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WO2007116916A1 - Préparation médicamenteuse liquide pour administration orale - Google Patents

Préparation médicamenteuse liquide pour administration orale Download PDF

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Publication number
WO2007116916A1
WO2007116916A1 PCT/JP2007/057595 JP2007057595W WO2007116916A1 WO 2007116916 A1 WO2007116916 A1 WO 2007116916A1 JP 2007057595 W JP2007057595 W JP 2007057595W WO 2007116916 A1 WO2007116916 A1 WO 2007116916A1
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WO
WIPO (PCT)
Prior art keywords
liquid pharmaceutical
liquid
drugs
pharmaceutical preparation
discharge device
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/JP2007/057595
Other languages
English (en)
Japanese (ja)
Inventor
Atsushi Matsuo
Hiroko Iwano
Hiroyuki Matsumura
Takashi Tsuboi
Hiroo Yamasaki
Hironobu Nakagawa
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Kobayashi Pharmaceutical Co Ltd
Original Assignee
Kobayashi Pharmaceutical Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Kobayashi Pharmaceutical Co Ltd filed Critical Kobayashi Pharmaceutical Co Ltd
Publication of WO2007116916A1 publication Critical patent/WO2007116916A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M11/00—Sprayers or atomisers specially adapted for therapeutic purposes
    • A61M11/06—Sprayers or atomisers specially adapted for therapeutic purposes of the injector type
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10—Laxatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/10—Expectorants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/02—Nutrients, e.g. vitamins, minerals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M2210/00—Anatomical parts of the body
    • A61M2210/06—Head
    • A61M2210/0625—Mouth
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M2210/00—Anatomical parts of the body
    • A61M2210/06—Head
    • A61M2210/0625—Mouth
    • A61M2210/0643—Tongue

Definitions

  • Liquid pharmaceutical formulation for oral administration Liquid pharmaceutical formulation for oral administration
  • the present invention relates to a liquid pharmaceutical preparation for oral administration.
  • liquid preparations are promoted as pharmaceuticals and are actually sold.
  • These liquid preparations include, for example, oral drugs for oral administration (for example, Patent Documents 1 to 4), nasal sprays for nasal administration (for example, Patent Document 5), and external drugs for pharyngeal diseases (for example, Patent Document 6).
  • Liquid pharmaceutical preparations for oral administration are commercially available as "internal liquids” and “syrups”!
  • internal liquids and “syrups”!
  • the dose is inaccurate and a separate measuring cup is required for weighing when taking it immediately.
  • measuring the liquid and washing the cup after use is cumbersome and Speak.
  • Patent Document 1 JP-A-8-193023
  • Patent Document 2 Japanese Patent Laid-Open No. 10-265369
  • Patent Document 3 Japanese Patent Laid-Open No. 2000-273050
  • Patent Document 4 Japanese Patent Laid-Open No. 2003-206242
  • Patent Document 5 Japanese Patent Laid-Open No. 11 171762
  • Patent Document 6 JP-A-10-259124
  • An object of the present invention is to provide a liquid pharmaceutical formulation for oral administration that reduces the burden on patients and reduces the burden on patients and enables safe medication.
  • a liquid pharmaceutical preparation for oral administration accommodated in a container provided with a discharge device, which is non-contact from the discharge device on or around the tongue in the oral cavity.
  • the liquid pharmaceutical formulation is provided for administration by direct injection.
  • on or around the tongue includes, for example, dentition, gingiva, sputum, and the floor of the mouth, and by injecting into the area and taking the medicine, liquid droplets of liquid preparations into the trachea and lungs Inflow is prevented and safe oral administration is possible.
  • the liquid pharmaceutical formulation of the present invention is administered by injection onto the tongue.
  • the liquid pharmaceutical preparation of the present invention is a liquid pharmaceutical composition containing a solvent (for example, water, ethanol, glycerin, propylene glycol) that can be used as a component of the pharmaceutical preparation, and includes a solution, a suspension, It may be an emulsion or dispersion.
  • a solvent for example, water, ethanol, glycerin, propylene glycol
  • the liquid pharmaceutical preparation of the present invention may be an aqueous liquid preparation, for example, an aqueous solution.
  • water that can be used in the present invention include, for example, Japanese Pharmacopoeia purified water, and can be contained at a ratio of, for example, 10 to 99% by weight, preferably 45 to 98% by weight, based on the entire preparation.
