WO2013123623A1 - Comprimé se désintégrant oralement et son procédé de préparation - Google Patents

Comprimé se désintégrant oralement et son procédé de préparation Download PDF

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Publication number
WO2013123623A1
WO2013123623A1 PCT/CN2012/000239 CN2012000239W WO2013123623A1 WO 2013123623 A1 WO2013123623 A1 WO 2013123623A1 CN 2012000239 W CN2012000239 W CN 2012000239W WO 2013123623 A1 WO2013123623 A1 WO 2013123623A1
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Prior art keywords
weight
orally disintegrating
tablet
preparation
prescriptions
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PCT/CN2012/000239
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English (en)
Chinese (zh)
Inventor
王丛威
王洪飞
刘荣
周立运
Original Assignee
量子高科（北京）研究院有限公司
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Priority to PCT/CN2012/000239 priority Critical patent/WO2013123623A1/fr
Priority to CN201280046054.0A priority patent/CN103889406A/zh
Priority to KR1020137030665A priority patent/KR20140122650A/ko
Publication of WO2013123623A1 publication Critical patent/WO2013123623A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73—Polysaccharides
    • 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
    • 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
    • A61K47/42—Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/0216—Solid or semisolid forms
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • 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
    • 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
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61J—CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
    • A61J3/00—Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
    • A61J3/10—Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of compressed tablets
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/10—General cosmetic use
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
    • A61K2800/22—Gas releasing
    • A61K2800/222—Effervescent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
    • A61K2800/92—Oral administration

Definitions

  • the present invention relates to an orally disintegrating tablet: a method for preparing the same, and particularly to an orally disintegrating tablet comprising a two component as a binder and a method for preparing the same.
  • Orally disintegrating tablets, or orally dissolving tablets are preparations that rapidly disintegrate or dissolve in the oral cavity. Such preparations can rapidly disintegrate and dissolve in the mouth when they encounter saliva, and can be taken without water. Oral disintegration preparations emerged in the late 1970s, and Gregory et al. used freeze-drying techniques to create high-porosity pharmaceutical dosage forms that disintegrated after oral exposure to saliva.
  • Oral disintegration preparations are mainly suitable for the following situations: children, the elderly, patients in bed position and water shortage conditions; patients with dysphagia (such as esophageal cancer), such as antiemetic drug ondansetron, ramosetron hydrochloride Etc.; patients who do not take the initiative or do not cooperate, such as anti-depressant rizatriptan benzoate, zolmitriptan, etc.; drugs that need to increase contact area or reduce gastrointestinal irritation, such as aspirin, ibuprofen Etc.; a first-aid drug that can be absorbed through the oral mucosa or a drug that must be activated quickly, such as nitroglycerin, nifedipine, salbutamol sulfate, and the like.
  • dysphagia such as esophageal cancer
  • antiemetic drug ondansetron ramosetron hydrochloride Etc.
  • patients who do not take the initiative or do not cooperate
  • Orally disintegrating tablets are especially suitable for infants, throat diseases, Parkinson's disease, AIDS, thyroid gland, head and neck radiotherapy, migraine, mental disorders, cerebral palsy, renal failure and other patients with long-term bed rest. If there are dozens of such varieties listed in various countries. China National Food and Drug Administration has adopted orally disintegrating tablets as a new dosage form, and the National Drug Evaluation Center has accepted more than 300 applications for this variety, and the market is growing rapidly.
  • the preparation method of the orally disintegrating preparation includes a direct compression method in addition to the freeze-drying method, and the direct compression method adopts gelatin as a binder, sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, The croscarmellose sodium, the cross-linked polyvinylpyrrolidone, and the like are used as a disintegrating agent, and a small amount of an effervescent agent, a disintegrant, a flavoring agent, and a lubricant are added, and the tablet is directly compressed at a small pressure.
  • the method has simple process equipment and short production cycle.
  • the orally disintegrating preparations currently on the market are prepared by the technique, but the preparation is rapidly disintegrated in the oral cavity mainly by using a disintegrating agent.
  • the orally disintegrating preparation prepared by this method disintegrates into the oral cavity of the patient, and since the disintegrating agent only disintegrates into small particles, there is often a feeling of grit.
