WO2010038695A1 - Préparation moulée par compression et son procédé de production - Google Patents

Préparation moulée par compression et son procédé de production Download PDF

Info

Publication number
WO2010038695A1
WO2010038695A1 PCT/JP2009/066753 JP2009066753W WO2010038695A1 WO 2010038695 A1 WO2010038695 A1 WO 2010038695A1 JP 2009066753 W JP2009066753 W JP 2009066753W WO 2010038695 A1 WO2010038695 A1 WO 2010038695A1
Authority
WO
WIPO (PCT)
Prior art keywords
compression
starch
polyvinyl alcohol
molded preparation
molded
Prior art date
Application number
PCT/JP2009/066753
Other languages
English (en)
Japanese (ja)
Inventor
裕里子 小野
陽彦 洞口
信夫 山田
Original Assignee
大洋薬品工業株式会社
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 大洋薬品工業株式会社 filed Critical 大洋薬品工業株式会社
Priority to JP2010531841A priority Critical patent/JP5694773B2/ja
Priority to CN2009801387678A priority patent/CN102170912A/zh
Publication of WO2010038695A1 publication Critical patent/WO2010038695A1/fr

Links

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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin

Definitions

  • the present invention relates to a compression-molded preparation such as an orally disintegrating tablet and a method for producing the same. More specifically, the present invention has excellent disintegrability in the oral cavity while having hardness that does not cause wear during production and transportation. Furthermore, the present invention relates to a compression-molded preparation with improved manufacturability in existing facilities and a method for producing the same.
  • oral preparations such as tablets, capsules, granules, and powders are most widely used as pharmaceutical dosage forms from the viewpoint of simplicity and ease of administration.
  • many of such oral preparations have a problem that it is difficult to take for elderly people, children and patients who have difficulty swallowing.
  • lozenges that can be taken without water and quickly disintegrate in the oral cavity, or tablets that dissolve quickly in an aqueous solvent when taken in water for the purpose of solving the problem of dosing.
  • the development of lozenges is ongoing.
  • a method for producing an orally disintegrating tablet (Table 1) that compresses a mixture containing water at a level where the particle surface is moistened, or an amorphous saccharide is mainly used.
  • a method for producing an orally disintegrating tablet (Patent Documents 2 and 3) is known in which a tablet is compression-molded at a low pressure, moistened and moistened, and further dried.
  • Patent Documents 2 and 3 all of these technologies are capable of rapid disintegration in aqueous solvents and preparations that retain the hardness required for portability, but they can handle moisture during the manufacturing process and under high humidity.
  • the present inventor uses mannitol, which is entirely or partially delta-type crystals, as a carrier component, so that even if the compression molding time is shortened, An orally disintegrating tablet that is a compression-molded preparation having a hardness that can withstand rapid disintegration, production, and transportation can be obtained, and powder scattering can be suppressed by reducing the amount of fine powder during granulation,
  • Patent Document 5 The inventors found that damage to the preparation during production and transportation can be reduced by improving the compression moldability, and filed a patent application (Patent Document 5).
  • the inventors of the present invention have been diligently researching on a compression molding preparation, and granulating sugar alcohol such as mannitol using a solution containing starch or a starch-derived processed product and a specific polymer binder such as polyvinyl alcohol. As a result, it was found that a compression-molded preparation having excellent disintegration properties and sufficient hardness as an orally disintegrating tablet can be obtained even under extremely high-speed tableting conditions, and the present invention has been completed.
  • the present invention is a compression-molded preparation containing a sugar-based alcohol, starch or a starch-derived compound, and a polymer-based binder selected from the group consisting of a polyvinyl alcohol-based polymer and copolyvidone.
  • the sugar alcohol is granulated with an aqueous solution in which starch or a starch-derived compound and a polymer binder selected from the group consisting of a polyvinyl alcohol polymer and copolyvidone are dissolved to form granules, and then compressed.
