WO2005051489A2 - Fast dissolving solid oral dosage forms of galanthamine - Google Patents

Fast dissolving solid oral dosage forms of galanthamine Download PDF

Info

Publication number
WO2005051489A2
WO2005051489A2 PCT/IB2004/003832 IB2004003832W WO2005051489A2 WO 2005051489 A2 WO2005051489 A2 WO 2005051489A2 IB 2004003832 W IB2004003832 W IB 2004003832W WO 2005051489 A2 WO2005051489 A2 WO 2005051489A2
Authority
WO
WIPO (PCT)
Prior art keywords
fast
tablet
dissolving
dissolving tablet
tablet according
Prior art date
Application number
PCT/IB2004/003832
Other languages
French (fr)
Other versions
WO2005051489A3 (en
Inventor
Swati Aggarwal
Romi Barat Singh
Vishnubhotla Naga Prasad
Sanjeev Kumar Sethi
Original Assignee
Ranbaxy Laboratories Limited
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ranbaxy Laboratories Limited filed Critical Ranbaxy Laboratories Limited
Publication of WO2005051489A2 publication Critical patent/WO2005051489A2/en
Publication of WO2005051489A3 publication Critical patent/WO2005051489A3/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Definitions

  • the present invention relates to fast-dissolving oral dosage forms of galanthamine for oral administration and processes for the preparation thereof.
  • Alzheimer's disease is the most common form of dementia among older people. Dementia is a collective name for progressive degenerative brain syndromes which affect memory, thinking, behaviour and emotion. Alzheimer's disease involves the parts of the brain that control thought, memory, and language. The primary symptoms include memory loss, disorientation, confusion and problems with reasoning and thinking. These symptoms worsen as brain cells die and the connections between cells are lost.
  • Galanthamine or galantamine is a tertiary alkaloid which is derived from the bulbs of the common snowdrop ⁇ Galanthus nivalis) and several Amaryllidaceae plants. Galanthamine belongs to the class of drugs called as acetylcholinesterase inhibitors.
  • galanthamine has been approved in several countries for the symptomatic treatment of senile dementia of the Alzheimer's type. Prior to its use in patients with Alzheimer's, galantamine was available in Eastern Europe as a curare-reversal agent in anesthesia to reverse the neuromuscular paralysis induced by turbocurarine-like muscle relaxants and as a treatment for neurologic conditions, such as myasthenia gravis.
  • Patent No 6,099,863 discloses a fast-dissolving tablet of galanthamine hydrobromide which includes a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier.
  • the carrier includes a spray- dried mixture of lactose monohydrate and microcrystalline cellulose (75:25) as a diluent, and an insoluble or poorly soluble cross-linked polymer disintegrant.
  • fast-dissolving tablets of galanthamine hydrobromide can be prepared without using either a spray-dried mixture of lactose monohydrate and microcrystalline cellulose (75:25) as a diluent or an insoluble or poorly soluble cross-linked polymer as disintegrant.
  • a fast-dissolving tablet which includes a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier, wherein the carrier includes a spray-dried mixture of lactose monohydrate and microcrystalline cellulose (75:25) as a diluent and a water-soluble disintegrant.
  • the galanthamine hydrobromide may include from about 1 % to about 15 % w/w of the tablet.
  • the carrier may include from about 50 % to about 95 % w/w of the tablet or it may include about 80 % to about 95 % w/w of the tablet.
  • the water-soluble disintegrant may include one or more of pregelatinized starch, sodium carboxymethyl cellulose and sodium alginate.
  • the water soluble disintegrant may be pregelatinized starch.
  • the tablet may further include a lubricant and a glidant.
  • a fast-dissolving tablet which includes a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier, wherein the carrier includes a simple blend of lactose monohydrate and microcrystalline cellulose as a diluent and a water-soluble disintegrant.
  • a fast-dissolving tablet which includes a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier, wherein the carrier includes a simple blend of lactose monohydrate and microcrystalline cellulose as a diluent and a poorly soluble or insoluble disintegrant.