  • the injection amount from the discharge device by one injection is, for example, 0.03 to 3 mL, preferably 0.1 to 2 mL, more preferably 0.3 to LmL.
  • the particles of the droplets at the time of ejection have a particle diameter that exceeds a certain level in terms of preventing inflow into the trachea and lungs.
  • the particle diameter of the droplet may be, for example, 100 to 5500 111, preferably 100 to 3600 ⁇ m, more preferably 100 to 1600 ⁇ m.
  • the particle size of the droplet can be adjusted by selecting the nozzle of the discharge device, the configuration of the liquid agent flow path near the injection port, or the configuration of the discharge device such as the length of the pushing stroke.
  • the viscosity of the liquid pharmaceutical preparation of the present invention is not particularly limited, but the viewpoint of the rapid delivery of the active ingredient to the absorption site (such as the small intestine) of the active ingredient after the dispensing device force, and 0 8 to 500 cP, preferably 0.9 to: LOOcP, more preferably 1.00 to 50.
  • LOOcP more preferably 1.00 to 50.
  • OcP more preferably 1.00 to 25 cP, and even more preferably 1.00 to 2.5 cP (digital viscosity) (Measured with a UL adapter at 25 ° C using a total DV— DV + (Brookfield)).
  • the active ingredient applicable to the liquid pharmaceutical preparation of the present invention is not particularly limited as long as it is a liquid pharmaceutical preparation for oral administration.
  • an active ingredient as an active ingredient, an antitussive, bronchodilator, expectorant, antiphlogistic, antipyretic analgesic, antihistamine, antibacterial agent, caffeine, gastric mucosal protective agent, neurostimulant, antistimulant, Plasmin drugs, hypnotic sedatives, blood circulation improving drugs, hemostatic drugs, antipruritic drugs, analgesic antispasmodic drugs, stomachic medicines, digestive drugs, live intestinal components, antidiarrheal drugs, anti-constipation drugs, vitamins, nourishing tonics, circulatory organs Selected from medicines, herbal medicines and herbal ingredients
  • an already defined liquid pharmaceutical formulation comprising one or more ingredients.
  • the active ingredient is codine phosphate, dihydrocodine phosphate, dextromethorphan hydrobromide, dl-methylephedrine hydrochloride, guaifenesin, potassium guaiacol sulfonate, lysozyme chloride, malein
  • an already defined liquid pharmaceutical formulation further comprising one or more selected from acid chlorfelamin and anhydrous caffeine.
  • a liquid pharmaceutical preparation for oral administration which contains one or more selected from codine phosphate and dihydrocodein phosphate as an active ingredient and is contained in a container equipped with a discharge device
  • the liquid pharmaceutical preparation is provided by being directly injected in a non-contact manner onto or around the tongue in the oral cavity.
  • the liquid pharmaceutical preparation of the present invention includes, for example, as an additional active ingredient, bronchodilators, expectorants, antiphlogistics, antipyretic analgesics, antihistamines, bactericides, caffeine, gastric mucosa protective agents. It may contain one or more selected from herbal ingredients and antitussives and vitamins.
  • the liquid pharmaceutical formulation of the present invention comprises dl-methylephedrine hydrochloride, guaifenesin, potassium guaiacol sulfonate, lysozyme chloride, chlorfelamine maleate, and anhydrous caffeine as additional active ingredients.
  • dl-methylephedrine hydrochloride guaifenesin, potassium guaiacol sulfonate, lysozyme chloride, chlorfelamine maleate, and anhydrous caffeine as additional active ingredients.
  • an already defined liquid pharmaceutical formulation comprising one or more flavoring or sweetening agents.
  • the corrigent or sweetener comprises amatya, reduced maltose starch, glycine, dipotassium glycyrrhizinate, disodium glycyrrhizinate, monoammonium glycyrrhizinate, fructose sugar, glucose water White sucrose granules, honey, simple syrup, lactose, glucose, maltose, maltose, man-toll, starch, sorbitol, caramel, aspartame, stevia extract, kanzo , Licorice extract, xylitol, brown sugar, liquid sugar, fructose, fructose glucose liquid sugar, saccharin
  • Saccharin sodium, sucrose, glycerin power may also be selected.
