER TO THE DESIRED PLACE OF ACTION AND TO BE HELD THERE. APPLICATION TO ANTIFUNGAL AND ANTIBACTERIAL SUPPOSITORIES.

CONTROLLED RELEASE DRUG FORMULA

Tablet composition and method for problem pharmaceutical materials using citric acid

In accordance with the present invention an improved tablet composition for drugs or active ingredients prone to poor tabletting properties is disclosed. The improved composition comprises a premixture, consisting essentially of between about 85 and 99.9 percent by weight of the active ingredient and between about 0.1 and 15 percent by weight of citric acid, and one or more other formulation ingredients added to premixture. The present invention also involves the process for making such compositions and products therefrom.

Phosphonosulfonate squalen synthetase inhibitor salts and process for preparing thereof

Bilayer tablet formulations

The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations.

Patent CH674463A5

Extended release formulation for optimized delivery of an hiv attachment inhibitor

A pharmaceutical composition contains the compound 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1--yl)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-c]pyridin-3-yl]-1,2-dioxoethyl]-piperazine, and hydroxypropyl methyl cellulose (HPMC) having a viscosity of at least about 100 cP, wherein the composition does not contain any enzyme inhibitors.

Controlled release formulation

Bilayer tablet formulations

The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations.

Bilayer tablet formulations

A coated tablet that comprises: (1) a tablet core comprising metformin; (2) a first coating that coats the tablet core and optionally comprises saxagliptin; (3) a second coating 5 that coats the first coating and optionally comprises saxagliptin; and (4) optionally a third coating that coats the second coating; wherein at least one of the first coating and the second coating comprises saxagliptin.

Nefazodone dosage form

Extended-release nefazodone compositions containing nefazodone hydrochloride, ionic and non-ionic gelling polymers, an insoluble hydrophilic agent, and optional pharmaceutically acceptable excipients demonstrate pH-modulated release of nefazodone. These compositions are formulated into unit dosage forms for improved oral administration. The improvements comprise an extended drug release profile providing comparative levels of nefazodone with respect to immediate release dosage forms and, additionally, demonstrating the lack of a food effect.

Method of preparing liposomes and products produced thereby

A method for preparing stable liposome precursors in the form of water-soluble carrier materials coated with thin films of liposome components includes the steps of dissolving at least one liposome-forming amphipathic lipid, optionally at least one biologically active compound, and, optionally, at least one adjuvant in a suitable solvent and employing the resulting solution to coat a water-soluble carrier material to form thin films of liposome components thereon. Upon exposing the coated carrier material to water, the thin films of liposome components hydrate and the carrier material dissolves to give liposome preparations.

Alkylammonium complexes of diatrizoic acid as X-ray contrast agents

New X-ray contrast agents are provided which are alkylammonium complexes of diatrizoic acid having the structure ##STR1## X-ray contrast medium containing the above X-ray contrast agent and a carrier therefor such as a liposome carrier, and a method for the X-ray visualization of body cavities and organs are also provided.

Buoyant controlled release powder formulation

A buoyant controlled release pharmaceutical powder formulation is provided which may be filled into capsules and releases a pharmaceutical of a basic character at a controlled rate regardless of the pH of the environment, which formulation includes a basic pharmaceutical, up to about 45% by weight of a pH dependent polymer which is a salt of alginic acid, such as sodium alginate, up to about 35% by weight of a pH-independent hydrocarbon gelling agent having a viscosity of up to about 100,000,centipoises in 2% solution at 20°C and excipients.

Method of preparing liposomes and products produced thereby

ABSTRACT METHOD OF PREPARING LIPOSOMES AND PRODUCTS PRODUCED THEREBY A method is provided for preparing a stable liposome precursors in the form of a particulate carrier materials coated with thin films of liposome components, which method includes the steps of dissolving at least one liposome-forming amphipathic lipid, optionally, at least one biologically active compound, and, optionally, at least one adjuvant in a suitable solvent and employing the resulting solution to coat a suitable particulate carrier material which is substantially insoluble in the above-mentioned solvent, to form thin films of liposome components thereon. Upon exposing the coated carrier material to water, the thin films of liposome components hydrate. If the carrier material is water-insoluble, it is then separated e.g. by filtrationor centrifuging.

