EP1221941A1 - Formulations pharmaceutiques en poudre - Google Patents

Formulations pharmaceutiques en poudre

Info

Publication number
EP1221941A1
EP1221941A1 EP00982684A EP00982684A EP1221941A1 EP 1221941 A1 EP1221941 A1 EP 1221941A1 EP 00982684 A EP00982684 A EP 00982684A EP 00982684 A EP00982684 A EP 00982684A EP 1221941 A1 EP1221941 A1 EP 1221941A1
Authority
EP
European Patent Office
Prior art keywords
powder formulation
medicament
agent
powder
individual
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.)
Withdrawn
Application number
EP00982684A
Other languages
German (de)
English (en)
Other versions
EP1221941A4 (fr
Inventor
Ronald L. Ream
William J. Wokas
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.)
WM Wrigley Jr Co
Original Assignee
WM Wrigley Jr Co
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 WM Wrigley Jr Co filed Critical WM Wrigley Jr Co
Publication of EP1221941A1 publication Critical patent/EP1221941A1/fr
Publication of EP1221941A4 publication Critical patent/EP1221941A4/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure

Definitions

  • the present invention generally relates to the delivery of medicaments and other agents. More specifically, the present invention relates to the delivery of medicaments and agents using powdered formulations.
  • agents can be used to treat diseases and as such are typically referred to as drugs or medicaments.
  • drugs or medicaments can be used for prophylactic purposes.
  • agents to an individual for a variety of non-medical purposes including enhancing performance or maintaining or initiating alertness.
  • agents run the gamut from stimulants such as caffeine to drugs such as analgesics, tranquilizers, cardiovascular products, insulin, etc. Some such agents are taken on an as needed basis while other agents must be taken at regular intervals by the individual.
  • drugs are administered parenterally or enterally.
  • parenteral administration is the administration of a drug intravenously directly into the blood stream.
  • Enteral refers to the administration of a drug into the gastrointestinal tract.
  • the goal of the drug administration is to move the drug from the site of administration towards the systemic circulation.
  • a drug must traverse several semipermeable cell membranes before reaching general circulation. These membranes act as a biological barrier that inhibits the passage of drug molecules. There are believed to be four processes by which drugs move across a biological barrier: passive diffusion; facilitated diffusion; active transport; and pinocytosis.
  • Passive diffusion is the transport across the cell membrane wherein the driving force for the movement is the concentration gradient of the solute. In orally administered drugs, this abso ⁇ tion occurs in the small intestines.
  • Facilitated diffusion is believed to be based on a carrier component that combines reversibly with the substrate molecule at the cell membrane exterior. The carrier substrate complex diffuses rapidly across the membrane with release of the substrate at the interior surface.
  • Active transport requires an energy expenditure by the cell and appears to be limited to agents with structural similarities to normal body constituents. These agents are usually absorbed from specific sites in the small intestines. Pinocytosis refers to the engulfing of particulars or fluid by a cell. It is believed to play a minor role in drug transport. Merck Manual, 16th Edition, pp. 2598-2599.
  • Drug abso ⁇ tion refers to the process of drug movement from the site of administration toward the systemic circulation.
  • Oral administration of drugs is by far the most common method.
  • drug abso ⁇ tion usually occurs due to the transport of cells across the membranes of the epithelial cells within the gastrointestinal tract. Abso ⁇ tion after oral administration is confounded by numerous factors. These factors include differences down the alimentary cannel in: the luminal pH; surface area per luminal volume; perfusion of tissue, bile, and mucus flow; and the epithelial membranes. See Merck Manual at page 2599.
  • a further issue effecting the abso ⁇ tion of orally administered drugs is the form of the drug.
  • Most orally administered drugs are in the form of tablets or capsules. This is primarily for convenience, economy, stability, and patient acceptance. Accordingly, these capsules or tablets must be disintegrated or dissolved before abso ⁇ tion can occur. There are a variety of factors capable of varying or retarding disintegration of solid dosage forms. Further, there are a variety of factors that effect the dissolution rate and therefore determine the availability of the drug for abso ⁇ tion. See Merck Manual at page 2600.
  • Parental administration allows for the direct placement of the drug into the blood stream. This usually insures complete delivery of the dose to the general circulation. However, administration by a route that requires drug transfer through one or more biologic membranes to reach the blood stream precludes a guarantee that all of the drug will eventually be absorbed. Even with parental administration, because capillaries tend to be highly porous, the perfusion (blood flow/gram of tissue) is a major factor in the rate of abso ⁇ tion. Thus, the injection site can markedly influence a drug's abso ⁇ tion rate; e.g., the abso ⁇ tion rate of diazepam injected EVI into a site with poor blood flow can be much slower than following an oral dose. See Merck Manual at page 2601.
