AU1968201A - Powder pharmaceutical formulations - Google Patents
Powder pharmaceutical formulations Download PDFInfo
- Publication number
- AU1968201A AU1968201A AU19682/01A AU1968201A AU1968201A AU 1968201 A AU1968201 A AU 1968201A AU 19682/01 A AU19682/01 A AU 19682/01A AU 1968201 A AU1968201 A AU 1968201A AU 1968201 A AU1968201 A AU 1968201A
- Authority
- AU
- Australia
- Prior art keywords
- powder formulation
- medicament
- agent
- individual
- powder
- 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.)
- Granted
Links
- 239000000843 powder Substances 0.000 title claims description 92
- 239000008194 pharmaceutical composition Substances 0.000 title description 2
- 239000003814 drug Substances 0.000 claims description 119
- 239000003795 chemical substances by application Substances 0.000 claims description 116
- 239000000203 mixture Substances 0.000 claims description 80
- 238000009472 formulation Methods 0.000 claims description 78
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 claims description 48
- 238000000034 method Methods 0.000 claims description 47
- 230000000873 masking effect Effects 0.000 claims description 44
- LPHGQDQBBGAPDZ-UHFFFAOYSA-N Isocaffeine Natural products CN1C(=O)N(C)C(=O)C2=C1N(C)C=N2 LPHGQDQBBGAPDZ-UHFFFAOYSA-N 0.000 claims description 24
- 229960001948 caffeine Drugs 0.000 claims description 24
- VJEONQKOZGKCAK-UHFFFAOYSA-N caffeine Natural products CN1C(=O)N(C)C(=O)C2=C1C=CN2C VJEONQKOZGKCAK-UHFFFAOYSA-N 0.000 claims description 24
- 235000003599 food sweetener Nutrition 0.000 claims description 18
- 239000003765 sweetening agent Substances 0.000 claims description 18
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical group CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 claims description 16
- 230000000694 effects Effects 0.000 claims description 14
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims description 12
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- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims description 10
- WHMDKBIGKVEYHS-IYEMJOQQSA-L Zinc gluconate Chemical compound [Zn+2].OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O WHMDKBIGKVEYHS-IYEMJOQQSA-L 0.000 claims description 10
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- 229960005489 paracetamol Drugs 0.000 claims description 8
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical group CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims description 7
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- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 claims description 6
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- 235000019204 saccharin Nutrition 0.000 claims description 6
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 claims description 6
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- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 5
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- 239000002327 cardiovascular agent Substances 0.000 claims description 5
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- 229940124581 decongestants Drugs 0.000 claims description 5
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- IMCGHZIGRANKHV-AJNGGQMLSA-N tert-butyl (3s,5s)-2-oxo-5-[(2s,4s)-5-oxo-4-propan-2-yloxolan-2-yl]-3-propan-2-ylpyrrolidine-1-carboxylate Chemical compound O1C(=O)[C@H](C(C)C)C[C@H]1[C@H]1N(C(=O)OC(C)(C)C)C(=O)[C@H](C(C)C)C1 IMCGHZIGRANKHV-AJNGGQMLSA-N 0.000 claims description 5
- 239000000811 xylitol Substances 0.000 claims description 5
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- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 5
- 229960002675 xylitol Drugs 0.000 claims description 5
- AEQDJSLRWYMAQI-UHFFFAOYSA-N 2,3,9,10-tetramethoxy-6,8,13,13a-tetrahydro-5H-isoquinolino[2,1-b]isoquinoline Chemical compound C1CN2CC(C(=C(OC)C=C3)OC)=C3CC2C2=C1C=C(OC)C(OC)=C2 AEQDJSLRWYMAQI-UHFFFAOYSA-N 0.000 claims description 4
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- 229940005574 sodium gluconate Drugs 0.000 claims description 4
- MWOOGOJBHIARFG-UHFFFAOYSA-N vanillin Chemical compound COC1=CC(C=O)=CC=C1O MWOOGOJBHIARFG-UHFFFAOYSA-N 0.000 claims description 4
- FGQOOHJZONJGDT-UHFFFAOYSA-N vanillin Natural products COC1=CC(O)=CC(C=O)=C1 FGQOOHJZONJGDT-UHFFFAOYSA-N 0.000 claims description 4
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Classifications
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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]
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- 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
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- 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
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
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- Organic Chemistry (AREA)
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- General Chemical & Material Sciences (AREA)
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- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
