CA1202899A - Sustained release theophylline - Google Patents
Sustained release theophyllineInfo
- Publication number
- CA1202899A CA1202899A CA000406752A CA406752A CA1202899A CA 1202899 A CA1202899 A CA 1202899A CA 000406752 A CA000406752 A CA 000406752A CA 406752 A CA406752 A CA 406752A CA 1202899 A CA1202899 A CA 1202899A
- Authority
- CA
- Canada
- Prior art keywords
- sustained release
- theophylline
- micropellets
- release dosage
- dosage formulation
- 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
Links
Abstract
ABSTRACT OF DISCLOSURE
Theophylline is provided in a sustained release formulation which comprises a plurality of micropellets of theophylline which is coated over a seed in a first coat with polyvinylpyrrolidone and a second coat of cellulose derivatives. The sustained release theo-phylline form is sprinkled into the normal food of a patient, particularly a child or elderly patient.
Theophylline is provided in a sustained release formulation which comprises a plurality of micropellets of theophylline which is coated over a seed in a first coat with polyvinylpyrrolidone and a second coat of cellulose derivatives. The sustained release theo-phylline form is sprinkled into the normal food of a patient, particularly a child or elderly patient.
Description
HC~-18487A-CA
SUSTAINED RELEASE THEOPHYLLINE
A zero order release theophylline product, THEO-DUR, has received widespread acceptance in the marketplace and among the medical profession as a broncho-dilator. It is desired to provide a sustained release broncho-dilator which is in a form more suitable for administration to children and the elderly.
In accordance with the present invention there are provided micropellets of sustained release theophylline which are designed for administration to children or the elderly who may have difficulty swallowing a relatively large table. The micropellets are provided in a capsule as the dosage unit form, each capsule containing about 1000 microparticles or less to yield the total desired dosage. For example, in one embodiment, a 100 mg dosage of theophylline is provided with 845 microparticles.
The microparticles are provided by coating theo-phylline in micronized form onto a sugar seed having 60/80 mesh with polyvinylpryrrolidone having a molecular weight of from about 30,000 to about 50,000, with a molecular weight of about 40,000 being a preferred embodiment ("Kollidon~30"). A sustained release coating is provided of cellulose derivatives. In a preferre embodiment a mixture of ethylcellulose ~Dow, "E~oce N-10") and hydroxypropylcellulose (Hercules, "Kluce ~ F") is used. The average diameter of each particle is roughly about 0.6mm.
The following example illustrates the invention:
EXAMPLE
3.2 kg polyvinylpyrrolidone (mw 40,000, Kollidon~ 0) is dissolved in 32 1 isopropanol. Therein there is dis-persed 12.8 kg of micronized theophylline. Into a Glatt~
column (six inch, Glatt CPCG) there is charged 4.0 kg .~
lZ02~99
SUSTAINED RELEASE THEOPHYLLINE
A zero order release theophylline product, THEO-DUR, has received widespread acceptance in the marketplace and among the medical profession as a broncho-dilator. It is desired to provide a sustained release broncho-dilator which is in a form more suitable for administration to children and the elderly.
In accordance with the present invention there are provided micropellets of sustained release theophylline which are designed for administration to children or the elderly who may have difficulty swallowing a relatively large table. The micropellets are provided in a capsule as the dosage unit form, each capsule containing about 1000 microparticles or less to yield the total desired dosage. For example, in one embodiment, a 100 mg dosage of theophylline is provided with 845 microparticles.
The microparticles are provided by coating theo-phylline in micronized form onto a sugar seed having 60/80 mesh with polyvinylpryrrolidone having a molecular weight of from about 30,000 to about 50,000, with a molecular weight of about 40,000 being a preferred embodiment ("Kollidon~30"). A sustained release coating is provided of cellulose derivatives. In a preferre embodiment a mixture of ethylcellulose ~Dow, "E~oce N-10") and hydroxypropylcellulose (Hercules, "Kluce ~ F") is used. The average diameter of each particle is roughly about 0.6mm.
The following example illustrates the invention:
EXAMPLE
3.2 kg polyvinylpyrrolidone (mw 40,000, Kollidon~ 0) is dissolved in 32 1 isopropanol. Therein there is dis-persed 12.8 kg of micronized theophylline. Into a Glatt~
column (six inch, Glatt CPCG) there is charged 4.0 kg .~
lZ02~99
-2-sugar, 60/80 mesh. AFter the air suspension system is in operation with the sugar, the dispersed theophylline is charged into the Glatt column with the inlet air having a temperature of 60C and the spray pressure at 4 bars, and the spray rate being 100 ml/min.
After completion of the above procedure, the Glatt column is stopped, and the product reserved as "Theo-phylline pellets, Active I".
A second batch of 3.2 kg polyvinylpyrrolidone (mw 40,000, Kollidon 30) is dissolved into 32.0 1 isopro-panol, and dispersed into the resultant mixture is 12.8 kg micronized theophylline. 4.0 kg of Theophylline pellets, Active I are then charged into the same Glatt column under the same conditions of temperature, pressure and rate. The second batch having the theophylline dispersed therein is then charged into the Glatt column to further build up the coating.
The Glatt column is emptied and the product labelled "Theophylline pettets, Active II".
