WO2002087544A1 - Flavored product containing medicament or other active agent - Google Patents
Flavored product containing medicament or other active agent Download PDFInfo
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- WO2002087544A1 WO2002087544A1 PCT/US2001/009478 US0109478W WO02087544A1 WO 2002087544 A1 WO2002087544 A1 WO 2002087544A1 US 0109478 W US0109478 W US 0109478W WO 02087544 A1 WO02087544 A1 WO 02087544A1
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- agent
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- medicament
- compressible
- individual
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
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 products that provide a pleasant taste.
- 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.
- 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 absorption 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 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.
- 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 a ⁇ iministration 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 medicament or agent to an individual. Improved formulations including medicaments and agents are also provided by the present invention.
- compacted powders are provided including medicaments or agents.
- the medicament or agent, in a powder form is mixed with at least a masking agent, the resultant powder is then compressed or compacted into a defined shape. It has been found that the masking agent and medicament in a compacted powder form provides a product that covers up the bitter and bad flavors produced by the medicament or agent while allowing the product to be delivered through the buccal cavity.
- 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.
- the present invention provides a compacted powder including medicament that is designed to dissolve in the mouth of the user or that can be chewed.
- the compacted powder medicament includes a sufficient amount of a masking agent to improve the organoleptic properties of the powdered formula.
- the powder includes a release agent.
- the medicament is chosen from the group consisting of: analgesics; muscle relaxants; antihistamines; decongestants; antacids; anti- inflammatories; 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; sucrolose; saccharin; fructose; xylitol; spray dried licorice root; glycyrrhizin; 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 release agent is chosen from the group consisting of calcium and magnesium stearate.
- the present invention provides a method for delivering a medicament to an individual comprising the steps of: providing a compressible formulation that includes a medicament in powder form and a sufficient amount of a masking agent to provide acceptable organoleptic properties, the compressible formulation being compressed into a defined structure; and allowing at least a portion of the defined structure 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.
- the compressible formulation includes a compressible mono or di-saccharide, e.g., dextrose or sucrose, or a combination, or compressible sugar alcohols, e.g., sorbitol, mannitol, and iso-maltitol.
- a compressible mono or di-saccharide e.g., dextrose or sucrose, or a combination
- compressible sugar alcohols e.g., sorbitol, mannitol, and iso-maltitol.
- the quantity of which is chosen so that it masks the taste of the medicaments.
- the present invention provides a method of enhancing an individual's performance, the method comprising the steps of: providing a compressible powder formulation including a performance enhancing amount of caffeine in powder form and a masking agent; compressing the powder into a solid structure; and allowing at least a portion of the solid structure to dissolve in the mouth of the individual not more than ten minutes before the performance.
- the performance to be enhanced is athletic.
- the performance to be enhanced is cognitive.
- 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 compacted formulation that contains a stimulant and a masking agent; and placing the compacted formulation into the buccal cavity causing the stimulant to be released by the compacted formulation into an oral mucosa located in a buccal cavity of the individual.
- the present invention provides a compressible 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 compressible 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; compacting the compressible formulation into a defined structure; placing the defined structure in a buccal cavity of an individual; and allowing at least a portion of the defined structure to dissolve in the buccal cavity.
- the present invention provides a product including a medicament.
- the product includes a compressible powder medicament having an offensive taste; a sufficient amount of a compressible masking agent to provide acceptable organoleptic properties; and a release agent. Accordingly, an advantage of the present invention is to provide new methods and compositions 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.
- an advantage of the present invention is to provide improved methods 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.
- a medicament or agent is contained in a compacted 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 a 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 su ⁇ risingly found that by solubilizing a powdered matrix of medicament and masking agent, this increases the ability of the masking agent to cover up any bitter and/or 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.
- astringent flavor such as aspirin
- masking agents found to be effective against astringency
- astringency such as fructose and high-intensity sweeteners, e.g., sucrolose, saccharin, aspartame, and acesulfame-K.
