WO2010090614A1 - Formulation pharmaceutique comprenant du risédronate, du carbonate de calcium et de la vitamine d3 combinés en une forme posologique unique - Google Patents

Formulation pharmaceutique comprenant du risédronate, du carbonate de calcium et de la vitamine d3 combinés en une forme posologique unique Download PDF

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Publication number
WO2010090614A1
WO2010090614A1 PCT/TR2010/000026 TR2010000026W WO2010090614A1 WO 2010090614 A1 WO2010090614 A1 WO 2010090614A1 TR 2010000026 W TR2010000026 W TR 2010000026W WO 2010090614 A1 WO2010090614 A1 WO 2010090614A1
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Prior art keywords
calcium
sodium
range
composition according
weight
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PCT/TR2010/000026
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English (en)
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Bilgic Mahmut
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Bilgic Mahmut
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Publication of WO2010090614A1 publication Critical patent/WO2010090614A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/59—Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
    • A61K31/593—9,10-Secocholestane derivatives, e.g. cholecalciferol, i.e. vitamin D3
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/06—Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
    • A61K33/10—Carbonates; Bicarbonates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • A61K9/0007—Effervescent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis

Definitions

  • the invention relates to stable pharmaceutical compositions comprising combination of the active ingredients in a single dosage for in order to increase the patients' complience to the treatment and hence the success of the treatment.
  • the present invention provides an effective combination for the prevention and/or treatment and/ or supplement of diseases and conditions associated with the abnormal bone resorption.
  • the effect caused by the combination prepared according to the present invention is named as "desired effect" thoughout this document.
  • the combination of the present invention includes a calcium salt, vitamin-D and risedronate or pharmaceutically acceptable salt, derivative or hydrate thereof.
  • Risedronic acid is a bisphosphonate whose chemical name is [l-hydroxy-2-(3- pyridinyl)ethylidene] bisphosphonic acid (Formula I).
  • risedronic acid is first disclosed in the patent numbered US5583122A (with EPO 186405 in its patent family).
  • the patent discloses processes for preparation of risedronic acid and use of risedronic acid for treatment of diseases related to abnormal bone and phosphate metabolism.
  • Risedronate is a strong antiresorptive agent that does not effect mineralization in bone. Like other bisphosphonates, it inhibits osteoclast (a kind of bone cell that destroys bone tissue by removing the bone matrix) mediated bone resorption. Bone resorption occurs by ruffled edges of osteoclasts that are in contact with the bone which are capable of making resorption. Risedronate inhibits the resorption by localizing specially under the resorption area of osteoclasts. Bisphosphonates that are taken in by the osteoclasts on one hand cause disruption of the bone structure and on the other hand they cause loss of the ruffled edges. Risedronate may cause osteoclast apoptosis. In time normal bone tissues which are produced by osteoblasts plank down onto risedronate.
  • Gastrointestinal side effect indicidents are much lower for risedronate compared to other bisphosphonates.
  • Risedronate decelarates the bone cycle. It causes an increase in bone mass where the bone formation exceeds bone resorption. It also decreases the direct resorption of bone in Paget disease which is a progressive and idiopathic disease wherein the bone metabolism is accelarated and re-shaped. After the six months treatment, deformed bone is transformed into the normal bone structure. It sharply increases the bone mineral density in postmenopausal osteoporosis which is characterized with progressive loss of bone causing increase in fragility of bone density. It decreases vertebral fracture incidence in postmenopausal osteoporosis by a ratio of 65% in a year.
  • Vitamin D is a group of fat-soluble prohormones, the two. major forms of which are vitamin D 2 (or ergocalciferol) and vitamin D 3 (or cholecalciferol). In addition to that D 1 , D 4 ve D 5 forms and metabolites and analogs of these compounds are persent too.
  • Vitamin D3 is a form of vitamin D with the chemical name of (3 ⁇ ,5Z,7E)-9,10-secocholesta-5,7,10(19)-trien-3-ol (Formula II)
  • Vitamin D3 is a form of Vitamin D that is synthesized in human body naturally. Vitamin D3 is synthesized naturally in the mammal skin from 7-dehydrocholesterol under the action of UV light. It can be partially provided by animal products. Vitamin D3 undergoes biotransformation in kidney and liver and turn into its active form of 1,25-dihydroxycholecalciferol ( [1,25-(OH) 2 D 3 ] veya calcitriol).
  • Calcium is the chemical element shown with the symbol "Ca”. It is the most abundant mineral found in the human body. 99% of body calcium is found in bone tissue. It plays an important role on bone structure and muscle contractions. The blood coagulation, neural transmission and the provision of electrical conduction in the heart depends on calcium. Parathyroid hormone, , vitamin D, calcitonin, glucocorticoids and magnesium can affect the balance of calcium.