WO 01/28523 PCT/USOO/41225 SPECIFICATION TITLE "POWDER PHARMACEUTICAL FORMULATIONS" 5 BACKGROUND OF THE INVENTION 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. It is of course known to provide agents to individuals for various purposes. These 10 agents can be used to treat diseases and as such are typically referred to as drugs or medicaments. Likewise, drugs or medicaments can be used for prophylactic purposes. Still, it is known to provide agents to an individual for a variety of non-medical purposes including enhancing performance or maintaining or initiating alertness. There are a great variety of such agents. These agents run the gamut from stimulants such as caffeine 15 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. Typically, drugs (medicaments) are administered parenterally or enterally. Of course, parenteral administration is the administration of a drug intravenously directly 20 into the blood stream. Enteral refers to the administration of a drug into the gastrointestinal tract. In either case, the goal of the drug administration is to move the drug from the site of administration towards the systemic circulation. Except when provided intravenously, a drug must traverse several semipermeable cell membranes before reaching general circulation. These membranes act as a biological 25 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 30 drugs, this absorption 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 -1- WO 01/28523 PCT/USOO/41225 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 5 a cell. It is believed to play a minor role in drug transport. Merck Manual, 16th Edition, pp. 2598-2599. In determining the efficacy of a drug and the effectiveness of the use of a drug to treat a disease, drug absorption is a critical concern. Drug absorption refers to the process of drug movement from the site of administration toward the systemic 10 circulation. Oral administration of drugs is by far the most common method. When administered orally, drug absorption usually occurs due to the transport of cells across the membranes of the epithelial cells within the gastrointestinal tract. Absorption after oral administration is confounded by numerous factors. These factors include differences 15 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 absorption of orally administered drugs is the form of the drug. Most orally administered drugs are in the form of tablets or capsules. This 20 is primarily for convenience, economy, stability, and patient acceptance. Accordingly, these capsules or tablets must be disintegrated or dissolved before absorption 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 absorption. See Merck Manual at 25 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 30 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 -2- WO 01/28523 PCT/USOO/41225 of absorption. Thus, the injection site can markedly influence a drug's absorption rate; e.g., the absorption rate of diazepam injected IM into a site with poor blood flow can be much slower than following an oral dose. See Merck Manual at page 2601. Not only is drug absorption an issue in drug delivery, but, also the bioavailability 5 of the drug is also critical. 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 10 Merck Manual at page 2602. When a drug rapidly dissolves from a drug product and readily passes across membranes, absorption from most site administration tends to be complete. This is not always the case for drugs given orally. Before reaching the vena cava, the drug must move down the alimentary cannel and pass through the gut wall and liver, which are 15 common sites of drug metabolism. Thus, the drug may be metabolized before it can be measured in the general circulation. This causes a decrease in drug input that is called the first pass effect. A large number of drugs show low bioabilities owing to an extensive first pass metabolism. The two other most frequent causes of low bioavailability are insufficient time in the GI tract and the presence of competing reactions. See Merck 20 Manual at page 2602. Bioavailability considerations are most often encountered for orally administered drugs. Differences in bioavailability can have profound clinical significance. Although parental administration does provide a method for eliminating a number of the variables that are present with oral administration, parental administration is not 25 a preferable route. Typically, 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. Even when required parenteral administration is not preferred due to patient concerns including comfort, infection, etc., as well as the equipment and costs involved. However, despite best efforts certain therapies require parenterally injected 30 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 -3- WO 01/28523 PCT/USOO/41225 only administered intravenously. A limited number of medicaments have been administered in the form of a powder. For example, headache powders have been used to provide an enteral method for the delivery of aspirin and other analgesics. Examples of such headache powders are 5 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. There