  • the masking agent is used in the present invention from the viewpoint of masking unpleasant taste derived from the active ingredient and preventing the generation of solids when the product is stored for a long period of time.
  • Sweeteners' flavoring agents are selected, for example, asunameme, saccharin sodium power 1 or more; stevia, caramel, kanzo power 1 or more selected; and sugar alcohol (sorbitol, maltose, maltose, mannitol, xylitol), glycerin One or more combinations selected from may be used.
  • the antitussive agent includes, for example, codine phosphate, dihydrocodine phosphate, hydrocodone, hydromorphone, methadone, morphine, oximetebanol, aloclamide hydrochloride, cloperastine hydrochloride, pentoxyberine citrate, ken Tipepidine acid, dibutanato sodium, dextromethorphan hydrobromide, dextromethorphan phenol phthalic acid, tipepidine hibenzate, cloperastine fendizoate, nospin, maou, nantenjit, clofedanol, levopropoxy
  • One or more force-selected ones such as phen, hominoben, oxerazine, pentoxyberine, benproberine, dimemorphane, dibutate, eprazinone, carbetapentane and isoamyl can be used.
  • the antitussive agent is codin phosphate, dihydrocodine phosphate, aloclamide hydrochloride, cloperastine hydrochloride, pentoxyberine citrate, tipepidine citrate, sodium dibutate, dextromethorphan hydrobromide, One or more selected from dextromethorphan phenol phthalic acid, tipepidine hibenzate, cloperastine fendizoate, noss force pin, maou and nantenji can be used.
  • examples of bronchodilators include ex-adrenergic receptor stimulators.
  • ⁇ -adrenergic receptor stimulators e.g., trimethquinol hydrochloride, methoxyphenamine hydrochloride
  • Dl-methylephedrine hydrochloride tyramine, ephedrine, methylephedrine saccharinate, amphetamine, methamphetamine, methoxyphenamine, orciprenaline, chlorprenalin, isoproterenol, donomine, dobutamine, isoprenaline, salbutamol, terbutaline, hex Soprenalin, allobuteronole, fenoteronore, pro force tellonore, pinolebuteronore, talenbuteronore,
  • ⁇ -adrenergic receptor stimulators e.g., trimethquinol hydrochloride, methoxyphenamine hydrochloride
  • tyramine ephedrine
  • methylephedrine saccharinate amphe
  • bronchodilators include ⁇ -adrenergic receptor stimulants (eg, trimethquinol hydrochloride, methoxyphenamine hydrochloride, methylephedrine hydrochloride) and xanthine derivatives (eg, aminophylline, diprofylline, theophylline, proxyphylline).
  • ⁇ -adrenergic receptor stimulants eg, trimethquinol hydrochloride, methoxyphenamine hydrochloride, methylephedrine hydrochloride
  • xanthine derivatives eg, aminophylline, diprofylline, theophylline, proxyphylline.
  • One or more can be used.
  • the expectorants include, for example, ammonium chloride, 1 menthol, ammonia, wikial, lysozyme chloride, ethyl cystine hydrochloride, methyl cystine hydrochloride, potassium guaiacol sulfonate, guaifenesin, crezo-one.
  • One or more selected forces may be used, such as potassium sulfonate, bromhexine hydrochloride, ambroquinol hydrochloride, L carbocystine, and hoodine.
  • the expectorants include salt-molybdenum, 1-menthol, ammonia 'wikial, lysozyme chloride, ethyristine hydrochloride, methylcystine hydrochloride, potassium guaiacol sulfonate, guaifenesin and potassium cresolol sulfonate.
  • One or more selected can be used.
  • the anti-inflammatory agent one or more selected from lysozyme chloride, glycyrrhizic acid, dipotassium glycyrrhizinate, sodium azulene sulfonate and the like can be used.
  • antipyretic analgesic for example, one or more selected from force such as acetaminophen, ibuprofen, aspirin, ethenzamide and the like can be used.
  • the antihistamines include, for example, isothipenzil hydrochloride, iproheptin hydrochloride, dipheterol hydrochloride, diphenylpyrroline hydrochloride, diphenhydramine hydrochloride, triprolidine hydrochloride, triberenamine hydrochloride, tonsylamine hydrochloride, phenetazine hydrochloride, and methazine hydrochloride.
