CA1326632C - Long-active drug formulations comprising galanthamine for treatment of alzheimer's disease - Google Patents
Long-active drug formulations comprising galanthamine for treatment of alzheimer's diseaseInfo
- Publication number
- CA1326632C CA1326632C CA 581365 CA581365A CA1326632C CA 1326632 C CA1326632 C CA 1326632C CA 581365 CA581365 CA 581365 CA 581365 A CA581365 A CA 581365A CA 1326632 C CA1326632 C CA 1326632C
- Authority
- CA
- Canada
- Prior art keywords
- particles
- galanthamine
- alzheimer
- disease
- treatment
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
-
- 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
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/665—Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
A B S T R A C T
Long acting Galanthamine formulation is prepared by coating particles of drug with polyvinyl pyrrolidone, sizing the particles and incorporating them into a capsule or tablet.
Long acting Galanthamine formulation is prepared by coating particles of drug with polyvinyl pyrrolidone, sizing the particles and incorporating them into a capsule or tablet.
Description
~32~32 The present invention relates to long-acting formul~tions for treatment of Alzheimer's disease and related dementias, United States Patent No. 4,663,318 ~Davis issued May 51 l9B7) describes the use of galanthamine and its salts for treatment of Alzheimer's disease and related dementias.
The possibility o~ using a long-acting fo~mulation o~ the drug is suggested therein.
Ac~ording to the present invention, there is provided a sustained release formulation in ~he form of a tablet o~ capsule for oral administration for treatment of Alzheimer's disease and related dementias comprising particles of galanthamine or a pharmaceutically acceptable salt thereof.
A pr~ferred compound of the above ~ormula is , galanthamine hydrobromide.
,~, Suikable pharmaceutically acceptable coating agents ~-:
include polyvinyl pyrrolidone.
A par~icularly useful method for producing I formulations o~ the present invention i~ to coat the drug ;~ substance with polyvinyl pyrrolidone alcohol 601ution to form :~ granules. These granules are the~p~s~sed thru a sieve machine to obtain various ~izes o~ granules. A dete~mlned amount of each of dif~erant ~ize granules are mixed with excipient such ~ : as hydroxypropyl methyI c211ulose, ethyl cellulose, starch, ¦ ~ilicon dioxide, and with a lubricant such as magnesium i tearate or polyethylene glycol to form a tablet or to be 1~ ~ incorporated into a capsule.
l~ The final drug preparation i6 tested for dissolution . :
.1 pro~ile in addition to the general testing requirements. A :
useful dis~olution profile for a ~ustained release preparation according to ~h~ presen~ invention is:
, ~ .
Activ~ drug 1-2 hours 10-20%
~ dissolved 2-4 hours 20-40 :1 in ga~tric ~-8 hour~ 40-80% -~ uiae 12 hours balance ~
~!
!
~32~3~
Typically the sizing of the particles incorporated i~to a table or capsule will be chosen so as to produce a sustained release over a four to twelve hour period, for example, over a eight hour period.
Typically capsules or tablets according to the present invention contain a quarter to a half of the typical daily dose of drug, although dosage units outside this range are also possible. Such daily doses are normally or 10 to 2000 mg per day, more typically 100 to 600 mg per day.
Typically, therefore, tablets or capsules comprise 25 to 250 mg o~ active compound.
,f~ '"
.~
,~ :
.j .
',
The possibility o~ using a long-acting fo~mulation o~ the drug is suggested therein.
Ac~ording to the present invention, there is provided a sustained release formulation in ~he form of a tablet o~ capsule for oral administration for treatment of Alzheimer's disease and related dementias comprising particles of galanthamine or a pharmaceutically acceptable salt thereof.
A pr~ferred compound of the above ~ormula is , galanthamine hydrobromide.
,~, Suikable pharmaceutically acceptable coating agents ~-:
include polyvinyl pyrrolidone.
A par~icularly useful method for producing I formulations o~ the present invention i~ to coat the drug ;~ substance with polyvinyl pyrrolidone alcohol 601ution to form :~ granules. These granules are the~p~s~sed thru a sieve machine to obtain various ~izes o~ granules. A dete~mlned amount of each of dif~erant ~ize granules are mixed with excipient such ~ : as hydroxypropyl methyI c211ulose, ethyl cellulose, starch, ¦ ~ilicon dioxide, and with a lubricant such as magnesium i tearate or polyethylene glycol to form a tablet or to be 1~ ~ incorporated into a capsule.
l~ The final drug preparation i6 tested for dissolution . :
.1 pro~ile in addition to the general testing requirements. A :
useful dis~olution profile for a ~ustained release preparation according to ~h~ presen~ invention is:
, ~ .
Activ~ drug 1-2 hours 10-20%
~ dissolved 2-4 hours 20-40 :1 in ga~tric ~-8 hour~ 40-80% -~ uiae 12 hours balance ~
~!
!
~32~3~
Typically the sizing of the particles incorporated i~to a table or capsule will be chosen so as to produce a sustained release over a four to twelve hour period, for example, over a eight hour period.
Typically capsules or tablets according to the present invention contain a quarter to a half of the typical daily dose of drug, although dosage units outside this range are also possible. Such daily doses are normally or 10 to 2000 mg per day, more typically 100 to 600 mg per day.