  • a method for producing a compression-molded preparation characterized by molding.
  • the present invention even if tableting is performed at a speed exceeding 50,000 tablets / hour using a high-speed tableting machine, no special device is required, and tableting troubles such as sticking, capping, and die friction are prevented.
  • a compression-molded preparation having both disintegration and hardness can be obtained without causing it.
  • the hardness of the preparation or the disintegration time in the oral cavity can be adjusted by appropriately adjusting the tableting pressure.
  • sugar alcohol used in the compression-molded preparation of the present invention examples include mannitol, xylitol, sorbitol, erythritol, etc. Among them, mannitol is preferable. Further, when mannitol is used as the sugar alcohol, it is preferable that all mannitol is delta type, or a part of mannitol is delta type, and other crystal forms are other than that.
  • mannitol has alpha, beta, and delta crystal polymorphs that are identified from the results of X-ray diffraction. It is desirable that at least a part of delta mannitol is contained in order to have an action such as reduction.
  • the amount of delta-type mannitol is not particularly limited, but is 3% by mass (hereinafter simply referred to as “%”) or more, preferably 5% or more of the whole mannitol. Yes, more preferably 10% or more, still more preferably 20% or more.
  • starch or starch-derived compound (hereinafter referred to as “starch”) used in the present invention is used as a binder that dissolves or swells in water at room temperature (hereinafter sometimes simply referred to as “binder”). Is.
  • starch-derived compounds are those in which starch, which is not normally dissolved in water, is dissolved in whole or in part by some method. Specifically, starch starch is pregelatinized or hydrolyzed. Things.
  • pregelatinization refers to a state in which water enters the crystal structure by breaking the hydrogen bond for maintaining the crystal structure by heating the starch soaked in water.
  • starch can be suspended in water and the suspension can be heated to alpha.
  • Pregelatinized starch also includes starch that is at least partially pregelatinized, that is, substantially pregelatinized starch.
  • pregelatinized starch is commercially available as a pregelatinized compound, it can be used. Further, since partially pregelatinized starch is commercially available as substantially pregelatinized starch, it may be used.
  • additives obtained by hydrolyzing starch are also “starches” and can be sufficiently used in the present invention.
  • starch hydrolyzate is dextrin.
  • this patent also relates to pullulan, which is a natural polysaccharide in which maltotriose is regularly ⁇ -1,6-linked, obtained by culturing Aureobasidium pullulans , a kind of black yeast. Fully demonstrate the effect.
  • polyvinyl alcohol polymers and copolyvidone used in the present invention also act as binders (hereinafter, these may be collectively referred to as “polymer binders”).
  • the polyvinyl alcohol-based polymer is polyvinyl alcohol or a copolymer of vinyl alcohol and other monomers described later.
  • a copolymer of polyvinyl alcohol a copolymer in which another polymer branches from a part of the main chain such as a graft copolymer, a copolymer in which polymer structural units are randomly arranged, such as a random copolymer, or Examples thereof include block copolymers.
  • the graft copolymer include polyvinyl alcohol-polyethylene glycol graft copolymer
  • specific examples of the random copolymer include polyvinyl alcohol-acrylic copolymer.
  • polyvinyl alcohol having a molecular weight of about 10,000 to 300,000, particularly about 30,000 to 200,000 is preferable.
  • This polyvinyl alcohol can be produced or obtained by polymerizing vinyl acetate and saponifying it.
  • the saponification type is classified into a complete saponification type and a partial saponification type, but the present invention sufficiently exhibits the effect of the present invention regardless of which polyvinyl alcohol is used.
  • the polyvinyl alcohol-polyethylene glycol graft copolymer has a main chain of polyethylene glycol (PEG) portion and a side chain of polyvinyl alcohol (PVA) portion as represented by the following formula (I): It is a graft copolymer of PEG and PVA composed of
  • the polyvinyl alcohol-polyethylene glycol graft copolymer preferably has a molecular weight of about 10,000 to 100,000, particularly about 30,000 to 70,000.