  • Bioavailability is defined as the rate at which and the extent to which the active moiety (drug or metabolite) enters the general circulation, thereby gaining access to the site of action. Bioavailability depends upon a number of factors, including how a drug product is designed and manufactured, its physicochemical properties, and factors that relate to the physiology and pathology of the patient. See Merck Manual at page 2602.
  • Bioavailability considerations are most often encountered for orally administered drugs. Differences in bioavailability can have profound clinical significance.
  • parental administration does provide a method for eliminating a number of the variables that are present with oral administration
  • parental administration is not a preferable route.
  • parental administration requires the use of medical personnel and is just not warranted nor practical for the administration of most agents and drugs, e.g., analgesics.
  • agents and drugs e.g., analgesics.
  • parenteral administration is not preferred due to patient concerns including comfort, infection, etc., as well as the equipment and costs involved.
  • certain therapies require parenterally injected drugs. For example, research for decades has focused on an attempt to deliver insulin to an individual through a non-parental means. Despite such efforts today insulin is still only administered intravenously.
  • a limited number of medicaments have been administered in the form of a powder.
  • headache powders have been used to provide an enteral method for the delivery of aspirin and other analgesics. Examples of such headache powders are marketed under the brand names BG and Dr. Goodys. These powders are very bitter and typically are not the desired method to enterally ingest an analgesic.
  • the present invention provides improved methods for delivering a powder medicament or agent to an individual. Improved powder formulations including medicaments and agents are also provided by the present invention. To this end, powders are provided including medicaments or agents.
  • the medicament or agent is present in a powder form mixed with at least a masking agent. It has been found that the masking agent and medicament in powder form have a greater ability to cover up bitter and bad flavors produced by the medicament or agent.
  • the present invention allows a variety of medicaments and agents to be delivered directly into the systemic system of the individual through the oral mucosa contained in the buccal cavity.
  • Such a method can greatly enhance the abso ⁇ tion of the drug into the systemic system as well as the bioavailability of the drug within the system. Abso ⁇ tion of the drug is further enhanced by allowing the consumer to hold the dissolved powder in the mouth for 1 or 2 minutes or longer if comfortable.
  • the present invention provides a powder medicament that is designed to dissolve in the mouth of user.
  • the powder medicament includes a sufficient amount of a masking agent to improve the organoleptic properties of the powdered formula.
  • the medicament is chosen from the group consisting of: analgesics; muscle relaxants; antihistamines; decongestants; antacids; anti- infiammatories; antibiotics; antivirals; stimulants; psychotherapeutic agents; and cardiovascular agents.
  • the masking agent is chosen from the group consisting of: zinc gluconate; ethyl maltol; glycine; acesulfame-K; aspartame, saccharin; fructose; xylitol; spray dried licorice root; glycerrhizine; sodium gluconate; glucono delta-lactone; vanillin; normal and high-potency sweeteners; and a variety of appropriate flavors.
  • the formulation creates a saliva content of medicament of at least 5 ppm to about 66% medicament by weight in the saliva, depending on the medicament.
  • the present invention provides a method of enhancing an individual's performance comprising the steps of: providing a powder formulation including a performance enhancing amount of caffeine and a sufficient amount of a masking agent to provide a powder formula with acceptable organoleptic properties; and placing the powder formulation into the buccal cavity not more than ten minutes before the performance.
  • the performance to be enhanced is athletic.
  • the performance to be enhanced is cognitive. In an embodiment, the performance to be enhanced is alertness.
  • the powder formulation is placed in the buccal cavity not more than 5 minutes before the performance.
  • the present invention provides a method of increasing the stimulatory effect of a stimulant that has been previously ingested by an individual comprising the steps of: providing a powder formulation that contains a powder stimulant and a masking agent; and placing the powder formulation into the buccal cavity causing the stimulant to be released by the powdered formulation into the oral mucosa of the individual.
  • the present invention provides a powder formulation comprising a powder medicament and a sufficient amount of a masking agent to provide a powder formulation having acceptable organoleptic properties.
  • a method of delivering a medicament comprising the steps of: providing a powder formulation including a powder medicament and a masking agent; and placing the powder formulation in a buccal cavity of an individual and allowing same to dissolve.
  • an advantage of the present invention is to provide new methods for delivering medicaments or agents to an individual.
  • an advantage of the present invention is to provide a method of delivering medicaments to an individual that provides for increase abso ⁇ tion and bioavailability as compared to medicaments that are designed to be absorbed in the GI tract.
  • an advantage of the present invention is to provide a method of administering a medicament or agent to an individual at a level that is lower than is typically administered orally while still achieving the same effect.