  • Diphenhydramine salicylate carbinoxamine diphenol disulfonate, Almemazine tartrate, diphenhydramine tannate, phenetazine tannate, diferruleline teuroate, promethazine methylene disalicylate, carbinoxamine maleate, dl-chlorfelamine maleate, d-chlorfelamine maleate and phosphoric acid
  • One or more selected forces such as dipheterol can be used.
  • fungicide for example, one or more kinds selected from local fungicides such as salt cetylpyridium, decalyl chloride and chlorhexidine hydrochloride may be used.
  • caffeine for example, one or more selected from powers such as sodium benzoate caffeine, strength fein and anhydrous caffeine can be used.
  • the gastric mucosa protective agent includes, for example, aminoacetic acid, magnesium silicate, synthetic aluminum silicate, synthetic hydrotalcite, magnesium oxide, dihydroxy aluminum, amino acetate, hydroxyaluminum gel, and dry water.
  • One or more selected from the group consisting of a coprecipitation product of magnesium hydroxide and potassium aluminum sulfate, magnesium carbonate and magnesium aluminate metasilicate may be used.
  • the neurostimulant for example, one or more selected from caffeine, anhydrous caffeine, caffeine benzoate and the like can be used.
  • antiplasmin drug for example, one or more selected from tranexamic acid, aminocaproic acid and the like can be used.
  • hypnotic sedative one or more kinds selected from, for example, bromoreryl urea, allyl isopropylacetyl urea, diphenhydramine hydrochloride and the like may be used.
  • the blood circulation improving agent for example, one or more selected from force such as inositol hexanicotinate can be used.
  • hemostatic agent for example, one or more selected from the group consisting of tranexamic acid and sodium carbazochrome sulfonate can be used.
  • antipruritic agent for example, one or more kinds selected from force such as diphedol hydrochloride and scopolamine hydrobromide can be used.
  • analgesic and antispasmodic agent for example, one or more selected from the group consisting of ethyl aminobenzoate, methylbenactidium bromide, butylscopolamine bromide, funnel extract and the like can be used.
  • stomachic medicine for example, one or more selected from powers such as Keihi, Obata, Shokyo, and sempri can be used.
  • the digestive agent for example, one or more selected from the group consisting of ursodesoxycholic acid, fat digestive enzyme, starch digestive enzyme and the like can be used.
  • the live intestinal bacterium component for example, one or more kinds selected from lactic acid bacteria powder, bifidobacteria, butyric acid bacteria powder and the like can be used.
  • an antidiarrheal agent for example, one or more selected from oral peramide hydrochloride, albumin tannate, bismuth subgallate and the like can be used.
  • constipation therapeutic agent for example, one or more kinds of which power is also selected such as sennoside, senna, daio, Brantagovabata seed can be used.
  • the vitamin agent for example, one or more selected from the strengths such as tocopherol acetate, ascorbic acid, thiamine, pyridoxine, cyanobalamine may be used.
  • the nourishing tonic for example, one or more selected from power such as taurine, calcium pantothenate, nicotinamide, etc. can be used.
  • the circulatory organ agent for example, one or more selected by force such as ubidecarenone, carrot, and agate can be used.
  • the traditional Chinese medicine for example, one or more kinds, for which power is selected, such as kakachi, kazuka detoxification water, etc. can be used.
  • herbal medicine components include, for example, ziryu, sansoonin, ohhi, onji, kandu, kikiyou, kiyounin, shazenshi, shazenso, sexan, senega, tokon, baimo, azajak, wiki, ougon, caronin, kehi, go, Gomin, Saishin, Zion, Jiakou, Shajin, Shokiyo, Sohakuhi, Soyo, Chikusenjin, Chin
  • species such as pi, carrots, buttermonds, and roe, can be selected.
  • Examples of combinations of active ingredients in the liquid pharmaceutical preparation of the present invention include the following:
  • Dextromethorphan hydrobromide, guaifenesin and chlorpheniramine maleate Dextromethorphan hydrobromide, guaifenesin and chlorpheniramine maleate.
  • the liquid preparation of the present invention is used as a pharmaceutical for oral administration, and includes, for example, general cold medicine, cough, rhinitis, antipyretic analgesics, gastrointestinal drugs, antidiarrheals, motion sickness preventives or palliatives, etc.