A mixture of 13.2 l chloroform and 3.3 1 methanol is prepared, into which are dispersed 992.0 g ethylcellulose (Ethocel N-10, Dow) and 329.0 g hydroxypropyl cellulose (Hercules, Klucel LF)/ Into the Glatt column is charged 19.0 kg of Theophylline pellets, Active II, which are then coated with the coating mixture under conditions of 30C, spray pressure 3 bars and spray rate 100 ml/min.
The resultant coated pellets are small white micropellets which to make up a dosage unit of 100 mg used 845 of such micropellets which are placed into capsules for con-venience. For a child or an elderly patient, the micro-particles are typically sprinkled into food which is then taken as part of a meal, to provide the sustained theo-phylline effect.
After completion of the above procedure, the Glatt column is stopped, and the product reserved as "Theo-phylline pellets, Active I".
A second batch of 3.2 kg polyvinylpyrrolidone (mw 40,000, Kollidon 30) is dissolved into 32.0 1 isopro-panol, and dispersed into the resultant mixture is 12.8 kg micronized theophylline. 4.0 kg of Theophylline pellets, Active I are then charged into the same Glatt column under the same conditions of temperature, pressure and rate. The second batch having the theophylline dispersed therein is then charged into the Glatt column to further build up the coating.
The Glatt column is emptied and the product labelled "Theophylline pettets, Active II".
A mixture of 13.2 l chloroform and 3.3 1 methanol is prepared, into which are dispersed 992.0 g ethylcellulose (Ethocel N-10, Dow) and 329.0 g hydroxypropyl cellulose (Hercules, Klucel LF)/ Into the Glatt column is charged 19.0 kg of Theophylline pellets, Active II, which are then coated with the coating mixture under conditions of 30C, spray pressure 3 bars and spray rate 100 ml/min.
The resultant coated pellets are small white micropellets which to make up a dosage unit of 100 mg used 845 of such micropellets which are placed into capsules for con-venience. For a child or an elderly patient, the micro-particles are typically sprinkled into food which is then taken as part of a meal, to provide the sustained theo-phylline effect.
Claims (5)
1. A sustained release dosage formulation of theo-phylline which comprises a container having therein a plurality of micropellets, the sum of such micropellets in said container forming a dosage unit of theophylline, each of siad micropellets being based upon a seed having coated thereon a mixture of theophylline and polyvinylpyrrolidone, the thus coated seed having further coated thereon a mixture of cellulose derivatives.
2. A sustained release dosage formulation of claim 1 wherein said cellulose derivative is selected from the group consisting of hydroxypropyl cellulose and ethyl cellulose.
3. A sustained release dosage formulation of claim 2 wherein said cellulose derivative is a mixture of hydroxypropylcellulose and ethyl cellulose.
4. A sustained release dosage formulation of claim 1 wherein said polyvinylpyrrolidone has a molecular weight of about 40,000.
5. A sustained release dosage formulation of claim 1 wherein said seed is sugar having a mesh of 60/80.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US28344681A | 1981-07-15 | 1981-07-15 | |
| US283,446 | 1981-07-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA1202899A true CA1202899A (en) | 1986-04-08 |
Family
ID=23086109
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA000406752A Expired CA1202899A (en) | 1981-07-15 | 1982-07-07 | Sustained release theophylline |
Country Status (1)
| Country | Link |
|---|---|
| CA (1) | CA1202899A (en) |
-
1982
- 1982-07-07 CA CA000406752A patent/CA1202899A/en not_active Expired
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| EP0067539B1 (en) | Sustained release pharmaceutical composition | |
| CA2038245C (en) | Pharmaceutically useful micropellets | |
| CA2140254C (en) | Controlled release morphine preparation | |
| US4794001A (en) | Formulations providing three distinct releases | |
| EP0202051B1 (en) | Therapeutic compositions for oral administration | |
| US4587118A (en) | Dry sustained release theophylline oral formulation | |
| US4851226A (en) | Chewable medicament tablet containing means for taste masking | |
| CA1309951C (en) | Press coated dhp tablets | |
| EP0459695B1 (en) | Taste masking and sustained release coatings for pharmaceuticals | |
| EP0717986B1 (en) | Rotor granulation and coating of acetaminophen, pseudoephedrine, chlorpheniramine, and, optionally, dextromethorphan | |
| WO1983000284A1 (en) | Sustained release theophylline | |
| SE455836B (en) | PREPARATION WITH CONTROLLED RELEASE CONTAINING A SALT OF METOPROLOL AND METHOD FOR PREPARING THIS PREPARATION | |
| GB2209940A (en) | Sustained release etodolac | |
| JPH05200099A (en) | Tablet stable mechanically and decomposa- ble easily as produced from fine particle molded previously containing active component | |
| US4859469A (en) | Novel galenic forms of verapamil, their preparation and medicines containing said novel galenic forms | |
| EP0317274B1 (en) | Chewable medicament tablet containing means for taste masking | |
| EP1154762B1 (en) | Pharmaceutical capsule compositions containing loratadine and pseudoephedrine | |
| EP0156243B1 (en) | Controlled-release composition and the preparation thereof | |
| EP0538034B1 (en) | Taste mask coatings for preparing chewable pharmaceutical tablets | |
| HU224193B1 (en) | Multiparticulate pharmaceutical form with programmed and timed release and preparation method | |
| GB2098867A (en) | Sustained release pharmaceutical composition | |
| EP0291923B1 (en) | improved dry sustained release theophylline oral formulation | |
| CA1202899A (en) | Sustained release theophylline | |
| EP0113373B1 (en) | Sustained release quinidine dosage form |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MKEX | Expiry |