is therefore a need for an improved method of delivering drugs and agents to an individual. SUMMARY OF THE INVENTION 10 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 15 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 absorption of the drug into the 20 systemic system as well as the bioavailability of the drug within the system. Absorption 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. To this end, in an embodiment, the present invention provides a powder medicament that is designed to dissolve in the mouth of user. The powder medicament 25 includes a sufficient amount of a masking agent to improve the organoleptic properties of the powdered formula. In an embodiment, the medicament is chosen from the group consisting of: analgesics; muscle relaxants; antihistamines; decongestants; antacids; anti inflammatories; antibiotics; antivirals; stimulants; psychotherapeutic agents; and 30 cardiovascular agents. In an embodiment, the masking agent is chosen from the group consisting of: -4- WO 01/28523 PCT/USOO/41225 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. In an embodiment, the formulation creates a saliva content of medicament of at 5 least 5 ppm to about 66% medicament by weight in the saliva, depending on the medicament. In another embodiment, 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 10 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. In an embodiment, the performance to be enhanced is athletic. In an embodiment, the performance to be enhanced is cognitive. 15 In an embodiment, the performance to be enhanced is alertness. In an embodiment, the powder formulation is placed in the buccal cavity not more than 5 minutes before the performance. Yet further, the present invention provides a method of increasing the stimulatory effect of a stimulant that has been previously ingested by an individual comprising the 20 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. In another embodiment, the present invention provides a powder formulation comprising a powder medicament and a sufficient amount of a masking agent to provide 25 a powder formulation having acceptable organoleptic properties. In a further embodiment of the present invention, a method of delivering a medicament is provided. The method 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. 30 Accordingly, an advantage of the present invention is to provide new methods for delivering medicaments or agents to an individual. -5- WO 01/28523 PCT/USOO/41225 Still further, an advantage of the present invention is to provide a method of delivering medicaments to an individual that provides for increase absorption and bioavailability as compared to medicaments that are designed to be absorbed in the GI tract. 5 Further, 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. Furthermore, an advantage of the present invention is to provide a method for administering drugs or agents to an individual that heretofore were administered 10 parentally. Additionally, 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. 15 Moreover, an advantage of the present invention is to provide an improved method for drug delivery. Still, 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. 20 Additional features and advantages of the present invention will be described in and apparent from the detailed description of the presently preferred embodiments. DETAILED DESCRIPTION OF THE PRESENTLY PREFERRED EMBODIMENTS 25 The present invention provides improved methods for delivering medicaments and other agents to an individual as well as improved formulations including such medicaments and agents. Pursuant to the present invention, a medicament or agent is contained in a powder formulation that includes a masking agent. As used herein, the term "masking agent" includes compounds and agents that alter or disguise the taste of 30 a product that is ingested or placed in the mouth. As such, the term masking agent includes sweeteners and flavors. -6- WO 01/28523 PCT/USOO/41225 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. In this regard, even though the medicament in its powder form may be bitter or have an offensive taste, the powder matrix of the present invention, including the masking agent, 5 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. By selecting specific masking agents based on the bad or off taste produced by the medicament, one can provide a palatable powder formulation. 10 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 15 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, in an embodiment, are selected from the group consisting of: zinc gluconate; ethyl maltol; glycine; acesulfame-k; aspartame; saccharin; fructose; 20 xylitol; spray dried licorice root; glycerrhizine; sodium gluconate; glucono delta-lactone; and vanillin. In use, the powder formulation is placed in the mouth of the user. Due to the present invention, the powder formulation has acceptable organoleptic properties allowing the consumer to maintain the powder in his mouth for a sufficient time to allow 25 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 absorption. In contrast to a typically orally ingested drug, wherein the solution is in contact 30 too briefly for absorption to be appreciable through the oral mucous, if the powder is allowed to dissolve in the mouth, an increase in the absorption of the drug is achieved as -7- WO 01/28523 PCT/USOO/41225 well as an increase in the bioavailability of the drug as compared to typical oral administration. It has been found that the drug or agent is absorbed much quicker when it is allowed to dissolve in the mouth of the consumer than if it was swallowed as in a typical oral administration. 