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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 thermograms of SUL and formulations described in Table 2 taken at heating rate of 10°C/min from 40°C to 200°C.
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fig3: DSC thermograms of SUL and formulations described in Table 2 taken at heating rate of 10°C/min from 40°C to 200°C.

Mentions: Thermal analysis by DSC for SUL showed a sharp endotherm at 188°C as observed in Figure 3. Solid dispersions of SUL prepared by hot melt mixing did not show any sharp endotherm from 40°C to 200°C. A sharp endotherm was observed in thermogram of SUL with peak at 188°C. In the formulations of SUL prepared by hot melt mixing, no endothermal peak for SUL was observed at 188°C or at a lower temperature suggesting possible molecular dispersion of SUL in polymer-plasticizer combination. DSC results confirm that SUL has been molecularly dispersed in the matrix of polymer and plasticizer. A broad endotherm at 56°C in case of combinations SUL + HPC + PEG1000 and SUL + HPMC + PEG100 is due the melting of PEG1000. A small dip in the baseline at around 80°C in SUL + PPP + PEG100 and SUL + PPP + TEC could be due to glass transition temperature of PPP at around 70°C. Formulations containing TEC as plasticizer, endothermic events were not observed.


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 thermograms of SUL and formulations described in Table 2 taken at heating rate of 10°C/min from 40°C to 200°C.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig3: DSC thermograms of SUL and formulations described in Table 2 taken at heating rate of 10°C/min from 40°C to 200°C.
Mentions: Thermal analysis by DSC for SUL showed a sharp endotherm at 188°C as observed in Figure 3. Solid dispersions of SUL prepared by hot melt mixing did not show any sharp endotherm from 40°C to 200°C. A sharp endotherm was observed in thermogram of SUL with peak at 188°C. In the formulations of SUL prepared by hot melt mixing, no endothermal peak for SUL was observed at 188°C or at a lower temperature suggesting possible molecular dispersion of SUL in polymer-plasticizer combination. DSC results confirm that SUL has been molecularly dispersed in the matrix of polymer and plasticizer. A broad endotherm at 56°C in case of combinations SUL + HPC + PEG1000 and SUL + HPMC + PEG100 is due the melting of PEG1000. A small dip in the baseline at around 80°C in SUL + PPP + PEG100 and SUL + PPP + TEC could be due to glass transition temperature of PPP at around 70°C. Formulations containing TEC as plasticizer, endothermic events were not observed.

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.