Application of Film-Casting Technique to Investigate Drug–Polymer Miscibility in Solid Dispersion and Hot-Melt Extrudate

Parikh, Tapan; Gupta, Simerdeep Singh; Meena, Anuprabha; Vitéz, I; Mahajan, Nidhi; Serajuddin, Abu T.M.

doi:10.1002/jps.24446

Cited by 71 publications

(36 citation statements)

References 31 publications

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“…It is also important to investigate the relative miscibility of drugs in different polymers. In a recent investigation, a cellulosic polymer, HPMC phthalate, had about three times the miscibility as that of Kollidon ® VA 64 (24). It will also be interesting to know how miscible Affinisol™ polymers are relative to Kollidon ® VA 64 and other polymers.…”

Section: Discussionmentioning

confidence: 99%

Investigation of Thermal and Viscoelastic Properties of Polymers Relevant to Hot Melt Extrusion, IV: Affinisol™ HPMC HME Polymers

2015

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Abstract. Most cellulosic polymers cannot be used as carriers for preparing solid dispersion of drugs by hot melt extrusion (HME) due to their high melt viscosity and thermal degradation at high processing temperatures. Three HME-grade hydroxypropyl methylcelluloses, namely Affinisol™ HPMC HME 15 cP, Affinisol™ HPMC HME 100 cP, and Affinisol™ HPMC HME 4 M, have recently been introduced by The Dow Chemical Co. to enable the preparation of solid dispersion at lower and more acceptable processing temperatures. In the present investigation, physicochemical properties of the new polymers relevant to HME were determined and compared with that of Kollidon ® VA 64. Powder X-ray diffraction (PXRD), modulated differential scanning calorimetry (mDSC), thermogravimetric analysis (TGA), moisture sorption, rheology, and torque analysis by melt extrusion were applied. PXRD and mDSC showed that the Affinisol™ polymers were amorphous in nature. According to TGA, the onset of degradation for all polymers was >220°C. The Affinisol™ polymers exhibited less hygroscopicity than Kollidon ® VA 64 and another HPMC polymer, Methocel™ K100LV. The complex viscosity profiles of the Affinisol™ polymers as a function of temperature were similar. The viscosity of the Affinisol™ polymers was highly sensitive to the shear rate applied, and unlike Kollidon ® VA 64, the viscosity decreased drastically when the angular frequency was increased. Because of the very high shear rate encountered during melt extrusion, Affinisol™ polymers showed capability of being extruded at larger windows of processing temperatures as compared to that of Kollidon ® VA 64.

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Section: Discussionmentioning

confidence: 99%

Investigation of Thermal and Viscoelastic Properties of Polymers Relevant to Hot Melt Extrusion, IV: Affinisol™ HPMC HME Polymers

2015

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“…They belong to two different classes of polymers; while Soluplus® is a polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer, HPMCAS is a semi-synthetic cellulosic polymer. It was reported by Parikh et al (14) that ITZ was miscible with Soluplus up to 40% w/w (6:4 polymer-drug ratio), and, in a separate study in our laboratory, it was observed that ITZ was miscible with HPMCAS to the extent of 50% w/w (S. Gumaste, Personal communication. Indeed, because of its relatively lower T g , Soluplus® was specifically marketed by its manufacturer for its potential use as a carrier for SD by melt extrusion (43), while HPMCAS is commonly used for solid dispersion by spray drying or other solvent evaporation methods.…”

Section: Introductionmentioning

confidence: 55%

“…Polymer-surfactant and polymer-drug-surfactant miscibility studies were conducted by a film casting method described earlier by Parikh et al (14). Miscibility of each of the two polymers (Soluplus® and HPMCAS) in the binary mixtures with poloxamer 188 was studied at ratios of 9:1, 8:2, 7:3, 6:4, and 5:5 w/w between them.…”

Section: Film Castingmentioning

confidence: 99%

“…Miscibility of each of the two polymers (Soluplus® and HPMCAS) in the binary mixtures with poloxamer 188 was studied at ratios of 9:1, 8:2, 7:3, 6:4, and 5:5 w/w between them. Previously, polymer-to-drug ratios of 9:1, 8:2, 7:3, 6:4, and 5:5 w/w were used to study the miscibility of Soluplus® and HPMCAS with ITZ (14). Previously, polymer-to-drug ratios of 9:1, 8:2, 7:3, 6:4, and 5:5 w/w were used to study the miscibility of Soluplus® and HPMCAS with ITZ (14).…”

Section: Film Castingmentioning

confidence: 99%

“…In particular, the need for large volumes of organic solvents to dissolve both the waterinsoluble drug and the water-soluble polymer in a common medium for the preparation of SDs by other common techniques, such as spray drying, and solvent evaporation (9), can be avoided by applying melt extrusion. Parikh et al (14) has recently published a relatively simple and practical film-casting method that was able to predict drug-polymer miscibility and the absence of drug crystallization in SD. Parikh et al (14) has recently published a relatively simple and practical film-casting method that was able to predict drug-polymer miscibility and the absence of drug crystallization in SD.…”

Section: Introductionmentioning

confidence: 99%

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Investigation of Polymer-Surfactant and Polymer-Drug-Surfactant Miscibility for Solid Dispersion

Gumaste

Gupta

Serajuddin

2016

AAPS J

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In a solid dispersion (SD), the drug is generally dispersed either molecularly or in the amorphous state in polymeric carriers, and the addition of a surfactant is often important to ensure drug release from such a system. The objective of this investigation was to screen systematically polymer-surfactant and polymer-drug-surfactant miscibility by using the film casting method. Miscibility of the crystalline solid surfactant, poloxamer 188, with two commonly used amorphous polymeric carriers, Soluplus® and HPMCAS, was first studied. Then, polymer-drug-surfactant miscibility was determined using itraconazole as the model drug, and ternary phase diagrams were constructed. The casted films were examined by DSC, PXRD and polarized light microscopy for any crystallization or phase separation of surfactant, drug or both in freshly prepared films and after exposure to 40°C/75% RH for 7, 14, and 30 days. The miscibility of poloxamer 188 with Soluplus® was <10% w/w, while its miscibility with HPMCAS was at least 30% w/w. Although itraconazole by itself was miscible with Soluplus® up to 40% w/w, the presence of poloxamer drastically reduced its miscibility to <10%. In contrast, poloxamer 188 had minimal impact on HPMCAS-itraconazole miscibility. For example, the phase diagram showed amorphous miscibility of HPMCAS, itraconazole, and poloxamer 188 at 54, 23, and 23% w/w, respectively, even after exposure to 40°C/75% RH for 1 month. Thus, a relatively simple and practical method of screening miscibility of different components and ultimately physical stability of SD is provided. The results also identify the HPMCAS-poloxamer 188 mixture as an optimal surface-active carrier system for SD.

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Bioadhesive Films for Drug Delivery Systems

Huanbutta

Sangnim

2020

Bioadhesives in Drug Delivery

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Application of Film-Casting Technique to Investigate Drug–Polymer Miscibility in Solid Dispersion and Hot-Melt Extrudate

Cited by 71 publications

References 31 publications

Investigation of Thermal and Viscoelastic Properties of Polymers Relevant to Hot Melt Extrusion, IV: Affinisol™ HPMC HME Polymers

Investigation of Thermal and Viscoelastic Properties of Polymers Relevant to Hot Melt Extrusion, IV: Affinisol™ HPMC HME Polymers

Investigation of Polymer-Surfactant and Polymer-Drug-Surfactant Miscibility for Solid Dispersion

Bioadhesive Films for Drug Delivery Systems

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