- a moderately bitter active ingredient such as caffeine
- ingredients such as glycine, ethyl maltol, zinc gluconate, licorice root powder, high- intensity sweeteners, etc.
- combinations of these masking agents or larger quantities may have to be used in order to combat the undesirable bitterness, e.g., peppermint and a high- intensity sweetener.
- the masking agents are selected from the group consisting of: sucrolose; zinc gluconate; ethyl maltol; glycine; acesulfame-K; aspartame; saccharin; fructose; xylitol; maltitol; isomalt; spray dried licorice root; glycyrrhizin; sodium gluconate; glucono delta-lactone; ethyl vanillin; and vanillin.
- the powder formulation can be compacted into a pill-like, mint-like, tablet-like, or similar structure.
- the compacted powder has a matte finish, although if desired, the product can be coated.
- the compacted powder formulation is placed in the mouth of the user. Due to the present invention, as the compacted powder formulation begins to dissolve, it has acceptable organoleptic properties allowing the consumer to maintain the product in his mouth for a sufficient time to allow as much of the product as possible to dissolve. As the product dissolves, the powder medicament or agent is released into the saliva. The medicament or agent in the saliva then passes through the oral mucosa in the buccal cavity.
- the oral mucosa has a thin epithelium and a rich vascularity.
- the oral mucosa favors drug abso ⁇ tion.
- a typically orally ingested drug wherein the solution is in contact too briefly for abso ⁇ tion to be appreciable through the oral mucous
- an increase in the abso ⁇ tion of the drug is achieved as 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.
- 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.
- active agent refers to a compound that has a desired therapeutic or physiological effect once ingested and/or metabolized.
- the therapeutic effect may be one which decreases the growth of a xenobiotic or other gut flora or fauna, alters the activity of an enzyme, provides the physical relief from a malady (e.g., diminishes pain, acid reflux, or other discomfort), has an effect on the brain chemistry of molecules that determine mood and behavior.
- a malady e.g., diminishes pain, acid reflux, or other discomfort
- the active agent may be any agent that is traditionally used as a medicament and lends itself to being administered through the oral cavity.
- active agents may be vitamins, cancer chemotherapeutics; antimycotics; oral contraceptives, nicotine, nicotine replacement agents, minerals, analgesics, antacids, muscle relaxants, antihistamines, decongestants, anesthetics, antitussives, diuretics, anti-inflammatories, antibiotics, antivirals, psychotherapeutic agents, anti-diabetic agents, and cardiovascular agents, bioengineered pharmaceuticals, nutraceuticals, and nutritional supplements.
- Vitamins and co-enzymes that may be delivered using this invention include but are not limited to water or fat soluble vitamins such as thiamin, riboflavin, nicotinic acid, pyridoxine, pantothenic acid, biotin, flavin, choline, inositol, and paraminobenzoic acid, carnitine, vitamin C, vitamin D, and its analogs, vitamin A and the carotenoids, retinoic acid, vitamin E, and vitamin K.
- water or fat soluble vitamins such as thiamin, riboflavin, nicotinic acid, pyridoxine, pantothenic acid, biotin, flavin, choline, inositol, and paraminobenzoic acid, carnitine, vitamin C, vitamin D, and its analogs, vitamin A and the carotenoids, retinoic acid, vitamin E, and vitamin K.
- cancer chemotherapeutics agents include, but are not limited to, cisplatin (CDDP), procarbazine, mechlorethamine, cyclophosphamide, camptothecin, ifosfamide, melphalan, chlorambucil, bisulfan, nitrosurea, dactinomycin: danunorubicin, doxorubicin, bleomycin, plicomycin, mitomycin, etoposide (VP16), tamoxifen, taxol, transplatinum, 5-fluorouracil, vincristin, vinblastin, and methotrexate or any analog or derivative variant thereof.
