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WO2011024029A1 - Fast disintegrating dosage forms of cinnarizine and dimenhydrinate combination - Google Patents

Fast disintegrating dosage forms of cinnarizine and dimenhydrinate combination Download PDF

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Publication number
WO2011024029A1
WO2011024029A1 PCT/IB2009/053702 IB2009053702W WO2011024029A1 WO 2011024029 A1 WO2011024029 A1 WO 2011024029A1 IB 2009053702 W IB2009053702 W IB 2009053702W WO 2011024029 A1 WO2011024029 A1 WO 2011024029A1
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WO
WIPO (PCT)
Prior art keywords
cinnarizine
dimenhydrinate
combination
fast
tablet
Prior art date
Application number
PCT/IB2009/053702
Other languages
French (fr)
Inventor
Farhad Farshi
Serdar Soylemez
Fikret Koc
Original Assignee
Abdi Ibrahim Ilac Sanayi Ve Ticaret Anonim Sirketi
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
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Application filed by Abdi Ibrahim Ilac Sanayi Ve Ticaret Anonim Sirketi filed Critical Abdi Ibrahim Ilac Sanayi Ve Ticaret Anonim Sirketi
Priority to PCT/IB2009/053702 priority Critical patent/WO2011024029A1/en
Publication of WO2011024029A1 publication Critical patent/WO2011024029A1/en