  • Calcium and its salts are used for treatment or prophylaxis of calcium deficiency.
  • Calcium can be administered by oral route in carbonate, chloride, citrate, glubionate, gluceptate, gluconate, lactate, or phosphate salt forms; and it can be administered by parenteral route in acetate, chloride, gluceptate, gluconate, and glycerophosphate / lactate salt forms.
  • Minimum daily requirement of calcium in the postmenopausal women is 1500 mg. In the premenopausal women, this amount is 1000 mg. This indicates that in the in the post menopausal period a woman needs at least 500 mg / day of additional calcium supplementation. Vitamin D is required for absorption of calcium. It was determined that vitamin D deficiency and osteoporosis that develops as a result of this is a risk factor for falls and fractures. In the postmenopausal women, due to vitamin D deficiency, calcium absorption is reduced. Various clinical studies have showed that daily calcium and vitamin D intake in men, just like in women, is lower than the recommended dose. This increases the probability of ratio of diseases (osteoporosis, osteomalacia, etc.) originating from vitamin D and calcium deficiency in adults of advanced age. Therefore in addition to paying attention to dietary factors, the use of various drugs supplements is also recommended.
  • WO03086415 Al a pharmaceutical composition comprising a compination of an inactive metabolite of vitamin D 2 and/or D 3 and at least one biphosphonate is disclosed.
  • the patent numbered WO2005027921 Al describes a pharmaceutical composition which includes 2-methylene-19-nor-20(S)- l ⁇ ,25-dihydroxyvitamin D3 and a biphosphonate.
  • WO9906051 Al 5 a pharmaceutical composition which is characterized in that it comprises a binding agent chosen from the group consisting of propylene glycol, a polyethylene glycol with a molecular weight between 300 and 1500, liquid paraffin or silicone oil and that the Vitamin D is present at the rate of 1 - 2 g of calcium for 500 1000 LU. of Vitamin D. has been described.
  • a binding agent chosen from the group consisting of propylene glycol, a polyethylene glycol with a molecular weight between 300 and 1500, liquid paraffin or silicone oil and that the Vitamin D is present at the rate of 1 - 2 g of calcium for 500 1000 LU. of Vitamin D. has been described.
  • Patent numbered EP0969849 Bl describes pharmaceutical preparations containing a combination of an active form of vitamin D3 and tricalcium phosphate.
  • a bone mineral supplement which comprises calcium in the form of calcium citrate maleate in the range of 100-1000 mg (on an elemental basis), and vitamin D wherein said vitamin D is administered as its biologically active metabolites or precursors selected from l ⁇ , 25- (OH) 2 vitamin D; 25 OH vitamin D 5 l ⁇ OH vitamin D 2 or D 3 , or analogues of the dihydroxy compound in amounts equivalent to 0.60-30 ⁇ g vitamin D has been described.
  • a complicated dose regime, especially multiple drug use in several times a day is one of the most significant factor to prevent the patient's complience to treatment.
  • the patient compliance and therefore the success of treatment will be higher if the treatment regimen is much simpler.
  • the combination of the active ingredients in a single dosage form will simplify treatment and increase patient's complience to treatment[Blonde L. Compliance and Persistence With Medication Therapy. Managed Care (2000). Volume 9, Number 9; archives.who.int/icium/icium2004/resources/ppt/AC016.ppt.].
  • the negative impact of talcing multiple drug on patients will also be eliminated by the use of a combined medication in the form of a single dosage form.
  • the present invention is directed to obtain a triple combination of risedronate (or pharmaceutically acceptable salts, derivatives or hydrates thereof), a calcium salt and vitamin D in a single dosage form so as to increase patient complience to the treatment and thus the treatment success.
  • the invention is characterized in that risedronate (or pharmaceutically acceptable salts, derivatives or hydrates thereof), a calcium salt and pharmaceutically acceptable, non-toxic and therapeutic amount of vitamin D are combined in a single dosage form to achieve desired effect by providing a suitable formulation of these three active agents prepared according to the present invention.
  • formulations containing vitamin D are faced with stability problems because vitamin D tends to degrade upon exposure to heat, light, air, moisture, oxidizing agents or when exposed to an environment with acidic pH. This condition brings along the necessity of the selection of suitable cxcipients so as to ensure stability of vitamin D in tablet.
  • the present invention provides a stabilized pharmaceutical composition wherein risedronate (or pharmaceutically acceptable salts, derivatives or hydrates thereof), a calcium salt and vitamin D are combined in a single dosage form so as to obtain desired effect starting from increasing patient's compliance and thus the success of the treatment.
  • the pharmaceutical preparations of the present invention may include at least one stabilizing agent to ensure stability of vitamin D.