- CDDP cisplatin
- procarbazine mechlorethamine
- cyclophosphamide camptothecin
- ifosfamide ifosfamide
- melphalan chlorambucil
- bisulfan nitrosurea
- dactinomycin danunor
- Antimicrobial agents that may be used include, but are not limited to, naficillin, oxacillin, vancomycin, clindamycin, erythromycin, trimethoprim-sulphamethoxazole, rifampin, ciprofloxacin, broad spectrum penicillin, amoxicillin, gentamicin, ceftriazoxone, cefotaxime, chloramphenicol, clavunate, sulbactam, probenecid, doxycycline, spectinomycin, cefixime, penicillin G, minocycline, P-lactamase inhibitors; meziocillin, piperacillin, aztreonam, norfloxacin, trimethoprim, ceftazidime, dapsone.
- Antifungal agents that may be delivered include but are not limited to ketoconazole, fluconazole, nystatin, itraconazole, clomitrazole, and amphotericin B.
- Antiviral agents that may be used include but are not limited to acyclovir, trifluridine, idoxorudine, foscamet, ganciclovir, zidovudine, dideoxycytosine, dideoxyinosine, stavudine, famciclovir, didanosine, zalcitabine, rifimantadine, and cytokines.
- Antacids include cimetidine, ranitidine, nizatidine, famotidine, omeprazole, bismuth antacids, metronidazole antacids, t tracyloine antacids, clarthromycin antacids, hydroxides of aluminum, magnesium, sodium bicarbonates, calcium bicarbonate, and other carbonates, silicates, and phosphates.
- Antihistamines are represented by, but are not limited to, cimetidine, ranitidine, diphenydramine, prylamine, promethazine, chlo ⁇ heniramine, chlorcyclizine, terfenadrine, carbinoxamine maleate, clemastine fumarate, diphenhydramine hydrochloride, dimenhydrinate, prilamine maleate, tripelennamine hydrochloride, tripelennamine citrate, chlo ⁇ heniramine maleate, brompheniramine maleate, hydroxyzine pamoate, hydroxyzine hydrochloride, cyclizine lactate, cyclizine hydrochloride, meclizine hydrochloride, acrivastine, cetirizine hydrochloride, astemizole, levocabastine hydrochloride, and loratadine.
- Decongestants and antitussives include agents such as dextrometho ⁇ han hydrobromide, levopropoxyphene napsylate, noscapine, caretapentane, caramiphen, chlophedianol, pseudoephedrine hydrochloride, pseudoephedrine sulfate, phenylephidrine, diphenhydramine, glaucine, pholcodine, and benzonate.
- Anesthetics include etomidate, ketamine, propofol, and benodiazapines (e.g., chlordiazepoxide, diazepame, clorezepate, halazepam, flurazepam, quazepam, estazolam, triazolam, alprozolm, midazolam, temazepam, oxazepam, lorazepam), benzocaine, dyclonine, bupivacaine, etidocaine, lidocaine, mepivacaine, promoxine, prilocaine, procaine, proparcaine, ropivacaine, tetracaine.
- benodiazapines e.g., chlordiazepoxide, diazepame, clorezepate, halazepam, flurazepam, quazepam, estazolam, triazolam, alprozolm, mida
- Other useful agents may include amobartital, aprobarbital, butabarbital, butalbital mephobarbital, methohexital, pentobarbital, phenobarbital, secobarbital, thiopental, paral, chloralhydrate, ethchlorvynol, clutethimide, methoprylon, ethinamate, and meprobarnate.
- Analgesics include opioids and other medicaments such as mo ⁇ hine, mepidine, dentanyl, sufentranil, alfentanil, aspirin, acetaminophen, ibuprofen, indomethacine, naproxen, atrin, isocome, midrin, axotal, firinal, phrenilin, ergot, and ergot derivatives (wigraine, cafergot, ergostat, ergomar, dihydroergotamine), imitrex, and ketoprofen.
