WO2013100112A1 - Composition pharmaceutique solide contenant un composé ayant une activité antagoniste de l'angiotensine ii - Google Patents

Composition pharmaceutique solide contenant un composé ayant une activité antagoniste de l'angiotensine ii Download PDF

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Publication number
WO2013100112A1
WO2013100112A1 PCT/JP2012/084001 JP2012084001W WO2013100112A1 WO 2013100112 A1 WO2013100112 A1 WO 2013100112A1 JP 2012084001 W JP2012084001 W JP 2012084001W WO 2013100112 A1 WO2013100112 A1 WO 2013100112A1
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Prior art keywords
magnesium
calcium
hydrate
pharmaceutical composition
solid pharmaceutical
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PCT/JP2012/084001
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English (en)
Japanese (ja)
Inventor
智治 谷野
宏史 更田
友里 槌谷
隆信 岩城
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ニプロ株式会社
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Priority to JP2013551847A priority Critical patent/JP6081376B2/ja
Publication of WO2013100112A1 publication Critical patent/WO2013100112A1/fr

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    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/2853—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

Definitions

  • the present invention relates to a solid pharmaceutical composition containing a compound having an angiotensin II antagonistic action.
  • Valsartan which is one of the compounds having an angiotensin II antagonism used as a therapeutic agent for hypertension, is sold as “Diovan (registered trademark) tablet” (Non-patent Document 1).
  • Patent Document 1 describes that the content of valsartan in the preparation is increased, and if necessary, hydrochlorothiazide is added to the preparation.
  • An object of the present invention is to provide a solid pharmaceutical composition containing a compound having an angiotensin II antagonistic action and having excellent stability.
  • the present inventors have formulated a solid pharmaceutical composition by blending an alkaline earth metal salt and / or a hydrate thereof with a solid pharmaceutical composition containing a compound having an angiotensin II antagonistic action.
  • the present inventors have found that the stability of a product, particularly moisture resistance, can be improved, and the present invention has been completed.
  • the present invention is a solid pharmaceutical composition containing a compound having an angiotensin II antagonistic activity and an alkaline earth metal salt and / or a hydrate thereof.
  • the compound having angiotensin II antagonism is a group consisting of losartan, eprosartan, candesartan cilexetil, candesartan, valsartan, telmisartan, irbesartan, olmesartan, tasosartan, azilsartan, and salts or esters thereof At least one compound selected from the group consisting of:
  • the content of the compound having angiotensin II antagonism is 30% by mass or more based on the mass of the composition.
  • the alkaline earth metal is at least one metal selected from the group consisting of calcium, strontium, barium, radium, magnesium, and beryllium.
  • the alkaline earth metal salt and / or hydrate thereof is calcium chloride hydrate, calcium citrate, calcium gluconate hydrate, calcium glycerophosphate, calcium carbonate, precipitated calcium carbonate, calcium lactate.
  • Hydrate anhydrous calcium hydrogen phosphate, calcium monohydrogen phosphate, calcium monohydrogen phosphate hydrate, calcium dihydrogen phosphate hydrate, magnesium L-aspartate, magnesium chloride, dried magnesium sulfate, magnesium gluconate ,
  • Magnesium silicate, magnesium aluminum silicate, magnesium oxide, magnesium hydroxide, magnesium alumina hydroxide, magnesium sulfate hydrate, magnesium metasilicate aluminate, and magnesium carbonate, and combinations thereof Is at least one compound selected.
  • the content of the alkaline earth metal salt and / or hydrate thereof is 2% by mass to 10% by mass based on the mass of the composition.
  • a solid pharmaceutical composition containing a compound having an angiotensin II antagonistic action and having excellent stability can be provided.
  • the solid pharmaceutical composition of the present invention contains a compound having an angiotensin II antagonism and an alkaline earth metal salt and / or a hydrate thereof.
  • the compound having an angiotensin II antagonistic action is not particularly limited, and examples thereof include losartan, eprosartan, candesartan cilexetil, candesartan, valsartan, telmisartan, irbesartan, olmesartan, tasosartan, azilsartan, and salts or esters thereof, and These combinations are mentioned.