  • the present invention relates to a pharmaceutical composition for use in the treatment and/or prophylaxis of diseases and conditions associated with abnormal bone resorption and/or used as a supplement characterized in that the pharmaceutical composition comprises therapeutically effective amount of risedronate or pharmaceutically acceptable salt, derivative or hydrate thereof, therapeutically effective amount of a calcium salt and therapeutically effective amount of vitamin D combined in a single dosage form.
  • the present invention provides a stabilized pharmaceutical composition in a single dosage form which comprises risedronate or pharmaceutically acceptable salt, derivative or hydrates thereof, a calcium salt and vitamin D to increase patient compliance and thus the success of treatment and to achieve the desired effect.
  • the formulations in a single dosage form comprise a certain proportion of risedronate (or pharmaceutically acceptable salt, derivative or hydrate thereof), a certain proportion of calcium salts and a certain proportion of vitamin D, and optionally one or more pharmaceutically acceptable excipients selected from diluent, binder, disintegrant, lubricant, glidant, surface active agent, stabilizing agent, sweetener and flavoring agent in which the formulation is effective for the prevention and/or treatment and/or supplementation of diseases associated with abnormal bone resorption and mentioned formulations increase the compliance of patient to treatment and thus the success of the treatment.
  • risedronate or pharmaceutically acceptable salt, derivative or hydrate thereof
  • calcium salts and a certain proportion of vitamin D
  • optionally one or more pharmaceutically acceptable excipients selected from diluent, binder, disintegrant, lubricant, glidant, surface active agent, stabilizing agent, sweetener and flavoring agent in which the formulation is effective for the prevention and/or treatment and/or supplementation of diseases associated with abnormal bone
  • the term of "the use for the prevention and/or treatment and/or supplementation of disease and conditions associated with abnormal bone resorption" in the invention means in osteoporosis treatment; to reduce the risk of fracture in bones including vertebra and hip in the postmenopausal women; to reduce the risk of bone fractures in men in the treatment of osteoporosis; Idiopathis osteoporosis; various diseases caused by osteoporosis, and glucocorticoid and steroid mediated osteoporosis, osteopenia, osteomalacia, osteogenesis imperfecta, osteocondrodysplasia, Sudek's atrophy, rheumatoid arthritis, Paget's disease, malignant tumors of bone metastases, hypercalcaemia, or in the treatment of diseases such as hyperthyroidism; and nutritional supplements especially for woman which are in growth, pregnant or breast-feeding in the period before and after menopause to maintain bone health, but the explained usage areas are not limited with these.
  • a certain proportion and “optionally” mean that in order to obtain the desired therapeutic effect, preferred amount of risedronate ( or pharmaceutically acceptable salt, derivative or hydrate thereof) in the range of 0.1-980 mg, an amount of calcium salt( on the basis of elemental calcium) in the range of 250-5000 mg, an amount of vitamin D in the range of 100-
  • one or more pharmaceutically acceptable excipients to be used when necessary which are selected from a group of a diluent, binder, disintegrant, lubricant, glidant, surface active agent, sweetener and flavoring agent.
  • a pharmaceutically acceptable salt, derivative or hydrate of risedronate implies that salts can be selected from sodium, potassium, calcium, magnesium and ammonium salts; derivatives can be selected from ester and amide derivatives; hydrates can be selected from monohydrates, dihydrates, trihydrates, hemihydrates, 1 A hydrate, 1 A hydrate, 2 A hydrate, 3 A hydrate, V 4 hydrate, 4 / 3 hydrate, V 2 hydrate and 3 / 2 hydrate; preferably alendronate is alendronate monosodium trihydrate.
  • calcium salt implies that it can be selected from carbonate, chloride, citrate. glubionat, gluceptate, gluconate, lactate, phosphate, maleate, glycerophosphate, bicarbonate or tartarate salts.
  • the pharmaceutically acceptable diluents can be selected from a group consisting of lactose, macrocrystalline cellulose, starch, pregelatinized starch, modified starch, calcium phosphate (dibasic and / or tribasic), calcium sulfate trihydrate, calcium sulfate dihydrate, calcium carbonate, kaolin, lactilol, powdered cellulose, dextrose, dextares, dextrin, sucrose, maltose, fructose, mannitol, sorbitol, xylitol.
  • the diluent is present in the formulations preferably in the range of 0-85% by weight and more preferably 0.1-75% by weight.
  • the pharmaceutically acceptable binder can be selected from a group consisting of starch (potato starch, com starch, wheat starch, etc.), sugars such as sucrose, glucose, dextrose, lactose, maltodextrin, natural and synthetic gums (e.g. acacia), gelatin, cellulose derivatives (e.g. microcrystalline cellulose, HPC, HEC, HPMC, carboxymethylcellulose, methylcellulose, ethylcellulose). polyvinylpyrollidone, polyethylene glycol, waxes, calcium carbonate, calcium phosphate, alcohols ( e.g. sorbitol, xylitol, mannitol) and water.
  • the binder is present in the formulations preferably in the range of 0-10% by weight and more preferably in the range of 0.1- 5% by weight.