  • a pharmaceutical for oral administration includes, for example, general cold medicine, cough, rhinitis, antipyretic analgesics, gastrointestinal drugs, antidiarrheals, motion sickness preventives or palliatives, etc.
  • Table 1 shows examples of active ingredient prescriptions when the present invention is used as a general cold medicine.
  • the active ingredients shown in Table 1 can be used as a solution in an appropriately selected solvent.
  • liquid pharmaceutical preparation containing the components shown in Table 1 as an active ingredient.
  • the liquid pharmaceutical composition of the present invention comprises, as optional ingredients, a flavoring agent, sweetening agent, preservative, flavoring agent, diluent, solubilizer, PH regulator, viscosity modifier, colorant, stabilizer, It may contain additives such as surfactants, suspension agents, antioxidants, cooling agents, flavoring agents, and fragrances.
  • a liquid pharmaceutical formulation as defined above comprising one or more flavoring or sweetening agents.
  • the corrigent and sweetener used in the present invention are not particularly limited, and for example, the corrigent and sweetener usually used in pharmaceutical preparations can be used.
  • Specific examples of flavoring and sweetening agents include fructose, glucose liquid sugar, sucrose, strength lamella, aspartame, neotame, stevia extract, licorice extract, brown sugar, saccharin sodium, sorbitol, and sugar alcohols (e.g. , Xylitol, erythritol, maltitol and latathitol) and glycerin.
  • one or more, preferably two or more selected from aspartame, neotame, stevia extract, licorice extract, brown sugar, sodium saccharin, caramel and sorbitol can be used as a corrigent or sweetener.
  • the blending amount of the sweetener and the flavoring agent contained in the liquid pharmaceutical preparation of the present invention is, for example, 2 to 95% by weight, preferably 2 to 50% by weight, more preferably 2 to 23% by weight.
  • the daily dose in the liquid preparation of the present invention is not particularly limited, and can be appropriately determined according to the daily dose of the active ingredient contained in the liquid preparation. From the viewpoint of the number of administrations per day and convenience at the time of administration, the daily dose may be, for example, 1.5 to 18 mL, preferably 3.0 to 15 mL, more preferably 6.0 to 9 mL. Good.
  • the single dose in the liquid preparation of the present invention is not particularly limited, and can be appropriately determined according to the daily dose of the active ingredient contained in the liquid preparation, the number of daily doses, and the like. From the viewpoint of the number of administrations per day and safety at the time of taking, it may be, for example, 0.5 to 5 mL, preferably 0.75 to 3 mL, and more preferably 1.0 to 2 mL. According to the present invention, since the ingestion is performed safely and reliably, the necessary amount of the active ingredient can be ingested in a small amount compared with a normal oral liquid pharmaceutical preparation.
  • the liquid pharmaceutical preparation of the present invention has the effect of eliminating complexity at the time of taking and reducing the burden on the patient in frequent administration, the present invention can take two or more times a day. Suitable for such drugs.
  • the number of doses of the liquid pharmaceutical preparation of the present invention is, for example, 1 to 6 times a day, Preferably, it may be 4 to 6 times.
  • the container used in the present invention is not particularly limited as long as it is normally used as a container for a liquid pharmaceutical preparation, and for example, a brown light-shielding glass container or the like may be used.
  • a discharge device that is capable of measuring a dose of a liquid pharmaceutical preparation with a substantially constant discharge amount at one time is used.
  • a device having a function capable of directly injecting a liquid pharmaceutical preparation on or around the tongue in the oral cavity without contact is used.
  • a discharge device that can be used in the present invention is not particularly limited, and a so-called push pump type discharge device, a so-called trigger type discharge device, and the like can be used.
  • the discharge device is a push pump type discharge device.
  • the push pump type discharge device includes, for example, a cylinder suspended in a container, and a stem that has a cylindrical piston at the lower end and is urged upward from the cylinder, By pushing down the stem, the pressure of the liquid stored in the internal space between the upper valve on the stem side and the lower valve on the cylinder side increases, and the liquid passes through the upper valve and is provided above the stem.
  • It may be a discharge device that is discharged from the outlet of the push-down head and configured to suck up the liquid in the container through the lower valve and into the cylinder by raising the stem.
  • the particle size of the liquid droplet at the time of liquid injection can be adjusted by the shape of the flow path of the liquid agent at the jet nozzle.