  • the content of the compound having an angiotensin II antagonistic action in the solid pharmaceutical composition of the present invention is not particularly limited, but is preferably 30% by mass or more, more preferably 30% by mass based on the mass of the composition. It is 70 mass% or less.
  • alkaline earth metal means calcium, strontium, barium, radium, magnesium, or beryllium.
  • the alkaline earth metal salt and / or hydrate thereof of the present invention is not particularly limited, and examples thereof include calcium chloride hydrate, calcium citrate, calcium gluconate hydrate, calcium glycerophosphate, calcium carbonate, and precipitated carbonic acid.
  • precipitated calcium carbonate, anhydrous calcium hydrogen phosphate, magnesium carbonate, magnesium oxide, or a combination thereof are preferable because they can be obtained at low cost.
  • the content of the alkaline earth metal salt and / or hydrate thereof in the solid pharmaceutical composition of the present invention is not particularly limited, but is preferably 2% by mass to 10% by mass based on the mass of the composition, More preferably, the content is 3% by mass to 7% by mass.
  • the shape of the solid pharmaceutical composition of the present invention is not particularly limited, and examples thereof include tablets, capsules, pills, troches, granules, and powders. A tablet is preferred.
  • the solid pharmaceutical composition of the present invention includes other excipients, disintegrants, binders, fluidizers, lubricants, colorants, solubilizers, sweeteners, fragrances, foaming agents, surfactants, preservatives. And additives such as a pH adjusting agent and a coating agent.
  • the excipient is not particularly limited, and examples thereof include crystalline cellulose, low-substituted hydroxypropyl cellulose, starch, corn starch, saccharides (such as glucose, fructose, lactose, sucrose, reduced maltose, trehalose), and sugar alcohol (D -Mannitol, erythritol, sorbitol, xylitol, maltitol, lactitol, etc.), and combinations thereof.
  • saccharides such as glucose, fructose, lactose, sucrose, reduced maltose, trehalose
  • sugar alcohol D -Mannitol, erythritol, sorbitol, xylitol, maltitol, lactitol, etc.
  • the disintegrant is not particularly limited, and for example, crospovidone, sodium carboxy starch, sodium carboxymethyl starch, starch, partially pregelatinized starch, corn starch, lactose, calcium carbonate, precipitated calcium carbonate, calcium citrate, light anhydrous silicic acid Synthetic aluminum silicate crystalline cellulose, low substituted hydroxypropyl cellulose, croscarmellose sodium, carboxymethylcellulose calcium, carmellose, and hydroxypropyl starch, and combinations thereof.
  • the binder is not particularly limited, and examples thereof include gelatin, agar, alginic acid, sodium alginate, dextrin, chitansan gum, gum arabic powder, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, polyvinylpyrrolidone, partially saponified polyvinyl alcohol, methylcellulose, Examples include pullulan, partially pregelatinized starch, and saccharides, and combinations thereof.
  • the fluidizing agent examples include silicates such as calcium silicate, silicic anhydride such as light anhydrous silicic acid, hydrated silicon dioxide, talc, and combinations thereof.
  • the lubricant is not particularly limited, for example, magnesium stearate, calcium stearate, talc, sucrose fatty acid ester, polyethylene glycol, stearic acid, light anhydrous silicic acid, hydrogenated rapeseed oil, hydrogenated castor oil, glycerin fatty acid ester, Examples include sodium stearyl fumarate, sodium benzoate, L-leucine, and L-valine, and combinations thereof.
  • the colorant is not particularly limited, and examples thereof include ferric oxide, yellow ferric oxide, edible red No. 2, edible red No. 3, edible yellow No. 4, and edible yellow No. 5, and combinations thereof.
  • the solubilizing agent is not particularly limited, and examples thereof include magnesium oxide, calcium oxide, sodium citrate, magnesium chloride, sodium carbonate, sodium bicarbonate, and combinations thereof.
  • the sweetener is not particularly limited, and examples thereof include aspartame, sodium saccharin, dipotassium glycyrrhizin, stevia, and thaumatin, and combinations thereof.
  • the fragrance is not particularly limited, and examples thereof include mint, lemon, orange, and combinations thereof.
  • the foaming agent is not particularly limited, and examples thereof include tartrate, citrate, bicarbonate, and combinations thereof.