  • an advantage of the present invention is to provide a method for administering drugs or agents to an individual that heretofore were administered parentally.
  • an advantage of the present invention is to provide a method for administering drugs that is more palatable than current methods.
  • Another advantage of the present invention is to provide a method for enhancing the performance of an individual through the administration of an agent. Moreover, an advantage of the present invention is to provide an improved method for drug delivery.
  • an advantage of the present invention is to provide a method for creating a triggering effect that creates a synergistic effect with an agent that is present in the systemic circulation of the individual. Additional features and advantages of the present invention will be described in and apparent from the detailed description of the presently preferred embodiments.
  • a medicament or agent is contained in a powder formulation that includes a masking agent.
  • a masking agent includes compounds and agents that alter or disguise the taste of a product that is ingested or placed in the mouth.
  • the term masking agent includes sweeteners and flavors. It has been found that by adding a masking agent to the powder formulation, that a much more palatable formulation, including a powder medicament, can be provided.
  • the powder matrix of the present invention including the masking agent, will afford a product having acceptable organoleptic properties. It has been surprisingly found that by solubilizing a powdered matrix of medicament and masking agent, this increases the ability of the masking agent to cover up bitter and bad flavors produced by the medicament or agent.
  • specific masking agents based on the bad or off taste produced by the medicament, one can provide a palatable powder formulation. For example, if one is attempting to cover an astringent flavor such as aspirin, one would use masking agents found to be effective against astringency such as fructose and macro sweeteners, e.g.
  • saccharin, aspartame, and acesulfame-k In the case of a moderately bitter active ingredient, such as caffeine, one would use ingredients such as glycine, ethyl maltol, zinc gluconate, licorice root powder, micro sweeteners, etc. In the case of a very bad tasking active ingredient such as acetaminophen, combinations of these masking agents or larger quantities may have to be used in order to combat the undesirable bitterness.
  • the masking agents are selected from the group consisting of: zinc gluconate; ethyl maltol; glycine; acesulfame-k; aspartame; saccharin; fructose; xylitol; spray dried licorice root; glycerrhizine; sodium gluconate; glucono delta-lactone; and vanillin.
  • the powder formulation is placed in the mouth of the user. Due to the present invention, the powder fo ⁇ nulation has acceptable organoleptic properties allowing the consumer to maintain the powder in his mouth for a sufficient time to allow as much as possible of the powder to dissolve. As the powder formulation dissolves, the powder medicament or agent is released into the saliva. The medicament or agent in the saliva can then pass through the oral mucosa in the buccal cavity.
  • the oral mucosa has a thin epithelium and a rich vascularity. Thus, the oral mucosa favors drug abso ⁇ tion.
  • caffeine is commonly used as a stimulant to alleviate the effects of sleep deprivation. It is almost completely metabolized in the liver and therefore classified as a low clearance, flow independent drug. This means its rate of inactivation is unaffected by delivery to the liver and can only be modified by a change in the hepatic enzyme activity.
  • such medicaments include, inter alia, analgesics, antibiotics, antivirals, antihistamines, anti-inflammatories, decongestants, antacids, muscle relaxants, psychotherapeutic agents, insulin, and cardiovascular agents.
  • the resultant powder formulation can be used to treat, inter alia: coughs; colds; motion sickness; allergies; fevers; pain; inflammation; sore throats; cold sores; sinus problems; diarrhea; diabetics; depression; anxiety; and other maladies and symptoms.
  • agents/medicaments include, by way of example and not limitation: caffeine; aspirin; acetaminophen; ibuprofen; hydroxycitric acid; chromium picolinate; phosphatidylserine; nicotine; insulin; Echinacea pu ⁇ urea; zinc; vitamin C; ginseng; kola nut; kaua kaua; and chamomile.
  • the agents or medicaments are contained in the powder formulation at levels of approximately 50 micrograms to 1000 milligrams.
  • the specific levels will depend on the active ingredient. For example, if chromium picolinate is the active ingredient in an embodiment, it would be present at a level of approximately 20 to about 50 micrograms per dosage; aspirin would be preset at a level of approximately 50 to about 650 milligrams per dosage; caffeine would be preset at a level of approximately 20 to about 600 milligrams per dosage; and acetaminophen would be preset at a level of approximately 87 to about 1000 milligrams per dosage.
  • the level of medicament or agent in the powdered formulation is selected so as to create, when the powder formulation is placed in the mouth, a sufficiently high concentration of the medicament or agent in the saliva.
  • the level of the stimulant in the powder formulation should be such that it creates a saliva content of stimulant of approximately 1% to about 66% after the formulation is placed in the mouth. At this level, a sufficient amount of stimulant will be delivered to the user to create the effects set forth in the application.
  • a medicament such as a medicinal (e.g., analgesics)