  • the polyvinyl alcohol-polyethylene glycol graft copolymer preferably has a weight ratio of PEG part to PVA part of 1: 0.1 to 10.
  • Kollicoat IR (trade name) manufactured by BASF is commercially available, and can be used, but other products may also be used.
  • the polyvinyl alcohol-acrylic copolymer is a copolymer containing PVA, acrylic acid and methyl (meth) acrylate as represented by the following formula (II).
  • the polyvinyl alcohol-acrylic copolymer preferably has a molecular weight of about 10,000 to 200,000, particularly about 30,000 to 100,000.
  • the polyvinyl alcohol copolymer preferably has a weight ratio of PVA to acrylic acid and methyl methacrylate of 1: 0.01 to 0.1: 0.1 to 0.5.
  • POVACOAT trade name manufactured by Nisshin Kasei Co., Ltd. is commercially available. This can be used, but other products may also be used.
  • copolyvidone is a copolymer of 1-vinyl-2-pyrrolidone and vinyl acetate, as represented by the following formula (III).
  • the copolyvidone preferably has a molecular weight of about 10,000 to 100,000, particularly about 45,000 to 70,000.
  • the weight ratio of 1-vinyl-2-pyrrolidone and vinyl acetate in this copolyvidone is not particularly limited, but is preferably 1: 5 to 0.1, more preferably 1: 1 to 0.5.
  • Kollidon VA64 (trade name) is commercially available from BASF, and can be used, but other products may also be used.
  • the amount of sugar alcohol is about 30 to 98%, preferably 50 to 95% in the preparation.
  • the compounding amount of starches is about 0.01 to 10% in the preparation, preferably about 0.05 to 5%
  • the amount of the polymer binder is about 0.01 to 10% in the preparation, preferably Is about 0.05 to 2%.
  • the blending ratio of starch to sugar alcohol is preferably 0.1 to 5 with respect to sugar alcohol 100, and the blending ratio of polymer binder to sugar alcohol 100 is 0.5 to sugar alcohol 100. Or 10 is preferred.
  • the granulator used in this case is not particularly limited as long as it is a granulator capable of forming a granular material with almost no fine powder like ordinary tableting granules.
  • a fluidized bed granulator preferably a stirring granulator, an extrusion granulator, a rolling granulator, a Wurster granulator, or a granulator that combines these is best.
  • Such granulators include fluidized bed granulators.
  • This compression molding can be used without particular limitation as long as it is a general compression molding method.
  • a preferred compression molding machine is a rotary tableting machine.
  • the productivity per hour of compression molding is not particularly limited, but is preferably 50,000 tablets or more per hour, more preferably 100,000 tablets. That's it.
  • the rotary tableting machine greatly affects the tableting characteristics because the compression molding time varies depending on the number of rotations of the turntable. It is also known that the size of the turntable as well as the rotation speed of the turntable affects the tableting characteristics.
  • the pressure at the time of compression molding is not particularly limited as long as the disintegration time and texture in the oral cavity are appropriate, and there are no cracks at the time of production and transportation, preferably 100 to 2000 kgf, More preferably, compression molding is performed at 300 to 1500 kgf.
  • the compression-molded preparation of the present invention can be made into an orally disintegrating tablet.
  • the orally disintegrating tablet of the present invention may be rapidly disintegrated when a compression-molded preparation is included in the oral cavity, and the specific disintegration time is preferably within 3 minutes after being included in the oral cavity. Is within 1 minute, more preferably within 30 seconds.
  • the orally disintegrating tablet which reached this invention is improved more than before with respect to the cracks, chipping, etc. of transportation etc., and has provided the durability similar to a normal compression molding formulation.
  • evaluation is carried out using the tablet friability test method described in the 15th revised Japanese Pharmacopoeia.
  • a tablet weight reduction rate of 5.0% or less is a preferred compression molding preparation of the present invention, and a compression molding preparation of 2.0% or less, particularly 1.0% or less is preferred.
  • Reduction rate (%) (weight before test-weight after test) / weight before test x 100
  • binders can be used in addition to the aforementioned starches and polymer binders.
