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WO2007129522A1 - Préparation obtenue par voie sèche - Google Patents

Préparation obtenue par voie sèche Download PDF

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Publication number
WO2007129522A1
WO2007129522A1 PCT/JP2007/057832 JP2007057832W WO2007129522A1 WO 2007129522 A1 WO2007129522 A1 WO 2007129522A1 JP 2007057832 W JP2007057832 W JP 2007057832W WO 2007129522 A1 WO2007129522 A1 WO 2007129522A1
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WO
WIPO (PCT)
Prior art keywords
solid preparation
production method
dry
preparation according
formulating
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/JP2007/057832
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English (en)
Japanese (ja)
Inventor
Naoki Wakiyama
Tomoyuki Watanabe
Atsutoshi Ito
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Daiichi Sankyo Co Ltd
Original Assignee
Daiichi Sankyo Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Daiichi Sankyo Co Ltd filed Critical Daiichi Sankyo Co Ltd
Publication of WO2007129522A1 publication Critical patent/WO2007129522A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • 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
    • A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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

Definitions

  • the present invention relates to a solid preparation comprising a step of formulating a composition containing a fructose 1,6-bisphosphatase (FBPase) inhibitor by a dry production method.
  • FBPase fructose 1,6-bisphosphatase
  • the FBPase inhibitor is a therapeutic agent and Z or preventive agent for diabetes, hyperglycemia, glucose intolerance, obesity, diabetic complications, etc. (preferably a therapeutic agent and Z or preventive agent for diabetes). It is a drug expected as such (see Patent Document 1).
  • Patent Document 1 Pamphlet of International Publication No. 2001/047935
  • An object of the present invention is to provide a solid preparation containing an FBPase inhibitor and excellent in drug dissolution, content uniformity, mass uniformity, hardness and abrasion resistance.
  • the present inventors include a step of formulating a composition containing an FBPase inhibitor by a dry production method. As a result, it was found that the drug dissolution and content uniformity, mass uniformity, hardness and abrasion resistance were improved, and the present invention was completed.
  • the present invention includes a solid preparation (particularly a preparation for the prevention or treatment of diabetes) characterized by comprising a step of formulating a composition containing an FBPase inhibitor by a dry production method, Use of an FBPase inhibitor to produce a preparation (especially a preparation for the prevention or treatment of diabetes), and a solid preparation containing a pharmacologically effective amount of an FBPase inhibitor to a warm-blooded animal (particularly human)
  • the present invention provides a method for the prevention or treatment of diseases (particularly diabetes) administered to).
  • the present invention provides: (1) A solid preparation characterized in that a composition containing an FBPase inhibitor is formulated in a process including a dry production method.
  • a composition containing an FBPase inhibitor is formulated in a process including a dry production method.
  • the above FBPase inhibitor has the following general formula (I)
  • X a represents a nitrogen atom, an oxygen atom or a sulfur atom
  • R la represents a hydrogen atom, a halogen atom, a C1-6 alkyl group or an amino group (the amino group is a C1-6 alkyl group, 1 or 2 R 2a and R 3a are the same or different and each represents a hydrogen atom or a C1-4 alkyl group
  • R 4a represents a C 1-4 alkyl group
  • R 5a represents A hydrogen atom, a C 1-6 alkyl group or a C 1-6 alkylthio group; Or a pharmacologically acceptable salt thereof.
  • the dissolution property of the FBPase inhibitor is improved, comprising a step of producing the solid preparation according to any one of (1) to (12) above by a dry production method.
  • a method for producing a solid preparation
  • a solid preparation with improved disintegration characterized by comprising a step of preparing the solid preparation according to any one of (1) to (12) above by a dry production method Production method,
  • a method for improving the disintegration property of a solid preparation comprising a step of producing the solid preparation according to any one of (1) to (12) above by a dry production method ,
  • a solid preparation comprising a step of formulating a composition containing an FBPase inhibitor in a step including a dry production method.
