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      • Cellulose Ethers
      • CMC and Croscarmellose Sodium
      • Converted Starch
      • Dried Starch
      • Microcrystalline Cellulose
      • Modified Starch
      • Starch
      • Sugars
      • Sugar Alcohols
    • Petrochemicals
      • Acrylic Polymers
      • Glycols
      • Mineral Hydrocarbons
      • Mineral Oils
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      • Petrolatum
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      • Povidones
      • Propylene Glycol
      • Other Petrochemical Excipients
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Startseite » News » Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology

Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology

23. November 2020
Solid Dispersion

Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology

Solid dispersion is the preferred technology to prepare efficacious forms of BCS class-II/IV APIs. To prepare solid dispersions, there exist a wide variety of polymeric carriers with interesting physicochemical and thermochemical characteristics available at the disposal of a formulation scientist. Since the advent of the solid dispersion technology in the early 1960s, there have been more than 5000 scientific papers published in the subject area. This review discusses the polymeric carrier properties of most extensively used polymers PVP, Copovidone, PEG, HPMC, HPMCAS, and Soluplus® in the solid dispersion technology. The literature trends about preparation techniques, dissolution, and stability improvement are analyzed from the Scopus® database to enable a formulator to make an informed choice of polymeric carrier. The stability and extent of dissolution improvement are largely dependent upon the type of polymeric carrier employed to formulate solid dispersions. With the increasing acceptance of transfer dissolution setup in the research community, it is required to evaluate the crystallization/precipitation inhibition potential of polymers under dynamic pH shift conditions. Further, there is a need to develop a regulatory framework which provides definition and complete classification along with necessarily recommended studies to characterize and evaluate solid dispersions.

Download the full publication here: Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology

or continue reading here: Nair, A.R., Lakshman, Y.D., Anand, V.S.K. et al. Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology. AAPS PharmSciTech 21, 309 (2020). https://doi.org/10.1208/s12249-020-01849-z

This article gives a great overview and covers the following topics:

  • CLASSIFICATION OF POLYMERIC CARRIERS
  • SELECTION CRITERIA FOR POLYMERIC CARRIERS
  • VINYL PYRROLIDONE DERIVATIVES
  • POLY VINYL PYRROLIDONE (PVP)
  • COPOVIDONE
  • POLY ETHYLENE GLYCOL (PEG)
  • CELLULOSE DERIVATIVES
  • HYDROXY PROPYL METHYL CELLULOSE (HPMC)
  • HYDROXY PROPYL METHYL CELLULOSE ACETATE SUCCINATE (HPMCAS)
  • SOLUPLUS®
  • MANUFACTURING ISSUES OF POLYMERS IN SOLID DISPERSION TECHNOLOGY

Some interesting “outtakes” from this publication

Table I Various Types of Solid Dispersions and Their Relative Potential for Stability and Solubility Improvement

Table II Physicochemical Properties of Polymers Commonly Used in the Preparation of Solid Dispersions

PolymerTypePhysical formMolecular weight (g/Mol)Water solubilityHygroscopicityGlass transition/Melting temperature (°C)Degradation temperature (°C)Solubility parameter (Mpa1/2)
Poly-Vinyl-Pyrrolidone (PVP)PVP K-12Amorphous5000Water solubleHigh120a19621.74
Poly-Vinyl-Pyrrolidone (PVP)PVP K-15Amorphous9700Water solubleHigh130a21521.63
Poly-Vinyl-Pyrrolidone (PVP)PVP K-30Amorphous66,800Water solubleHigh163a17121.69
Poly-Vinyl-Pyrrolidone (PVP)PVP K-60Amorphous396,000Water solubleHigh170aNA21.7
Poly-Vinyl-Pyrrolidone (PVP)PVP K-90Amorphous1,570,000Water solubleHigh174a19421.73
Poly-Vinyl-Pyrrolidone (PVP)PVP K-120Amorphous3,470,000Water solubleHigh174a19421.7
CopovidoneCopovidoneAmorphous45,000–70,000AmphiphilicModerate100–10523021.2
Poly ethylene glycol (PEG)PEG 400Crystalline400IntermediateHighNANA18.9
Poly ethylene glycol (PEG)PEG 600Crystalline600IntermediateHighNA16023.7
Poly ethylene glycol (PEG)PEG 800Crystalline800IntermediateHighNA16023.7
Poly ethylene glycol (PEG)PEG 1000Crystalline1000IntermediateModerate37–4016023.7
Poly ethylene glycol (PEG)PEG 1500Crystalline1500IntermediateModerate44–4816023.7
Poly ethylene glycol (PEG)PEG 2000Crystalline2000IntermediateModerate45–5016017.6
Poly ethylene glycol (PEG)PEG 3000Crystalline3000IntermediateModerate48–54NANA
Poly ethylene glycol (PEG)PEG 4000Crystalline4000IntermediateModerate50–58NANA
Poly ethylene glycol (PEG)PEG 6000Crystalline6000IntermediateModerate55–63NANA
Poly ethylene glycol (PEG)PEG 8000Crystalline8000IntermediateModerate60–63NA19.8
Poly ethylene glycol (PEG)PEG 10000Crystalline10,000IntermediateModerate62–65NA16.6
Poly ethylene glycol (PEG)PEG 20000Crystalline20,000IntermediateModerate60–63NANA
Hydroxypropyl methylcellulose (HPMC)HPMC-EAmorphous85,000–150,000Water solubleHigh141cNA29.95b
Hydroxypropyl methylcellulose (HPMC)HPMC-FAmorphous85,000–150,000Water solubleHigh160c24029.05b
Hydroxypropyl methylcellulose (HPMC)HPMC-KAmorphous85,000–150,000Water solubleHigh172c26030.57b
Hydroxypropyl methylcellulose acetate succinate (HPMCAS)HPMCAS LAmorphous50,000Water soluble above pH 5.0High11920429.1
Hydroxypropyl methylcellulose acetate succinate (HPMCAS)HPMCAS MAmorphous50,000Water soluble above pH 5.0High12019029.1
Hydroxypropyl methylcellulose acetate succinate (HPMCAS)HPMCAS HAmorphous50,000Water soluble above pH 5.0High122NA29.1
Soluplus®Soluplus®Amorphous118,000AmphiphilicModerate7025019.4
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