Typically, therefore, tablets or capsules comprise 25 to 250 mg o~ active compound.
,f~ '"
.~
,~ :
.j .
',
Claims (4)
1. A sustained release formulation for oral administration in the form of a tablet or capsule for treatment of Alzheimer's disease and related dementias comprising particles of galanthamine or a pharmaceutically acceptable salt thereof, said particles being coated with a pharmaceutically acceptable coating agent that is soluble in the intestinal tract, the thickness of the coatings varying between individual particles, a plurality of said particles having various coating thickness chosen so as to result, after administration, in release of the drug from its coated particles at different times.
2. A sustained release formulation as claimed in claim 1 wherein said particles comprise galanthamine hydrobromide.
3. A sustained release formulation as claimed in claim 1 wherein said coating material is polyvinyl pyrrolidone.
4. A sustained release formulation as claimed in claim 1 containing 25 to 250 mg of active compound.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CA 581365 CA1326632C (en) | 1988-10-26 | 1988-10-26 | Long-active drug formulations comprising galanthamine for treatment of alzheimer's disease |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CA 581365 CA1326632C (en) | 1988-10-26 | 1988-10-26 | Long-active drug formulations comprising galanthamine for treatment of alzheimer's disease |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA1326632C true CA1326632C (en) | 1994-02-01 |
Family
ID=27167974
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA 581365 Expired - Lifetime CA1326632C (en) | 1988-10-26 | 1988-10-26 | Long-active drug formulations comprising galanthamine for treatment of alzheimer's disease |
Country Status (1)
| Country | Link |
|---|---|
| CA (1) | CA1326632C (en) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000038686A1 (en) * | 1998-12-24 | 2000-07-06 | Janssen Pharmaceutica N.V. | Controlled release galantamine composition |
| EP1133230A1 (en) * | 1998-11-23 | 2001-09-19 | Bonnie M. Davis | Dosage formulations for acetylcholinesterase inhibitors |
| WO2007121537A1 (en) | 2006-04-26 | 2007-11-01 | Alphapharm Pty Ltd | Controlled release formulations comprising uncoated discrete unit(s) and an extended release matrix |
| AU2004242546B2 (en) * | 1998-11-23 | 2008-05-15 | Bonnie Davis | Dosage formulations for acetylcholinesterase inhibitors |
| WO2011064797A2 (en) | 2009-11-26 | 2011-06-03 | Usv Limited | Controlled release pharmaceutical compositions of galantamine |
-
1988
- 1988-10-26 CA CA 581365 patent/CA1326632C/en not_active Expired - Lifetime
Cited By (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2004242546B2 (en) * | 1998-11-23 | 2008-05-15 | Bonnie Davis | Dosage formulations for acetylcholinesterase inhibitors |
| EP1133230A1 (en) * | 1998-11-23 | 2001-09-19 | Bonnie M. Davis | Dosage formulations for acetylcholinesterase inhibitors |
| EP1133230A4 (en) * | 1998-11-23 | 2004-05-26 | Bonnie M Davis | Dosage formulations for acetylcholinesterase inhibitors |
| US7939522B1 (en) | 1998-11-23 | 2011-05-10 | Bonnie M Davis | Dosage formulations for acetylcholinesterase inhibitors |
| EP2311441A1 (en) * | 1998-11-23 | 2011-04-20 | Bonnie M. Davis | Dosage formulations for acetylcholinesterase inhibitors |
| AP1414A (en) * | 1998-12-24 | 2005-06-13 | Janssen Pharmaceutica Nv | Controlled release galantamine composition. |
| BG65306B1 (en) * | 1998-12-24 | 2008-01-31 | Janssen Pharmaceutica N.V. | Galantamine-containing composition with controlled release |
| CN100370990C (en) * | 1998-12-24 | 2008-02-27 | 詹森药业有限公司 | Controlled release galantamine composition |
| US7160559B1 (en) | 1998-12-24 | 2007-01-09 | Janssen Pharmaceutica N.V. | Controlled release galantamine composition |
| CZ301658B6 (en) * | 1998-12-24 | 2010-05-19 | Janssen Pharmaceutica N. V. | Pharmaceutical compositions with controlled release of galanthamine |
| HRP20010463B1 (en) * | 1998-12-24 | 2011-02-28 | Janssen Pharmaceutica N.V. | Controlled release galantamine composition |
| WO2000038686A1 (en) * | 1998-12-24 | 2000-07-06 | Janssen Pharmaceutica N.V. | Controlled release galantamine composition |
| AU775914B2 (en) * | 1998-12-24 | 2004-08-19 | Janssen Pharmaceutica N.V. | Controlled release galantamine composition |
| WO2007121537A1 (en) | 2006-04-26 | 2007-11-01 | Alphapharm Pty Ltd | Controlled release formulations comprising uncoated discrete unit(s) and an extended release matrix |
| EP2010158B1 (en) | 2006-04-26 | 2016-02-17 | Alphapharm Pty Ltd. | Controlled release formulations comprising uncoated discrete unit(s) and an extended release matrix |
| WO2011064797A2 (en) | 2009-11-26 | 2011-06-03 | Usv Limited | Controlled release pharmaceutical compositions of galantamine |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MKEX | Expiry |
Effective date: 20110201 |