Abstract
Objectives
This research examined the application of hot melt extrusion (HME) in the preparation of matrix formulations containing hydroxypropyl cellulose (HPC) as a base polymer in combination with methyl cellulose (MC) and hydroxypropyl methylcellulose (HPMC).
Methods
The limit to which formulations could control drug release under varying paddle speeds, high alcohol environments and high and low drug loads was investigated on a Caleva 10 ST dissolution tester. Rheological studies and hot plate imaging highlighted the impact of thermoresponsive polymers on drug release. The rate and percentage release of drug were analysed using a one‐way ANOVA and Tukey's HSD test.
Key findings
No significant differences in the amount of drug released were calculated as a result of paddle speed variation or in the presence of 40% v/v ETOH. The phase separation effects of temperature‐sensitive polymers HPC and MC and the characteristic gel shrinkage and fluid expulsion were shown to be contributing factors. The use of the partition activity, α, identified the extent to which formulations were affected by phase separation.
Conclusion
Hot melt extrusion was successfully used to manufacture cellulose‐based formulations. Thermoresponsive polymers HPC and MC significantly impacted drug release properties.
This research examined the application of hot melt extrusion (HME) in the preparation of matrix formulations containing hydroxypropyl cellulose (HPC) as a base polymer in combination with methyl cellulose (MC) and hydroxypropyl methylcellulose (HPMC).
Methods
The limit to which formulations could control drug release under varying paddle speeds, high alcohol environments and high and low drug loads was investigated on a Caleva 10 ST dissolution tester. Rheological studies and hot plate imaging highlighted the impact of thermoresponsive polymers on drug release. The rate and percentage release of drug were analysed using a one‐way ANOVA and Tukey's HSD test.
Key findings
No significant differences in the amount of drug released were calculated as a result of paddle speed variation or in the presence of 40% v/v ETOH. The phase separation effects of temperature‐sensitive polymers HPC and MC and the characteristic gel shrinkage and fluid expulsion were shown to be contributing factors. The use of the partition activity, α, identified the extent to which formulations were affected by phase separation.
Conclusion
Hot melt extrusion was successfully used to manufacture cellulose‐based formulations. Thermoresponsive polymers HPC and MC significantly impacted drug release properties.
| Original language | English |
|---|---|
| Pages (from-to) | 32-42 |
| Number of pages | 11 |
| Journal | JOURNAL OF PHARMACY AND PHARMACOLOGY |
| Volume | 69 |
| Issue number | 1 |
| Early online date | 17 Oct 2016 |
| DOIs | |
| Publication status | Published (in print/issue) - Jan 2017 |
Keywords
- controlled release
- hot melt extrusion
- hydroxypropyl cellulose
- low critical solution temperature
- phase separation