  • the poorly soluble or insoluble disintegrant may include one or more of cross- linked povidone, cross-linked carboxymethylcellulose, sodium starch glycolate and croscarmellose sodium.
  • the poorly soluble or insoluble disintegrant may be cross-linked povidone.
  • a fast-dissolving tablet which includes a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier, wherein the carrier includes anhydrous lactose as a diluent and a water-soluble disintegrant.
  • a fast-dissolving tablet which includes a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier, wherein the carrier includes anhydrous lactose as a diluent and an insoluble or poorly soluble cross-linked polymer as disintegrant.
  • a process for preparing a fast dissolving tablet of galanthamine hydrobromide is provided.
  • the process includes blending galanthamine hydrobromide, a pharmaceutically acceptable carrier, and a disintegrant to form a mixture; and compressing the mixture into a tablet using appropriate tooling to form a tablet.
  • the process may further include adding a glidant and a lubricant to the mixture of step (a).
  • the tablet may also include a film coating.
  • the method includes administering a fast-dissolving tablet, wherein the tablet includes a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier, wherein the carrier comprises a spray-dried mixture of lactose monohydrate and microcrystalline cellulose (75:25) as a diluent and a water-soluble disintegrant.
  • fast-dissolving tablets of galanthamine hydrobromide which are prepared by direct compression of a simple blend of lactose monohydrate and microcrystalline cellulose and a water soluble or poorly soluble disintegrant.
  • the fast-dissolving tablets of galanthamine hydrobromide can also be prepared by direct compression of anhydrous lactose and a water-soluble or poorly soluble disintegrant.
  • fast-dissolving as used herein relates to tablets having a dissolution of at least 80 % in 30 minutes in a USP type II apparatus.
  • the tablet is prepared by direct compression, although they can also be manufactured using conventional tabletting procedures.
  • excipients in a direct compression process should be taken into consideration to prepare tablets of desired physical characteristics and dissolution profile.
  • the excipients include fillers, including directly compressible fillers, lubricants, glidants and disintegrants.
  • Suitable fillers/carriers include one or more of anhydrous lactose, lactose monohydrate, dicalcium phosphate dihydrate, microcrystalline cellulose, modified (spray processed) lactose, spray dried mixture of lactose and microcrystalline cellulose, modified starch, mannitol, sorbitol and the like.
  • the filler may be used in a concentration of about 50 % to about 95 %, particularly about 80 % to about 95 % w/w of the tablet.
  • Disintegrants have major role in the disintegration and the dissolution process of tablets. To ensure a high disintegration rate, choice of suitable type and an optimal amount of disintegrant should be taken into consideration.
  • Suitable disintegrants include one or more of water-soluble disintegrants, such as pregelatinized starch, sodium carboxymethyl cellulose and sodium alginate, and water- insoluble cross-linked polymers, such as cross-linked carboxymehthylcellulose, croscarmellose sodium, sodium starch glycolate and cross-linked povidone.
  • the concentration of the disintegrant may vary from about 0.5 % to about 15 % w/w, particularly from about 1 % to about 10 % w/w of the tablet.
  • Suitable lubricants include one or more of talc, magnesium stearate, zinc stearate, calcium stearate, sodium stearyl fumarate and stearic acid.
  • Suitable glidants include talc and colloidal silicon dioxide.
  • the lubricant and glidant may be used in a concentration varying from about 0.1% to about 1.0 % w/w of the tablet. It would be appreciated that a person skilled in the art is cognizant of the fact that certain excipients in a direct compression process can be used both as a lubricant and glidant.
  • the tablet of galanthamine hydrobromide may be prepared by: a.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Psychiatry (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Zoology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

The present invention relates to fast-dissolving oral dosage forms of galanthamine for oral administration and processes for the preparation thereof.

Description

FAST DISSOLVING SOLID ORAL DOSAGE FORMS OF GALANTHAMINE
Technical Field of the Invention The present invention relates to fast-dissolving oral dosage forms of galanthamine for oral administration and processes for the preparation thereof.
Background of the Invention Alzheimer's disease is the most common form of dementia among older people. Dementia is a collective name for progressive degenerative brain syndromes which affect memory, thinking, behaviour and emotion. Alzheimer's disease involves the parts of the brain that control thought, memory, and language. The primary symptoms include memory loss, disorientation, confusion and problems with reasoning and thinking. These symptoms worsen as brain cells die and the connections between cells are lost. Galanthamine (or galantamine) is a tertiary alkaloid which is derived from the bulbs of the common snowdrop {Galanthus nivalis) and several Amaryllidaceae plants. Galanthamine belongs to the class of drugs called as acetylcholinesterase inhibitors. It directly inhibits the activity of acetylcholinesterase (an enzyme responsible for the breakdown of acetylchol ne). By virtue of this property, galanthamine has been approved in several countries for the symptomatic treatment of senile dementia of the Alzheimer's type. Prior to its use in patients with Alzheimer's, galantamine was available in Eastern Europe as a curare-reversal agent in anesthesia to reverse the neuromuscular paralysis induced by turbocurarine-like muscle relaxants and as a treatment for neurologic conditions, such as myasthenia gravis. U.S. Patent No 6,099,863 discloses a fast-dissolving tablet of galanthamine hydrobromide which includes a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier. The carrier includes a spray- dried mixture of lactose monohydrate and microcrystalline cellulose (75:25) as a diluent, and an insoluble or poorly soluble cross-linked polymer disintegrant. We have now discovered that fast-dissolving tablets of galanthamine hydrobromide can be prepared without using either a spray-dried mixture of lactose monohydrate and microcrystalline cellulose (75:25) as a diluent or an insoluble or poorly soluble cross-linked polymer as disintegrant.
Summary of the Invention In one general aspect there is provided a fast-dissolving tablet which includes a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier, wherein the carrier includes a spray-dried mixture of lactose monohydrate and microcrystalline cellulose (75:25) as a diluent and a water-soluble disintegrant. The galanthamine hydrobromide may include from about 1 % to about 15 % w/w of the tablet. The carrier may include from about 50 % to about 95 % w/w of the tablet or it may include about 80 % to about 95 % w/w of the tablet. The water-soluble disintegrant may include one or more of pregelatinized starch, sodium carboxymethyl cellulose and sodium alginate. For example, the water soluble disintegrant may be pregelatinized starch. The tablet may further include a lubricant and a glidant. In another general aspect there is provided a fast-dissolving tablet which includes a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier, wherein the carrier includes a simple blend of lactose monohydrate and microcrystalline cellulose as a diluent and a water-soluble disintegrant. In another general aspect there is provided a fast-dissolving tablet which includes a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier, wherein the carrier includes a simple blend of lactose monohydrate and microcrystalline cellulose as a diluent and a poorly soluble or insoluble disintegrant. The poorly soluble or insoluble disintegrant may include one or more of cross- linked povidone, cross-linked carboxymethylcellulose, sodium starch glycolate and croscarmellose sodium. For example, the poorly soluble or insoluble disintegrant may be cross-linked povidone. In yet another general aspect there is provided a fast-dissolving tablet which includes a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier, wherein the carrier includes anhydrous lactose as a diluent and a water-soluble disintegrant. In another general aspect there is provided a fast-dissolving tablet which includes a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier, wherein the carrier includes anhydrous lactose as a diluent and an insoluble or poorly soluble cross-linked polymer as disintegrant. In another general aspect there is provided a process for preparing a fast dissolving tablet of galanthamine hydrobromide. The process includes blending galanthamine hydrobromide, a pharmaceutically acceptable carrier, and a disintegrant to form a mixture; and compressing the mixture into a tablet using appropriate tooling to form a tablet. The process may further include adding a glidant and a lubricant to the mixture of step (a). The tablet may also include a film coating. In another general aspect there is provided a method for treating Alzheimer's disease and related dementias in a patient in need thereof. The method includes administering a fast-dissolving tablet, wherein the tablet includes a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier, wherein the carrier comprises a spray-dried mixture of lactose monohydrate and microcrystalline cellulose (75:25) as a diluent and a water-soluble disintegrant.
Detailed Description of the Invention The inventors have developed fast-dissolving tablets of galanthamine hydrobromide which are prepared by direct compression of a simple blend of lactose monohydrate and microcrystalline cellulose and a water soluble or poorly soluble disintegrant. The fast-dissolving tablets of galanthamine hydrobromide can also be prepared by direct compression of anhydrous lactose and a water-soluble or poorly soluble disintegrant. The term fast-dissolving as used herein relates to tablets having a dissolution of at least 80 % in 30 minutes in a USP type II apparatus. The tablet is prepared by direct compression, although they can also be manufactured using conventional tabletting procedures. The choice of excipients in a direct compression process should be taken into consideration to prepare tablets of desired physical characteristics and dissolution profile. The excipients include fillers, including directly compressible fillers, lubricants, glidants and disintegrants. Suitable fillers/carriers include one or more of anhydrous lactose, lactose monohydrate, dicalcium phosphate dihydrate, microcrystalline cellulose, modified (spray processed) lactose, spray dried mixture of lactose and microcrystalline cellulose, modified starch, mannitol, sorbitol and the like. The filler may be used in a concentration of about 50 % to about 95 %, particularly about 80 % to about 95 % w/w of the tablet. Disintegrants have major role in the disintegration and the dissolution process of tablets. To ensure a high disintegration rate, choice of suitable type and an optimal amount of disintegrant should be taken into consideration. Suitable disintegrants include one or more of water-soluble disintegrants, such as pregelatinized starch, sodium carboxymethyl cellulose and sodium alginate, and water- insoluble cross-linked polymers, such as cross-linked carboxymehthylcellulose, croscarmellose sodium, sodium starch glycolate and cross-linked povidone. The concentration of the disintegrant may vary from about 0.5 % to about 15 % w/w, particularly from about 1 % to about 10 % w/w of the tablet. Suitable lubricants include one or more of talc, magnesium stearate, zinc stearate, calcium stearate, sodium stearyl fumarate and stearic acid. Suitable glidants include talc and colloidal silicon dioxide. The lubricant and glidant may be used in a concentration varying from about 0.1% to about 1.0 % w/w of the tablet. It would be appreciated that a person skilled in the art is cognizant of the fact that certain excipients in a direct compression process can be used both as a lubricant and glidant. The tablet of galanthamine hydrobromide may be prepared by: a. blending galanthamine hydrobromide with a filler, a disintegrant and glidants in a mixer; b. mixing the lubricant with the above blend; c. compressing the mixture into a tablet using appropriate tooling. Tablets are additionally coated with coating compositions like Opadry® or Lustreclear®, sold by Colorcon, to impart aesthetic appeal. Such a coating may comprise up to 3% w/w of the uncoated tablet. The invention described herein is further illustrated by the following examples but these should not be construed as limiting the scope of the invention. EXAMPLE 1
Figure imgf000006_0001
Procedure: Galanthamine hydrobromide was blended with spray-dried mixture of lactose monohydrate and microcrystalline cellulose (75:25), pregelatinized starch and colloidal silicon dioxide in a mixer. Magnesium stearate was added to the above blend and the mixture was compressed into tablets using appropriate tooling. EXAMPLE 2
Figure imgf000006_0002
Procedure: Galanthamine hydrobromide was blended with lactose (anhydrous), crospovidone and colloidal silicon dioxide in a mixer. Magnesium. stearate was added to the above blend and the mixture was compressed into tablets using appropriate tooling. EXAMPLE 3
Figure imgf000007_0001
Procedure: Galanthamine hydrobromide was blended with lactose (anhydrous), pregelatinized starch and colloidal silicon dioxide in a mixer. Magnesium stearate was added to the above blend and the mixture was compressed into tablets using appropriate tooling. EXAMPLE 4
Figure imgf000007_0002
Procedure: Galanthamine hydrobromide was blended with lactose monohydrate, microcrystalline cellulose, crospovidone and colloidal silicon dioxide in a mixer. Magnesium stearate was added to the above blend and the mixture was compressed into tablets using appropriate tooling. EXAMPLE 5
Figure imgf000007_0003
Procedure: Galanthamine hydrobromide was blended with lactose monohydrate, microcrystalline cellulose, crospovidone and colloidal silicon dioxide in a mixer. Magnesium stearate was added to the above blend and the mixture was compressed into tablets using appropriate tooling. EXAMPLE 6
Figure imgf000008_0001
Procedure: Galanthamine hydrobromide was blended with lactose monohydrate, microcrystalline cellulose, pregelatinized starch and colloidal silicon dioxide in a mixer. Magnesium stearate was added to the above blend and the mixture was compressed into tablets using appropriate tooling. The tablets of examples 1-4 were subjected to dissolution testing in a USP type II dissolution apparatus at 50 rpm in 500 ml of purified water at 37 °C. The dissolution profiles in comparison to Reminyl tablets (Galanthamine tablets sold by Janssen Pharma) are given in TABLE 1.
TABLE 1: Dissolution profile of tablets of Example 1-4 as compared to Reminyl tablets in a USP type II dissolution apparatus at 50 rpm in 500 ml of purified water at 37 °C
Figure imgf000008_0002