  • Preferred examples of such a binder include a compound that can dissolve in water by substituting a part of cellulose with a hydrophilic substituent, and can be dissolved in water by hydrolyzing and pregelatinizing starches. Examples include compounds obtained by chemically changing cellulose, starch, and the like as described above with microorganisms. Specific examples include hydroxypropylcellulose, hydroxyethylcellulose, hydroxypropylmethylcellulose, carmellose sodium, dextrin, pullulan, and soluble polyvinylpyrrolidone.
  • the addition method of the inorganic compound is not particularly limited.
  • a method of adding during granulation a method of adding to a binder liquid (granulation liquid), a granule after granulation
  • a method of adding to a method of adding to.
  • you may employ adopt the method of coating an inorganic compound on the granulated material of sugar alcohol, starches, and a polymer type binder.
  • the preferred method is the method of adding to the binder solution, the method of coating the granules after granulation, the method of adding to the granules after granulation, and the best method is dissolving in mannitol and water at room temperature.
  • it is a method of coating on a granulated product of a swelling binder or a method of adding after granulation.
  • the compression-molded preparation of the present invention basically contains a physiologically active substance as an active ingredient.
  • the compounding of the physiologically active substance into the compression molding preparation may be carried out at any stage of the production of the compression molding preparation. For example, a method of blending a physiologically active ingredient together with sugar alcohol at the time of granulation, or adding to a binder solution And a method of blending with granulated granules.
  • physiologically active ingredient that can be blended as an active ingredient is not particularly limited.
  • Agent autonomic nerve agent, antispasmodic agent, cardiotonic agent, arrhythmic agent, diuretic agent, antihypertensive agent, vasoconstrictor, vasodilator, hyperlipidemia agent, antitussive agent, expectorant, bronchodilator, antipruritic agent Peptic ulcer agent, healthy stomach digestive agent, antacid, laxative, hormone agent, vitamin agent, nourishing tonic, enzyme preparation, diabetic agent, antihistamine, allergic agent, antibiotic preparation, synthetic antibacterial agent, sickness prevention
  • a physiologically active ingredient which is an active ingredient such as an agent can be used.
  • physiologically active components of sleep sedatives and anxiolytic agents for example, alprazolam, estazolam, quazepam, triazolam, brotizolam, amobarbital, tandospirone, etc.
  • physiologically active components of antiepileptic agents for example, phenytoin, Carbamazepine, clonazepam, phenytoin, etc.
  • physiologically active components of antipyretic analgesics for example, acetaminophen, phenacetin, mefenamic acid, aspirin, ethenamide, isopropylantipyrine, sodium salicylate, indomethacin, diclofenac, tiaramid, actarit, ampiroxicam, Ibuprofen, etodolac, ketoprofen, zaltoprofen, piroxicam, pranoprofen, loxoprofen, etc.
  • bioactive ingredients of anti-parkinsonian drugs For example, amantadine, biperidene, selegiline, trihexyphenidyl, cabergoline, pergolide, and the like as the physiologically active ingredients of the neuropsychiatric agent, for example, chlorpromazine, perphenazine, triproperazine, imipramine, etizolam, olanzapine, Quazepam, sulpiride, haloperidol, risperidone, etc.
  • amantadine, biperidene, selegiline, trihexyphenidyl, cabergoline, pergolide, and the like as the physiologically active ingredients of the neuropsychiatric agent, for example, chlorpromazine, perphenazine, triproperazine, imipramine, etizolam, olanzapine, Quazepam, sulpiride, haloperidol, risperidone, etc.
  • physiologically active components of autonomic nerve agents such as carpronium, distigmine, tolazoline, etc.
  • physiologically active components of antispasmodics are butylscopolamine bromide, papaverine, eperisone, tizanidine , Baclofen and the like.
  • cardiotonic agent examples include dichitoxin, digoxin, methyldigoxin, aminophylline, caffeine, ethylephrine, ubidecalenone, and examples of the arrhythmia agent include procainamide, atenolol, oxprenolol, carteolol, propranolol, and nadolol.
  • Pindolol Pindolol, bisoprolol, ajmarin, pirucainide, propaphenone, methiciletin, disopyramide, etc., as diuretics, for example, hydrochlorothiazide, spironolactone, acetazolamide, isosorbide, torasemide, furosemide, etc.