  • the discharge device in the present invention may be a spray type.
  • the ejection device may be configured such that the ejection port of the ejection device is closed by a valve member, and the ejection port is opened by the movement of the valve member when the medicine is injected. Good.
  • it is accommodated in a container equipped with a push pump type discharge device, and is directly injected in a non-contact manner onto or around the tongue in the oral cavity.
  • a liquid pharmaceutical formulation for oral administration that is already defined, wherein the discharge device is energized by an elastic force so as to occlude the jet port of the liquid pharmaceutical formulation. Sometimes by staking the elastic force and moving
  • the liquid pharmaceutical preparation which is a discharge device including a valve member that opens the spout.
  • Examples of the discharge device in the present invention include a so-called push-bump type discharge device which is widely used.
  • Japanese Utility Model Publication No. 58-9358 Japanese Utility Model Application Publication No. 2-95562, No. 5-13563, JP-A 8-169462, JP-A 9-15 5254, JP-A 2002-326044, JP-A 2001-171764, JP-A 2-004-359242, It is possible to use discharge devices disclosed in Japanese Unexamined Patent Publication Nos. 2004-359241, 2004-359238, 2004-352343, 2004-352333, and the like.
  • the discharge device may be attached to the mouth and neck of the container by fitting, and the fitting may be performed in a manner that makes the fitting difficult to remove.
  • the mating mode is considered to contribute to prevention of breakage of the container during transportation and carrying and prevention of accidental ingestion of the liquid pharmaceutical preparation of the present invention.
  • the fitting portion of the container neck of the container and the mounting cap of the discharge device includes an outer tooth formed on the outer peripheral surface of the container neck of the container forming the inner layer of the fitting portion.
  • the ratchet may be an annular fitting portion configured to prevent rotation in a direction in which the container neck and neck portion and the mounting cap are loosened.
  • the inner teeth and the outer teeth have a shape that allows rotation in the direction in which the screwing of the attachment cap and the container mouth neck is tightened but does not allow rotation in the loosening direction.
  • the tooth surface on the side that contacts and presses when the rotational force in the direction in which the screwing between the mounting cap and the container neck is loosened is perpendicular to the rotational force.
  • the tip of the tooth tip side may be inclined to the forward direction in the direction of the rotational force (or the opposite direction) as compared with the tooth base side.
  • Examples of the discharge device in the present invention include a discharge device having a pressing head described in JP-A-2004-834 (see FIGS. 4 to 7).
  • the pressing head is a pressing head that is attached to a pump in which the stem 2 is erected so that it can be pushed in an upward biased state.
  • the mounting cylinder 8 fitted to the upper end of the stem 2 is suspended from the bottom surface of the top plate 9 and the mounting cylinder member 3 is formed by standing the sliding cylinder 10 communicating with the inside of the stem 2 above the top plate 9;
  • a main body provided with a valve chamber having a spout 21 opened at the tip above the cylinder 16 fitted to the outer periphery of the sliding cylinder 10 so as to be slidable and capable of being pushed down with respect to the mounting cylinder member. 4 and a flow passage extending from the communication port 19 communicating with the inside of the cylinder to the jet port 21 while the rear outer circumference is slidably fitted to the valve chamber circumference, and the jet port 21 is closed in a forward biased state.
  • the upper end is linked to the rear end of the valve member 6 and the rear end of the valve member 6, the lower end is brought into contact with and locked to the upper surface of the top plate 9, and the valve member is pressed when the main body is pressed against the mounting cylinder member And a saddle member 7 pivotally attached to the main body so as to be swingable so as to be pulled out rearward.
  • the valve member 6 biased forward by the coil spring 26 always biases the upper part of the vertical plate portion 28 of the flange member 7 forward, and is mounted by pushing down the main body 4.
  • the top plate 9 of the cylindrical member 3 pushes up the inclined plate portion 29 and rotates the flange member 7, and the valve member portion 6 is pulled out against the front biasing force of the coil spring 26, so that a fluid flow path is secured. It is done.
  • the use of the discharge device including the pressing head described above prevents deterioration due to the chemical solution not coming into contact with the outside air, improves hygiene due to dripping, and improves the quantification of the chemical solution by improving the chemical solution.
  • the viewpoint power is also preferable.
