Sequestered antagonist formulations
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Benefits of technology
Problems solved by technology
Method used
Image
Examples
Example
[0215] In Example 1, a substantially non-releasable form of an opioid antagonist (naltrexone HCL) was prepared by coating naltrexone particles with a coating that renders the antagonist substantially non-releasable.
[0216] Naltrexone HCl 2 mg Capsules (Formulation A)
[0217] Formula
2 Amt / unit Amt / batch Ingredient (mg) (kg) Naltrexone HCl 2.0 0.04 Eudragit RSPO 88.0 1.76 Stearyl Alcohol 15.0 0.3 Stearic Acid 15.0 0.3 Butylated Hydroxytoluene 1.0 0.02 (BHT) Size #2 Hard Gelatin N / A N / A Capsules Total 121.0 2.42
[0218] Process
[0219] 1. Milling Pass stearyl alcohol flakes through a mill.
[0220] 2. Blending Mix Naltrexone HCl, Eudragit, milled Stearyl Alcohol, Stearic Acid and BHT in a twin shell blender.
[0221] 3. Extrusion Continuously feed the blended material into a twin screw extruder and collect the resultant strands on a conveyor.
[0222] 4. Cooling Allow the strands to cool a Conveyor.
[0223] 5. Pelletizing Cut the cooled strands into pellets using a Pelletizer.
[0224] 6. Screening Screen ...
Example
Example 2
[0236] In Example 2, a substantially non-releasable form of an opioid antagonist (naltrexone HCL) was prepared by coating naltrexone particles with a coating that renders the antagonist substantially non-releasable.
[0237] Naltrexone HCl 2 mg Capsules (Formulation B)
[0238] Formula:
5 Amt / unit Amt / batch Ingredient (mg) (kg) Naltrexone HCl 2.0 0.04 Eudragit RSPO 96.0 1.92 Stearyl Alcohol 22.0 0.44 Dibasic Calcium 6.0 0.12 Phosphate Butylated Hydroxytoluene 1.0 0.02 (BHT) Size #2 Hard Gelatin N / A N / A Capsules Total 127.0 2.54
[0239] Process:
[0240] 1. Milling Pass stearyl alcohol flakes through a mill.
[0241] 2. Blending Mix Naltrexone HCl, Eudragit, milled Stearyl Alcohol, Dibasic Calcium Phosphate and BHT in a twin shell blender.
[0242] 3. Extrusion Continuously feed the blended material into a twin screw extruder and collect the resultant strands on a conveyor.
[0243] 4. Cooling Allow the strands to cool a Conveyor.
[0244] 5. Pelletizing Cut the cooled strands into pellets using a ...
Example
Example 3
Immediate Release Naltrexone HCl 0.5 mg Tablets
[0257] Formula:
8 Amt / unit Amt / batch Ingredient (mg) (kg) Wet Granulation Naltrexone HCl 0.5 0.1 Plasdone C-30 5.0 1.0 Avicel PH-102 58.0 11.6 Sterile Water for Injection 25.0* 5.0* Dry Mixing Avicel PH-102 58.0 11.6 Cab-O-Sil 0.3 0.06 Ac-Di-Sol 2.5 0.5 Magnesium Stearate 0.7 0.14 Total 125.0 25.0 * Remains as residual moisture only. Not included in total weight.
[0258] Process:
[0259] 1. Solution Preparation Dissolve Naltrexone HCl and Plasdone in Sterile Water for Injection.
[0260] 2. Wet Granulation Granulate Avicel PH-102 with solution as prepared in step 1.
[0261] 3. Drying Dry granulated material from step 2 in a fluid bed dryer.
[0262] 4. Milling Pass dried granulation through a Comil
[0263] 5. Mixing Mix milled granulation with remaining Avicel PH-102, Cab-O-Sil, Ac-Di-Sol, and Magnesium Stearate.
[0264] 6. Compression Compress granulation into tablets using a tablet press.
[0265] Dissolution Method
[0266] 9. Apparatus-USP Type I...
PUM
Property | Measurement | Unit |
---|---|---|
Time | aaaaa | aaaaa |
Time | aaaaa | aaaaa |
Time | aaaaa | aaaaa |
Abstract
Description
Claims
Application Information
- R&D Engineer
- R&D Manager
- IP Professional
- Industry Leading Data Capabilities
- Powerful AI technology
- Patent DNA Extraction
Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.
© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap