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Effect of melt extrudability and melt binding efficiency of polyvinyl caprolactam polyvinyl acetate polyethylene glycol graft copolymer (Soluplus®) on release pattern of hydrophilic and high dose drugs.
Mater Sci Eng C Mater Biol Appl. 2019 Jun; 99:563-574.MS

Abstract

The present study explores the effect of melt binding of Soluplus® on in vitro release profiles of two hydrophilic drugs, metformin hydrochloride, and paracetamol. The melt viscosities of bulk polymer and physical mixtures with different concentrations of selected APIs were analyzed by using a rheometer. The rheological evaluation revealed both the suitable temperature range for melt extrusion process and drug-polymer extrudability. The effect of formulation and processing parameters (e.g. polymer/drug ratio, temperature, screw speed) on extrudability were evaluated in terms of torque and residence time analysis. The extrudates obtained via hot melt extrusion (HME) processing exhibited good flow and compressibility. Differential scanning calorimetry (DSC) and X-ray diffraction studies examined the change in glass transition temperature (Tg) and crystalline pattern of extruded formulations where all extruded formulations seemed to have retained their crystallinity. The thermogravimetric analysis determined the thermal stability (weight loss) as a function of operating temperature whereas scanning electron microscopy (SEM) showed agglomerated microstructure and rough surface with a porous network and void spaces. The tablets obtained after compression of milled extrudates showed excellent hardness with robust tablet characteristics. The in vitro release studies of individual batches performed in various USP recommended dissolution media (for paracetamol) showed the pH-independent release of the hydrophilic drugs from the polymer matrices.

Authors+Show Affiliations

Department of Pharmaceutical Science and Technology, Institute of Chemical Technology, Matunga, Mumbai 400019, India. Electronic address: tousifpharma89@gmail.com.Department of Pharmaceutical Science and Technology, Institute of Chemical Technology, Matunga, Mumbai 400019, India.Department of Pharmacy, School of Life Sciences, University of Sussex, Falmer, Brighton BN1 9QJ, United Kingdom.Department of Pharmaceutical Science and Technology, Institute of Chemical Technology, Matunga, Mumbai 400019, India.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

30889730

Citation

Tousif Ayyub, K, et al. "Effect of Melt Extrudability and Melt Binding Efficiency of Polyvinyl Caprolactam Polyvinyl Acetate Polyethylene Glycol Graft Copolymer (Soluplus®) On Release Pattern of Hydrophilic and High Dose Drugs." Materials Science & Engineering. C, Materials for Biological Applications, vol. 99, 2019, pp. 563-574.
Tousif Ayyub K, Moravkar K, Maniruzzaman M, et al. Effect of melt extrudability and melt binding efficiency of polyvinyl caprolactam polyvinyl acetate polyethylene glycol graft copolymer (Soluplus®) on release pattern of hydrophilic and high dose drugs. Mater Sci Eng C Mater Biol Appl. 2019;99:563-574.
Tousif Ayyub, K., Moravkar, K., Maniruzzaman, M., & Amin, P. (2019). Effect of melt extrudability and melt binding efficiency of polyvinyl caprolactam polyvinyl acetate polyethylene glycol graft copolymer (Soluplus®) on release pattern of hydrophilic and high dose drugs. Materials Science & Engineering. C, Materials for Biological Applications, 99, 563-574. https://doi.org/10.1016/j.msec.2019.01.126
Tousif Ayyub K, et al. Effect of Melt Extrudability and Melt Binding Efficiency of Polyvinyl Caprolactam Polyvinyl Acetate Polyethylene Glycol Graft Copolymer (Soluplus®) On Release Pattern of Hydrophilic and High Dose Drugs. Mater Sci Eng C Mater Biol Appl. 2019;99:563-574. PubMed PMID: 30889730.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effect of melt extrudability and melt binding efficiency of polyvinyl caprolactam polyvinyl acetate polyethylene glycol graft copolymer (Soluplus®) on release pattern of hydrophilic and high dose drugs. AU - Tousif Ayyub,K, AU - Moravkar,Kailas, AU - Maniruzzaman,Mohammed, AU - Amin,Purnima, Y1 - 2019/01/29/ PY - 2018/01/05/received PY - 2019/01/26/revised PY - 2019/01/28/accepted PY - 2019/3/21/entrez PY - 2019/3/21/pubmed PY - 2019/7/11/medline KW - Drug release KW - Extrudability KW - Hydrophilic drugs KW - Melt binding KW - Soluplus® SP - 563 EP - 574 JF - Materials science & engineering. C, Materials for biological applications JO - Mater Sci Eng C Mater Biol Appl VL - 99 N2 - The present study explores the effect of melt binding of Soluplus® on in vitro release profiles of two hydrophilic drugs, metformin hydrochloride, and paracetamol. The melt viscosities of bulk polymer and physical mixtures with different concentrations of selected APIs were analyzed by using a rheometer. The rheological evaluation revealed both the suitable temperature range for melt extrusion process and drug-polymer extrudability. The effect of formulation and processing parameters (e.g. polymer/drug ratio, temperature, screw speed) on extrudability were evaluated in terms of torque and residence time analysis. The extrudates obtained via hot melt extrusion (HME) processing exhibited good flow and compressibility. Differential scanning calorimetry (DSC) and X-ray diffraction studies examined the change in glass transition temperature (Tg) and crystalline pattern of extruded formulations where all extruded formulations seemed to have retained their crystallinity. The thermogravimetric analysis determined the thermal stability (weight loss) as a function of operating temperature whereas scanning electron microscopy (SEM) showed agglomerated microstructure and rough surface with a porous network and void spaces. The tablets obtained after compression of milled extrudates showed excellent hardness with robust tablet characteristics. The in vitro release studies of individual batches performed in various USP recommended dissolution media (for paracetamol) showed the pH-independent release of the hydrophilic drugs from the polymer matrices. SN - 1873-0191 UR - https://www.unboundmedicine.com/medline/citation/30889730/Effect_of_melt_extrudability_and_melt_binding_efficiency_of_polyvinyl_caprolactam_polyvinyl_acetate_polyethylene_glycol_graft_copolymer__Soluplus��__on_release_pattern_of_hydrophilic_and_high_dose_drugs_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0928-4931(18)30063-8 DB - PRIME DP - Unbound Medicine ER -