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.


Solubility of sulindac and its formulations described in Table 2.
© Copyright Policy - open-access
Related In: Results  -  Collection


getmorefigures.php?uid=PMC4590819&req=5

fig6: Solubility of sulindac and its formulations described in Table 2.

Mentions: The solubility of SUL and its formulations is shown in Figure 6. SUL has a very low solubility in water, pH 1.2, and pH 4.5 due to its pKa of 4.7. A high solubility of SUL is expected above pH 4.7 due to formation of salt. At low pH value conditions of pH 1.2 and pH 4.5, formulations B, E, and F were superior. At basic pH value conditions of pH 6.8 and pH 7.4, formulations A, B, C, and F were superior. There was an 8-fold increase in the solubility of SUL in water and pH 4.5 for formulations E and F and up to 40-fold increase in solubility of SUL in pH 1.2 for formulation B. The solubility of SUL in pH 6.8 and pH 7.4 was high (pKa 4.7). Up to 4-fold increase in solubility of SUL in pH 6.8 for formulations A and B was observed. Up to 2-fold increase in solubility of SUL in pH 7.4 for formulation C was observed. The results confirm the increase in solubility of SUL due to its amorphization and thus increased surface area exposure to the solvent.


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)

Solubility of sulindac and its formulations described in Table 2.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig6: Solubility of sulindac and its formulations described in Table 2.
Mentions: The solubility of SUL and its formulations is shown in Figure 6. SUL has a very low solubility in water, pH 1.2, and pH 4.5 due to its pKa of 4.7. A high solubility of SUL is expected above pH 4.7 due to formation of salt. At low pH value conditions of pH 1.2 and pH 4.5, formulations B, E, and F were superior. At basic pH value conditions of pH 6.8 and pH 7.4, formulations A, B, C, and F were superior. There was an 8-fold increase in the solubility of SUL in water and pH 4.5 for formulations E and F and up to 40-fold increase in solubility of SUL in pH 1.2 for formulation B. The solubility of SUL in pH 6.8 and pH 7.4 was high (pKa 4.7). Up to 4-fold increase in solubility of SUL in pH 6.8 for formulations A and B was observed. Up to 2-fold increase in solubility of SUL in pH 7.4 for formulation C was observed. The results confirm the increase in solubility of SUL due to its amorphization and thus increased surface area exposure to the solvent.

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.