  • vasoconstrictors for example, midodrine, dihydroergotamine, etc.
  • vasodilators for example, isosorbide mononitrate, Etaphenone, diltiazem, benidipine, dipyridamole, isosorbide nitrate, nicorandil, nisoldipine, nitroglycerin, nifedipine and the like as the hyperlipidemic agent, for example, clofebrate, fenof
  • antitussives for example, ephedrine, methylephedrine, noscapine, benproperin and the like
  • expectorant for example, carbocysteine, bromhexine, ambroxol, cherry bark, codeine, dihydrocodeine, tipepidine and the like are bronchodilators.
  • theophylline, fenoterol, salbutamol, clenbuterol, tulobuterol, trimethoquinol, procaterol, formoterol, etc. as antidiarrheal agent / intestinal, for example, berberine, albumin, bifidobacteria, lactamine, dimethicone, loperamide, etc.
  • ulcers examples include glutamine, azulene, ranitidine, cimetidine, famotidine, nizatidine, loxatidine, aldioxa, pirenzepine, omeprazole, gefa Nart, sucralfate, sulpiride, cefircon, teprenone, troxipide, irsogladine, rabeprazole, lansoprazole and the like as gastric digestive agents, for example, amylase, diastase, pancreatin, fomikatinki, carnitine, galactosidase, etc.
  • examples include magnesium silicate, magnesium oxide, sodium hydrogen carbonate, magnesium carbonate, precipitated calcium carbonate, and examples of laxatives include senna extract, sennoside, magnesium sulfate, and picosulfate.
  • hormonal agents for example, levothyroxine, liothyronine, thiamazole, propylliouracil, cortisone, parameterzone, dexamethasone, betamethasone, prednisolone, testosterone, phosfestol, estriol, chlormadinone, allylestrenol, clomiphene, tanazole, Tamsulosin, flavoxate, midodrine, gamma oryzanol, etc.
  • vitamin agents for example, vitamin A, calcitriol, thiamine, fursultiamine, riboflavin, panthetin, pantothenic acid, pyridoxine, folic acid, cobamide, mecobalamin, ascorbic acid, tocopherol Phytonadione, menatetrenone, biotin, etc.
  • enzyme preparations such as lysozyme, serrapeptase, etc.
  • antidiabetic agents include gliclazide, glibenclamide, glimepiride, tolbutamide, metformin, acarbose, voglibose, etc.
  • antihistamines include, for example, diphenhydramine, promethazine, mequitazine, chlorpheniramine, clemastine, etc.
  • antihistamines include, for example, diphenhydramine, promethazine, mequitazine, chlorpheniramine, clemastine, etc.
  • examples include ibudilast, azelastine, epinastine, cetirizine, suplatast, tranilast, ketotifen, pranlukast, pemirolast, loratadine and the like.
  • antibiotics include, for example, clindamycin, lincomycin, vancomycin, kanamycin, amoxicillin, ampicillin, cefaclor, cephalexin, cefixime, cefpodoxime, cefdinir, cefteram, cefpodoxime, fosfomycin, faropenem, erythromycin, azithromycin, clarithromycin , Roxithromycin, chloramphenicol, tetracycline, minocycline, salazosulfapyridine, ciprofloxacin, gatifloxacin, norfloxacin, acyclovir, itraconazole, terbinafine, fluconazole, miconazole and the like.
  • any optional components such as various lubricants, solubilizers, buffers, adsorbents, etc., as long as the effects of the present invention other than the above components are not impaired.
  • Suspending agents, antioxidants, fillers, pH adjusting agents, excipients, dispersants, disintegrating agents, disintegrating aids, moisture-proofing agents, preservatives, solvents, solubilizing agents, fluidizing agents, etc. be able to.
  • excipients include lactose, purified white sugar, crystalline cellulose, dextran, dextrin, glucose, and powdered sugar.
  • disintegrant examples include carmellose, carmellose calcium, croscarmellose sodium, low-substituted hydroxypropyl methylcellulose, crystalline cellulose, and hydroxypropyl starch.
  • Examples of the lubricant include magnesium stearate, calcium stearate, stearic acid, talc, and sucrose fatty acid ester.
  • Examples of the coating agent include hydroxypropyl methylcellulose, ethyl acrylate / methyl methacrylate copolymer, aminoalkyl methacrylate copolymer E, aminoalkyl methacrylate copolymer RS, hydroxypropyl methylcellulose phthalate, methacrylic acid copolymer L, methacrylic acid copolymer LD, methacrylic acid Acid copolymer S etc. are mentioned.
  • examples of the taste masking component include citric acid, tartaric acid, malic acid and the like.
  • foaming agent examples include sodium bicarbonate.
  • artificial sweetener examples include saccharin sodium, dipotassium glycyrrhizin, aspartame, stevia, thaumatin and the like.