  • the “FBPase inhibitor” is not particularly limited as long as it is a drug that inhibits the action of FBPase (fructose 1,6-bisphosphatase), but for example, in WO 00/14095 pamphlet And the compounds described in International Publication No. 01/47935 pamphlet, and the phosphoric acid ester amide compounds having a prodrug skeleton of the phosphoric acid ester amide described in the above patent document are particularly preferable. Include jetyl N, ⁇ '-[5- (2-amino-5-isobutyl-1,3-thiazol-4-yl) -2-furylphosphonol] di-L-alaninate and its salts. is there.
  • the solid preparation of the present invention can be used, for example, for the treatment and Z or prevention of diabetes, hyperglycemia, glucose intolerance, obesity, diabetes complications, etc. (preferably treatment and Z or prevention of diabetes). It is valid.
  • the solid preparation of the present invention is excellent in content uniformity, mass uniformity, hardness and abrasion resistance of the FBPase inhibitor. Therefore, the solid preparation of the present invention is useful as a preparation having good quality and stable drug efficacy with little variation in FBPase inhibitor content per single preparation (for example, one tablet).
  • the active ingredient of the solid preparation of the present invention is an FBPase inhibitor.
  • FBPase inhibitor that is an active ingredient in the solid preparation of the present invention
  • various drugs have been proposed, and those skilled in the art can select an appropriate drug that exhibits the effects of the present invention. is there.
  • FBPase inhibitors include, for example, general formula (I)
  • X a represents a nitrogen atom, an oxygen atom or a sulfur atom
  • R la represents a hydrogen atom, a halogen atom, a C1-6 alkyl group or an amino group (the amino group is a C1-6 alkyl group) 1 or 2 may be substituted)
  • R 2a and R 3a are the same or different and represent a hydrogen atom or a C1-4 alkyl group
  • R 4a represents a C 1-4 alkyl group
  • R 5a represents a hydrogen atom, a C 1-6 alkyl group or a C 1-6 alkylthio group.
  • R la represents an amino group (the amino group may be substituted with one or two C1-6 alkyl groups), and R 3a represents a hydrogen atom or a C1-4 alkyl group.
  • R 1 ⁇ 2 represents a C 1-4 alkyl group.
  • the compounds represented by the general formulas (1) and (la) and pharmacologically acceptable salts thereof are described in WO 01/47935 and can be produced.
  • the “Cl-6 alkyl group” means a linear or branched alkyl group having 1 to 6 carbon atoms, and examples thereof include the above-mentioned “Cl-4 alkyl group”.
  • R la and R 5a are preferably a linear or branched alkyl group having 1 to 4 carbon atoms.
  • halogen atom is a fluorine atom, a chlorine atom, a bromine atom or an iodine atom
  • Rla is preferably a bromine atom, a chlorine atom or a fluorine atom, and more preferably a bromine atom or a chlorine atom. Is an atom.
  • the "C1_4 alkylthio group” is a group to which the "C1_4 alkyl group” is bonded via a sulfur atom.
  • methylthio, ethylthio, n-propylthio, isopropylthio, n-butylthio examples thereof include an isobutylthio group, a s-butylthio group, and a tert-butylthio group, and R 5a is preferably an n-propylthio group.
  • X a is preferably a sulfur atom.
  • R la is preferably an amino group (which may be substituted with a C 1-6 alkyl group), and more preferably an amino group. It is.
  • R 2a is the same or different and is preferably a hydrogen atom.
  • R 3a is the same or different and is preferably a C 1-4 alkyl group.
  • R 1 ⁇ 2 is the same or different and is preferably a methyl group or an ethyl group.
  • R is preferably a C1-6 alkyl group or a C1-6 alkylthio group, and more preferably a C1-4 alkyl group.
  • the solid preparation of the present invention may further contain appropriate pharmacologically acceptable excipients, lubricants, binders, disintegrants, emulsifiers, stabilizers, flavoring agents, diluents, and the like.
  • An agent can be included.
  • excipient examples include sugar derivatives such as lactose, sucrose, sucrose, mannitol or sorbitol; starch derivatives such as corn starch, potato starch, OC-starch or dextrin; Cellulose derivatives such as crystalline cellulose, methylcellulose; gum arabic; dextran; or organic excipients such as pullulan; or silicates such as light anhydrous silicic acid, synthetic aluminum silicate, calcium silicate or magnesium metasilicate Derivatives; phosphates such as calcium hydrogen phosphate; carbonates such as calcium carbonate; or inorganic excipients such as sulfates such as calcium sulfate.
  • sugar derivatives such as lactose, sucrose, sucrose, mannitol or sorbitol
  • starch derivatives such as corn starch, potato starch, OC-starch or dextrin
  • Cellulose derivatives such as crystalline cellulose, methylcellulose; gum arabic; dextran; or
