Limits...
Formulation and Characterization of Solid Dispersion Prepared by Hot Melt Mixing: A Fast Screening Approach for Polymer Selection.

Enose AA, Dasan PK, Sivaramakrishnan H, Shah SM - J Pharm (Cairo) (2014)

Bottom Line: Solid dispersion is molecular dispersion of drug in a polymer matrix which leads to improved solubility and hence better bioavailability.Solvent evaporation technique was employed to prepare films of different combinations of polymers, plasticizer, and a modal drug sulindac to narrow down on a few polymer-plasticizer-sulindac combinations.The formulations were characterized by advanced techniques like optical microscopy, differential scanning calorimetry, hot stage microscopy, dynamic vapor sorption, and X-ray diffraction.

View Article: PubMed Central - PubMed

Affiliation: Piramal Enterprise Limited, 1 Nirlon Knowledge Park, Goregaon East, Mumbai, Maharashtra 400063, India.

ABSTRACT
Solid dispersion is molecular dispersion of drug in a polymer matrix which leads to improved solubility and hence better bioavailability. Solvent evaporation technique was employed to prepare films of different combinations of polymers, plasticizer, and a modal drug sulindac to narrow down on a few polymer-plasticizer-sulindac combinations. The sulindac-polymer-plasticizer combination that was stable with good film forming properties was processed by hot melt mixing, a technique close to hot melt extrusion, to predict its behavior in a hot melt extrusion process. Hot melt mixing is not a substitute to hot melt extrusion but is an aid in predicting the formation of molecularly dispersed form of a given set of drug-polymer-plasticizer combination in a hot melt extrusion process. The formulations were characterized by advanced techniques like optical microscopy, differential scanning calorimetry, hot stage microscopy, dynamic vapor sorption, and X-ray diffraction. Subsequently, the best drug-polymer-plasticizer combination obtained by hot melt mixing was subjected to hot melt extrusion process to validate the usefulness of hot melt mixing as a predictive tool in hot melt extrusion process.

No MeSH data available.


DSC and X-ray diffraction of hot melt extrudates prepared using SUL (20% w/w) and PPP and PEG1000 (20% w/w) using a mini lab extruder.
© Copyright Policy - open-access
Related In: Results  -  Collection


getmorefigures.php?uid=PMC4590819&req=5

fig9: DSC and X-ray diffraction of hot melt extrudates prepared using SUL (20% w/w) and PPP and PEG1000 (20% w/w) using a mini lab extruder.

Mentions: Based on the initial film screening technique followed by screening using hot melt mixing a final combination of drug-polymer-plasticizer was selected for hot melt extrusion. The formula consisted of SUL (20% w/w of polymer), PPP, and PEG1000 (20% w/w of polymer). To validate the claim of hot melt mixing as a preliminary tool for selecting right drug-polymer-plasticizer combination using minimal amount of drug, DSC and X-ray (Figure 9) diffraction studies were performed to ascertain the molecularly dispersed form of SUL in the hot melt extrudates of SUL-PPP-PEG1000. The DSC investigation showed similar thermal behavior of extrudates with that prepared by hot melt mixing. Also X-ray diffraction pattern pointed towards the amorphous nature of the drug in the extrudates comparable to the ones prepared by hot melt mixing.


Formulation and Characterization of Solid Dispersion Prepared by Hot Melt Mixing: A Fast Screening Approach for Polymer Selection.

Enose AA, Dasan PK, Sivaramakrishnan H, Shah SM - J Pharm (Cairo) (2014)

DSC and X-ray diffraction of hot melt extrudates prepared using SUL (20% w/w) and PPP and PEG1000 (20% w/w) using a mini lab extruder.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4590819&req=5

fig9: DSC and X-ray diffraction of hot melt extrudates prepared using SUL (20% w/w) and PPP and PEG1000 (20% w/w) using a mini lab extruder.
Mentions: Based on the initial film screening technique followed by screening using hot melt mixing a final combination of drug-polymer-plasticizer was selected for hot melt extrusion. The formula consisted of SUL (20% w/w of polymer), PPP, and PEG1000 (20% w/w of polymer). To validate the claim of hot melt mixing as a preliminary tool for selecting right drug-polymer-plasticizer combination using minimal amount of drug, DSC and X-ray (Figure 9) diffraction studies were performed to ascertain the molecularly dispersed form of SUL in the hot melt extrudates of SUL-PPP-PEG1000. The DSC investigation showed similar thermal behavior of extrudates with that prepared by hot melt mixing. Also X-ray diffraction pattern pointed towards the amorphous nature of the drug in the extrudates comparable to the ones prepared by hot melt mixing.

Bottom Line: Solid dispersion is molecular dispersion of drug in a polymer matrix which leads to improved solubility and hence better bioavailability.Solvent evaporation technique was employed to prepare films of different combinations of polymers, plasticizer, and a modal drug sulindac to narrow down on a few polymer-plasticizer-sulindac combinations.The formulations were characterized by advanced techniques like optical microscopy, differential scanning calorimetry, hot stage microscopy, dynamic vapor sorption, and X-ray diffraction.

View Article: PubMed Central - PubMed

Affiliation: Piramal Enterprise Limited, 1 Nirlon Knowledge Park, Goregaon East, Mumbai, Maharashtra 400063, India.

ABSTRACT
Solid dispersion is molecular dispersion of drug in a polymer matrix which leads to improved solubility and hence better bioavailability. Solvent evaporation technique was employed to prepare films of different combinations of polymers, plasticizer, and a modal drug sulindac to narrow down on a few polymer-plasticizer-sulindac combinations. The sulindac-polymer-plasticizer combination that was stable with good film forming properties was processed by hot melt mixing, a technique close to hot melt extrusion, to predict its behavior in a hot melt extrusion process. Hot melt mixing is not a substitute to hot melt extrusion but is an aid in predicting the formation of molecularly dispersed form of a given set of drug-polymer-plasticizer combination in a hot melt extrusion process. The formulations were characterized by advanced techniques like optical microscopy, differential scanning calorimetry, hot stage microscopy, dynamic vapor sorption, and X-ray diffraction. Subsequently, the best drug-polymer-plasticizer combination obtained by hot melt mixing was subjected to hot melt extrusion process to validate the usefulness of hot melt mixing as a predictive tool in hot melt extrusion process.

No MeSH data available.