  • a liquid pharmaceutical formulation for oral administration which is contained in a container equipped with the discharge device of the present invention and is administered by direct non-contact injection of the discharge device force on or around the tongue in the oral cavity.
  • the ejection device is biased by an elastic force so as to close the ejection port of the liquid pharmaceutical preparation, and is moved into an elastic state when the liquid pharmaceutical formulation is ejected to move to open the ejection port.
  • the liquid pharmaceutical preparation which is a discharge device including a valve member.
  • the pressing force of the main body against the stem 2 is configured to be smaller than the pressing force of the stem itself.
  • the pressing head is a pressing head that is mounted on a pump in which the stem 2 is erected so that it can be pushed in an upward biased state, and a mounting cylinder 8 that is fitted to the upper end of the stem 2 is attached to the top plate.
  • a mounting cylinder that is suspended from the bottom surface, and is provided with a sliding cylinder 10 that communicates with the inside of the stem 2 erected above the top plate 9 and a locking plate 12 that extends vertically on both sides of the top plate 9
  • the member 3 and the cylinder 16 fitted so as to be able to slide down on the outer periphery of the sliding cylinder 10 are It is suspended from the lower surface of the horizontal tube 15 that is open at the front end of the wall 14a and has a space around it, and engages with the outer surface of the locking plate so that both sides of the inner surface of the peripheral wall 14a cannot rotate and move up and down.
  • Main body 4 a cylindrical jetting member 5 fitted to the horizontal cylinder 15 and having an outlet 21 opened at the tip, and a rear wall 15a of the horizontal cylinder 15 and a seal cylinder 18 projecting from the front surface
  • the outer periphery of the rear part is slidably fitted to the periphery, the outlet 21 is closed in a forward biased state, and a flow path from the communication port 19 communicating with the inside of the cylinder to the outlet 21 is defined.
  • the upper end is linked to the valve member 6 and the rear end portion of the valve member 6 protruding rearward through the window hole 17 of the horizontal cylinder rear wall 15a, and the lower end portion is brought into contact with and locked to the upper surface of the top plate 9 And a collar member pivotally attached to the main body so that the valve member can be pulled out rearward when the main body is pressed against the mounting cylinder member 7 And the pressing resistance of the main body against the stem 2 is smaller than the pressing resistance of the stem itself.
  • the chemical liquid is ejected after opening the spout, which makes it easy to push down the head, and can be reliably ejected to an appropriate part in the oral cavity.
  • the distance between the valve member serving as the flow path and the ejection port is, for example, 0.1 to 1 mm
  • the cross-sectional area of the flow path of the chemical liquid at the time of ejection is, for example, 0.1 to 3.5 mm 2 .
  • the discharge amount of the liquid agent and the cross-sectional area of the flow path can be adjusted, and thereby the flow speed of the discharged chemical liquid and the particle diameter of the droplets can be controlled.
  • the liquid pharmaceutical preparation of the present invention is a liquid preparation having an advantage that a dose measured in a simple and accurate manner can be taken. Furthermore, the preparation of the present invention does not require water and can be safely taken, and is quickly delivered to the active ingredient absorption site after taking to exhibit a desired medicinal effect.
  • a liquid pharmaceutical preparation was prepared based on the following prescription and filled into a container equipped with a push pump type discharge device (with an on-off valve at the spout, SP500LR shut-off nozzle, purchased from Yoshino Kogyo Co., Ltd.).
  • the discharge volume was measured as the volume of chemical liquid (g) discharged at one time, and the volume (mL) of the chemical liquid discharged from the specific gravity (1.05) of the chemical liquid was converted. The results are shown in Table 3.
  • FIG. 1 is a graph showing an example of test results for confirming the drug efficacy of the drug of the present invention as an internal cough solution.
  • FIG. 2 is a graph showing an example of test results for confirming the efficacy of the drug of the present invention as a cough medication solution.
  • FIG. 3 is a cross-sectional view showing a structure for preventing removal of a fitting portion (screwing portion) of a container mouth neck portion and a mounting cap of a discharge device used in the present invention.
  • FIG. 4 is a longitudinal sectional view showing an example of a pressing head used in a discharge device used in the pharmaceutical composition of the present invention.
  • FIG. 5 is a longitudinal sectional view taken along line AA in FIG. 6 is a cross-sectional view taken along line BB in FIG.