Claims

We Claim:1. A fast-dissolving tablet comprising a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier, wherein the carrier comprises a spray-dried mixture of lactose monohydrate and microcrystalline cellulose (75:25) as a diluent and a water-soluble disintegrant.
2. The fast-dissolving tablet according to claim 1, wherein the galanthamine hydrobromide comprises from about 1 % to about 15 % w/w of the tablet.
3. The fast-dissolving tablet according to claim 1, wherein the carrier comprises from about 50 % to about 95 % w/w of the tablet.
4. The fast-dissolving tablet according to claim 3, wherein the carrier comprises from about 80 % to about 95 % w/w of the tablet.
5. The fast-dissolving tablet according to claim 1, wherein the water-soluble disintegrant comprises one or more of pregelatinized starch, sodium carboxymethyl cellulose and sodium alginate.
6. The fast-dissolving tablet according to claim 5, wherein the water soluble disintegrant comprises pregelatinized starch.
7. The fast-dissolving tablet according to claim 1, wherein the tablet further comprises a lubricant and a glidant.
8. A fast-dissolving tablet comprising a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier, wherein the carrier comprises a simple blend of lactose monohydrate and microcrystalline cellulose as a diluent and a water-soluble disintegrant.
9. The fast-dissolving tablet according to claim 10 wherein the galanthamine hydrobromide comprises a concentration ranging from about 1 % to about 15 % w/w of the tablet.
10. The fast-dissolving tablet according to claim 10, wherein the carrier comprises from about 50 % to about 95 % w/w of the tablet.
11. The fast-dissolving tablet according to claim 12, wherein the carrier comprises from about 80 % to about 95 % w/w of the tablet.
12. The fast-dissolving tablet according to claim 10, wherein the water-soluble disintegrant comprises one or more of pregelatinized starch, sodium carboxymethyl cellulose and sodium alginate.
13. The fast-dissolving tablet according to claim 14, wherein the water-soluble disintegrant comprises pregelatinized starch.
14. The fast-dissolving tablet according to claim 10, wherein the tablet further comprises a lubricant and a glidant.
15. A fast-dissolving tablet comprising a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier, wherein the carrier comprises a simple blend of lactose monohydrate and microcrystalline cellulose as a diluent and a poorly soluble or insoluble disintegrant.
16. The fast-dissolving tablet according to claim 15, wherein the galanthamine hydrobromide comprises a concentration ranging from about 1 % to about 15 % w/w of the tablet.
17. The fast-dissolving tablet according to claim 15, wherein the carrier comprises from about 50 % to about 95 % w/w of the tablet.
18. The fast-dissolving tablet according to claim 17, wherein the carrier comprises from about 80 % to about 95 % w/w of the tablet.
19. The fast-dissolving tablet according to claim 15, wherein the poorly soluble or insoluble disintegrant comprises one or more of cross-linked povidone, cross- . linked carboxymethylcellulose, sodium starch glycolate and croscarmellose sodium.
20. The fast-dissolving tablet according to claim 19, wherein the poorly soluble or insoluble disintegrant comprises cross-linked povidone.
21. The fast-dissolving tablet according to claim 15, wherein the tablet further comprises a lubricant and a glidant.
22. A fast-dissolving tablet comprising a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier, wherein the carrier comprises anhydrous lactose as a diluent and a water-soluble disintegrant.
23. The fast dissolving tablet according to claim 22, wherein the galanthamine hydrobromide comprises from about 1 % to about 15 % w/w of the tablet.
24. The fast-dissolving tablet according to claim 22, wherein the carrier comprises from about 50 % to about 95 % w/w of the tablet.
25. The fast-dissolving tablet according to claim 24, wherein the carrier comprises from about 80 % to about 95 % w/w of the tablet.
26. The fast-dissolving tablet according to claim 22, wherein the water-soluble disintegrant comprises one or more of pregelatinized starch, sodium carboxymethyl cellulose and sodium alginate.
27. The fast-dissolving tablet according to claim 26, wherein the water-soluble disintegrant comprises pregelatinised starch.
28. The fast-dissolving tablet according to claim 22, wherein the tablet further comprises a lubricant and a glidant.
29. A fast-dissolving tablet comprising a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier, wherein the carrier comprises anhydrous lactose as a diluent and an insoluble or poorly soluble cross-linked polymer as disintegrant.
30. The fast-dissolving tablet according to claim 29, wherein the galanthamine hydrobromide comprises from about 1 % to about 15 % w/w of the tablet.
31. The fast-dissolving tablet according to claim 29, wherein the carrier comprises from about 50 % to about 95 % w/w of the tablet.
32. The fast-dissolving tablet according to claim 31, wherein the carrier comprises from about 80 % to about 95 % w/w of the tablet.
33. The fast-dissolving tablet according to claim 29, wherein the insoluble or poorly soluble cross-linked polymer comprises one or more of cross-linked povidone, cross-linked carboxymethylcellulose, sodium starch glycolate and croscarmellose sodium.
34. The fast-dissolving tablet according to claim 33, wherein the insoluble or poorly soluble cross-linked polymer comprises cross-linked povidone.
35 The fast-dissolving tablet according to claim 29 wherein the tablet further comprises a lubricant and a glidant.
36 A process for preparing fast dissolving tablet of galanthamine hydrobromide, the process comprising: a. blending galanthamine hydrobromide, a pharmaceutically acceptable carrier, and a disintegrant to form a mixture; and b. compressing the mixture into a tablet using appropriate tooling to form a tablet.
37. The process according to claim 36, wherein the mixture of step (a) further comprises a glidant.
38. The process according to claim 36, further comprising adding a lubricant to the mixture of step (a).
39. The process according to claim 36, further comprising film-coating the tablet:
40. A method for treating Alzheimer's disease and related dementias in a patient in need thereof, the method comprising administering a fast-dissolving tablet, wherein the tablet comprises a therapeutically effective amount of galanthamine hydrobromide and a pharmaceutically acceptable carrier, wherein the carrier comprises a spray-dried mixture of lactose monohydrate and microcrystalline cellulose (75:25) as a diluent and a water-soluble disintegrant.
PCT/IB2004/003832 2003-11-28 2004-11-23 Fast dissolving solid oral dosage forms of galanthamine WO2005051489A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN1498/DEL/2003 2003-11-28
IN1498DE2003 2003-11-28