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates

Definitions

  • the present invention is related to fast dissolving or fast disintegrating dosage forms of combination of cinnarizine and dimenhydrinate.
  • Cinnarizine is an antihistamine and vasodilator and is delineated in patent of US
  • Dimenhydrinate is an antihistamine used as an antiemetic and against travel sickness and is described in patents of US 2,499,058 or US 2,534,813.
  • a compound preparation for dizziness comprising cinnarizine and dimenhydrinate is embraced by EP 1622622 and literature for example ; 'Supportive therapy with dimenhydrinate in combination with cinnarizine in vertigo' THERAPIEWOCHE 1996 GERMANY, Bd. 46, Nr. 3, 1996, Miracle 175.
  • the present invention provides a fast disintegrating dosage forms of cinnarizine and dimenhydrinate.
  • Fast disintegrating dosage forms include an effective amount of cinnarizine or a pharmaceutically acceptable salt thereof, and an effective amount of dimenhydrinate or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient.
  • pharmaceutical formulations are disintegrated in less than three minutes in oral cavity . More preferably, the pharmaceutical formulations are disintegrated in a oral cavity in less than two minutes and most preferably the pharmaceutical formulations are disintegrated in oral cavity in less than one minute.
  • One subject of the present invention is the use of fast disintegrating formulations of combination of cinnarizine and dimenhydrinate or their pharmaceutically acceptable salts for the treatment, amelioration or prevention of dizziness, including vertigo and Meniere's disorder.
  • the fast disintegrating formulations are used in treating all forms of vertigo. Vertigo which cannot be clearly diagnosed is included.
  • the pharmaceutical formulation is in a dosage form may be, but not limited to,rapidly disintegrating tablets, lingual strips, sublingual tablets, lyophilized wafers, granulated particles, sublingual strips, spray and whatsoever.
  • a fast-disintegrating tablets may have many numerous shapes, such as dish-like , ellipsoid , rods, granules, blocks, cubes with rounded edges, or any other shape suitable for pharmaceutical administration.
  • Cinnarizine and dimenhydrinate can be administered in pharmaceutically acceptable doses.
  • fast disintegrating or fast dissolving dosage form may include one or more pharmaceutically acceptable excipients, carriers, or diluents.
  • surfactants, diluents, sweeteners, disintegrants, binders, lubricants, glidants, colorants, flavors and mixtures thereof can be used.
  • Acceptable excipients are, but not limited to, calcium sulfate, starch, mannitol,
  • kaolin sorbitol, xylitol, sodium chloride, sodium bicarbonate, citric acid, powdered cellulose derivatives, microcrystalline cellulose, pullulan, silicified microcrystalline cellulose, ammonium bicarbonate, carrageenan, carbohydrates such as PharmaburstTM, magnesium carbonate, tribasic calcium phosphate, calcium sulfate, magnesium oxide, poloxamer,gums, hydroxypropyl methylcellulose, gelatin, mixtures thereof, and the like .
  • Diluents may be, but not limited to, mannitol, sorbitol, xylitol, microcrystalline
  • cellulose silicified microcrystalline cellulose , hydroxypropyl methylcellulose, hydroxypropyl cellulose , pullulan and fast dissolving carbohydrates such as
  • Glidants may be, but not limited to, silicon dioxide, colloidal silicon dioxide, calcium silicate, magnesium silicate, magnesium trisilicate, talc, starch , mixtures thereof or whatsoever.
  • Binders are, but not limited to, sodium alginate, cellulose, methylcellulose, ethyl- cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, sodium car- boxymethyl cellulose, polypropylpyrrolidone, polyvinylprrolidone, gelatin, polyethylene glycol, starch, pre-gelatinized starch, sugars, trehalose,
  • Lubricants may be, but not limited to, calcium stearate, glyceryl monostearate,
  • glyceryl behenate glyceryl palmitostearate, hydrogenated vegetable oil, light mineral oil, magnesium stearate, mineral oil, polyethylene glycol, poloxamer, sodium benzoate, sodium lauryl sulfate, sodium stearyl fumarate, stearic acid, talc, zinc stearate, mixtures thereof or whatsoever .
  • Disintegrants are, but not limited to, sodium starch glycolate, sodium carboxymethyl cellulose, calcium carboxymethyl cellulose, croscarmellose sodium, crospovidone, alginic acid, chitosan, methyl cellulose, microcrystalline cellulose, powdered cellulose, lower alkylsubstituted hydroxypropyl cellulose, polacrilin potassium, starch, prege- latinized starch, sodium alginate, mixtures thereof or whatsoever.
  • Flavors are, but not limited to, cinnamon oil,essence of apple, essence of pear,
  • Sweeteners are but not limited to, corn syrup, dextrose, invert sugar, fructose,
  • saccharin aspartame, acesulfame-K, Stevia rebaudiana, sucralose, sorbitol, mannitol, zylitol, mixtures thereof and the like.
  • the fast-disintegrating or fast dissolving dosage form of combination of cinnarizine and dimenhydrinate is a solid dosage form that does not require water for swallowing.
  • These fast disintegrating or fastdissolving dosage forms are typically tablets and thin films that dissolve or disperse rapidly when in contact with saliva.
  • compositions of the present invention can be prepared through using pharmaceutical technologies including, but not limited to, spray drying, freeze-drying, heat molding,tablet molding, sublimation, consumable thin film manufacture and tablet .
  • Fast dissolving and/or fast disintegrating dosage forms of combination of cinnarizine and dimenhydrinate are selected from the group consisting of lingual strips, sublingual strips, oral mists, rapidly disintegrating tablets, lyophilized wafers, granulated particles and gums.
  • Cinnarizine and dimenhydrinate can be in microparticulate form with one or more excipients. Microparticulation can also be usedas taste-masking method.
  • microencapsulation methods can also be applied to cinnarizine and dimenhydrinate.
  • Excipients useful for microencapsulation, are, but not limited to, methylcellulose phthalate; hydroxypropylmethylcellulose phthalate; hy- droxypropylmethylcellulose succinate; hydroxyethyl-ethylcellulose phthalate, cellulose aceto succinate, polylactic acid, polyglycolic acid, polyvinyl alcohol, cellulose acetate phthalate, ethyl cellulose, resins, proteins, gelatinized starch, gums, cyclodextrins, chitosan, liposomes, ammonium hydroxide, sodium hydroxide, potassium hydroxide, magnesium hydroxide, calcium hydroxide, triethylamine, diethylamine, trimethylamine, methylamine, dimethylamine, isopropylamine, triethanolamine, di- ethanolamine, disodium monohydrogen phosphate
  • one or more taste masking ex- cipients such as flavors, sweeteners, acidic amino acids, lipids, and surfactants can be used.
  • Another embodiment of the present invention provides a carbohydrate-based fast dissolving dosage form.
  • Co-processed carbohydrates can be used in embodiments.
  • one or more sugar - based excipients may be used. These excipients are, but not limited to, amylose, dextrose, fructose, sucrose,maltose, erythritol, isomalt, lacitol, maltitol, mannitol, sorbitol, starch hydrolysate, polydextrose, glucose, xylitol, mixtures thereof and the like.
  • inert solid ingredients that volatize readily are, but not limited to, urea, ammonium bicarbonate, ammonium carbonate, hexamethylene tetramine, naphthalene, phthalic anhydride, benzoic acid, camphor, menthol, mixtures of thereof and the like.
  • any method can be used such as, but not limited to, extrusion, film coating, casting and the like.
  • the film-forming agents are but not limited to, pullulan, hydroxypropylmethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, polyvinyl pyrrolidone, car- boxymethyl cellulose, polyvinyl alcohol, sodium alginate, polyethylene glycol, xanthan gum, tragacanth gum, guar gum, acacia gum, arabic gum, locust bean gum, polyacrylic acid, methylmethacrylate copolymer, carboxyvinyl polymer, amylose, high amylose starch, hydroxypropylated high amylose starch, dextrin, pectin, chitin, chitosan, levan, elsinan, collagen, gelatin, zein, gluten, soy protein isolate,whey protein isolate, casein, mixtures thereof and
  • Tablet molding excipients are, but not limited to polyvinyl alcohol, methylcellulose, hydroxyethyl cellulose, hydroxypropyl cellulose , hydroxypropyl starch, starch , mixtures thereof and the like.
  • Fast disintegrating or fast dissolving pharmaceutical formulations may be prepared by different methods as below;
  • active pharmaceutical ingredients may be granulated seperately and then granulates may be assemblied namely the active pharmaceutical ingredients are each dispersed within its own pharmaceutically acceptable carrier .
  • One of them may be direct compression (DC) form.
  • One active pharmaceutical ingredient may be granulated and then granulated active pharmaceutical ingredient may be assemblied with non granulated active pharmaceutical ingredient
  • One active pharmaceutical ingredient may be dissolved alone or with one or more excipient and then other active pharmaceutical ingredient alone or with one or more excipients may be coated with said solution
  • One active pharmaceutical ingredient may be dispersed alone or with one or more excipient and then other active pharmaceutical ingredient alone or with one or more excipient may be coated with said dispersion
  • a bilayer pharmaceutical tablet comprising a first layer containing dimenhydrinate and a second layer containing cinnarizine or vice versa .
  • a tablet-in-tablet composition comprising: a) a core tablet
  • a compressed outer tablet layer comprising cinnarizine or vice versa .

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
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Abstract

The present invention is related to fast dissolving or fast disintegrating dosage forms of combination of cinnarizine and dimenhydrinate.

Description

Description
Title of Invention: FAST DISINTEGRATING DOSAGE FORMS OF CINNARIZINE AND DIMENHYDRINATE COMBINATION
[1] The present invention is related to fast dissolving or fast disintegrating dosage forms of combination of cinnarizine and dimenhydrinate.
[2] Cinnarizine is an antihistamine and vasodilator and is delineated in patent of US
2,882,271.
[3] Dimenhydrinate is an antihistamine used as an antiemetic and against travel sickness and is described in patents of US 2,499,058 or US 2,534,813.
[4] A compound preparation for dizziness comprising cinnarizine and dimenhydrinate is embraced by EP 1622622 and literature for example ; 'Supportive therapy with dimenhydrinate in combination with cinnarizine in vertigo' THERAPIEWOCHE 1996 GERMANY, Bd. 46, Nr. 3, 1996, Seite 175.
[5] The present invention provides a fast disintegrating dosage forms of cinnarizine and dimenhydrinate. Fast disintegrating dosage forms include an effective amount of cinnarizine or a pharmaceutically acceptable salt thereof, and an effective amount of dimenhydrinate or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient.
[6] According to this invention, In fast disintegrating dosage forms, pharmaceutical formulations are disintegrated in less than three minutes in oral cavity . More preferably, the pharmaceutical formulations are disintegrated in a oral cavity in less than two minutes and most preferably the pharmaceutical formulations are disintegrated in oral cavity in less than one minute.
[7] One subject of the present invention is the use of fast disintegrating formulations of combination of cinnarizine and dimenhydrinate or their pharmaceutically acceptable salts for the treatment, amelioration or prevention of dizziness, including vertigo and Meniere's disorder. The fast disintegrating formulations are used in treating all forms of vertigo. Vertigo which cannot be clearly diagnosed is included.
[8] Fast-dissolving or fast-disintegrating tablets are useful for elderly people, children and patients who have difficulties swallowing tablets. Such peoples are unwilling and/ or unable to swallow tablets, capsules or other traditional solid dosage forms. This is especially the case of pharmaceuticals for paediatric or geriatric use. Where patients who are not able to take it with water, fast disintegrating dosage forms would be beneficial . To solve this problem, tablets that disintegrate rapidly in the mouth was developed. Such tablets are rapidly disintegrated when contact with saliva in the oral cavity. [9] According to this invention, the pharmaceutical formulation is in a dosage form may be, but not limited to,rapidly disintegrating tablets, lingual strips, sublingual tablets, lyophilized wafers, granulated particles, sublingual strips, spray and whatsoever.
[10] A fast-disintegrating tablets may have many numerous shapes, such as dish-like , ellipsoid , rods, granules, blocks, cubes with rounded edges, or any other shape suitable for pharmaceutical administration.
[11] Cinnarizine and dimenhydrinate can be administered in pharmaceutically acceptable doses.
[12] According to this invention, fast disintegrating or fast dissolving dosage form may include one or more pharmaceutically acceptable excipients, carriers, or diluents. In fast disintegrating or fast dissolving formulations, surfactants, diluents, sweeteners, disintegrants, binders, lubricants, glidants, colorants, flavors and mixtures thereof can be used.
[13] Acceptable excipients are, but not limited to, calcium sulfate, starch, mannitol,
kaolin, sorbitol, xylitol, sodium chloride, sodium bicarbonate, citric acid, powdered cellulose derivatives, microcrystalline cellulose, pullulan, silicified microcrystalline cellulose, ammonium bicarbonate, carrageenan, carbohydrates such as Pharmaburst™, magnesium carbonate, tribasic calcium phosphate, calcium sulfate, magnesium oxide, poloxamer,gums, hydroxypropyl methylcellulose, gelatin, mixtures thereof, and the like .
[14] Diluents may be, but not limited to, mannitol, sorbitol, xylitol, microcrystalline