Dosage of nefazodone

Jsou popsány prostředky s prodlouženýmuvolňováním, které obsahují nefazadon-hydrochlorid, iontové a neiontové polymety tvořící gel, nerozpustnou hydrofilní látku a případné farmaceuticky přijatelné expicienty demonstrující uvolňování nefazodonu uvolňované pH. Tyto prostředkyjsou formulovány dojednotkových dávkových forempro zdokonalené perorální podávání. Zdokonalení zahrnují profil prodlouženého uvolňování léčiva, který poskytuje srovnatelné hladiny nefazodonu v porovnání s dávkovými formami s okamžitýmuvolňováníma navíc demonstruje postrádání závislosti účinků najídle. Extended release means are described they contain nephazadone hydrochloride, ionic and nonionic gel forming polymers, insoluble hydrophilic substance and optionally pharmaceutically acceptable release demonstrating excipients the pH of nefazodone. These resources are formulated unit dose forempro improved oral administration. Improvements include a profile prolonged release of the drug which provides comparable levels of nefazodone compared to dosage forms moreover, with immediate election, it demonstrates lack dependence effects.

Tablet composition and method for problem pharmaceutical materials

TU30 TABLET COMPOSITION AND METHOD FOR PROBLEM PHARMACEUTICAL MATERIALS Abstract In accordance with the present invention an improved tablet composition for drugs or active ingredients prone to poor tabletting properties is disclosed. The improved composition comprises a premixture, consisting essentially of between about 85 and 99.9 percent by weight of the active ingredient and between about 0.1 and 15 percent by weight of citric acid, and one or more other formulation ingredients added to the premixture. The present invention also involves the process for making such compositions and products therefrom.

Phosphonosulfonate squalene synthetase inhibitor salts and method

Suppositories

Method of preparing liposomes and products produced thereby

A method is provided for preparing a stable liposome precursors in the form of a particulate carrier materials coated with thin films of liposome components, which method includes the steps of dissolving at least one liposome-forming amphipathic lipid, optionally, at least one biologically active compound, and, optionally, at least one adjuvant in a suitable solvent and employing the resulting solution to coat a suitable particulate carrier material which is substantially insoluble in the above-mentioned solvent, to form thin films of liposome components thereon. Upon exposing the coated carrier material to water, the thin films of liposome components hydrate. If the carrier material is water-insoluble, it is then separated e.g. by filtration or centrifuging.

Controlled release formulation

A controlled release pharmaceutical formulation is provided which releases a pharmaceutical of a basic character at a controlled rate regardless of the pH of the environment, which formulation includes a basic pharmaceutical, up to about 45% by weight of a pH dependent polymer which is a salt of alginic acid, such as sodium alginate, up to about 35% by weight of a pH-independent hydrocarbon gelling agent having a viscosity of up to about 100,000 centipoises in 2% solution at 20 DEG C., binder and excipients. [US4792452A]

Bilayer tablet formulations

The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations.

Phosphonosulphonate salts of squale synthetase inhibitor and method of their production

Bilayer tablet formulations

A coated tablet that comprises: (1) a tablet core comprising metformin; (2) a first coating that coats the tablet core and optionally comprises saxagliptin; (3) a second coating 5 that coats the first coating and optionally comprises saxagliptin; and (4) optionally a third coating that coats the second coating; wherein at least one of the first coating and the second coating comprises saxagliptin.