5 It is believed that less powder medicament or agent can be placed in the powder formulation than is typically orally administered to an individual to achieve an effect and the same bioequivalence can be achieved. For example, caffeine is commonly used as a stimulant to alleviate the effects of sleep deprivation. It is almost completely metabolized in the liver and therefore 10 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. The pharmacokinetics of caffeine have been well documented and there is no significant difference between oral and intravenous administration. However, data set 15 forth in detail below, suggests that the absorption rate constant (Ka) is significantly increased when caffeine is administered through chewing gum. This means that the caffeine is moving into the systemic circulation at a significantly faster rate. A similar change in the onset of dynamic response has also been noted, e.g., alertness and performance. 20 It is believed that for at least certain agents that placing the agent in a powder formulation that is placed in the mouth can have a triggering effect on the agent that may be in the systemic circulation. For example, it has been found that with respect to caffeine that is ingested orally, that after the ingestion of a certain amount of caffeine, and the elapse of a certain period of time, that further ingestion of caffeine has a 25 negligible effect on the individual. However, it is believed that if caffeine is placed in a powdered formulation with caffeine there has been observed a triggering effect that appears to create a synergistic effect with the caffeine that is in the systemic circulation. It is believed that this triggering effect will also be present with other agents, e.g., analgesics. 30 It is envisioned, that a variety of different powder medicaments and agents can be used in the powder formulation. For example, such agents include, inter alia, -8- WO 01/28523 PCT/USOO/41225 stimulants such as caffeine. Generally, such medicaments include, inter alia, analgesics, antibiotics, antivirals, antihistamines, anti-inflammatories, decongestants, antacids, muscle relaxants, psychotherapeutic agents, insulin, and cardiovascular agents. It is envisioned, that depending on the medicament, the resultant powder formulation can be 5 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. Specific agents/medicaments include, by way of example and not limitation: caffeine; aspirin; acetaminophen; ibuprofen; hydroxycitric acid; chromium picolinate; phosphatidylserine; nicotine; insulin; Echinacea 10 purpurea; zinc; vitamin C; ginseng; kola nut; kaua kaua; and chamomile. Preferably, 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 15 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 20 to create, when the powder formulation is placed in the mouth, a sufficiently high concentration of the medicament or agent in the saliva. For example, when the agent is a stimulant such as caffeine, 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. 25 At this level, a sufficient amount of stimulant will be delivered to the user to create the effects set forth in the application. If a medicament is used 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%. For botanicals (e.g., chamomile, kava, kola, nut, ginseng, and Echinacea), the agent should be present in a sufficient 30 amount to create a saliva content of approximately 1% to about 66%. For a metabolizer, for example, chromium picolineate and hydroxi-chitic acid, the agents should be present -9- WO 01/28523 PCT/USOO/41225 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%. 5 Pursuant to the present invention, depending on the agent or medicament, 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 10 often than four to five times a day. If 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 15 organoleptic properties to the powder product. As used herein to provide "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 20 agent can be used, e.g., zinc gluconate and a sweetener or flavor. Generally, it is believed that the masking agent will comprise approximately 50% to about 99+% by weight of the powder formulation. For example, if 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 25 masking agent should be present per milligram of aspirin; and for acetaminophen, approximately 4 to about 32 milligrams of masking agent should be present per milligram of acetaminophen. Of course, more than one masking agent can be used. The medicament or agent can be contained in a variety of different powder formulation compositions. For example, the formulation can be low or high moisture, 30 sugar or sugarless, and/or low calorie. The formulation can include a water soluble bulk portion and one or more -10- WO 01/28523 PCT/USOO/41225 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 5 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. 