  • the surfactant is not particularly limited, and examples thereof include anionic surfactants such as sodium alkyl sulfate, sucrose fatty acid esters, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene fatty acid esters, and polyoxyethylene castor oil derivatives. Nonionic surfactants and the like can be mentioned.
  • the preservative is not particularly limited, and examples thereof include benzoic acid, paraoxybenzoic acid, and salts thereof.
  • the pH regulator is not particularly limited, and examples thereof include organic acids such as citric acid, tartaric acid, acetic acid and lactic acid, inorganic acids such as hydrochloric acid and phosphoric acid, and inorganic bases such as sodium hydrogen carbonate, sodium carbonate and sodium hydroxide. Can be mentioned.
  • the coating agent is not particularly limited, and examples thereof include hydroxypropyl methylcellulose (hypromellose), titanium oxide, polyethylene glycol (Macrogol 6000), and combinations thereof.
  • the content of the additive in the solid pharmaceutical composition of the present invention is appropriately set according to the purpose of blending the additive.
  • the method for producing the solid pharmaceutical composition of the present invention is not particularly limited, and for example, the steps included in the method for producing a solid pharmaceutical preparation usually used by those skilled in the art can be used.
  • granulation step for example, granulation by a wet granulation method or a dry granulation method can be employed.
  • a solid pharmaceutical composition containing a compound having an angiotensin II antagonism was sometimes produced by a dry granulation method, but the method for producing a solid pharmaceutical composition of the present invention is limited to the dry granulation method.
  • a wet granulation method can be selected. The wet granulation method is not particularly limited.
  • a granulating means such as a fluidized bed granulator / dryer, a stirring granulator, a cylindrical extrusion granulator, a rolling fluidized bed granulating / coating machine, or a spray dryer is used.
  • Granulation can be employed. It does not specifically limit as a dry granulation method,
  • the tableting process that can be used in the present invention is not particularly limited.
  • a tableting mortar, a tableting upper punch and a lower punch, a hydraulic hand press machine, a single-shot tableting machine, a rotary type Tableting using a tableting means such as a tableting machine may be employed.
  • Tableting pressure is not particularly limited, for example, in the range of 2kN / cm 2 ⁇ 7kN / cm 2.
  • the coating process that can be used in the present invention is not particularly limited.
  • a coating method in which a coating agent is dissolved or dispersed in a solvent such as water to prepare a coating solution, and the coating solution is sprayed onto the main agent particles a film Coating using a method such as a coating machine, a pan coating method, a fluid coating method, and a rolling coating method may be employed.
  • the solid pharmaceutical composition of the present invention is granulated by mixing, for example, an angiotensin II antagonistic compound, an alkaline earth metal salt and / or hydrate thereof, an excipient, a disintegrant and a binder. It is manufactured by adding and mixing a fluidizing agent, lubricant, if necessary, disintegrating agent to tablets, and coating the resulting uncoated tablet with a coating agent and, if necessary, a coloring agent. .
  • the solid pharmaceutical composition of the present invention can be produced, for example, as a tablet.
  • Example 1 Tablets containing valsartan were produced according to the formulation described in Table 1 below.
  • Valsartan (Patent Document 1) 800 g, magnesium carbonate 100 g, low-substituted hydroxypropylcellulose 770 g, crystalline cellulose 100 g, light anhydrous silicic acid 100 g, and magnesium stearate 30 g were mixed in a container-rotating mixer (S-3 manufactured by Tsutsui Rika Kikai Co., Ltd.) The mixture was mixed and the mixture was consolidated using a roller compactor (TF-MINI manufactured by Freund Sangyo Co., Ltd.) at a compaction force of 60 kg / cm 2 and a roller speed of 4 rpm.
  • TF-MINI manufactured by Freund Sangyo Co., Ltd.