  • the freeze-drying method since the disintegrant is not used and the auxiliary materials used are all water-soluble, the principle of disintegration is the multi-void property left by the solvent drying in the preparation.
  • the drug and the auxiliary material can be quickly and completely dispersed in the saliva, thereby overcoming the defect of the squeegee of the orally disintegrating agent prepared by the direct compression method in the oral cavity, so in the long-term perspective,
  • the method for preparing an orally disintegrating preparation has a very broad market prospect.
  • the tablet Since the orally disintegrating tablet is prepared by the freeze-drying preparation process, the tablet is molded by liquid injection molding, and is formed by pre-freezing the fixed volume of the matrix liquid after the injection of the orally disintegrating tablet, and then freeze-drying.
  • the volume of the orally disintegrating tablet is basically the same as the volume of the injection-type elbow stromal fluid. "The volume of the matrix fluid is converted into the volume of the tablet, and the volume after the conversion is used to characterize the solid volume of the orally disintegrating tablet.
  • the volume of the orally disintegrating tablet is the same, and therefore, the drug loading amount of the orally disintegrating tablet drug prepared by the freezing process is expressed by the ratio of the drug to the tablet volume.
  • the orally disintegrating preparation is prepared by freeze-drying method, and for the slightly soluble, slightly soluble, very slightly dissolved, almost insoluble or insoluble drugs (Chinese Pharmacopoeia 2010 edition stipulates that slightly soluble lg solute is soluble in 30 ⁇ less than 100ml Solvent, slightly soluble refers to lg Solute dissolved in 100 ⁇ less than 1000ml solvent; very slightly soluble means lg solute dissolved in 1000 ⁇ less than 10000ml solvent, almost insoluble or insoluble means lg solute can not be completely dissolved in 10000ml solvent, only suitable for preparation of drugs containing small doses
  • the freeze-dried tablets that is, the ratio of the weight of the pharmaceutically active ingredient contained in each lyophilized tablet to the volume of the lyophilized tablet is less than 62.5 mg/cm 3 .
  • the injection volume in the preparation process is increased from 0.4 ml to 1.0 ml or more, and accordingly, in order to maintain the appearance structure and morphology of the lyophilized sheet, it is also necessary to increase the auxiliary materials such as the skeleton support agent and the binder. Dosage. But the increase in the volume of drugs, one is not conducive to the patient swallow the drug, bringing the convenience of medication; the second is to increase the volume of drugs s will bring a corresponding increase in materials, resulting in increased production costs, for example, when tablets If the volume is doubled, the amount of the corresponding auxiliary compound will be doubled. The cost of the medicine will be increased by 3 ⁇ 4 30% ⁇ 50% in addition to the cost of the process.
  • the volume of the drug will increase, which will cause the packaging volume to become larger. Conveniently, this can seriously impair the inherent advantages of the ease of carrying the orally disintegrating tablet.
  • the fourth is that even if the orally disintegrating tablet prepared by the method is used, the solution to the problem is that the ratio of the weight of the pharmaceutically active ingredient in the prepared lyophilized tablet to the volume of the lyophilized tablet is less than 62.5 mg/cm 3 , which is not
  • the solution of the lyophilized tablet has a ratio of the weight of the pharmaceutically active ingredient to the lyophilized tablet volume of the lyophilized tablet of more than 62.5 mg/cm 3 , which is difficult to disintegrate and incompletely dissolve.
  • a disintegrating agent is added to the formulation, and the orally disintegrating tablet is prepared by a dry pressing method.
  • the method cannot be applied to the orally disintegrating tablet prepared by the lyophilization method due to the difference in the preparation process.
  • 3 ⁇ 4 grid is 20mg/tablet, which is a technical bottleneck in the development of frozen-type orally disintegrating tablets due to the limitation of the drug loading of the active ingredient. Therefore, how to realize the lyophilized oral cavity and the large-dose drug-loading of the disintegrating tablet without changing or reducing the volume of the tablet has become an urgent technical problem to be solved.
  • the technical problem to be solved by the present invention is to provide a pharmaceutical excipient combination of an excellent lyophilized orally disintegrating tablet.
  • the application of the specific excipient combination can solve the bottleneck of large drug loading in the lyophilized orally disintegrating tablet, which is slightly soluble, slightly soluble, very slightly soluble, almost insoluble or insoluble, and has good practical application value.