10 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, 15 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. In order to provide longer lasting sweetness and flavor perception, it may be desirable to encapsulate or otherwise control the release of at least a portion of the artificial sweetener. Such techniques as wet granulation, wax granulation, spray drying, 20 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 25 or medicament, sweeteners can comprise a part of, or the entire masking agent. If a low calorie formulation is desired, a low caloric bulking agent can be used. Examples of low caloric bulking agents include: polydextrose; Raftilose, Raftilin; Fructooligosaccharides (NutraFlora); Palatinose oligosaccharide; Guar Gum Hydrolysate (Sun Fiber); or indigestible dextrin (Fibersol). However, other low calorie bulking agents 30 can be used. A variety of flavoring agents can also be used, if desired. If present, the flavor -11- WO 01/28523 PCT/USOO/41225 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 5 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. There are a variety of methods for constructing powder formulations. Generally, 10 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. By way of example, and not limitation, examples of some powdered formulations including a medicament or agent are as follows: 15 Caffeine Powder Formula Dextrose 95.50% 93.75% 90.75% Flow Agent 1.00% 1.00% 1.00% Zinc Gluconate 0.15% 0.15% - 0.15% Caffeine 2.00% 2.00% 5.00% 20 Flavors 1.35% 1.35% 1.35% Macro Sweetener 0.00% 1.75% 1.75% 100.00% 100.00% 100.00% Acetaminophen Powder Formula 25 Dextrose 90.50% 88.50% 78.80% Flow Agent 1.00% 1.00% 1.00% Zinc Gluconate 0.15% 0.15% 0.15% Acetaminophen 7.00% 7.00% 16.70% Flavors 1.35% 1.35% 1.35% 30 Macro Sweetener 0.00% 2.00% 2.00% 100.00% 100.00% 100.00% It should be understood that various changes and modifications to the presently preferred embodiments described herein will be apparent to those skilled in the art. Such 35 changes and modifications can be made without departing from the spirit and scope of the present invention and without diminishing its attendant advantages. It is therefore intended that such changes and modifications be covered by the appended claims. -12-
Claims (29)
1. A method for delivering a medicament in a powder form to an individual comprising the steps of: providing a powder formulation that includes a medicament in powder form and 5 a sufficient amount of a masking agent to provide acceptable organoleptic properties; and allowing at least a portion of the powder formulation to dissolve in a mouth of an individual to cause the medicament to be released from the formulation into a buccal cavity of the individual. 10
2. The method of Claim 1 wherein the powder formulation includes a sweetener.
3. The method of Claim 1 wherein the powder formulation creates a temporary saliva content of medicament of approximately 5 ppm to about 66% by 15 weight.
4. The method of Claim 1 wherein the medicament in a powder form is chosen from the group consisting of: analgesics; muscle relaxants; antibiotics; antivirals; stimulants; antihistamines; decongestants; anti-inflammatories; antacids; 20 psychotherapeutic agents; insulin; vitamins; minerals; and cardiovascular agents.
5. The method of Claim 1 wherein the 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 25 delta-lactone; vanillin; and ethyl maltol.
6. The method of Claim 1 wherein the masking agent comprises approximately 50% to about 99% by weight of the formulation. 30
7. A method for reducing the amount of agent necessary to achieve an effect in an individual as compared a typical agent that is swallowed comprising the steps of: -13- WO 01/28523 PCT/USOO/41225 providing a powder formulation including an agent that is typically swallowed by an individual to achieve a specific effect, the powder formulation including less than the typical amount of agent that is swallowed by the individual to achieve the effect and a sufficient amount of a masking agent to provide acceptable organoleptic properties to 5 the powder formulation; and placing the powder formulation in the buccal cavity of the individual and allows at least a portion of the powder formulation to dissolve in the mouth of the individual and thereby causing the agent to be released into the salvia of the individual. 10
8. The method of Claim 7 wherein the agent is a medicament.
9. The method of Claim 8 wherein the medicament is chosen from the group consisting of: analgesics; muscle relaxants; antibiotics; antivirals; stimulants; antihistamines; decongestants; anti-inflammatories; antacids; psychotherapeutic agents; 15 and cardiovascular agents.
