Amorphous Solid Dispersions

Shah, Navnit; Sandhu, Harpreet; Choi, Duk Soon; Chokshi, Hitesh; Malick, A. Waseem

doi:10.1007/978-1-4939-1598-9

Cited by 108 publications

(3 citation statements)

References 562 publications

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“…Five pharmaceutical polymers, which are commonly used as carriers for the manufacturing of ASDs, hydroxypropyl methylcellulose acetate succinate (HPMCAS, AQOAT AS-LG, Shin-Etsu, Venlo, Netherlands), methacrylic acid copolymer (Eudragit L100–55, Evonik, Essen, Germany), aminoalkyl methacrylate copolymer (Eudragit EPO, Evonik, Essen, Germany), hydroxypropyl methylcellulose (HPMC, AFFINISOL HPMC HME 15 cP, DuPont, Milano, Italy) and vinylpyrrolidone vinylacetate copolymer (Kollidon VA64, BASF, Basel, Switzerland) were investigated ( Baghel et al, 2016 ; Shah et al, 2014 ). Microcrystalline cellulose (MCC, Vivapur 102, JRS Pharma, Rosenberg, Germany), a hydrophilic and water-insoluble excipient, and mannitol (PEARLITOL 200 SD, Roquette, Vernier, Switzerland), a hydrophilic and water-soluble excipient, were used as fillers ( Paul et al, 2018 ; Thoorens et al, 2014 ).…”

Section: Methodsmentioning

confidence: 99%

Tablet formulation development focusing on the functional behaviour of water uptake and swelling

Lenz

Finke

Bunjes

et al. 2021

International Journal of Pharmaceutics: X

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Section: Methodsmentioning

confidence: 99%

Tablet formulation development focusing on the functional behaviour of water uptake and swelling

Lenz

Finke

Bunjes

et al. 2021

International Journal of Pharmaceutics: X

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“…14 ASDs improve drug solubility through multiple mechanisms, including wettability, particle size reduction, intermolecular interactions, and amorphization. 15,16 Further, spray drying, 17 hot-melt extrusion, 18 freeze drying, 19 quench cooling, 20 and solvent evaporation 21 were widely used techniques to prepare ASDs. Amorphous Salt Solid Dispersion (ASSD) is a novel strategy that combines the advantages of amorphization and salt formation to improve amorphous drug physical stability, aqueous solubility, and dissolution rate.…”

Section: Introductionmentioning

confidence: 99%

Solid State Characterization and Miscibility of Raltegravir in Soluplus Using Solid Dispersion Technology

Yarlagadda,

Nayak,

Bhat

2023

Ind. J. Pharm. Edu. Res.

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Background: Raltegravir Potassium (RTGP), a BCS class II drug used in the treatment of HIV, has minimal solubility in the aqueous medium, resulting in poor bioavailability; Further, RTGP poor dissolution and limited solubility are also major factors responsible for the significant inter-and intra-patient variability in absorption following oral administration. Objectives: To enhance the solubility of Raltegravir potassium and its free acid using Soluplus ® by solid dispersion technology. Materials and Methods: In the current study, Amorphous Solid Dispersions (ASDs) of RTGP and Raltegravir free acid (RTG) of 20:80% w/w with Soluplus ® (SLP) were prepared using quench cooling. The prepared ASDs analyzed for homogenous single-phase formation and intermolecular interactions employing DSC, XRD, and FT-IR. The drug-polymer miscibility was calculated theoretically as well as experimentally with the aid of Hansen solubility parameter and melting point depression methods. The solubility of the ASDs was evaluated by the shake flask method. Results: Quench cooling yielded an RTGP-SLP and RTG-SLP homogeneous amorphous systems. DSC and XRPD results showed the complete transformation of crystalline to the amorphous phase for ASDs. Intermolecular interactions in specific hydrogen bonding were observed between the carbonyl (-C=O) group of Soluplus ® and the Raltegravir -N-H moiety. RTG solubility in salt solid dispersion increases by 10.7 and 17.4 folds, respectively, compared to pure forms. Furthermore, free acid ASDs improved solubility by 8.7 and 14.1 folds, respectively, compared to their pure compounds. Conclusion: Salt solid dispersion showed a greater extent of miscibility and improved solubility of RTG compared to free acid solid dispersion.

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“…PVP/VA copolymer, PVP or PEG) as carrier polymer. Technologies to produce solid dispersion includes spray drying, hot melt extrusion, co-precipitation, fluid bed granulation, and recently the Kinetisol process and others have been reported ( Friesen et al, 2008 ; Hughey et al, 2015 ; Mendonsa et al, 2020 ; Sandhu et al, 2014 ). However commercial products mostly rely on spray drying and hot melt extrusion technology ( Matić et al, 2020 ; Solanki et al, 2019 ; Zhang et al, 2018 ).…”

Section: Introductionmentioning

confidence: 99%

Downstream processing of spray-dried ASD with hypromellose acetate succinate – Roller compaction and subsequent compression into high ASD load tablets

Sauer¹,

Warashina

Mishra³

et al. 2021

International Journal of Pharmaceutics: X

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Despite wide commercial application of hypromellose acetate succinate (HPMCAS) in spray-dried amorphous solid dispersion (ASD) drug products, little information is available in the references on downstream processing of spray-dried dispersions with HPMCAS. Poor flow and high dilution factor are a challenge in formulating spray-dried ASDs into tablets, leaving little space for other excipients facilitating binding and disintegration. Direct compression is not possible due to the poor powder flow of spray-dried ASDs. Moisture has to be avoided due to the plasticizing properties of water on the ASD, resulting in reduced stability of the amorphous state. Thus, dry granulation by roller compaction and subsequent tablet compression is the preferred downstream process. We report the investigation of downstream processing by roller compaction and tablet compression of a high load formulation with 75% of spray-dried amorphous solid dispersion (Nifedipine:HPMCAS 1:2). A head to head comparison of microcrystalline cellulose/croscarmellose (MCC/cl-NaCMC) as binder/disintegrant vs. MCC and low-substituted hydroxypropyl cellulose (L-HPC) as excipient for binding and disintegration showed improved re-workability of the formulation with MCC/L-HPC after roller compaction. Upon transfer to the rotary press, a 45% higher tensile strength of tablets is observed after dry granulation with MCC/L-HPC.

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Amorphous Solid Dispersions

Cited by 108 publications

References 562 publications

Tablet formulation development focusing on the functional behaviour of water uptake and swelling

Tablet formulation development focusing on the functional behaviour of water uptake and swelling

Solid State Characterization and Miscibility of Raltegravir in Soluplus Using Solid Dispersion Technology

Downstream processing of spray-dried ASD with hypromellose acetate succinate – Roller compaction and subsequent compression into high ASD load tablets

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