  • the inventors of the present invention have conducted long-term research and experimental exploration, and after extensive experiments, it was found that gelatin and pullulan can make up for their respective shortcomings. On this basis, "the inventor carried out a multi-round drainage test using gelatin or other auxiliary binders and the amount and addition method of pullulan. Finally, it was found that the addition of the pullulan and the dosage were successfully prepared.
  • a large-dose orally disintegrating tablet with good disintegration and dissolution effect plays a very important role, and has been successfully developed by using a specific amount of pullulan and a specific amount of auxiliary binder as a binder.
  • the orally disintegrating tablet has a large drug loading, rapid disintegration, and complete dissolution.
  • the orally disintegrating tablet prepared by the freeze-drying process is expressed by the ratio of the drug to the tablet volume. This representation is the most scientific representation of the inventor after extensive experimentation, research and discussion. Since the solid volume of the orally disintegrating tablet prepared by the freeze-drying method is substantially the same as the volume of the injection volume of the matrix liquid, when the volume of the tablet is constant, the drug loading amount is about the drug active ingredient contained in the unit volume. The greater the weight, when the unit volume of Chinese medicine When the weight of the active ingredient exceeds a certain value, it is difficult to prepare an orally disintegrating tablet which is rapidly disintegrated and completely dissolved by a conventional prescription, and the present invention can be used to prepare a qualified PJ air-disintegrating tablet.
  • the orally disintegrating tablet according to the present invention comprises a dose of a drug's active ingredient, a skeleton support agent, a binder and a suspending agent, which may further comprise a sweetener and a fragrance for carrying out a chocolate.
  • the binder can be prepared when the binder comprises 0.16% to 5.98% by weight of the pullulan and 0.88% to 40.13% by weight of the auxiliary binder. Rapid disintegration, dissolution of the pharmaceutically active ingredient fully with the freeze-dried sheet weight ratio of volume 'chamber 62.5mg / cm 3 ⁇ 500mg / cm 3 disintegrating tablet.
  • the unit used is mg/cm 3 , which represents the ratio of the weight of the pharmaceutically active ingredient to the volume of the solid tf sheet in the orally disintegrating tablet.
  • the binder preferably comprises 0.27% to 2.60% by weight of the tablet, and the auxiliary binder preferably accounts for 0.90% to 15.0% by weight of the tablet.
  • the weight percentage of the pullulan in the tablet is 0.28% to 3,42%, Preferably, it is 0.48% to 1.58%, and the auxiliary binder accounts for 1.56 26.72% by weight of the tablet, preferably 1.65% to 9.49%.
  • the weight percentage of said pullulan weight of the tablet is 0.16% ⁇ 1.84%, preferably 0.27% ⁇ 0.88%
  • the auxiliary binder accounts for 0.88% ⁇ 16.02% by weight of the tablet weight, preferably 0.90% ⁇ 5.45%.
  • the weight ratio of pullulan and binder in the binder has a great significance for successfully preparing a large drug-loading lyophilized tablet with a fast disintegration rate and complete dissolution, preferably pullulan and auxiliary bonding.
  • the weight ratio of the agent is 1:1 ⁇ 1:2, 1:3.3-1:5 3 ⁇ 4 1 :6.4-1 :10, more preferably 1:2, 1:3.3, 1:5, 1:6.4 or 1 : 10.
  • the ratio of the pullulan weight to the disintegrating tablet volume in the binder is 1 mg/cm 3 to 5 mg/cm 3 , preferably 1.5 mg/ Cm 3 ⁇ 2.5mg cm 3 ;
  • the ratio of the weight of the auxiliary binder in the binder to the volume of the disintegrating sheet is 5 mg/cm 3 to 50 mg/cm 3 , preferably 5 mg/cm 3 to 16 mg/cm 3 .
  • the auxiliary binder may be selected from, but not limited to, one or more of the following materials: ethyl methyl cellulose, ethyl cellulose, chitin, chitosan, methyl cellulose, celery gum, he Latex, Indian gum, Kappa, red algae, scutellaria, gum arabic, peach gum, maltitol, carrageenan, tamarind gum, invert sugar, fructose, karaya gum, modified starch, moor Lomsham, alginic acid, sodium alginate, pregelatinized starch, hydrolyzed gelatin and dextran, of which gelatin, hydrolyzed gelatin and sodium alginate are preferred.