10. The method of Claim 7 wherein the masking agent comprises approximately 50 to about 99 percent by weight of the powder formulation. 20
11. The method of Claim 7 wherein the powder formulation creates a saliva content of approximately 5 ppm to about 66% by weight agent.
12. A powder formulation comprising: a medicament having an offensive taste; and 25 a sufficient amount of a masking agent to provide acceptable organoleptic properties.
13. The powder formulation of Claim 12 wherein the masking agent is chosen from the group consisting of: zinc gluconate, ethyl maltol, glycine, acesulfame-k, 30 aspartame; saccharin; fructose; xylitol; spray dried licorice root; glycerrhizine; sodium gluconate; glucono delta-lactone; and vanillin. -14- WO 01/28523 PCT/USOO/41225
14. The powder formulation of Claim 12 including a sweetener.
15. The powder formulation of Claim 12 wherein the agent is a stimulant. 5
16. The powder formulation of Claim 12 wherein approximately 50% to about 99+% by weight of the formulation is the masking agent.
17. The powder formulation of Claim 12 wherein the medicament is aspirin and the masking agent is a fructose or macro sweetener. 10
18. The powder formulation of Claim 12 wherein the medicament is acetaminophen and the masking agent is zinc gluconate.
19. A method of enhancing an individual's performance comprising the steps 15 of: providing a powder formulation including a performance enhancing amount of caffeine in powder form and a masking agent; and allowing at least a portion of the powder formulation to dissolve in the mouth of the individual not more than ten minutes before the performance. 20
20. The method of Claim 19 wherein the performance to be enhanced is athletic.
21. The method of Claim 19 wherein the performance to be enhanced is 25 cognitive.
22. The method of Claim 19 wherein the performance to be enhanced is alertness. 30
23. The method of Claim 19 wherein the formulation is allowed to dissolve five minutes or less before the performance. -15- WO 01/28523 PCT/USOO/41225
24. A method of delivering a medicament comprising the steps of: providing a powder formulation including a medicament in powder form and a sufficient amount of a masking agent to mask any offensive tastes that are associated with the medicament; and 5 placing the powder formulation in a buccal cavity of an individual and allowing same to dissolve therein.
25. The method of Claim 24 wherein the medicament is chosen from the group consisting of: analgesics; muscle relaxants; antibiotics; antivirals; antihistamines; 10 decongestants; anti-inflammatories; antacids; psychotherapeutic agents; and cardiovascular agents.
26. A method of increasing the stimulatory effect of a stimulant that has been previously swallowed by an individual comprising the steps of: 15 providing a powder formulation that contains the stimulant and a masking agent; and placing the powder formulation into the buccal cavity causing the stimulant to be released by the powder formulation into an oral mucosa located in a buccal cavity of the individual. 20