Publications (2)

Publication Number Publication Date
WO2005051489A2 true WO2005051489A2 (en) 2005-06-09
WO2005051489A3 WO2005051489A3 (en) 2006-04-20

Family

ID=34631116

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2004/003832 WO2005051489A2 (en) 2003-11-28 2004-11-23 Fast dissolving solid oral dosage forms of galanthamine

Country Status (1)

Country Link
WO (1) WO2005051489A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8663684B2 (en) 2008-09-19 2014-03-04 Molkerei Meggle Wasserburg Gmbh & Co. Kg Lactose and cellulose-based tableting aid

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6099863A (en) * 1996-06-14 2000-08-08 Janssen Pharmaceutica N.V. Fast-dissolving galanthamine hydrobromide tablet

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6099863A (en) * 1996-06-14 2000-08-08 Janssen Pharmaceutica N.V. Fast-dissolving galanthamine hydrobromide tablet

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8663684B2 (en) 2008-09-19 2014-03-04 Molkerei Meggle Wasserburg Gmbh & Co. Kg Lactose and cellulose-based tableting aid

Also Published As

Publication number Publication date
WO2005051489A3 (en) 2006-04-20

Similar Documents

Publication Publication Date Title
JP4172820B2 (en) Fast-dissolving galantamine hydrobromide tablets
CA2350195C (en) Rapid onset formulation of pyridoxine hydrochloride and doxylamine succinate
US20030158261A1 (en) Sustained release pharmaceutical dosage forms with minimized pH dependent dissolution profiles
US20070237824A1 (en) Sustained-Release Preparations Of Quinolone Antibiotics
US20210093576A1 (en) Oral antimicrobial pharmaceutical compositions
AU2001272243A1 (en) Rapid onset formulation
US20230018600A1 (en) Controlled release formulations comprising drotaverine or salt thereof
KR20050035250A (en) Bicifadine formulation
WO2005051489A2 (en) Fast dissolving solid oral dosage forms of galanthamine
US20050142193A1 (en) Galantamine formulations
US9173925B2 (en) Ferrimannitol-ovalbumin tablet composition
WO2018186650A2 (en) Double composite tablet for oral administration containing tramadol and celecoxib
WO2011126327A2 (en) Pharmaceutical composition with controlled-release properties comprising mosapride or levodropropizine, and preparing method thereof
KR102033716B1 (en) Double composite tablet for oral administration including tramadol and celecoxib
NO323835B1 (en) Solids preparation with high absorbency
IE83699B1 (en) Rapid onset formulation
EP2340813A1 (en) Solid dosage formulations of galantamine
NZ519709A (en) Rapid onset formulation comprising pyridoxine HCL and doxylamine succinate
EP1713451A1 (en) Solid dosage formulations of galanthamine

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BW BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE EG ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NA NI NO NZ OM PG PH PL PT RO RU SC SD SE SG SK SL SY TJ TM TN TR TT TZ UA UG US UZ VC VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): BW GH GM KE LS MW MZ NA SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LU MC NL PL PT RO SE SI SK TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
NENP Non-entry into the national phase in:

Ref country code: DE

WWW Wipo information: withdrawn in national office

Country of ref document: DE

122 Ep: pct application non-entry in european phase