  • the skeleton support agent is selected from one or more of the following materials: glycine, serine, arginine, mannitol, sorbitol, maltitol, xylitol, lactitol, erythritol, iso Maltitol, xylose, raffinose, maltose, glucose, galactose; trehalose, dextrin, propyl cyclodextrin, sodium phosphate, sodium chloride, aluminum silicate, preferably mannitol and glycine.
  • the content of the skeleton support agent is '1.93% to 41.81%, preferably 4.51% to 33.30% by weight.
  • the suspending agent is selected from one or more of the following raw materials: chitin, chitosan, celery gum, tara gum, gum arabic, red algae gum, scutellaria gum red saras gum, Luo Zizi gum, karaya gum, modified starch, sea Alginic acid, propylene glycol alginate, sodium alginate, hydroxyethyl methylcellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, dextran, polyvinyl alcohol, xanthan gum, konjac gum, arab Glue, seaweed gum, guar gum, agar, hydroxymethylcellulose, ethylhydroxyethylcellulose, methylcellulose, kappain, carrageenan, pectin, locust bean gum, polyvinylpyrrole Anthrone, sodium carboxymethylcellulose, dextrin, preferably xanthan gum.
  • the weight percentage of the suspension to the weight of the tablet is from 0.02% to 1.2
  • a freeze-drying method comprises the following steps: (a) preparation of a matrix solution: adding a pharmaceutically active ingredient, a skeleton support agent, a binder and other excipients to a fully dissolved suspending solvent solvent to form a matrix liquid; (b) degassing : degassing the substrate solution prepared in the above step (a); (c) injection molding - injecting the degassed substrate liquid in step (b) into the mold in one volume; (d) pre-freezing: The mold with the substrate liquid in the step (C) is pre-frozen; (e) Freeze-drying: The preparation obtained in (d) is freeze-dried to remove the solvent.
  • the solvent is water or a volatile organic solvent, preferably water, intoxication, ethanol, acetone, ethyl acetate or dimethyl sulfoxide.
  • the injection volume in the step (c) is 0.1 to 2.0 ml, preferably 0.4 ml.
  • the main drug involved in the present invention is not particularly limited, and is particularly suitable for a slightly soluble, slightly soluble, very slightly soluble, almost insoluble or insoluble drug, and may be selected from, but not limited to, one of the following drugs or a combination of several drugs. Things.
  • Antipyretic analgesic anti-inflammatory drugs such as aspirin, diflunisal, salicylate, acetaminophen, indomethacin, ibuprofen, naproxen, ketoprofen, piroxine, sullo, Flurbiprofen, piroxicam, meloxicam, nimesulide, benzbromarone, and the like.
  • Central stimulants such as pemoline, aprefini, piracetam, etc.
  • migraine drugs such as sumatriptan succinate.
  • Analgesics such as rotundin, buprenorphine, pentazocine, naloxone, and the like.
  • Anti-Parkinson's disease and treatment of Alzheimer's drugs such as levodopa, compound carbidopa, compound benserazide, amantadine hydrochloride, piracetil, prolamine, donepezil, huperzine A, and the like.
  • Antipsychotic drugs such as chlorpromazine, isopropyl hydrazine, pethidine, thioridazine, cloprofen, clozapine, sulpiride, tiapride, penfluridol, risperidone, and the like.
  • Anti-epileptic and anti-drugs such as phenytoin, carbamazepine, primidone, gabapentin, lamotrigine, sodium valproate, clonazepam, and the like.
  • Sedative hypnotics such as diazepam, nitrazepam, oxazepam, lorazepam, benzophene, etc.
  • a cholinesterase inhibitor such as scopolamine.
  • Antiarrhythmic drugs such as propionate, dexamethasone, ethiazine, phenytoin, propafenone, amiodarone, and the like.
  • Anti-angina and anti-atherosclerosis drugs such as propranolol, nifedipine, gemfibrozil, bezafibrate, lovastatin, simvastatin, pravastatin and the like. ':
  • Antihypertensive drugs such as enalapril, captopril, hydrochlorothiazide, and amlodipine.