  • the pharmaceutically acceptable disintegrants can be selected from a group consisting of starch (corn starch, potato starch), sodium starch glycolate, pregelatinized starch, cellulose derivatives (e.g. croscarmellose sodium or microcrystalline cellulose), polyvinylpyrollidone, crospovidone, alginic acid, sodium alginat, clays (e.g. xanthan gum or veegum), ion-exchange resins and effervescent systems (alkali or alkaline earth metal carbonates [e.g.
  • the disintegrant is present in the formulations preferably in the range of 0-85% by weight and more preferably in the range of 0.1-75% by weight.
  • Pharmaceutically acceptable lubricants can be selected from a group consisting of metallic stearales (magnesium stearate, calcium stearate, aluminum stearate, etc.), fatty acid esters (e.g.
  • the lubricant is present in the formulations preferably in the range of 0-10% by weight and more preferably in the range of 0.1-5% by weight.
  • the pharmaceutical acceptable glidants can be selected from a group consisting of silicon dioxide, magnesium trisilicate, powdered cellulose, starch, talc, tribasic calcium phosphate, metallic stearates, calcium silicate and metallic lauryl sulfate.
  • the glidant is found in a range below 1% by weight in the formulations.
  • the pharmaceutically acceptable surface active agents can be selected from a group consisting of polyoxyethylene-sorbitane-fatty acid esters (polysorbates), sodium lauryl sulfate, sodium stearyl fumarate, polyoxyethylene alkyl ethers, sorbitane fatty acid esters, polyethylene glycols, polyoxyethylene castor oil derivatives, docusate sodium, quaternary ammonium compounds, aminoacids like L-leucine, sugar esters of fatty acids, glycerides of fatty acids.
  • the surface active agent is present in the formulations preferably in the range of 0-10% by weight and more preferably in the range of 0.1 -5% by weight.
  • the stabilizing agent and/or agents can be selected from a group consisting of antioxidants, chelating agents, alkaline agents and photo-protectors.
  • the stabilization agent and/or agents is present in the formulations preferably in the range of 0-85% by weight and more preferably in the range of 0.1 -75% by wei ght
  • the antioxidants can be selected from a group consisting of butylated hydroxyanisole (BHA), sodium ascorbate, butylated hydroxytoluene (BHT), sodium sulfite, gallates (e.g. propyl gallate), tocopherol, citric acid, malic acid, ascorbic acid, acetylcysteine, fumaric acid, lecithin, ascorbil palmitate, ethylenediamine tetraacetate.
  • BHA butylated hydroxyanisole
  • BHT butylated hydroxytoluene
  • gallates e.g. propyl gallate
  • tocopherol citric acid, malic acid, ascorbic acid, acetylcysteine, fumaric acid, lecithin, ascorbil palmitate, ethylenediamine tetraacetate.
  • the chelating agents can be selected from a group consisting of disodium EDTA, edetic acid, citric acid, sodium citrate, potassium citrate or combinations thereof.
  • the alkalizing agents can be selected from a group consisting of sodium carbonate, sodium hydrogen carbonate, sodium hydroxide, sodium silicate, disodium hydrogen ortophosphate.
  • alkali metal salts such as sodium aluminate; calcium carbonate, calcium hydroxide, dibasic calcium phosphate, tribasic calcium phosphate, calcium sulfate, calcium acetate, calcium gluconate, calcium glycerophosphate, magnesium carbonate, magnesium hydroxide, magnesium sulfate, magnesium acetate, magnesium silicate, earth alkali metal salts like magnesium aluminate and primary, secondary and tertiary amines, cyclic amines, organic compounds such as N-N '-dibenzyl ethyl enediamine, diethanoleamine, ethyl enediamine, meglumine, monosodium glucamate, polyacryline sodium, sodium alginate.
  • the photo-protector agents can be selected from a group consisting of metal oxides such as titanium oxide, iron oxide or zinc oxide.
  • the pharmaceutically acceptable sweeteners can be selected from a group consisting of sucralose, sucrose, fructose, glucose, galactose, xylose, dextrose, levulose, lactose, maltose, maltodextrin, mannitol, maltitol, maltol, sorbitol, xylitol, erytritol, lactitol, isomalt, com syrup, saccharin, saccharin salts, acesulphame potassium, aspartam, D-tryptophan, monoammonium glycerrizinate, neohesperidin dihydrochalcone, taumatine, neotam, alitam, steviosite and cyclamates.
  • the sweetener is present in the formulations preferably in the range of 0-5% by weight and more preferably in the range of 0.1-3% by weight.
  • the pharmaceutically acceptable flavoring agents can be selected from a group consisting of natural, aroma oils (peppermint oil, partridge currant oil, clove bud oil, parsley oil, eucalyptus oil, lemon oil, orange oil, etc.), menthol, menthan, anetole, methyl salicylate, ocaliptole, cinnamon, 1 -methyl acetate, ogenol, oxanone, alpha-irisone, marjoram, lemon, orange, propenyl guaetol acetyl, sinnamon, vanilla, timole, linalol, cinnamaldehyde glycerol acetal, N-substituted p-mentane-3-carboxyamide,3,l-methoxy propane 1,2-diol.
  • the flavoring agent is present in the formulations preferably in the range of 0-5% by weight and more preferably in the range of 0.1- 3% by weight.
  • the dosage form can be in the form of tablets, capsules, soluble tablets, fast-dissolving tablets, effervescent tablets, effervescent granules, fast-dissolving powder mixtures or dry powder mixture for preparation of syrup.
  • Granule includes approximately 100,000 IU per 1 gr