Extended release formulation for optimized delivery of an hiv attachment inhibitor

A pharmaceutical composition contains the compound 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-c]pyridin-3-yl]-1,2-dioxoethyl]-piperazine, and hydroxypropyl methyl cellulose (HPMC) having a viscosity of at least about 100 cP, wherein the composition does not contain any enzyme inhibitors.

Process for producing powdery pharmaceutical compositions with floaring properties and controlled release of active ingredient

A találmány tárgya eljárás a gyomornedvben lebegni képes,kalciumionoktól mentes, szabályozott hatóanyag-- leadású, por alakúgyógyszerkészítmény előállítására, melyből egy bázikus jellegűhatóanyag a környezet pH-jától függetlenül, szabályozott mértékbenszabadul fel, amely abban áll, hogy egy bázikus jellegű hatóanyagot,15– 50 tömeg% mennyiségben egy vagy több pH-függő polimert, amely egypoliuronsav-só, 5–35 tömeg% mennyiségben egy vagy több, pH-tólfüggetlen, hidrokolloid gélképző szert, melynek viszkozitása 0,015–100Pa·s 2%-os oldatban, 20 °C-on, a gyógyszerkészítésben szokásosanalkalmazott segédanyagokkal összekeverve gyógyszerkészítménnyéalakítanak. ŕ

Phosphonosulfonate squalene synthetase inhibitor salts and method

Phosphonosulfonate squalene synthetase inhibitor salts and method

New salt forms of the phosphonosulfonate squalene synthetase inhibitor are provided which include the calcium, the t-butylamine salt, t-octylamine salt and the dehydroabietylamine salt. These salts inhibit cholesterol biosynthesis and therefore are used in lowering serum cholesterol and in treating atherosclerosis.

Amorphous form of 5-bromopyridin-3-yl 3-deoxy-3-[4-(3,4,5-trifluorophenyl)-1h-1,2,3-triazol-1-yl]-1-thio-alpha-d-galactopyranoside

The present invention relates to a stabilized amorphous form of a compound of formula (I) as well as compositions for oral administration comprising the compound of formula (I) in a therapeutically effective amount.

Reduced mass metformin formulations

The present invention relates to metformin extended release (XR) formulations with improved compactability to provide reduced mass tablets, granulations, and capsules.

Bilayer tablet formulations

Formulazione a rilascio controllato.

Φαρμακοτεχνικες μορφες διστρωματικου δισκιου

Η παρούσα εφεύρεση σχετίζεται με φαρμακοτεχνικές μορφές διστρωματικού δισκίου που περιλαμβάνουν φαρμακοτεχνική μορφή μετφορμίνης παρατεταμένης απελευθέρωσης (ΠΑ) ή φαρμακοτεχνική μορφή μετφορμίνης ΠΑ μειωμένης μάζας ως το πρώτο στρώμα, φαρμακοτεχνική μορφή SGLT2 αναστολέα ως το δεύτερο στρώμα, και προαιρετικά επικάλυψη υμενίου. Η παρούσα εφεύρεση παρέχει μεθόδους παρασκευής των φαρμακοτεχνικών μορφών διστρωματικού δισκίου και μεθόδους αγωγής παθήσεων ή διαταραχών συνδεόμενων με SGLT2 ενεργότητα με χρήση των φαρμακοτεχνικών μορφών διστρωματικού δισκίου.

Neue metformin salze und verfahren

Stabile pharmazeutische zusammensetzung zur optimierten abgabe eines hiv-attachment- inhibitors

Mehrschichtige tablette mit pravastatin und aspirin und verfahren

Solid tablet dosage form of ridinilazole

The present invention relates to solid tablet oral dosage forms of 2,2'-di(pyridin-4-yl)-1 H ,1' H -5,5'-bibenzo[d]imidazole (which may also be known as 2,2'-di-4-pyridinyl-6,6'-bi-1H-benzimidazole; 5,5'-bis[2-(4-pyridinyl)-1 H -benzimidazole]; 2,2'-bis(4-pyridyl)-3H,3'H-5,5'-bibenzimidazole; or 2-pyridin-4-yl-6-(2-pyridin-4-yl-3 H -benzimidazol-5-yl)-1 H -benzimidazole), referenced herein by the INN name ridinilazole , and pharmaceutically acceptable derivatives, salts, hydrates, solvates, complexes, bioisosteres, metabolites or prodrugs thereof.