  • Adrenal receptor blockers such as acebutolol, aplol, and the like.
  • Corticosteroids such as betamethasone, cortisone acetate, and the like.
  • Antidiabetic drugs such as repaglinide.
  • Antithyroid drugs such as propylthiouracil, carbimabazole, methimazole and the like.
  • Antihistamines such as cetirizine hydrochloride, loratadine, and the like.
  • Autoactive substances such as denoprostone, alprostadil, betahistine and the like.
  • Digestive system medications such as butyl bromide, granisetron hydrochloride, and the like.
  • Blood system drugs such as EPO, adenosine cobalamin, etc.
  • Urinary system drugs such as azosemide, furosemide, etc.
  • Reproductive system drugs such as estrogen, nandrolone phenylpropionate, etc.
  • Antiparasitic drugs such as albendazole, canbendazole and the like.
  • Antineoplastic agents such as aminoglutethimide, ampicillin, and the like. .
  • Antimicrobial agents such as ampicillin, benzylicillin sodium, and the like.
  • Antibiotics such as amoxicillin, cephalexin, cefprozil, cefuroxime axetil, roxithromycin, erythromycin ethylsuccinate, josamycin, and the like.
  • Traditional Chinese medicine active ingredients such as: breviscapine, artemisinin and so on.
  • Single-flavored Chinese herbal extracts such as: tanshinone, salvianolic acid, etc.
  • Compound Chinese herbal extracts such as: Compound Danshen Dripping Pill Extract, Niuhuang Shangqing Pill Compound Extract, etc.
  • the invention solves the problem that the prepared drug-distributing orally disintegrating tablet does not disintegrate, the disintegration rate is greatly improved, and the disintegration is within 35s.
  • the problem of incomplete dissolution of the large drug-loaded orally disintegrating tablet prepared by the prior art is solved, the dissolution rate is greatly improved, and the dissolution is complete, and the corresponding quality standard stipulated by the pharmacopoeia is met.
  • the lyophilized disintegrating tablet prepared by the present invention is not limited to an oral agent for releasing active activity in the oral cavity, and can also be applied to other body cavities such as the rectum, the vagina, the nose, the eye, and the like; Limited to applications in human medicine, it can also be widely used in cosmetics, health products, food, animal drugs. detailed description
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the disintegration effect and dissolution rate of the prepared orally disintegrating tablet are the same as the injection volume of 0.4ml.
  • the pieces are the same.
  • the ratio of the main dose/freeze tablet volume is equal to the mass of the drug active in each tablet into a distribution of 25 mg, divided by the volume of the tablet 0.4 cm 3 equal to 62.5 mg/cm 3 .
  • the following Example 3 was prepared by the method of this example, and the content calculation was also the same as this example. "
  • the pharmaceutically active ingredient is replaced by ibuprofen to the same weight of nimesulide, acetaminophen, roxithromycin, cefuroxime axetil, sumatriptan succinate, topiramate, lamotrigine, Tomoxetine, duloxetine hydrochloride, pioglitazone hydrochloride, atorvastatin, fenofibrate, valsartan, olmesartan medoxomil, irbesartan, carvedilol, quetiapine fumarate, Esomeprazole magnesium, lansoprazole, sildenafil citrate, atazanavir sulfate, raloxifene, erlotinib hydrochloride, ritonavir, darunavir, malate Tinib, telbivudine, capecitabine, gefitinib, imatinib mesylate, dipy
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the lyophilized tablet account for the weight of the components of the matrix solution.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • the preparation method was the same as in Example 1.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet. Each component accounts for the matrix fluid component.
  • the preparation method was the same as in Example 1.
  • the preparation method was the same as in Example 1.
  • the components account for the lyophilized tablet.
  • the components of the matrix component are the component weight / g.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below (
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • Each component accounts for the matrix component.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • 3 ⁇ 4r component accounts for lyophilized tablets. Each component accounts for the matrix component.
  • Ibuprofen weight / lyophilized tablet volume (mg / C m 3 ) : 125
  • the preparation method is the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below (
  • the preparation method was the same as in Example 1.
  • each component comprises freeze-dried tablets each component comprises a liquid matrix component Ingredient Weight / g
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method is the same as in the first embodiment.