  • masking agent examples include water-insoluble polymers such as ethyl cellulose and gastric polymers such as methyl methacrylate / butyl methacrylate / diethylaminoethyl methacrylate copolymer.
  • the compression-molded preparation of the present invention described above has both sufficient hardness during production and transportation and rapid disintegration in the oral cavity.
  • high productivity can be expected.
  • Example 1 Orally disintegrating tablets were produced according to the formulation and production method shown in Table 1 below.
  • Tablets 2 to 4 are the same as in the above production method except that polyvinyl alcohol-polyethylene glycol graft copolymer (tablet 2), copolyvidone (tablet 3), and polyvinyl alcohol-acrylic copolymer (tablet 4) are used instead of polyvinyl alcohol. It was prepared as follows.
  • Example 2 Evaluation of orally disintegrating tablets (1) For the orally disintegrating tablets prepared in Example 1, the tablets 1 to 4 obtained were evaluated for hardness, friability, disintegration time in the oral cavity, and tableting failure. The results are shown in Table 2.
  • Hardness The hardness of the tablet was measured using a hardness meter (tablet breaking strength measuring instrument TH-303MP: Toyama Sangyo Co., Ltd.).
  • Abrasion degree A friability tester (tablet friability tester: Minato Medical Co., Ltd.) was used to check the state of tablet abrasion (test time 30 minutes, tablet quantity 100 tablets).
  • Oral disintegration time An adult male was used as a panel, the manufactured tablet was included in the mouth, and the time until the tablet disintegrated was measured.
  • Presence / absence of tableting failure The presence or absence of tableting failure such as capping, lamination, sticking, die friction and wrinkle adhesion during tableting was evaluated.
  • Example 3 Evaluation of orally disintegrating tablets (2) In tablet 1 of Example 1, an orally disintegrating tablet was prepared in the same manner except that the turntable rotation speed was 40 times / minute and the tableting pressure was changed. The hardness, friability, The disintegration time and the presence or absence of tableting failure were evaluated in the same manner as in Example 2. The results are shown in Table 3.
  • the compression-molded preparation of the present invention combines the rapid disintegration property in the oral cavity with the hardness necessary for production, transportation, etc., and can be advantageously used when orally administering various physiologically active substances. It is.
  • a compression-molded preparation of the present invention it is possible to stably perform tableting without causing tableting troubles such as wrinkle adhesion, capping and die friction without using an external sliding device. Even if the time is shortened, a compression-molded preparation having rapid disintegration can be obtained. Further, since the compression molding can be performed at a high speed, the productivity is dramatically improved.
  • the method of the present invention is extremely advantageous as a method for producing a compression-molded preparation.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Inorganic Chemistry (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne une préparation moulée par compression telle qu’une préparation se délitant dans la bouche qui a la propriété de se déliter rapidement dans la cavité orale et possède également la dureté nécessaire pour la production, le transport, ou équivalents et simultanément ne cause pas de problème même si la préparation est produite avec une productivité élevée ; et un procédé de production de celle-ci. La préparation moulée par compression contient un alcool de sucre, de l’amidon ou un composé dérivé de l’amidon et un liant polymère choisi dans le groupe comprenant un polymère à base d’alcool polyvinylique et de la copolyvidone. Le procédé de production de la préparation moulée par compression comprend une étape consistant à granuler un alcool de sucre avec une solution aqueuse obtenue en dissolvant l’amidon ou un composé dérivé de l’amidon et un liant polymère choisi dans le groupe comprenant un polymère à base d’alcool polyvinylique et la copolyvidone afin de former des granulés, et ensuite une étape de moulage par compression des granulés résultants.
PCT/JP2009/066753 2008-09-30 2009-09-28 Préparation moulée par compression et son procédé de production WO2010038695A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2010531841A JP5694773B2 (ja) 2008-09-30 2009-09-28 圧縮成型製剤およびその製造方法
CN2009801387678A CN102170912A (zh) 2008-09-30 2009-09-28 压缩成型制剂及其制造方法