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Abstract

La présente invention porte sur une composition pharmaceutique stabilisée comprenant une combinaison d'agents actifs dans une forme posologique unique de façon à augmenter l'adaptation du patient et par conséquent le résultat du traitement.
PCT/TR2010/000026 2009-02-05 2010-02-02 Formulation pharmaceutique comprenant du risédronate, du carbonate de calcium et de la vitamine d3 combinés en une forme posologique unique WO2010090614A1 (fr)

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TR2009/00878 2009-02-05
TR2009/00878A TR200900878A2 (tr) 2009-02-05 2009-02-05 Tek bir dozaj formunda kombine edilen farmasötik formülasyonlar

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Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012093980A1 (fr) * 2011-01-06 2012-07-12 Mahmut Bilgic Formulation améliorée à base de risédronate
WO2012093974A1 (fr) * 2011-01-06 2012-07-12 Mahmut Bilgic Formulations améliorées de bisphosphonates
WO2014088385A1 (fr) 2012-12-03 2014-06-12 Landsteiner Scientific S.A. De C.V. Composition pharmaceutique stable pour le traitement de l'ostéoporose
EP2953632A4 (fr) * 2013-02-11 2016-09-21 Amorphical Ltd Carbonate de calcium amorphe pour croissance osseuse accélérée
CN107897934A (zh) * 2017-11-16 2018-04-13 广州市健鸣春生物科技有限公司 预防胎儿先天疾病、预防流产的复合维生素矿物质片及其制备方法
IT201700099708A1 (it) * 2017-09-06 2019-03-06 Abiogen Pharma Spa Composizione per l’integrazione di calcio
US10723700B2 (en) 2015-08-12 2020-07-28 Incyte Corporation Salts of an LSD1 inhibitor
US10800779B2 (en) 2015-04-03 2020-10-13 Incyte Corporation Heterocyclic compounds as LSD1 inhibitors
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US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
US11155532B2 (en) 2014-02-13 2021-10-26 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
US11247992B2 (en) 2014-02-13 2022-02-15 Incyte Corporation Cyclopropylamines as LSD1 inhibitors

Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0186405A2 (fr) 1984-12-21 1986-07-02 The Procter & Gamble Company Compositions pharmaceutiques contenant des diphosphonates géminaux
WO1999006051A1 (fr) 1997-07-30 1999-02-11 Menarini International Operations Luxembourg S.A. Compositions pharmaceutiques contenant de la vitamine d et du calcium, leur preparation et leur utilisation therapeutique
EP0969849B1 (fr) 1997-03-12 2003-07-23 MERCK PATENT GmbH Composition solide stable contenant de la vitamine d3 et du phosphate tricalcique
WO2003086415A1 (fr) 2002-04-05 2003-10-23 Merck & Co., Inc. Procede d'inhibition de resorption osseuse a l'aide d'une formulation a base d'alendronate et de vitamine d
EP0583378B1 (fr) 1991-05-06 2003-11-12 The Procter & Gamble Company Supplements combines de calcium et de vitamine d
WO2004022068A1 (fr) 2002-09-05 2004-03-18 Wisconsin Alumni Research Foundation Methode d'augmentation du dosage de composes a base de vitamine d
WO2005027921A1 (fr) 2003-09-19 2005-03-31 Pfizer Products Inc. Compositions pharmaceutiques et methodes de traitement consistant en des associations d'un derive de la 2-alkylidene-19-nor-vitamine d et d'un bisphosphonate
US20050261250A1 (en) 2004-05-19 2005-11-24 Merck & Co., Inc., Compositions and methods for inhibiting bone resorption
EP1651191A2 (fr) 2003-07-17 2006-05-03 Menarini International Operations Luxembourg S.A. Compositions pharmaceutiques effervescentes contenant de la vitamine d, du calcium et du phosphate et leur utilisation therapeutique
WO2006112889A1 (fr) * 2005-04-15 2006-10-26 The Procter & Gamble Company Formes galéniques du risedronate
WO2007031785A2 (fr) * 2005-09-16 2007-03-22 Selamine Ltd Formulation de bisphosphonate
EP1837019A1 (fr) * 2004-10-25 2007-09-26 Italfarmaco, S.A. Compositions pharmaceutiques dispersables par voie buccale
WO2008075930A1 (fr) 2006-12-20 2008-06-26 Landsteiner Scientific, S.A. De C.V. Compositions de risedronate et vitamine d3

Patent Citations (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0186405A2 (fr) 1984-12-21 1986-07-02 The Procter & Gamble Company Compositions pharmaceutiques contenant des diphosphonates géminaux
US5583122A (en) 1984-12-21 1996-12-10 The Procter & Gamble Company Pharmaceutical compositions containing geminal diphosphonates
EP0583378B1 (fr) 1991-05-06 2003-11-12 The Procter & Gamble Company Supplements combines de calcium et de vitamine d
EP0969849B1 (fr) 1997-03-12 2003-07-23 MERCK PATENT GmbH Composition solide stable contenant de la vitamine d3 et du phosphate tricalcique
WO1999006051A1 (fr) 1997-07-30 1999-02-11 Menarini International Operations Luxembourg S.A. Compositions pharmaceutiques contenant de la vitamine d et du calcium, leur preparation et leur utilisation therapeutique
WO2003086415A1 (fr) 2002-04-05 2003-10-23 Merck & Co., Inc. Procede d'inhibition de resorption osseuse a l'aide d'une formulation a base d'alendronate et de vitamine d
WO2004022068A1 (fr) 2002-09-05 2004-03-18 Wisconsin Alumni Research Foundation Methode d'augmentation du dosage de composes a base de vitamine d
EP1651191A2 (fr) 2003-07-17 2006-05-03 Menarini International Operations Luxembourg S.A. Compositions pharmaceutiques effervescentes contenant de la vitamine d, du calcium et du phosphate et leur utilisation therapeutique
WO2005027921A1 (fr) 2003-09-19 2005-03-31 Pfizer Products Inc. Compositions pharmaceutiques et methodes de traitement consistant en des associations d'un derive de la 2-alkylidene-19-nor-vitamine d et d'un bisphosphonate
US20050261250A1 (en) 2004-05-19 2005-11-24 Merck & Co., Inc., Compositions and methods for inhibiting bone resorption
EP1837019A1 (fr) * 2004-10-25 2007-09-26 Italfarmaco, S.A. Compositions pharmaceutiques dispersables par voie buccale
WO2006112889A1 (fr) * 2005-04-15 2006-10-26 The Procter & Gamble Company Formes galéniques du risedronate
WO2007031785A2 (fr) * 2005-09-16 2007-03-22 Selamine Ltd Formulation de bisphosphonate
WO2008075930A1 (fr) 2006-12-20 2008-06-26 Landsteiner Scientific, S.A. De C.V. Compositions de risedronate et vitamine d3