  • Example 39 Each component occupies a lyophilized tablet. Each component accounts for the matrix component. Component weight / g
  • Ibuprofen weight / lyophilized tablet volume (mg / cm 3 ); t 62.5
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix account for the composition of the substrate.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Oral disintegration tablets were prepared according to the prescriptions in the table below.
  • each component accounts for lyophilized 'tables, each component accounts for the weight of the matrix component
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below. Each component accounts for the weight of each component of the lyophilized tablet.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the table below.
  • Each component accounts for frozen tablets.
  • Each component accounts for the weight of the matrix component.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component occupies the lyophilized sheet. Each component accounts for the matrix fluid component component weight / g
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet. Each component accounts for the matrix fluid component.
  • the preparation method is the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below. 3 ⁇ 4'
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below. '
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below. Each component accounts for the weight of each component of the lyophilized tablet
  • the volume is reduced to 200ml by water. Finally made 500 pieces.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below. '
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below. , '
  • the components account for the lyophilized tablets.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Lo components account for lyophilized tablets. ⁇ % of substrate fluid component component weight / g
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the components account for the lyophilized sheet.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below ( Each component accounts for the weight of each component of the lyophilized tablet.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Example 91 The preparation method was the same as in Example 1.
  • Example 91 The preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for frozen tablets.
  • Each component accounts for the weight of the matrix component.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the components account for the lyophilized tablet.
  • the components of the matrix component are the component weight / g.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the components account for the lyophilized tablet.
  • the components of the matrix component are the component weight / g.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each of the components of the lyophilized component comprises a liquid matrix tablets of ancient Component Ingredient Weight / g
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Oral ffl solution was prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below. Each component accounts for the weight of each component of the lyophilized tablet.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Example 111 The preparation method was the same as in Example 1.
  • Example 111 The preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • Each component accounts for the component of the matrix fluid component.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the components account for the lyophilized tablets.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for frozen tablets.
  • Each component accounts for the weight of the matrix component.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the components account for the lyophilized tablet.
  • the components of the matrix component are the component weight / g.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below. Each component accounts for the weight of each component of the frozen liquid component of the matrix liquid component / g
  • Mint Flavor 0.10 0.60 0.05 Finally, the volume is made up to 200ml from water. Finally made 500 pieces.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below. - Each component occupies the lyophilized sheet. Each component occupies the matrix fluid component. Component weight / g
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Components account for lyophilized tablets. Component components account for substrate fluid component component weight / g
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the component weight of the component.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for lyophilized tablet.
  • the components of the lyophilized tablet account for the weight of the matrix component.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the volume is reduced to 200ml by water. Finally made 500 pieces.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the components account for the lyophilized tablet.
  • the components of the matrix component are the component weight / g.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets prepared according to the prescriptions in the table below ⁇ Each component accounts for the weight of each component of the lyophilized tablet.
  • Mint essence 0.10 0.47 0.05 ⁇ After the volume is reduced to 200ml by water. Finally made 500 pieces.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Example 151 The preparation method was the same as in Example 1.
  • Example 151 The preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the components account for the lyophilized tablet.
  • the components of the matrix component are the component weight / g.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for a thousand pieces of frozen components, and each component accounts for the weight of the components of the matrix liquid component /g
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below. .
  • each component accounts for a thousand pieces of frozen components, each component accounts for the component of the matrix liquid component weight / g
  • the preparation method was the same as in Example 1.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below. Each component accounts for the weight of each component of the lyophilized tablet.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet. Each component accounts for the matrix fluid component.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below. - ⁇
  • Each component accounts for the lyophilized tablet.
  • Each component of the ancient matrix liquid component component weight / g
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the components account for the lyophilized tablet.
  • the components of the matrix component are the component weight / g.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the weight of each component of the lyophilized tablet per component of the matrix liquid component / g;
  • 3 i is made up to 200ml from water. Finally made 500 pieces.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below. ;
  • the preparation component accounts for the lyophilized tablet.
  • the components of the matrix component are the component weight / g
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below. ' ⁇ Each component accounts for the weight of each component of the lyophilized tablet
  • the preparation method was the same as in Example 1.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the lyophilized tablet.