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2008-254536 2008-09-30
JP2008254536 2008-09-30

Publications (1)

Publication Number Publication Date
WO2010038695A1 true WO2010038695A1 (fr) 2010-04-08

Family

ID=42073459

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2009/066753 WO2010038695A1 (fr) 2008-09-30 2009-09-28 Préparation moulée par compression et son procédé de production

Country Status (4)

Country Link
JP (1) JP5694773B2 (fr)
CN (1) CN102170912A (fr)
TW (1) TW201023850A (fr)
WO (1) WO2010038695A1 (fr)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013087074A (ja) * 2011-10-17 2013-05-13 Daido Kasei Kogyo Kk 医薬用結合剤及び該結合剤を用いた製剤
JP2014501226A (ja) * 2010-12-17 2014-01-20 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング 直接圧縮可能なδ−マンニトールの調製方法
US20140356429A1 (en) * 2010-07-20 2014-12-04 Japan Tobacco Inc. Tablet containing ferric citrate
JP2014224086A (ja) * 2013-04-22 2014-12-04 テイカ製薬株式会社 口腔内速崩壊性固形製剤用組成物
JP2015063521A (ja) * 2013-09-02 2015-04-09 科研製薬株式会社 高い薬物含有率を有する錠剤及びその製造方法
JP6188183B1 (ja) * 2016-05-23 2017-08-30 大原薬品工業株式会社 薬物高含有圧縮錠剤の安定な製造方法
JP2020169145A (ja) * 2019-04-04 2020-10-15 ニプロ株式会社 アジルサルタンを含有する医薬組成物

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106236717A (zh) * 2016-08-30 2016-12-21 佛山市弘泰药物研发有限公司 一种扎托布洛芬口崩片及其制备方法

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH02502720A (ja) * 1987-03-25 1990-08-30 イー・アイ・デユポン・デ・ニモアス・アンド・カンパニー 活性物質を錠剤にするためのビニルアルコールホモ重合体および共重合体の使用
WO2000048575A1 (fr) * 1999-02-17 2000-08-24 Kyowa Hakko Kogyo Co., Ltd. Comprimes et procede de production de comprimes
JP2000516263A (ja) * 1997-12-29 2000-12-05 ザ、プロクター、エンド、ギャンブル、カンパニー 錠剤組成物
JP2005306778A (ja) * 2004-04-21 2005-11-04 Basf Ag 徐放性製剤及びその製造方法
WO2006106923A1 (fr) * 2005-03-31 2006-10-12 Taiyo Yakuhin Co., Ltd. Comprimé se désintégrant dans la cavité orale et méthode pour le produire
JP2007191474A (ja) * 2005-12-20 2007-08-02 Takeda Chem Ind Ltd 着色糖衣錠
WO2008078727A1 (fr) * 2006-12-26 2008-07-03 Daiichi Sankyo Company, Limited Composition pharmaceutique à capacité de dissolution améliorée

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1884242B1 (fr) * 2005-05-26 2013-04-17 Dainippon Sumitomo Pharma Co., Ltd. Composition pharmaceutique comprenant le lurasidone
EP1852108A1 (fr) * 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG Compositions d'inhibiteurs de la DPP IV

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH02502720A (ja) * 1987-03-25 1990-08-30 イー・アイ・デユポン・デ・ニモアス・アンド・カンパニー 活性物質を錠剤にするためのビニルアルコールホモ重合体および共重合体の使用
JP2000516263A (ja) * 1997-12-29 2000-12-05 ザ、プロクター、エンド、ギャンブル、カンパニー 錠剤組成物
WO2000048575A1 (fr) * 1999-02-17 2000-08-24 Kyowa Hakko Kogyo Co., Ltd. Comprimes et procede de production de comprimes
JP2005306778A (ja) * 2004-04-21 2005-11-04 Basf Ag 徐放性製剤及びその製造方法
WO2006106923A1 (fr) * 2005-03-31 2006-10-12 Taiyo Yakuhin Co., Ltd. Comprimé se désintégrant dans la cavité orale et méthode pour le produire
JP2007191474A (ja) * 2005-12-20 2007-08-02 Takeda Chem Ind Ltd 着色糖衣錠
WO2008078727A1 (fr) * 2006-12-26 2008-07-03 Daiichi Sankyo Company, Limited Composition pharmaceutique à capacité de dissolution améliorée