  • the "lubricant" used is, for example, stearic acid; a stearic acid metal salt such as calcium stearate or magnesium stearate; talc; colloidal silica; a wax such as bead wax or cocoon Boric acid; adipic acid; sulfate such as sodium sulfate; fumarate such as fumaric acid and sodium stearyl fumarate; glycol; sodium benzoate; fatty acid ester such as glycerin fatty acid ester and sucrose fatty acid ester D, L-leucine; lauryl sulfate such as sodium lauryl sulfate or magnesium lauryl sulfate; silicic acid such as anhydrous silicic acid or silicic acid hydrate; or the above-mentioned starch derivative.
  • a stearic acid metal salt such as calcium stearate or magnesium stearate
  • talc colloidal silica
  • a wax such as bead
  • binder examples include hydroxypropylcellulose, hydroxypropyl pillmethylcellulose, polybulurpyrrolidone, macrogol, synthetic hydrotalcite, or compounds similar to the above-mentioned excipients. Can do.
  • Examples of the "disintegrant" used include cellulose derivatives such as low-substituted hydroxypropylcellulose, force-ruboxymethylcellulose, carboxymethylcellulose calcium or sodium carboxymethylcellulose; cross-linked polybutyrididone; or Mention may be made of chemically modified starch such as carboxymethyl starch or carboxymethyl starch sodium.
  • Emulsifiers used include, for example, colloidal clays such as bentonite or bee gum; metal hydroxides such as magnesium hydroxide or aluminum hydroxide; sodium lauryl sulfate or Anionic surfactants such as calcium stearate; cationic surfactants such as salt benzalkonium; or polyoxyethylene alkyl ether, polyoxyethylene sorbitan fatty acid ester or sucrose fatty acid ester Nonionic surfactants.
  • colloidal clays such as bentonite or bee gum
  • metal hydroxides such as magnesium hydroxide or aluminum hydroxide
  • sodium lauryl sulfate or Anionic surfactants such as calcium stearate
  • cationic surfactants such as salt benzalkonium
  • polyoxyethylene alkyl ether, polyoxyethylene sorbitan fatty acid ester or sucrose fatty acid ester Nonionic surfactants.
  • stabilizer examples include parahydroxybenzoates such as methylparaben or propylparaben; alcohols such as chlorobutanol, benzyl alcohol or phenolethyl alcohol; Mention may be made of benzalco-um; phenols such as phenol or talesol; thimerosal; dehydroacetic acid; or sorbic acid.
  • sweeteners such as saccharin sodium or aspartame
  • acidulants such as citrate, malic acid or tartaric acid
  • menthol lemon or orange.
  • a fragrance like this can be mentioned.
  • Examples of the "diluent" used include latatose, mannitol, glucose, sucrose, calcium sulfate, calcium phosphate, hydroxypropylcellulose, microcrystalline cellulose, water, ethanol, polyethylene glycolol, Mention may be made of propylene glycolol, glycerol, starch, polybulur pyrrolidone, magnesium aluminate metasilicate or mixtures thereof.
  • solid preparation examples include tablets (including uncoated tablets, film-coated tablets, sugar-coated tablets, sublingual tablets, orally disintegrating tablets), capsules (including soft capsules and microcapsules), granules, Fine granules, powders, pills, lozenges and the like can be mentioned, and preferred are powders, fine granules, granules, capsules or tablets, and most preferred are tablets.
  • the dry production method in the present invention includes a direct tableting method and a dry granulation method.
  • the "direct tableting method” is a method for preparing a raw material powder by direct compression molding.
  • “Dry granulation method” means that raw material powder is compression-molded into slug or sheet form, It is a method of formulating using granules produced by crushing and dividing. These manufacturing methods are The T heory and Practice of Industrial Pharmacy (Third Edition (Leon Lachman et al .: LEA & FEBIGER 1986) P.317-320, Pharmaceutical Dosage Forms: Tablets volume 1 (Second Edition) (Herbert A ⁇ ieberman et al. : MARCEL DEKKER INC. 1989) P.135-139, P.297.
  • granulation refers to an operation for producing granules having a substantially uniform shape and size from raw materials such as powder, lump, solution or liquid melt, and is the final form of granules, powders, fine granules, etc.
  • raw materials such as powder, lump, solution or liquid melt
  • granulations that produce products and granulations that produce intermediate products such as tablets and capsules.
  • the compression molding process is a process in which the raw material powder is pressurized by mechanical force to make the raw material powder into a lump, such as a rotary tablet machine (manufactured by Kikusui Seisakusho, Hata Iron Works, Sugawara Seiki Etc.), dry granulators such as roller compactors, roll dullers, chillers, etc. (Freund, Turbo, Kurimoto, Matsubo, Nippon Dura-Yureta, Fuji Powder, etc.) There is.