cellulose, silicified microcrystalline cellulose , hydroxypropyl methylcellulose, hydroxypropyl cellulose , pullulan and fast dissolving carbohydrates such as
Pharmaburst™, mixtures thereof and the like.
[15] Glidants may be, but not limited to, silicon dioxide, colloidal silicon dioxide, calcium silicate, magnesium silicate, magnesium trisilicate, talc, starch , mixtures thereof or whatsoever.
[16] Binders are, but not limited to, sodium alginate, cellulose, methylcellulose, ethyl- cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, sodium car- boxymethyl cellulose, polypropylpyrrolidone, polyvinylprrolidone, gelatin, polyethylene glycol, starch, pre-gelatinized starch, sugars, trehalose,
glucose,tragacanth, sorbitol, acacia, alginates, carrageenan, xanthan gum, locust bean gum and gum arabic, waxes, poly acrylamide , mixtures thereof, and whatsoever.
[17] Lubricants may be, but not limited to, calcium stearate, glyceryl monostearate,
glyceryl behenate, glyceryl palmitostearate, hydrogenated vegetable oil, light mineral oil, magnesium stearate, mineral oil, polyethylene glycol, poloxamer, sodium benzoate, sodium lauryl sulfate, sodium stearyl fumarate, stearic acid, talc, zinc stearate, mixtures thereof or whatsoever . [18] Disintegrants are, but not limited to, sodium starch glycolate, sodium carboxymethyl cellulose, calcium carboxymethyl cellulose, croscarmellose sodium, crospovidone, alginic acid, chitosan, methyl cellulose, microcrystalline cellulose, powdered cellulose, lower alkylsubstituted hydroxypropyl cellulose, polacrilin potassium, starch, prege- latinized starch, sodium alginate, mixtures thereof or whatsoever.
[19] Flavors are, but not limited to, cinnamon oil,essence of apple, essence of pear,
essence of peach, essence of grape, essence of strawberry, essence of raspberry, essence of cherry ,essence of plum, essence of pineapple, essence of apricot, oil of win- tergreen, peppermint oils, clove oil, bay oil, anise oil, eucalyptus, thyme oil, cedar leaf oil, oil of nutmeg, oil of sage, oil of bitter almonds, cassia oil, citrus oils such as lemon, orange, grape, lime and grapefruit , vanilla, benzaldehyde , aldehyde C- 8 , aldehyde C-9, aldehyde C- 12 , tolyl aldehyde , mixtures thereof or whatsoever.
[20] Sweeteners are but not limited to, corn syrup, dextrose, invert sugar, fructose,
saccharin, aspartame, acesulfame-K, Stevia rebaudiana, sucralose, sorbitol, mannitol, zylitol, mixtures thereof and the like.
[21] Other ingredients such as colorants and titanium dioxide can also be used.
[22] The fast-disintegrating or fast dissolving dosage form of combination of cinnarizine and dimenhydrinate is a solid dosage form that does not require water for swallowing.
[23] These fast disintegrating or fastdissolving dosage forms are typically tablets and thin films that dissolve or disperse rapidly when in contact with saliva.
[24] The compositions of the present invention can be prepared through using pharmaceutical technologies including, but not limited to, spray drying, freeze-drying, heat molding,tablet molding, sublimation, consumable thin film manufacture and tablet .
[25] In case of tablet is prefereed, it comprising sugar-based excipients, super-disintegrating agents , effervescent agents and further suitable excipients .
[26] Fast dissolving and/or fast disintegrating dosage forms of combination of cinnarizine and dimenhydrinate are selected from the group consisting of lingual strips, sublingual strips, oral mists, rapidly disintegrating tablets, lyophilized wafers, granulated particles and gums.
[27] Cinnarizine and dimenhydrinate can be in microparticulate form with one or more excipients. Microparticulation can also be usedas taste-masking method.