  • FIG. 7 is a perspective view of a flange member used in the pressing head.
  • FIG. 8 is a longitudinal sectional view showing another example of the pressing head of the discharge device used in the pharmaceutical composition of the present invention.
  • FIG. 9 is a longitudinal sectional view of FIG.

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Abstract

L'invention vise à fournir une préparation médicamenteuse liquide pour administration orale, qui permette de réduire l'effort de prise de médicament afin de ménager le patient et de rendre la prise de médicament sûre. A cet effet, une préparation médicamenteuse liquide pour administration orale est conditionnée dans un contenant muni d'une unité de distribution et est administrée par passage direct de l'unité de distribution sur la langue ou à proximité de la langue dans la cavité buccale, et ce sans aucun contact.
PCT/JP2007/057595 2006-04-04 2007-04-04 Préparation médicamenteuse liquide pour administration orale Ceased WO2007116916A1 (fr)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102670819A (zh) * 2012-05-15 2012-09-19 张方元 一种治疗感冒的药物组合物

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Publication number Priority date Publication date Assignee Title
JP2013058650A (ja) 2011-09-09 2013-03-28 Renesas Electronics Corp 半導体装置
CN102657830A (zh) * 2012-05-08 2012-09-12 鲍旭刚 一种治疗小儿腹泻的药物及其制备方法

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JPH0578237U (ja) * 1992-03-31 1993-10-26 日本化薬株式会社 医薬用容器
JPH0956820A (ja) * 1995-08-21 1997-03-04 Toshihiro Handa 噴霧量を可変調整できる携帯用容器及びこの容器に充填して効果を発揮できる薬学、栄養学的組成物
JPH10167944A (ja) * 1996-12-12 1998-06-23 Kao Corp 口腔用組成物
JP2000273051A (ja) * 1999-03-19 2000-10-03 Kobayashi Pharmaceut Co Ltd 苦みがマスキングされた液状製剤
JP2003020058A (ja) * 2001-06-20 2003-01-21 Park Pangon 液体定量投入容器（Ｑｕａｎｔｉｆｙｉｎｇａｎｄｄｉｓｐｅｎｓｉｎｇａｐｐａｒａｔｕｓｆｏｒｌｉｑｕｉｄ）
JP2003081846A (ja) * 2001-09-11 2003-03-19 Nippon Tenganyaku Kenkyusho:Kk 液状鎮咳去痰薬
JP2004000834A (ja) * 2002-05-31 2004-01-08 Yoshino Kogyosho Co Ltd ポンプの押下ヘッド
JP2005532235A (ja) * 2002-07-11 2005-10-27 レミンタン、ヘルス、プラダクツ、エルエルシー 液体栄養補給剤を計量するための方法および装置

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0578237U (ja) * 1992-03-31 1993-10-26 日本化薬株式会社 医薬用容器
JPH0956820A (ja) * 1995-08-21 1997-03-04 Toshihiro Handa 噴霧量を可変調整できる携帯用容器及びこの容器に充填して効果を発揮できる薬学、栄養学的組成物
JPH10167944A (ja) * 1996-12-12 1998-06-23 Kao Corp 口腔用組成物
JP2000273051A (ja) * 1999-03-19 2000-10-03 Kobayashi Pharmaceut Co Ltd 苦みがマスキングされた液状製剤
JP2003020058A (ja) * 2001-06-20 2003-01-21 Park Pangon 液体定量投入容器（Ｑｕａｎｔｉｆｙｉｎｇａｎｄｄｉｓｐｅｎｓｉｎｇａｐｐａｒａｔｕｓｆｏｒｌｉｑｕｉｄ）
JP2003081846A (ja) * 2001-09-11 2003-03-19 Nippon Tenganyaku Kenkyusho:Kk 液状鎮咳去痰薬
JP2004000834A (ja) * 2002-05-31 2004-01-08 Yoshino Kogyosho Co Ltd ポンプの押下ヘッド
JP2005532235A (ja) * 2002-07-11 2005-10-27 レミンタン、ヘルス、プラダクツ、エルエルシー 液体栄養補給剤を計量するための方法および装置

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102670819A (zh) * 2012-05-15 2012-09-19 张方元 一种治疗感冒的药物组合物

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