Non-Patent Citations (12)

* Cited by examiner, † Cited by third party
Title
BLONDE L.: "Compliance and Persistence With Medication Therapy", MANAGED CARE, vol. 9, no. 9, 2000, Retrieved from the Internet <URL:archives.who.int/icium/icium2004/resources/ppt/AC016.ppt>
CHAPUY M. C: "Vitamin D3 and calcium to prevent hip fractures in elderly women", THE NEW ENGLAND JOURNAL OF MEDICINE, vol. 327, 1992, pages 1637 - 42
DEANE A. ET AL.: "The impact of vitamin D status on changes in bone mineral density during treatment with bisphosphonates and after discontinuation following long-term use in post-menopausal osteoporosis", BMC MUSCULOSKELETAL DISORDERS, vol. 8, 2007, pages 3
EMKEY R: "Alendronate and Risedronate for the Treatment of Postmenopausal Osteoporosis: Clinical Profiles of the Once-Weekly and Once-Daily Dosing Formulations", MEDGENMED, vol. 6, no. 3, 2004, pages 6
HARRIS S T ET AL: "Effects of risedronate treatment on vertebral and nonvertebral fractures in women with postmenopausal osteoporosis: a randomized controlled trial. Vertebral Efficacy With Risedronate Therapy (VERT) Study Group.", JAMA : THE JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION, vol. 282, no. 14, 13 October 1999 (1999-10-13), pages 1344 - 1352, XP002576184, ISSN: 0098-7484 *
HARRIS S. T. ET AL.: "Effects of Risedronate Treatment on Vertebral and Nonvertebral Fractures in Women With Postmenopausal Osteoporosis", JAMA, vol. 282, 1999, pages 1344 - 1352
HENEGHAN CJ; GLASZIOU P; PERERA R, THE COCHRANE LIBRARY
RESCH H ET AL: "Modern osteoporosis therapy with once-a-week risedronate in combination with calcium/vitamin D3 chewable tablets", JOURNAL FUER MINERALSTOFFWECHSEL, KRAUSE AND PACHERNEGG, PURKERSDORF, AT, vol. 10, no. 2, 1 January 2003 (2003-01-01), pages 24 - 26, XP009128626, ISSN: 1023-7763 *
RINGE J D ET AL: "Efficacy of risedronate in men with primary and secondary osteoporosis: results of a 1-year study", RHEUMATOLOGY INTERNATIONAL ; CLINICAL AND EXPERIMENTAL INVESTIGATIONS, SPRINGER, BERLIN, DE LNKD- DOI:10.1007/S00296-005-0004-4, vol. 26, no. 5, 1 March 2006 (2006-03-01), pages 427 - 431, XP019335335, ISSN: 1437-160X *
RINGE J. D.: "Efficacy of risedronate in men with primary and secondary osteoporosis: results of a 1-year study", RHEUMATOLOGY INTERNATIONAL, vol. 26, no. 5, 2006, pages 427 - 431
SABATE, E: "Adherence to Long tenn Therapies: Evidence for Action", WORLD HEALTH ORGANIZATION, 2003, pages 212
WALSH N.: "Risedronate Gains Approval for Male Osteoporosis", INTERNAL MEDICINE NEWS, 2006

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