  • sufficient medicinal should be present in the powder formulation to create a salvia content of approximately 1% to about 66%.
  • botanicals e.g., chamomile, kava, kola, nut, ginseng, and Echinacea
  • the agent should be present in a sufficient amount to create a saliva content of approximately 1% to about 66%.
  • the agents should be present in an amount to create a saliva content of approximately 1% to about 66%. If the agent is a vitamin or mineral (e.g., phosphatidy serine, vitamin C, and zinc), the agent should be present in the amount to create a saliva content of the vitamin or mineral of approximately 2%to about 30%.
  • the dosing regiment will change. For example, if the medicament is an analgesic, the powdered formulation would be taken on an as needed basis. Of course, similar to the oral administration of an analgesic, there would be restrictions on the doses taken, for example, not more often than one powdered formulation every four hours and not more often than four to five times a day.
  • the agent is a stimulant, such as caffeine, to be used to enhance performance than the powdered formulation would be ingested, in a preferred embodiment ten minutes or less before the performance.
  • Sufficient masking agent will be used to improve and provide acceptable organoleptic properties to the powder product.
  • acceptable organoleptic properties means that the powder formulation will have a sufficiently pleasant, or at least non-offensive taste, to allow the consumer to allow at least a majority of the powder formulation to dissolve in his mouth.
  • the amount of masking agent will thereby vary depending on medicament or agent. Of course, more than one masking agent can be used, e.g., zinc gluconate and a sweetener or flavor.
  • the masking agent will comprise approximately 50% to about 99+%o by weight of the powder formulation.
  • the agent is caffeine
  • approximately 10 to about 50 milligrams of masking agent should be present per milligram of caffeine
  • for aspirin approximately 4 to about 32 milligrams of masking agent should be present per milligram of aspirin
  • acetaminophen approximately 4 to about 32 milligrams of masking agent should be present per milligram of acetaminophen.
  • more than one masking agent can be used.
  • the medicament or agent can be contained in a variety of different powder formulation compositions.
  • the formulation can be low or high moisture, sugar or sugarless, and/or low calorie.
  • the formulation can include a water soluble bulk portion and one or more flavoring agents.
  • the water soluble portion can include bulk sweeteners, high intensity sweeteners, flavoring agents, softeners, emulsifiers, colors, acidulants, fillers, antioxidants, and other components that provide desired attributes.
  • Bulk sweeteners which also can function as the masking agent, include both sugar and sugarless components. Bulk sweeteners, if present, will typically constitute about 50% to about 98% by weight of the formulation.
  • Sugar sweeteners generally include saccharide-containing components commonly known in the confectionary art, including but not limited to, sucrose, dextrose, maltose, dextrin, dried invert sugar, fructose, levulose, glactose, corn syrup solids, and the like, alone or in combination.
  • Sugarless sweeteners include, but are not limited to, sugar alcohols such as sorbitol, mannitol, xylitol, hydrogenated starch hydrolysates, maltitol, and the like, alone or in combination.
  • High intensity artificial sweeteners can also be used, alone or in combination, with the above.
  • Preferred sweeteners include, but are not limited to, sucralose, aspartame, salts of acesulfame, altitame, saccharin and its salts, cyclamic acid and its salts, glycerrhizinate, dihydrochalcones, thaumatin, monellin, and the like, alone or in combination.
  • Such techniques as wet granulation, wax granulation, spray drying, spray chilling, fluid bed coating, coacervation, and fiber extension may be used to achieve the desired release characteristics.
  • Combinations of sugar and/or sugarless sweeteners may be used in the formulation. Additionally, the softener may also provide additional sweetness such as with aqueous sugar or alditol solutions. As noted above, depending on the powder agent or medicament, sweeteners can comprise a part of, or the entire masking agent.
  • a low caloric bulking agent can be used.
  • low caloric bulking agents include: polydextrose; Raftilose, Raftilin; Fructooligosaccharides (NutraFlora); Palatinose oligosaccharide; Guar Gum Hydrolysate (Sun Fiber); or indigestible dextrin (Fibersol).
  • other low calorie bulking agents can be used.
  • flavoring agents can also be used, if desired. If present, the flavor can be used in amounts of about 0.5 to about 10 weight percent of the formulation. As noted above, depending on the medicament or agent, flavor can comprise a part of, or the entire masking agent. Flavoring agents may include essential oils, synthetic flavors or mixtures thereof including, but not limited to, oils derived from plants and fruits such as citrus oils, fruit essences, peppermint oil, spearmint oil, other mint oils, clove oil, oil of wintergreen, anise and the like. Artificial flavoring agents and components may also be used. Natural and artificial flavoring agents may be combined in any sensorially acceptable fashion.
  • the formulations would be constructed by blending a medicament in powder form with a powder masking agent and other components as desired. The blend powder formulation would thus be placed in a package.
  • examples of some powdered formulations including a medicament or agent are as follows: Caffeine Powder Formula