[28] To reduce the unpleasant taste, microencapsulation methods can also be applied to cinnarizine and dimenhydrinate. Excipients, useful for microencapsulation, are, but not limited to, methylcellulose phthalate; hydroxypropylmethylcellulose phthalate; hy- droxypropylmethylcellulose succinate; hydroxyethyl-ethylcellulose phthalate, cellulose aceto succinate, polylactic acid, polyglycolic acid, polyvinyl alcohol, cellulose acetate phthalate, ethyl cellulose, resins, proteins, gelatinized starch, gums, cyclodextrins, chitosan, liposomes, ammonium hydroxide, sodium hydroxide, potassium hydroxide, magnesium hydroxide, calcium hydroxide, triethylamine, diethylamine, trimethylamine, methylamine, dimethylamine, isopropylamine, triethanolamine, di- ethanolamine, disodium monohydrogen phosphate, dipotassium monohydrogen phosphate, mixtures thereof and the like. Preparation microencapsulation methods are, but not limited to extrusion, spray-drying, coacervation, spray-chilling, fluidization, spray-congealing,phase separation,mixtures thereof and the like.
[29] In fast dissolving or fast disintegrating dosage forms one or more taste masking ex- cipients such as flavors, sweeteners, acidic amino acids, lipids, and surfactants can be used.
[30] Another embodiment of the present invention provides a carbohydrate-based fast dissolving dosage form. Co-processed carbohydrates can be used in embodiments.
[31] In case of preferred embodiment is created by sugar-based fast-dissolving method, one or more sugar - based excipients may be used. These excipients are, but not limited to, amylose, dextrose, fructose, sucrose,maltose, erythritol, isomalt, lacitol, maltitol, mannitol, sorbitol, starch hydrolysate, polydextrose, glucose, xylitol, mixtures thereof and the like.
[32] In case of preferred embodiment is created by sublimation method inert solid ingredients that volatize readily are, but not limited to, urea, ammonium bicarbonate, ammonium carbonate, hexamethylene tetramine, naphthalene, phthalic anhydride, benzoic acid, camphor, menthol, mixtures of thereof and the like.
[33] In case of preferred embodiment is created by thin film delivery method any method can be used such as, but not limited to, extrusion, film coating, casting and the like. The film-forming agents are but not limited to, pullulan, hydroxypropylmethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, polyvinyl pyrrolidone, car- boxymethyl cellulose, polyvinyl alcohol, sodium alginate, polyethylene glycol, xanthan gum, tragacanth gum, guar gum, acacia gum, arabic gum, locust bean gum, polyacrylic acid, methylmethacrylate copolymer, carboxyvinyl polymer, amylose, high amylose starch, hydroxypropylated high amylose starch, dextrin, pectin, chitin, chitosan, levan, elsinan, collagen, gelatin, zein, gluten, soy protein isolate,whey protein isolate, casein, mixtures thereof and the like.
[34] In case of preferred embodiment is created by tablet molding method, water-soluble ingredients are used so that tablet disintegrate and dissolve rapidly. Tablet molding excipients are, but not limited to polyvinyl alcohol, methylcellulose, hydroxyethyl cellulose, hydroxypropyl cellulose , hydroxypropyl starch, starch , mixtures thereof and the like.
[35] Fast disintegrating or fast dissolving pharmaceutical formulations may be prepared by different methods as below;
[36] -Both active pharmaceutical ingredients may be granulated seperately and then granulates may be assemblied namely the active pharmaceutical ingredients are each dispersed within its own pharmaceutically acceptable carrier . One of them may be direct compression (DC) form.
[37] -One active pharmaceutical ingredient may be granulated and then granulated active pharmaceutical ingredient may be assemblied with non granulated active pharmaceutical ingredient
[38] - One active pharmaceutical ingredient may be dissolved alone or with one or more excipient and then other active pharmaceutical ingredient alone or with one or more excipients may be coated with said solution
[39] - One active pharmaceutical ingredient may be dispersed alone or with one or more excipient and then other active pharmaceutical ingredient alone or with one or more excipient may be coated with said dispersion
[40] In case of choice is fast dissolving or fast disintegrating dosage form it may be in the form of bilayer tablet or tablet in tablet. A bilayer pharmaceutical tablet comprising a first layer containing dimenhydrinate and a second layer containing cinnarizine or vice versa . A tablet-in-tablet composition comprising: a) a core tablet
comprising: dimenhydrinate and b) a compressed outer tablet layer comprising cinnarizine or vice versa .
[41] Example 1- Orally Disintegrating Tablet Dosage Form
[Table 1]
[Table ]
Figure imgf000006_0001