  • a rotary tablet machine manufactured by Kikusui Seisakusho, Hata Iron Works, Sugawara Seiki Etc.
  • dry granulators such as roller compactors, roll dullers, chillers, etc.
  • the upper limit is 4MgZmm 3 or less, as preferably 3MgZmm 3 hereinafter, and further preferably a 2MgZmm 3 or less To do.
  • the crushing 'division process is a process of crushing the lump formed in the compression molding process to an appropriate size with a knife' cutter or the like.
  • Examples of the apparatus used include power mill, Fitz mill, Fiore, There are pulverizers such as Comil and granulators (Fuji Padal, Deoksugaku Factory, manufactured by Paurek, etc.).
  • the granulated product thus obtained is sized to a desired particle size, and can be made into a preparation in the form of powder, fine granule or granule.
  • the granulated product thus obtained may be provided with at least one coating layer.
  • These preparations can be filled into capsules to form capsules, or further, disintegrating agents, lubricants, etc. are added as necessary, and compressed into tablets using a tableting machine, etc. to form tablet-form preparations. You can also. Operations such as mixing and granulation are all commonly used in the field of pharmaceutical technology, and those skilled in the art can appropriately perform them.
  • the tablet should have at least one coating layer.
  • Coating is performed using, for example, a coating apparatus, and as a coating base Examples include sugar coating base, water-soluble film coating base, enteric film coating base, sustained-release film coating base, and the like.
  • sucrose is used, and further, talc, precipitated calcium carbonate, phosphate phosphate, calcium sulfate, gelatin, gum arabic, polybulurpyrrolidone, pullulan, etc., one or two selected A combination of the above can also be used.
  • water-soluble film coating base examples include cellulose derivatives such as hydroxypropylcellulose, hydroxypropinoremethinoresenorelose, hydroxyethinoresenorelose, methinorehydroxyethylcellulose, sodium carboxymethylcellulose; Synthetic polymers such as acetal jetylaminoacetate, aminoalkyl methacrylate copolymer, polybulur pyrrolidone, polybulal alcohol; polysaccharides such as pullulan.
  • cellulose derivatives such as hydroxypropylcellulose, hydroxypropinoremethinoresenorelose, hydroxyethinoresenorelose, methinorehydroxyethylcellulose, sodium carboxymethylcellulose
  • Synthetic polymers such as acetal jetylaminoacetate, aminoalkyl methacrylate copolymer, polybulur pyrrolidone, polybulal alcohol
  • polysaccharides such as pullulan.
  • Enteric film coating bases include, for example, cellulose derivatives such as hydroxypropyl methylcellulose phthalate, hydroxypropenolemethinolecellulose acetate succinate, canoleboxymethylethyl cellulose, cellulose acetate phthalate; Examples include acrylic acid derivatives such as copolymer L, methacrylic acid copolymer LD, and methacrylic acid copolymer S; and natural products such as shellac.
  • cellulose derivatives such as hydroxypropyl methylcellulose phthalate, hydroxypropenolemethinolecellulose acetate succinate, canoleboxymethylethyl cellulose, cellulose acetate phthalate
  • acrylic acid derivatives such as copolymer L, methacrylic acid copolymer LD, and methacrylic acid copolymer S
  • natural products such as shellac.
  • sustained-release film coating bases include cell mouth derivatives such as ethyl cellulose; acrylic acid such as aminoalkyl methacrylate copolymer RS, ethyl acrylate acrylate 'methyl methacrylate copolymer emulsion, etc. Derivatives and the like.
  • Two or more of the above coating bases may be mixed and used at an appropriate ratio. Further, if necessary, additives such as appropriate pharmacologically acceptable plasticizers, excipients, lubricants, masking agents, coloring agents, preservatives and the like can be included.
  • hardness refers to the hardness of a tablet, ie, an uncoated tablet, to which a coating or the like is applied, and the value is a commercially available tablet hardness measuring device (tablet continuous measuring device WHT- 2, etc., manufactured by P harmatest).
  • the hardness of the tablet (plain tablet) is preferably 5.0 kg or more and 20.0 kg or less, more preferably 5.0 kg or more and 17.5 kg or less, and most preferably 5.0 kg or more and 15.0 kg or less.
  • the dose of the FBPase inhibitor which is an active ingredient of the solid preparation of the present invention, depends on the activity of the drug, It may vary depending on various conditions such as a person's symptoms, age, weight, and the like.
  • the dose varies depending on symptoms, age, etc., but in the case of oral administration, it is usually lmg (preferably 10 mg, more preferably 25 mg) as the lower limit for adults, and 2000 mg as the upper limit. (Preferably 400 mg, more preferably 200 mg) can be administered.