  • the compacted mixed compact is passed through a granulator (P-02S, manufactured by Dalton Co., Ltd.) to form granules (dry granulation), low-substituted hydroxypropylcellulose 50 g, light anhydrous silicic acid 10 g, talc 20 g and 20 g of magnesium stearate was added and mixed, and the mixture was put into a tableting machine (VIRGO manufactured by Kikusui Seisakusho Co., Ltd.), and a tablet weight of 200 mg at a tableting pressure of 7 kN / cm 2 using a 8.5 mm diameter punch. Tableting was performed to obtain an uncoated tablet (core tablet part).
  • P-02S manufactured by Dalton Co., Ltd.
  • this uncoated tablet was put into a film coating machine (HCT-48N manufactured by Freund Sangyo Co., Ltd.), and a solution obtained by dissolving 128 g of hydroxypropylmethylcellulose, 16 g of polyethylene glycol and 16 g of titanium oxide in 1600 g of purified water was 8 mg per tablet. Film coating was performed by spraying the uncoated tablets so that the solid content was coated, and tablets were obtained.
  • HCT-48N manufactured by Freund Sangyo Co., Ltd.
  • Example 2 Tablets containing valsartan were produced according to the formulation described in Table 2 below. Production was carried out in the same manner as in Example 1 except that the magnesium carbonate in Example 1 was replaced with precipitated calcium carbonate.
  • Example 3 Tablets containing valsartan were produced according to the formulation described in Table 3 below.
  • 200 g of Valsartan (Patent Document 1), 25 g of magnesium carbonate, 210 g of low-substituted hydroxypropyl cellulose and 25 g of crystalline cellulose are put into a stirring granulator (VG-05 manufactured by Paulec Co., Ltd.) and mixed, and 15 g of hydroxypropyl cellulose is further added.
  • Wet granulation was performed by adding a solution dissolved in purified water.
  • this uncoated tablet is put into a film coating machine (HCT-48N manufactured by Freund Sangyo Co., Ltd.), and a solution obtained by dissolving 32 g of hydroxypropylmethylcellulose, 4 g of polyethylene glycol and 4 g of titanium oxide in 400 g of purified water is sprayed on the uncoated tablet. Film coating was performed to obtain tablets.
  • HCT-48N manufactured by Freund Sangyo Co., Ltd.
  • Example 4 Tablets containing valsartan were prepared according to the formulation described in Table 4 below. Production was carried out in the same manner as in Example 3 except that magnesium carbonate in Example 3 was replaced with magnesium oxide.
  • Valsartan (Patent Document 1) 800 g, low substituted hydroxypropylcellulose 870 g, crystalline cellulose 100 g, light anhydrous silicic acid 100 g, and magnesium stearate 30 g are charged into a rotating container mixer (S-3, manufactured by Tsutsui Rika Kikai Co., Ltd.) The mixture was consolidated using a roller compactor (TF-MINI manufactured by Freund Sangyo Co., Ltd.) at a compaction force of 60 kg / cm 2 and a roller speed of 4 rpm.
  • TF-MINI manufactured by Freund Sangyo Co., Ltd.
  • the compacted mixed compact is passed through a granulator (P-02S, manufactured by Dalton Co., Ltd.) to form granules (dry granulation), low-substituted hydroxypropylcellulose 50 g, light anhydrous silicic acid 10 g, talc 20 g and 20 g of magnesium stearate was added and mixed, and the mixture was put into a tableting machine (VIRGO manufactured by Kikusui Seisakusho Co., Ltd.), and a tablet weight of 200 mg at a tableting pressure of 7 kN / cm 2 using a 8.5 mm diameter punch. Tableting was performed to obtain an uncoated tablet (core tablet part).
  • P-02S manufactured by Dalton Co., Ltd.
  • this uncoated tablet was put into a film coating machine (HCT-48N manufactured by Freund Sangyo Co., Ltd.), and a solution obtained by dissolving 128 g of hydroxypropylmethylcellulose, 16 g of polyethylene glycol and 16 g of titanium oxide in 1600 g of purified water was 8 mg per tablet. Film coating was performed by spraying the uncoated tablets so that the solid content was coated, and tablets were obtained.
  • HCT-48N manufactured by Freund Sangyo Co., Ltd.
  • Example 1 to 4 and Comparative Examples 1 and 2 were stored for 3 days under conditions of 60 ° C., 75% humidity, and darkness, respectively, with aluminum packaging or without packaging.
  • the tablets after storage were subjected to a dissolution test for valsartan. Each test was performed three times. The results are shown in Table 7.
  • the tablets after storage in Examples 1 to 4 showed a very stable result with little decrease in dissolution of valsartan in either aluminum packaging or non-packaging.
  • an alkaline earth metal salt and / or a hydrate thereof added to a tablet containing valsartan, the stability of the tablet, particularly moisture resistance, could be increased.
  • a solid pharmaceutical composition containing a compound having an angiotensin II antagonistic action and having excellent stability can be provided.