Tablett med flere lag, inneholdende pravastatin og aspirin, og fremgangsmate

Det er tilveiebrakt en flerlagstablett med tre eller flere lag som er anvendelig for kolesterolnedsettelse og reduksjon av risiko for myokardinfarkt, som innbefatter et første lag inneholdende aspirin, et annet lag inneholdende pravastatin og et midtre barrierelag som fortrinnsvis inneholder et bufringsmiddel og som skiller det første lag inneholdende aspirin fra det andre lag inneholdende pravastatin og forhindrer eller minimaliserer interaksjon mellom aspirin og pravastatin. En fremgangsmåte for nedsettelse av kolesterol og reduksjon av risiko for myokardinfarkt ved anvendelse av slikt preparat er også tilveiebrakt.

Nefazodon dózisalak

A találmány tárgyát tartós kibocsátási idejű nefazodonkészítményekképezik, amelyek nefazodon-hidrokloridot, ionos és nem ionos gélesítőpolimereket, oldhatatlan hidrofil ágenst, és adott esetben gyógyászatiszempontból elfogadható segédanyagokat tartalmaznak, és amelyek anefazodon pH-függő (pH-modulált) kibocsátását teszik lehetővé. Atalálmány szerinti készítményekből - javított perorális adagoláscéljából - egységdózis-alakok állíthatók elő. A találmány szerintidózisalakok a korábbi készítményekhez képest annyiban javítottak, hogyaz azonnali kioldódású dózisalakokkal összehasonlítva hasonló mértékűnefazodon-koncentrációt biztosító, tartós hatóanyagfelszabadulásttesznek lehetővé, és hatóanyag-kibocsátásuk nem függ a gyomor- ésbélrendszer tápláléktartalmától. Ó

Preparazioni farmaceutiche per supposte bioadesive.

Forma amorfa de 5-bromopiridin-3-il 3-desoxi-3-[4-(3,4,5-trifluorofenil)-1h-1,2,3-triazol-1-il]-1-tio-alfa-d-galactopiranosídeo

forma amorfa de 5-bromopiridin-3-il 3-desoxi-3-[4-(3,4,5-trifluorofenil)-1h-1,2,3-triazol-1-il]-1-tio-alfa-d-galactopiranosídeo. a presente invenção está relacionada a uma forma amorfa estabilizada de um composto de fórmula (i), bem como composições para administração oral compreendendo o composto de fórmula (i) em uma quantidade terapeuticamente eficaz.

Amorphous form and process

The present invention relates to a stabilized amorphous form of a compound of formula I, and compositions for oral administration comprising the compound of formula I in a therapeutically effective amount. The compound of formula I is a galectin 3 inhibitor useful for treating disorders or diseases, including: inflammation; fibrosis; scarring; keloid formation; surgical adhesions; septic shock; cancer; autoimmune diseases; metabolic disorders; heart disease; heart failure; pathological angiogenesis; eye diseases; atherosclerosis; metabolic diseases; obesity; Diastolic HF; lung disease; and liver disorders. The amorphous form of the compound of formula I is stabilized with polymers when sprayed onto inert particles as well as when prepared as an amorphous solid dispersion.

Multilayered tablet containing pravastatin and aspirin and method

Tablett med flere lag inneholdende pravastatin og aspirin og fremgangsmate

Multilayered tablet containing pravastatin and aspirin and method

A multilayered tablet having three or more layers is provided which is useful for cholesterol lowering and reducing the risk of a myocardial infarction, which includes a first layer containing aspirin, another layer containing pravastatin, and a middle barrier layer, which preferably contains a buffering agent, which separates the first layer containing aspirin from the other layer containing pravastatin, and prevents or minimizes interaction of aspirin with pravastatin. A method for lowering cholesterol and reducing risk of a myocardial infarction employing such composition is also provided.

