Phase behavior of ASDs based on hydroxypropyl cellulose

Luebbert, Christian; Stoyanov, Edmont V.; Sadowski, Gabriele

doi:10.1016/j.ijpx.2020.100070

Cited by 17 publications

(24 citation statements)

References 60 publications

(26 reference statements)

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“…The CUR-MAG CM revealed an 8.4 °C negative deviation of T g from the theoretical value, indicating that there might be weak intermolecular interactions in CUR-MAG CM, which were further investigated by spectral analysis. The T g values of HPMC, HPC, and PVP K30 were determined to be 140.4 [ 10 ], 86.2 [ 47 ] and 176.0 °C [ 48 ], as previously reported, which were used to calculate the theoretical T g s of the ternary co-amorphous systems. When CUR-MAG CM was regarded as a single amorphous “component”, CUR-MAG-HPMC CM, CUR-MAG-HPC CM, and CUR-MAG-PVP K30 CM showed theoretical T g values of about 22.0, 21.9, and 22.0 °C, and their experimental T g values exhibited 4.1, 1.6, and 15.4 °C positive deviation from the theoretical values, respectively ( Figure 3 and Table 1 ).…”

Section: Resultsmentioning

confidence: 99%

Deaggregation and Crystallization Inhibition by Small Amount of Polymer Addition for a Co-Amorphous Curcumin-Magnolol System

Han

et al. 2021

Pharmaceutics

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Different from previously reported co-amorphous systems, a co-amorphous curcumin-magnolol (CUR-MAG CM) system, as compared with its crystalline counterparts, exhibited decreased dissolution due to its aggregation during dissolution. The main purpose of the present study is to deaggregate CUR-MAG CM to optimize drug dissolution and explore the deaggregation mechanism involved. Herein, a small amount of polymer (HPMC, HPC, and PVP K30) was co-formulated at 5% (w/w) with CUR-MAG CM as ternary co-amorphous systems. The polymer addition changed the surface properties of CUR-MAG CM including improved water wettability enhanced surface free energy, and hence exerted a deaggregating effect. As a result, the ternary co-amorphous systems showed faster and higher dissolution as compared with crystalline CUR/MAG and CUR-MAG CM. In addition, the nucleation and crystal growth of dissolved CUR and MAG molecules were significantly inhibited by the added polymer, maintaining a supersaturated concentration for a long time. Furthermore, polymer addition increased the Tg of CUR-MAG CM, potentially involving molecular interactions and inhibiting molecular mobility, resulting in enhanced physical stability under 25 °C/60% RH and 40 °C/75% RH conditions. Therefore, this study provides a promising strategy to optimize the dissolution and physical stability of co-amorphous systems by deaggregation and crystallization inhibition via adding small amounts of polymers.

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Section: Resultsmentioning

confidence: 99%

Deaggregation and Crystallization Inhibition by Small Amount of Polymer Addition for a Co-Amorphous Curcumin-Magnolol System

Han

et al. 2021

Pharmaceutics

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“…Unfortunately, our DSC method was not able to detect a T g for HPC SSL, which is a well-known issue of HPC. Therefore, we used a T g for HPC SSL which was recently published by Luebbert et al as a predicted T g of 81.8 °C ( Luebbert et al, 2020 ). Our DSC thermogram of HPC SSL can be found in the Supplementary Data (Fig.…”

Section: Resultsmentioning

confidence: 99%

Boost of solubility and supersaturation of celecoxib via synergistic interactions of methacrylic acid-ethyl acrylate copolymer (1:1) and hydroxypropyl cellulose in ternary amorphous solid dispersions

Pöstges

Kayser

Stoyanov³

et al. 2022

International Journal of Pharmaceutics: X

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“…A temperature ramp from 90 • C to 200 • C is applied to investigate the effect of the temperature on the rheological behaviors of HPMC and HPC. The glass transition temperatures of HPMC HME 4M and HPC GXF are reported at 115 • C [31] and 84 • C [32], respectively; therefore, the temperature ramp tested is directly in the range of interest. The complex viscosity and tan δ as a function of the temperature are depicted in Figure 5.…”

Section: Dissolution and Semmentioning

confidence: 99%

Comparison of Hydroxypropylcellulose and Hot-Melt Extrudable Hypromellose in Twin-Screw Melt Granulation of Metformin Hydrochloride: Effect of Rheological Properties of Polymer on Melt Granulation and Granule Properties

et al. 2021

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High-molecular-weight hypromellose (HPMC) and hydroxypropyl cellulose (HPC) are widely known, extended-release polymers. Conventional high-molecular-weight HPMCs are preferred in extended-release applications but not widely used in twin-screw melt granulation due to processability difficulties at low operating temperatures and potential drug degradation if high processing temperatures are used. Conversely, high-molecular-weight grade HPC (Klucel®) can be used in melt granulation processes. The purpose of this study was to evaluate the processability and dissolution behavior of HPC GXF ((Klucel® GXF) and a recently introduced type of hot-melt extrudable HPMC (Affinisol®) in extended-release metformin hydrochloride formulations using twin-screw melt granulation. Powder blends were prepared with 75% w/w metformin HCl and 25% w/w polymeric binder. Blends were granulated at processing temperatures of 160, 140, 120 and 100 °C. HPMC HME 4M (Affinisol® 4M) provided a fine powder, indicating minimum granulation at processing temperatures lower than 160 °C, and the tablets obtained with these granules capped during tableting. In contrast, acceptable tablets could be obtained with HPC GXF at all processing temperatures. Rheological studies including capillary rheometry to measure steady shear rate viscosity, and rotational rheometry to obtain time and temperature superposition data, showed that HPC GXF had a greater thermoplasticity than HPMC HME 4M, which made granulation possible with HPC GXF at low temperatures. Tablets compressed with granules obtained at 160 °C with both binders showed comparable dissolution profiles. High-molecular-weight HPC GXF provided a better processability at low temperatures and adequate tablet strength for the melt granulation of metformin HCl.

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Phase behavior of ASDs based on hydroxypropyl cellulose

Cited by 17 publications

References 60 publications

Deaggregation and Crystallization Inhibition by Small Amount of Polymer Addition for a Co-Amorphous Curcumin-Magnolol System

Deaggregation and Crystallization Inhibition by Small Amount of Polymer Addition for a Co-Amorphous Curcumin-Magnolol System

Boost of solubility and supersaturation of celecoxib via synergistic interactions of methacrylic acid-ethyl acrylate copolymer (1:1) and hydroxypropyl cellulose in ternary amorphous solid dispersions

Comparison of Hydroxypropylcellulose and Hot-Melt Extrudable Hypromellose in Twin-Screw Melt Granulation of Metformin Hydrochloride: Effect of Rheological Properties of Polymer on Melt Granulation and Granule Properties

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