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140356429A1 (en) * 2010-07-20 2014-12-04 Japan Tobacco Inc. Tablet containing ferric citrate
JP2014501226A (ja) * 2010-12-17 2014-01-20 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング 直接圧縮可能なδ−マンニトールの調製方法
JP2017036280A (ja) * 2010-12-17 2017-02-16 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ 直接圧縮可能なδ−マンニトールの調製方法
JP2013087074A (ja) * 2011-10-17 2013-05-13 Daido Kasei Kogyo Kk 医薬用結合剤及び該結合剤を用いた製剤
JP2014224086A (ja) * 2013-04-22 2014-12-04 テイカ製薬株式会社 口腔内速崩壊性固形製剤用組成物
JP2015063521A (ja) * 2013-09-02 2015-04-09 科研製薬株式会社 高い薬物含有率を有する錠剤及びその製造方法
JP6188183B1 (ja) * 2016-05-23 2017-08-30 大原薬品工業株式会社 薬物高含有圧縮錠剤の安定な製造方法
JP2017210470A (ja) * 2016-05-23 2017-11-30 大原薬品工業株式会社 薬物高含有圧縮錠剤の安定な製造方法
JP2020169145A (ja) * 2019-04-04 2020-10-15 ニプロ株式会社 アジルサルタンを含有する医薬組成物
JP7322475B2 (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

Also Published As

Publication number Publication date
TW201023850A (en) 2010-07-01
JP5694773B2 (ja) 2015-04-01
JPWO2010038695A1 (ja) 2012-03-01
CN102170912A (zh) 2011-08-31

Similar Documents

Publication Publication Date Title
JP5694773B2 (ja) 圧縮成型製剤およびその製造方法
JP6545839B2 (ja) 口腔内崩壊錠及びその製造方法
Nagar et al. Orally disintegrating tablets: formulation, preparation techniques and evaluation
JP4706785B2 (ja) 経口投与用粒子状医薬組成物
JP5219508B2 (ja) ドロキシドパを含有する安定な錠剤
Pandey et al. Oral disintegrating tablets: a review
JP2009292843A (ja) 固形製剤
WO2009128433A1 (fr) Composition du type film
WO2007119792A1 (fr) Comprimé à délitement rapide obtenu par compression directe à sec
JP2011157348A (ja) 崩壊性高強度球状粒子組成物
JP2006282551A (ja) 口腔内崩壊錠およびその製造方法
Swamivelmanickam et al. Mouth dissolving tablets: an overview
JPH1143429A (ja) 固形製剤
JP4965096B2 (ja) 圧縮成型製剤
JP5614445B2 (ja) 経口投与用粒子状医薬組成物
JPWO2015008825A1 (ja) 口腔内崩壊錠
Kumar et al. Development and characterization of melt-in-mouth tablets of haloperidol by sublimation technique
JP4601271B2 (ja) 圧縮成形製剤およびその製造方法
JP2002308760A (ja) 圧縮成型用組成物及びその利用
TWI762450B (zh) 超高速崩解錠劑及其製造方法
JP5513936B2 (ja) 口腔内崩壊製剤
Kiran et al. Fast dissolving tablet: A Future prospective
JP2010001242A (ja) レバミピド固形製剤及びその製造方法
JP2012197245A (ja) 新規な口腔内崩壊錠
JP2010159289A (ja) 圧縮成形製剤およびその製造方法

Legal Events

Date Code Title Description
WWE Wipo information: entry into national phase

Ref document number: 200980138767.8

Country of ref document: CN

121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 09817728

Country of ref document: EP

Kind code of ref document: A1

WWE Wipo information: entry into national phase

Ref document number: 2010531841

Country of ref document: JP

NENP Non-entry into the national phase

Ref country code: DE

122 Ep: pct application non-entry in european phase

Ref document number: 09817728

Country of ref document: EP

Kind code of ref document: A1