  • Jetyl N, N '-[5- (2-Amino-5-isobutyl-1,3-thiazol-4-yl) -2-furylphosphonoyl] di-L-ala-nate (hereinafter referred to as compound) A) can be produced according to the method described in International Publication No. 01/47935.
  • Compound A (3g), crystalline cellulose (3.66g), low substituted hydroxypropylcellulose (1.8g), hydroxypropylmethylcellulose (0.45g), magnesium stearate (0.09g) were mixed in an agate mortar for 2 minutes The mixture was sieved with a 40 mesh sieve and mixed again with an agate mortar to obtain a mixed powder.
  • Tableting was performed with a ⁇ 9.0 ⁇ 2 double R punch and a tableting pressure of 10 kN.
  • Table 1 shows the results of disintegration and dissolution tests on the obtained tablets.
  • Compound A (3g), crystalline cellulose (3.66g), low-substituted hydroxypropylcellulose (1.8g), hydroxypropylmethylcellulose (0.45g) were mixed in an agate mortar, and then purified water (amount of water added to the mixed powder was about 53%).
  • the resulting kneaded product is dried with a vacuum dryer, then sieved with a 20 mesh sieve, magnesium stearate (0.09 g) is added and mixed for 5 minutes with a V-type mixer to obtain mixed granules. It was.
  • the test was conducted using 50 mL of citrate buffer (pH 2.5) 900 mL as the test solution at 50 rpm. Test solutions at 5 minutes, 10 minutes, 15 minutes and 30 minutes after the start of the test were collected, and the elution rate of Compound A was measured by absorbance measurement. [Toyama Sangyo Co., Ltd .: Dissolution tester, Shimadzu Corporation spectrophotometer]. The test was conducted with 6 tablets, and the average value of the dissolution rate was calculated.
  • the obtained mixed powder was tableted using a rotary tableting machine with a 15 X 7.3 mm Oval type double R punch at a tableting pressure of 30 kN so that the tablet mass force was 00 mg. .
  • Table 2 shows the results of a content uniformity test on the obtained tablets.
  • the test was conducted by a liquid chromatograph (HPLC) method using an internal standard method using an ultraviolet absorptiometer as a detector. [Shimadzu: HPLC] From the obtained data, the content uniformity test judgment value was calculated by the method described in the Japanese Pharmacopoeia, 14th revision, content uniformity test judgment value and tablet mass standard Relative standard deviation (RSD) calculated from deviation and average tablet weight Shown in 2
  • the content uniformity test judgment value of the dry granulation preparation was 4.9, which was significantly lower than that of the direct compression tablet preparation (Comparative Example 2). Furthermore, the dry granulation method formulation (Example 2) had an RSD value of 2.89, which was significantly lower than the direct tableting formulation (Comparative Example 2). The remarkably less mass variation. Therefore, in the production of FBPase inhibitor preparations, it can be proved that the dry granulation method is particularly suitable among the dry production methods.
  • Compound V (14000g), crystalline cellulose (15694g), low-substituted hydroxypropyl cellulose (3500g), light anhydrous caustic acid (56g), magnesium stearate (700g), talc (1050g)
  • the tableting pressure (A1: 10kN A2: 30kN) is changed so that the tablet weight becomes about 500mg and various densities by using a rotary tableting machine.
  • the obtained tablet A was crushed with a granulator to obtain granules for tableting.
  • the obtained granule for tableting was mixed with a V-type mixer for 5 minutes, and then using a rotary tableting machine, the tablet mass became 250 mg with a double R punch of 8.5 mm. Thus, tableting was performed at a tableting pressure of 10 kN.
  • the obtained tablet B was measured for hardness and friability.
  • the hardness of the tablets was measured using a continuous tablet measuring device (WHT-2) manufactured by Pharmatest. The test was performed on 10 tablets, and the average hardness obtained was calculated and shown in Table 3.
  • Friction (%) [(mass before shaking—mass after shaking) / mass before shaking] X 100 (Table 3)
  • tablet B1 which was produced under the condition of low density of tablet A, had higher hardness and lower friability than tablet B2 with higher density of tablet A. Therefore, it was shown that the compression density of the granulation process in the dry granulation method affects the hardness and friability, and that a tablet with better quality can be produced with a smaller compression density.
  • the dissolution property and content uniformity of a drug containing an FBPase inhibitor In addition, a solid preparation excellent in mass uniformity, hardness and abrasion resistance can be obtained.