- opioids and other medicaments such as mo ⁇ hine, mepidine, dentanyl, sufentranil, alfentanil, aspirin, acetaminophen, ibuprofen, indomethacine, naproxen, atrin, isocome, midrin, axotal, firinal, phrenilin, ergot, and ergot derivatives (wigraine, ca
- Diuretics include but are not limited to acetazolamide, dichlo ⁇ henamide, methazolamide, furosemide, bumetanide, ethacrynic acid torseimde, azosemide, muzolimine, piretanide, tripamide, bendroflumethiazide, benthiazide, chlorothiazide, hydrochlorothiazide, hydroflumethiazide, methyclothiazide, polythiazide, trichlormethiazide, indapamide, metolazone, quinethazone, amiloride, triamterene, sprion olactone, canrenone, and potassium canrenoate.
- Anti-inflammatories include but are not limited to salicylic acid derivatives (e.g., aspirin), indole and indene acetic acids (indomethacin, sulindac, and etodalac) heteroaryl acetic acids (tolmetin diclofenac and ketorolac) aryl propionic acid derivatives (ibuprofen, naproxen, ketoprofen, fenopren, oxaprozine), anthranilic acids (mefanamic acid, meclofenamic acid) enolic acids (piroxicam, tenoxicam, phenylbutazone, and oxyphenthatrazone).
- salicylic acid derivatives e.g., aspirin
- indole and indene acetic acids indomethacin, sulindac, and etodalac
- heteroaryl acetic acids tolmetin diclofenac and ketorolac
- Psychotherapeutic agents include thorazine, serentil, mellaril, millazinetindal, permitil, prolixin, trilafon, stelazine, suprazine, taracf an, navan, haldol, halperon, loxitane, moban, orap, risperdal, alprazolam, chordiaepoxide, clonezepam, clorezepate, diazepam, halazepam, lorazepam, oxazepam, prazepam, buspirone, elvavil, anafranil, adapin, sinequan, tofranil, surmontil, asendin, no ⁇ ramin, pertofrane, ludiomil, pamelor, vivactil, prozac, luvox, paxil, zoloft, effexor, wellbutrin, serzone, desyrel, nard
- Cardiovascular agents include, but are not limited to, nitroglycerin, isosorbide dinitrate, sodium nitroprisside, captopril, enalaprill, enalaprilat, quinapril, lisinopril, ramipril, losartan, amrinone, linnone, vesnerinone, hydralazine, nicorandil, prozasin, doxazosin, bunazosin, tamulosin, yohimbine, propanolol, metoprolol, nadolol, atenolol, timolol, esmolol, pindolol, acebutolol, labetalol, phentolamine, carvedilol, bucindolol, verapamil, nifedipine, amlodipine, and dobutamine, or a sexual dysfunction agent like sildenafil
- the resultant product can be used to treat inter alia: coughs, colds, motion sickness; allergies; fevers; pain; inflammation; sore throats; cold sores; migraines; sinus problems; diarrhea; diabetes, gastritis; depression; anxiety, hypertension; angina, and other maladies and symptoms. Also these gums may be useful in ameliorating cravings in substance abuse withdrawal or for appetite suppression.
- Specific active agents or medicaments include by way of example and limitation: caffeine, aspirin, acetaminophen; ibuprofen; ketoprofen; cimetidine, ranitidine, famotidine, dramamine, omeprazole, dyclonine hydrochloride, chlo ⁇ heniramine maleate, pseudoephedrine hydrochloride, dextrometho ⁇ han hydrobromide, benzocaine, sodium naproxen, and nicotine.
- Nutraceuticals and nutritional supplements may also be added to the product as active agents.
- herbs and botanicals that include, but are not limited to, capsicum, chamomile, cat's claw, echinacea, garlic, ginger, ginko, various ginseng, green tea, golden seal, kava kava, nettle, passion flower, saw palmetto, St. John's wort, and valerian.
- mineral supplements such as calcium, copper, iodine, iron, magnesium, manganese, molybdenum, phosphorous, selenium, and zinc.
- nutraceuticals that also can be added to chewing gum as active agents are benzoin, fructo- oligosaccharides, glucosamine, grapeseed extract, guarana, inulin, phosphotidylserine, phytosterols, phytochemicals, isoflavones, lecithin, lycopene, oligofructose, polyphenol, and psyllium as well as weight loss agents such as chromium picolinate and phenylpropanolamine.
