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Journal ArticleDOI

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

12 Mar 2014-Vol. 2014, pp 105382-105382
TL;DR: 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.
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.

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TL;DR: This review attempts to address the critical molecular and thermodynamic aspects governing the physicochemical properties of amorphous solid dispersion systems and potential advantage of polymers as inert, hydrophilic, pharmaceutical carrier matrices.

680 citations

Journal ArticleDOI
TL;DR: A systematic step-by-step approach is presented, where thermodynamics, polymer screening, multivariate statistics and process optimization are combined, to increase the success of HME-based drug product development.

76 citations

Journal ArticleDOI
TL;DR: In this paper, different water-soluble polymers were applied to improve dissolution of K. parviflora by solid dispersions in different ratios were prepared by solvent evaporation method.

22 citations

Cites background or methods from "Formulation and Characterization of..."

  • ...[25] Enose AA, Dasan PK, Sivaramakrishnan H, et al....


  • ...From the study, the solid state of solid dispersions was obtained while using the high Tm (Tm of PVA-co-PEG was more than 200 °C [24] and decomposition temperature of HPMC was 190–200 °C [25])....


Journal ArticleDOI
TL;DR: In this article, a solution cast of polycaprolactone (PCL) and titanium dioxide nanoparticles (TiO2) was used to analyze the properties of PCL and its interaction with TiO2 nanoparticles.
Abstract: Organic/Inorganic hybrid materials have been attracting much attention since they combine the advantages of inorganic materials with the properties of organic polymers. Titanium dioxide nanoparticles (TiO2) present good thermal stability, accessibility and catalytic properties. Polycaprolactone (PCL) is a bi-ocompatible and bioresorbable material, which is being examined as biode-gradable packaging materials, controlled drug release carriers and other medical applications. Hybrids based on PCL containing different amounts of titanium dioxide nanoparticles, ranging from 0.05% to 0.35% w/w, were prepared using the solution cast method. These systems were characterized by X-ray diffraction (XRD), infrared spectroscopy (FTIR), low-field nuclear magnetic resonance (NMR), thermogravimetric analysis (TG) and differential scanning calorimetry (DSC). The FTIR analysis confirmed that there was an interaction between the PCL chains and the TiO2 nanoparticles. The XRD and DSC analysis showed that the PCL crystallization was affected by TiO2 incorporation, modifying its semi-crystalline structure to a less ordered structure. When TiO2 nanoparticles were added the values of T1H and T1ρH increased for all hybrids, therefore, their addition produced a new material with less molecular mobility. In the TG analysis, it was observed that the introduction of TiO2 nanoparticles decreased the thermal resistance of PCL. In DSC analysis, the PCL/TiO2 hybrids presented a reduction in the crystallization temperature and degree of crystallinity, except for PCL hybrids containing 0.15% w/w of TiO2 nanoparticles.

8 citations

Journal ArticleDOI
TL;DR: Ocimum basilicum (Lamiaceae family), a source of hydrophilic mucilage referred herein as Ocicum, was evaluated for the solubility enhancer of a model drug, aceclofenac, in solid dispersions prepared using different methods as discussed by the authors .
Abstract: Plant mucilages are commonly employed as excipients in pharmaceutical manufacturing. Ocimum basilicum (Lamiaceae family), a source of hydrophilic mucilage referred herein as Ocicum, was evaluated for the solubility enhancer of a model drug, aceclofenac, in solid dispersions prepared using different methods. Polymer was extracted from O. basilicum and solid dispersions of aceclofenac were fabricated with Ocicum or Poloxamer 407 using polymer-to-drug ratios of 1:1, 1:2 and 1:3 utilizing solvent evaporation, lyophilization and melt methods. Ocicum was evaluated for its safety via acute toxicity study including different biochemical and hematological parameters including liver and kidney profiles. Moreover, different characterization studies including melting-point, Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and differential thermal analysis (TGA) were used for evaluation of polymer and solid dispersions. Furthermore, solubility and dissolution studies were performed to confirm solubility enhancement. Ocicum was found to be safer, and different characterization studies confirmed the purity of the compounds. In addition, Ocicum exhibited up to 6.27-fold enhanced solubility as compared to pure aceclofenac; similarly, 4.51-fold increased solubility by the synthetic polymer in their respective solid dispersions was shown. Furthermore, Ocicum-based solid dispersions showed substantial improvement in dissolution of aceclofenac. Therefore, it can be concluded from the above-mentioned results that Ocicum might be used as an economical natural oral delivery carrier alternative to the synthetic polymers.

6 citations

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11,116 citations

Journal ArticleDOI
TL;DR: Viable formulation options for poorly water-soluble drugs, such as crystal modification, micronization, amorphization, self-emulsification, cyclodextrin complexation, and pH modification are reviewed on the basis of the biopharmaceutics classification system of drug substances.

961 citations

Journal ArticleDOI
TL;DR: Considering the Noyes-Whitney dissolution model shows that drug diffusivity, solubility in the gastrointestinal contents, the surface area of the solid wetted by the lumenal fluids and the GI hydrodynamics all play a role in determining the in vivo dissolution rate.

881 citations

Journal ArticleDOI
TL;DR: This review presents an overview of the interplay between manufacturing process, formulation parameters, physical structure, and performance of the solid dispersions with respect to stability and drug release characteristics.

478 citations

Journal ArticleDOI
TL;DR: Combining calculation of Hansen solubility parameters with thermal analysis of drug/excipient miscibility can be successfully applied to predict formation of glass solutions with melt extrusion.

396 citations

"Formulation and Characterization of..." refers methods in this paper

  • ...The amorphization of SUL was confirmed by optical microscopy, differential scanning calorimetry (DSC), X-ray diffraction, hot stage microscopy [18], and dynamic vapor sorption [6, 10, 11, 19–22]....