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  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne une composition pharmaceutique comprenant un inhibiteur de fructose 1,6-diphosphate (FBPase) qui possède de remarquables propriétés en termes de dissolution du médicament, d'uniformité de contenu, d'uniformité de masse, de dureté et de résistance à l'usure. Est également décrite une préparation solide dont le processus d'obtention consiste à préparer une composition contenant un inhibiteur de fructose 1,6 disphosphate par voie sèche.
PCT/JP2007/057832 2006-04-10 2007-04-09 Préparation obtenue par voie sèche Ceased WO2007129522A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2006107685 2006-04-10
JP2006-107685 2006-04-10

Publications (1)

Publication Number Publication Date
WO2007129522A1 true WO2007129522A1 (fr) 2007-11-15

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PCT/JP2007/057832 Ceased WO2007129522A1 (fr) 2006-04-10 2007-04-09 Préparation obtenue par voie sèche

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WO (1) WO2007129522A1 (fr)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004009118A1 (fr) * 2002-07-23 2004-01-29 Sankyo Company, Limited Prophylactique contre l'apparition des diabetes
JP2004508297A (ja) * 2000-07-06 2004-03-18 メタバシス・セラピューティクス・インコーポレイテッド 糖尿病の治療に有用なｆｂｐアーゼインヒビターおよび抗糖尿病薬の併用剤

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004508297A (ja) * 2000-07-06 2004-03-18 メタバシス・セラピューティクス・インコーポレイテッド 糖尿病の治療に有用なｆｂｐアーゼインヒビターおよび抗糖尿病薬の併用剤
WO2004009118A1 (fr) * 2002-07-23 2004-01-29 Sankyo Company, Limited Prophylactique contre l'apparition des diabetes

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
MATSUMOTO M. ET AL.: "Yakuzaiku Manual", vol. 1ST ED., 20 March 1989, NANZANDO CO., LTD., pages: 89 - 92, XP003024635 *

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