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  • Diabetes (AREA)
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  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Abstract

L'invention concerne des méthodes et des formulations en poudre qui permettent d'administrer un médicament ou un agent en poudre à un individu. La formulation en poudre inclut un médicament ou un agent, ainsi qu'une quantité suffisante d'un agent masquant qui permet au consommateur de laisser au moins une partie de la poudre se dissoudre dans sa bouche grâce aux capacités de masquage de l'arôme de la forme posologique orale pulvérulente. Lorsque la formulation en poudre est placée dans la bouche de l'usager, le médicament ou l'agent se libère et favorise l'absorption du médicament dans le système général, ainsi que la biodisponibilité du médicament à l'intérieur du système.
EP00982684A 1999-10-20 2000-10-18 Formulations pharmaceutiques en poudre Withdrawn EP1221941A4 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US42190599A 1999-10-20 1999-10-20
US421905 1999-10-20
PCT/US2000/041225 WO2001028523A1 (fr) 1999-10-20 2000-10-18 Formulations pharmaceutiques en poudre

Publications (2)

Publication Number Publication Date
EP1221941A1 true EP1221941A1 (fr) 2002-07-17
EP1221941A4 EP1221941A4 (fr) 2005-11-30

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Family Applications (1)

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EP00982684A Withdrawn EP1221941A4 (fr) 1999-10-20 2000-10-18 Formulations pharmaceutiques en poudre

Country Status (6)

Country Link
EP (1) EP1221941A4 (fr)
JP (1) JP2003512315A (fr)
CN (1) CN1374859A (fr)
AU (1) AU779170B2 (fr)
CA (1) CA2382978A1 (fr)
WO (1) WO2001028523A1 (fr)

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JP4373649B2 (ja) * 2002-08-01 2009-11-25 ロート製薬株式会社 経口用液剤
SE0500006L (sv) * 2005-01-04 2006-07-05 Peter Stigsson Anordning för intagande av koffein i en munhåla
DE102005040463A1 (de) * 2005-08-26 2007-03-01 Cognis Ip Management Gmbh Verwendung von Gemischen aus Polyphenolen und physiologisch aktiven ungesättigten Fettstoffen
JP5620040B2 (ja) * 2007-01-19 2014-11-05 エスエス製薬株式会社 経口組成物
CN103005367A (zh) * 2012-12-17 2013-04-03 楚大波 一种苦味遮蔽剂及其制备方法及用途

Citations (6)

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CA2382978A1 (fr) 2001-04-26
WO2001028523A1 (fr) 2001-04-26
EP1221941A4 (fr) 2005-11-30
CN1374859A (zh) 2002-10-16
JP2003512315A (ja) 2003-04-02
AU779170B2 (en) 2005-01-13
AU1968201A (en) 2001-04-30

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