- 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 ngredient 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 compacted powdered formulation is selected so as to create, when the compacted powder formulation is placed in the mouth, a sufficiently high concentration of the medicament or agent in the saliva.
- the agent is a stimulant such as caffeine
- the level of the stimulant in the compacted 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 compacted powder formulation to create a salvia content of approximately 1% to about 66%.
- the agent For 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%.
- a metabolizer for example, chromium picolineate and hydroxi-chitic acid
- the agents should be present in an amount to create a saliva content of approximately 1% to about 66%.
- 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.
- the medicament is an analgesic
- the compacted powdered formulation would be taken on an as needed basis.
- 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 compacted 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 compacted powder product.
- acceptable organoleptic properties means that the compacted 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 compacted 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. Generally, it is believed that the masking agent will comprise approximately 50% to about 99+% 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
- 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 compacted 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. Bulk 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.
- Bulk 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. As noted earlier, in a preferred embodiment, approximately 1.5 to about 3.0 grams of bulk sweeteners are present in the product.
- 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, alitame, 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. If a low calorie formulation is desired, a low caloric bulking agent can be used.
- low caloric bulking agents examples include: polydextrose; Raftilose, Raftilin;
- 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. In addition to the medicament and masking agent, preferably the product includes a release agent. The release agent functions to release the product from the mold or similar apparatus during compacting or compression of the powder formulation. A variety of release agents can be used including calcium and magnesium stearate. Preferably, the release agent comprises approximately 0.5% to about 3% by weight of the product.
- the formulations would be constructed by blending a medicament in powder form with a powder masking agent and other components as desired.
- the powder can then be, for example, made into a compacted product by conventional tablet forming machines.
- the product then would be packaged in bottles, blister packs, strip packs, roll wraps, or tins.
- examples of some product including a medicament or agent are as follows: Example No. 1
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Zoology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
Claims
Priority Applications (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP01937161A EP1387672A1 (en) | 2001-04-17 | 2001-04-17 | Flavored product containing medicament or other active agent |
PCT/US2001/009478 WO2002087544A1 (en) | 2001-04-17 | 2001-04-17 | Flavored product containing medicament or other active agent |
CA002406552A CA2406552A1 (en) | 2001-04-17 | 2001-04-17 | Release of lipophilic active agents from chewing gum |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/US2001/009478 WO2002087544A1 (en) | 2001-04-17 | 2001-04-17 | Flavored product containing medicament or other active agent |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2002087544A1 true WO2002087544A1 (en) | 2002-11-07 |
Family
ID=21742437
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/US2001/009478 WO2002087544A1 (en) | 2001-04-17 | 2001-04-17 | Flavored product containing medicament or other active agent |
Country Status (3)
Country | Link |
---|---|
EP (1) | EP1387672A1 (en) |
CA (1) | CA2406552A1 (en) |
WO (1) | WO2002087544A1 (en) |