27. The method of Claim 26 wherein the stimulant is caffeine.
28. The method of Claim 26 wherein the powder formulation creates a saliva content of medicament of approximately 5 ppm to about 66% by weight. 25
29. The method of Claim 26 wherein the masking agent is chosen from the group consisting of glycine, ethyl maltol, zinc gluconate, and licorice root powder. -16-
Applications Claiming Priority (3)
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US42190599A | 1999-10-20 | 1999-10-20 | |
US09/421905 | 1999-10-20 | ||
PCT/US2000/041225 WO2001028523A1 (en) | 1999-10-20 | 2000-10-18 | Powder pharmaceutical formulations |
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AU1968201A true AU1968201A (en) | 2001-04-30 |
AU779170B2 AU779170B2 (en) | 2005-01-13 |
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AU19682/01A Ceased AU779170B2 (en) | 1999-10-20 | 2000-10-18 | Powder pharmaceutical formulations |
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EP (1) | EP1221941A4 (en) |
JP (1) | JP2003512315A (en) |
CN (1) | CN1374859A (en) |
AU (1) | AU779170B2 (en) |
CA (1) | CA2382978A1 (en) |
WO (1) | WO2001028523A1 (en) |
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JP4373649B2 (en) * | 2002-08-01 | 2009-11-25 | ロート製薬株式会社 | Oral solution |
SE0500006L (en) * | 2005-01-04 | 2006-07-05 | Peter Stigsson | Device for ingesting caffeine in an oral cavity |
DE102005040463A1 (en) * | 2005-08-26 | 2007-03-01 | Cognis Ip Management Gmbh | Use of mixtures of polyphenols and physiologically active unsaturated fatty substances |
JP5620040B2 (en) * | 2007-01-19 | 2014-11-05 | エスエス製薬株式会社 | Oral composition |
CN103005367A (en) * | 2012-12-17 | 2013-04-03 | 楚大波 | Bitterness screening agent as well as preparation method and application thereof |
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US3433872A (en) * | 1966-11-25 | 1969-03-18 | Hoffmann La Roche | Palatable,free-flowing,non-agglomerating caffeine powder |
US4647450A (en) * | 1983-07-20 | 1987-03-03 | Warner-Lambert Company | Chewing gum compositions containing magnesium trisilicate absorbates |
US5262179A (en) * | 1989-09-13 | 1993-11-16 | Nicholas Kiwi Pty Ltd. | Non-effervescent ibuprofen compositions |
US5032411A (en) * | 1990-02-27 | 1991-07-16 | University Of Texas System Board Of Regents | Beverage compositions for human consumption |
US5631038A (en) * | 1990-06-01 | 1997-05-20 | Bioresearch, Inc. | Specific eatable taste modifiers |
US5785984A (en) * | 1993-02-05 | 1998-07-28 | Kao Corporation | Taste-modifying method and bitterness-decreasing method |
US5456677A (en) * | 1994-08-22 | 1995-10-10 | Spector; John E. | Method for oral spray administration of caffeine |
US5607697A (en) * | 1995-06-07 | 1997-03-04 | Cima Labs, Incorporated | Taste masking microparticles for oral dosage forms |
AU1274597A (en) * | 1996-11-27 | 1998-06-22 | Wm. Wrigley Jr. Company | Method of controlling release of caffeine in chewing gum and gum produced thereby |
JPH10298086A (en) * | 1997-04-30 | 1998-11-10 | Taisho Pharmaceut Co Ltd | Oral composition |
US5869098A (en) * | 1997-08-20 | 1999-02-09 | Fuisz Technologies Ltd. | Fast-dissolving comestible units formed under high-speed/high-pressure conditions |
US6355265B1 (en) * | 1999-04-06 | 2002-03-12 | Wm. Wrigley Jr. Company | Over-coated chewing gum formulations |
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2000
- 2000-10-18 WO PCT/US2000/041225 patent/WO2001028523A1/en active IP Right Grant
- 2000-10-18 CN CN 00812937 patent/CN1374859A/en active Pending
- 2000-10-18 EP EP00982684A patent/EP1221941A4/en not_active Withdrawn
- 2000-10-18 JP JP2001531353A patent/JP2003512315A/en active Pending
- 2000-10-18 CA CA002382978A patent/CA2382978A1/en not_active Abandoned
- 2000-10-18 AU AU19682/01A patent/AU779170B2/en not_active Ceased
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CA2382978A1 (en) | 2001-04-26 |
EP1221941A1 (en) | 2002-07-17 |
WO2001028523A1 (en) | 2001-04-26 |
EP1221941A4 (en) | 2005-11-30 |
CN1374859A (en) | 2002-10-16 |
AU779170B2 (en) | 2005-01-13 |
JP2003512315A (en) | 2003-04-02 |
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