Claims

Claims
[Claim 1] A fast disintegrating or fast dissolving dosage form of cinnarizine and dimenhydrinate combination, comprising:
- an effective amount of cinnarizine or a pharmaceutically acceptable salt and
- an effective amount of dimenhydrinate or a pharmaceutically acceptable salt thereof and
- at least one pharmaceutically acceptable excipient.
[Claim 2] According to claim 1, the fast disintegrating or fast dissolving dosage form of cinnarizine and dimenhydrinate combination is disintegrated in oral cavity in less than three minutes.
[Claim 3] According to claim 2, the fast disintegrating or fast dissolving dosage dosage form of cinnarizine and dimenhydrinate combination is disintegrated in oral cavity in less than two minutes.
[Claim 4] According to claim 3, the fast disintegrating or fast dissolving dosage dosage form of cinnarizine and dimenhydrinate combination is disintegrated in oral cavity in less than one minutes.
[Claim 5] The pharmaceutical formulation according to claim 1, wherein the pharmaceutical formulation is in a dosage form selected from the group consisting of lingual strips, sublingual strips, oral mists, orally disintegrating tablets, lyophilized wafers, granulated particles and gums.
[Claim 6] The pharmaceutical formulation as claimed in claim 5 is orally disintegrating tablet
[Claim 7] As claimed in claim 6, orally disintegrating tablets are in the form of bilayer tablet or tablet in tablet
[Claim 8] Pharmaceutical composition according to claim 1 , a pharmaceutical composition for the treatment, amelioration or prevention of dizziness, including vertigo and Meniere's disorder.
[Claim 9] A preparation method of cinnarizine and dimenhydrinate combination characterized in that both active pharmaceutical ingredients are seperately granulated and then granulates are assemblied .
[Claim 10] A preparation method of cinnarizine and dimenhydrinate combination characterized in that cinnarizine or dimenhydrinate may be granulated and then granulated active pharmaceutical ingredient is assemblied with non granulated active pharmaceutical ingredient
[Claim 11] A preparation method of cinnarizine and dimenhydrinate combination characterized in that cinnarizine or dimenhydrinate is dissolved alone or with one or more excipient and then other active pharmaceutical ingredient alone or with one or more excipients are coated with said solution.
[Claim 12] A preparation method of cinnarizine and dimenhydrinate combination characterized in that cinnarizine or dimenhydrinate is dispersed alone or with one or more excipients and then other active pharmaceutical ingredient alone or with one or more excipients are coated or adhered with said dispersion
PCT/IB2009/053702 2009-08-24 2009-08-24 Fast disintegrating dosage forms of cinnarizine and dimenhydrinate combination WO2011024029A1 (en)

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Cited By (4)

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Publication number Priority date Publication date Assignee Title
WO2012175747A1 (en) * 2011-06-24 2012-12-27 Hennig Arzneimittel Gmbh & Co. Kg Production method and dosage form
WO2013060343A1 (en) * 2011-10-25 2013-05-02 Expermed S.A. Sublingual pharmaceutical composition containing an antihistamine agent and method for the preparation thereof
AU2011379627B2 (en) * 2011-10-25 2015-09-10 Expermed S.A. Sublingual pharmaceutical composition containing an antihistamine agent and method for the preparation thereof
US9675551B2 (en) 2011-10-25 2017-06-13 Expermed S.A. Sublingual pharmaceutical composition containing an antihistamine agent and method for the preparation thereof
WO2014001268A1 (en) * 2012-06-25 2014-01-03 Hennig Arzneimittel Gmbh & Co. Kg Pharmaceutical form for extended release of active substances
KR20150041612A (en) * 2012-06-25 2015-04-16 헨니그 아르쯔나이미텔 게엠베하 운트 코. 카게 Pharmaceutical form for extended release of active substances
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EA035815B1 (en) * 2012-06-25 2020-08-14 Хенниг Арцнаймиттель Гмбх Унд Ко. Кг Pharmaceutical form in form of a layer tablet, method for the production thereof and use thereof for treating vertigo
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CN108578378A (en) * 2018-07-25 2018-09-28 江苏黄河药业股份有限公司 A kind of dramamine oral disnitegration tablet and preparation method thereof

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