  • the components of the matrix component are the weight of the components.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • EXAMPLES 196 Each component occupies a lyophilized tablet. Each component accounts for the matrix component. Component weight / g
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Components account for lyophilized tablets. Component components account for substrate fluid component component weight / g
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • Each component accounts for the weight of the components of the matrix liquid component per lyophilized tablet.
  • the preparation method was the same as in Example 1.
  • Orally disintegrating tablets were prepared according to the prescriptions in the table below.
  • the preparation method was the same as in Example 1.

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Abstract

L'invention concerne un comprimé se désintégrant oralement et un procédé de lyophilisation pour sa préparation. Le comprimé se désintégrant oralement comprend une quantité efficace de principes actifs, d'agents de support du squelette, d'agents adhésifs et d'agents de mise en suspension, les agents adhésifs étant constitués de pullulane et d'agent adhésif auxiliaire. Par l'utilisation d'une quantité spécifique de la combinaison de pullulane et d'agent adhésif auxiliaire, l'invention a résolu les problèmes de désintégration lente et de dissolution incomplète de comprimé se désintégrant oralement lors de la présence d'une charge élevée de principes actifs.
PCT/CN2012/000239 2012-02-24 2012-02-24 Comprimé se désintégrant oralement et son procédé de préparation WO2013123623A1 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
PCT/CN2012/000239 WO2013123623A1 (fr) 2012-02-24 2012-02-24 Comprimé se désintégrant oralement et son procédé de préparation
CN201280046054.0A CN103889406A (zh) 2012-02-24 2012-02-24 一种口腔崩解片及其制备方法
KR1020137030665A KR20140122650A (ko) 2012-02-24 2012-02-24 경구 분해 정제 및 이의 제조 방법

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CN103976974A (zh) * 2014-06-11 2014-08-13 青岛双鲸药业有限公司 一种植物性软胶囊的制备方法
CN104873443A (zh) * 2015-06-25 2015-09-02 湖南一九生物科技有限公司 一种sod护肤品及制备方法
CN105476968A (zh) * 2015-12-18 2016-04-13 北京万全德众医药生物技术有限公司 一种盐酸雷洛昔芬口腔崩解片及其制备方法
CN110664621A (zh) * 2019-11-15 2020-01-10 重庆登康口腔护理用品股份有限公司 一种冻干口腔护理用品的制备方法
CN110755298A (zh) * 2019-11-15 2020-02-07 重庆登康口腔护理用品股份有限公司 一种冻干口腔护理组合物及其应用
US11319566B2 (en) 2017-04-14 2022-05-03 Capsugel Belgium Nv Process for making pullulan
US11576870B2 (en) 2017-04-14 2023-02-14 Capsugel Belgium Nv Pullulan capsules
CN115990140A (zh) * 2023-02-15 2023-04-21 北京悦康科创医药科技股份有限公司 一种那非类化合物冻干片及其制备方法

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CN102614138A (zh) * 2011-01-26 2012-08-01 量子高科（北京）研究院有限公司 一种口腔崩解片及其制备方法

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CN103976974A (zh) * 2014-06-11 2014-08-13 青岛双鲸药业有限公司 一种植物性软胶囊的制备方法
CN104873443A (zh) * 2015-06-25 2015-09-02 湖南一九生物科技有限公司 一种sod护肤品及制备方法
CN105476968A (zh) * 2015-12-18 2016-04-13 北京万全德众医药生物技术有限公司 一种盐酸雷洛昔芬口腔崩解片及其制备方法
US11319566B2 (en) 2017-04-14 2022-05-03 Capsugel Belgium Nv Process for making pullulan
US11576870B2 (en) 2017-04-14 2023-02-14 Capsugel Belgium Nv Pullulan capsules
US11878079B2 (en) 2017-04-14 2024-01-23 Capsugel Belgium Nv Pullulan capsules
CN110664621A (zh) * 2019-11-15 2020-01-10 重庆登康口腔护理用品股份有限公司 一种冻干口腔护理用品的制备方法
CN110755298A (zh) * 2019-11-15 2020-02-07 重庆登康口腔护理用品股份有限公司 一种冻干口腔护理组合物及其应用
CN115990140A (zh) * 2023-02-15 2023-04-21 北京悦康科创医药科技股份有限公司 一种那非类化合物冻干片及其制备方法

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