Lagskipt tafla, sem inniheldur pravastatín og aspirín, og aðferð

Veäśslojna tableta, ki vsebuje pravastatin in aspirin, ter postopek

Comprimido de camadas múltiplas contendo pravastatina e aspirina e método

Lagskipt tafla, sem inniheldur pravastatín og aspirín, og aðferð

Mehrschichtige tablette mit pravastatin und aspirin und verfahren

Δισκιο πολλαπλων στρωματων που περιεχει πραβαστατινη και ασπιρινη και μεθοδος

Παρέχεται ένα δισκίο πολλαπλών στρωμάτων, που έχει τρία ή περισσότερα στρώματα, το οποίο είναι χρήσιμο για την ελάττωση της χοληστερίνης και την μείωση του κινδύνου ενός μυοκαρδιακού εμφράγματος, το οποίο δισκίο περιλαμβάνει ένα πρώτο στρώμα που περιέχει ασπιρίνη, ένα άλλο στρώμα που περιέχει πραβαστατίνη και ένα μεσαίο στρώμα φραγμού το οποίο περιέχει κατά προτίμηση ένα ρυθμιστικό του pΗ μέσον το οποίο διαχωρίζει το πρώτο στρώμα που περιέχει ασπιρίνη από το άλλο στρώμα που περιέχει πραβαστατινη και εμποδίζει ή ελαχιστοποιεί αλληλεπίδραση από ασπιρίνη με πραβαστατινη. Μία μέθοδος για την ελάττωση της χοληστερίνης και την μείωση του κινδύνου ενός μυοκαρδιακού εμφράγματος με χρησιμοποίηση μίας τέτοιας σύνθεσης παρέχεται επίσης.

Multilayered tablet containing pravastatin and aspirin

A multilayered tablet having three or more layers is provided which is useful for cholesterol lowering and reducing the risk of a myocardial infarction, which includes a first layer containing aspirin, another layer containing pravastatin, and a middle barrier layer, which preferably contains a buffering agent, which separates the first layer containing aspirin from the other layer containing pravastatin, and prevents or minimizes interaction of aspirin with pravastatin. A method for lowering cholesterol and reducing risk of a myocardial infarction employing such composition is also provided.

Kompozycja farmaceutyczna zawierająca prawastatynę i aspirynę

Solid tablet dosage form of ridinilazole

The present invention relates to solid tablet oral dosage forms of 2,2'-di(pyridin-4-yl)-1

Forma de dosificacion en tableta solida de ridinilazol.

La presente invención se refiere a formas de dosificación oral en tabletas sólidas de 2,2'-di(piridin-4-il)-1H,1'H-5,5'-bibenzo[d]im idazol (que también se puede conocer como 2,2'-di-4-piridinil-6,6' -bi-1H-bencimidazol; 5,5'-bis[2-(4-piridinil)-1H-bencimidazol]; 2,2'-bis(4-piridil)-3H,3'H-5,5'-bibencimidazol; o 2-piridin-4-il-6-(2-piridin-4-il-3H-bencimidazol-5-il)-1H-bencimi dazol), al que se hace referencia en la presente descripción con el nombre INN ridinilazol y derivados, sales, hidratos, solvatos, complejos, bioisósteros, metabolitos o profármacos farmacéuticamente aceptables del mismo.

Process for the preparation of antibacterial compounds

The present invention relates to a process for the production of an antibacterial compound suitable for use in the treatment of infection with, or disease caused or exacerbated by, Gram-negative bacteria of the order Enterobacterales and/or Gram-negative bacteria of the genus Haemophilus .

Schwimmende pulverformige formulierung mit gesteuerter freigabe