Cited By (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR101639580B1 (en) * | 2015-09-11 | 2016-07-14 | 주식회사한국야쿠르트 | Method for masking the bitters of food composition containing herbal medical extract and its products |
US9956211B2 (en) | 2011-04-29 | 2018-05-01 | Moberg Pharma Ab | Pharmaceutical compositions comprising a local anaesthetic such as bupivacaine for local administration to the mouth or throat |
US10772347B2 (en) * | 2018-02-23 | 2020-09-15 | Ankh Life Sciences Limited | Nutritional supplement |
JP2021004217A (en) * | 2019-06-27 | 2021-01-14 | 小林製薬株式会社 | Oral composition |
US11246902B2 (en) | 2018-02-23 | 2022-02-15 | Ankh Life Sciences Limited | Nutritional supplement for mammals |
CN114870430A (en) * | 2022-06-20 | 2022-08-09 | 信阳农林学院 | Continuous extraction device and extraction method for traditional Chinese medicine raw materials |
US11898184B2 (en) | 2017-09-07 | 2024-02-13 | Sweet Sense Inc. | Low glycemic sugar composition |
Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5262179A (en) * | 1989-09-13 | 1993-11-16 | Nicholas Kiwi Pty Ltd. | Non-effervescent ibuprofen compositions |
US5607697A (en) * | 1995-06-07 | 1997-03-04 | Cima Labs, Incorporated | Taste masking microparticles for oral dosage forms |
US5785989A (en) * | 1985-05-01 | 1998-07-28 | University Utah Research Foundation | Compositions and methods of manufacturing of oral dissolvable medicaments |
US5869098A (en) * | 1997-08-20 | 1999-02-09 | Fuisz Technologies Ltd. | Fast-dissolving comestible units formed under high-speed/high-pressure conditions |
US5980941A (en) * | 1997-08-20 | 1999-11-09 | Fuisz Technologies Ltd. | Self-binding shearform compositions |
US6077536A (en) * | 1990-04-07 | 2000-06-20 | Beecham Group Plc | Pharmaceutical formulation |
-
2001
- 2001-04-17 WO PCT/US2001/009478 patent/WO2002087544A1/en not_active Application Discontinuation
- 2001-04-17 EP EP01937161A patent/EP1387672A1/en not_active Withdrawn
- 2001-04-17 CA CA002406552A patent/CA2406552A1/en not_active Abandoned
Patent Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5785989A (en) * | 1985-05-01 | 1998-07-28 | University Utah Research Foundation | Compositions and methods of manufacturing of oral dissolvable medicaments |
US5262179A (en) * | 1989-09-13 | 1993-11-16 | Nicholas Kiwi Pty Ltd. | Non-effervescent ibuprofen compositions |
US6077536A (en) * | 1990-04-07 | 2000-06-20 | Beecham Group Plc | Pharmaceutical formulation |
US5607697A (en) * | 1995-06-07 | 1997-03-04 | Cima Labs, Incorporated | Taste masking microparticles for oral dosage forms |
US5869098A (en) * | 1997-08-20 | 1999-02-09 | Fuisz Technologies Ltd. | Fast-dissolving comestible units formed under high-speed/high-pressure conditions |
US5980941A (en) * | 1997-08-20 | 1999-11-09 | Fuisz Technologies Ltd. | Self-binding shearform compositions |
Cited By (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US9956211B2 (en) | 2011-04-29 | 2018-05-01 | Moberg Pharma Ab | Pharmaceutical compositions comprising a local anaesthetic such as bupivacaine for local administration to the mouth or throat |
US10493068B2 (en) | 2011-04-29 | 2019-12-03 | Moberg Pharma Ab | Pharmaceutical compositions comprising a local anaesthetic such as bupivacaine for local administration to the mouth or throat |
KR101639580B1 (en) * | 2015-09-11 | 2016-07-14 | 주식회사한국야쿠르트 | Method for masking the bitters of food composition containing herbal medical extract and its products |
US11898184B2 (en) | 2017-09-07 | 2024-02-13 | Sweet Sense Inc. | Low glycemic sugar composition |
US10772347B2 (en) * | 2018-02-23 | 2020-09-15 | Ankh Life Sciences Limited | Nutritional supplement |
US11246902B2 (en) | 2018-02-23 | 2022-02-15 | Ankh Life Sciences Limited | Nutritional supplement for mammals |
JP2021004217A (en) * | 2019-06-27 | 2021-01-14 | 小林製薬株式会社 | Oral composition |
JP7263151B2 (en) | 2019-06-27 | 2023-04-24 | 小林製薬株式会社 | oral composition |
CN114870430A (en) * | 2022-06-20 | 2022-08-09 | 信阳农林学院 | Continuous extraction device and extraction method for traditional Chinese medicine raw materials |
CN114870430B (en) * | 2022-06-20 | 2023-06-13 | 信阳农林学院 | Traditional Chinese medicine raw material continuous extraction device and extraction method |
Also Published As
Publication number | Publication date |
---|---|
CA2406552A1 (en) | 2002-11-07 |
EP1387672A1 (en) | 2004-02-11 |
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