Abstract

La présente invention concerne une composition pharmaceutique solide comprenant un composé ayant une activité antagoniste de l'angiotensine II et un sel de métal alcalino-terreux et/ou un hydrate de celui-ci. La composition pharmaceutique solide selon la présente invention présente une excellente stabilité, en particulier une excellente résistance à l'humidité.
PCT/JP2012/084001 2011-12-28 2012-12-27 Composition pharmaceutique solide contenant un composé ayant une activité antagoniste de l'angiotensine ii WO2013100112A1 (fr)

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JP2013551847A JP6081376B2 (ja) 2011-12-28 2012-12-27 アンギオテンシンｉｉ拮抗作用を有する化合物を含有する固形医薬組成物

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JP2015067608A (ja) * 2013-09-27 2015-04-13 キョーリンリメディオ株式会社 テルミサルタン含有製剤及びその製造方法
JP2015209386A (ja) * 2014-04-25 2015-11-24 沢井製薬株式会社 バルサルタン含有錠剤及びその製造方法
JP2017145238A (ja) * 2016-02-12 2017-08-24 エルメッド エーザイ株式会社 アジルサルタン含有湿製錠剤及びその製造方法
JP2019520428A (ja) * 2016-06-21 2019-07-18 オムヤ インターナショナル アクチェンゲゼルシャフト 投与製剤の製造方法
JP2019522053A (ja) * 2016-06-21 2019-08-08 オムヤ インターナショナル アクチェンゲゼルシャフト 投与製剤の製造方法
JP7322474B2 (ja) 2019-04-04 2023-08-08 ニプロ株式会社 アジルサルタンを含有する錠剤

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JP2009114113A (ja) * 2007-11-06 2009-05-28 Nipro Corp 口腔内崩壊錠及びその製造方法
JP2011507973A (ja) * 2007-12-31 2011-03-10 ルピン・リミテッド アムロジピンとバルサルタンとの医薬組成物
WO2009113420A1 (fr) * 2008-03-13 2009-09-17 第一三共株式会社 Amélioration de la solubilité d'une préparation contenant de l'olmésartan médoxomil
JP2011136908A (ja) * 2009-12-25 2011-07-14 Kyowa Yakuhin Kogyo Kk アンギオテンシンｉｉ受容体拮抗剤を含む固形製剤および固形製剤におけるアンギオテンシンｉｉ受容体拮抗剤の保存安定性向上方法

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JP2015067608A (ja) * 2013-09-27 2015-04-13 キョーリンリメディオ株式会社 テルミサルタン含有製剤及びその製造方法
JP2015209386A (ja) * 2014-04-25 2015-11-24 沢井製薬株式会社 バルサルタン含有錠剤及びその製造方法
JP2017145238A (ja) * 2016-02-12 2017-08-24 エルメッド エーザイ株式会社 アジルサルタン含有湿製錠剤及びその製造方法
JP2019520428A (ja) * 2016-06-21 2019-07-18 オムヤ インターナショナル アクチェンゲゼルシャフト 投与製剤の製造方法
JP2019522053A (ja) * 2016-06-21 2019-08-08 オムヤ インターナショナル アクチェンゲゼルシャフト 投与製剤の製造方法
JP7014787B2 (ja) 2016-06-21 2022-02-01 オムヤ インターナショナル アクチェンゲゼルシャフト 投与製剤の製造方法
JP7014786B2 (ja) 2016-06-21 2022-02-01 オムヤ インターナショナル アクチェンゲゼルシャフト 投与製剤の製造方法
US11400050B2 (en) 2016-06-21 2022-08-02 Omya International Ag Method for the production of a dosage form
JP7322474B2 (ja) 2019-04-04 2023-08-08 ニプロ株式会社 アジルサルタンを含有する錠剤

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