Solid state characteristics of ternary solid dispersions composed of PVP VA64, Myrj 52 and itraconazole

Solid multicomponent systems (SMS) are gaining an increasingly important role in the pharmaceutical industry, to improve the physicochemical properties of active pharmaceutical ingredients (APIs). In recent years, various processes have been employed for SMS manufacturing. Control of the particle solid-state properties, such as size, morphology, and crystal form is required to optimize the SMS formulation. By utilizing the unique and tunable properties of supercritical fluids, supercritical anti-solvent (SAS) process holds great promise for the manipulation of the solid-state properties of APIs. The SAS techniques have been developed from batch to continuous mode. Their applications in SMS preparation are summarized in this review. Many pharmaceutical co-crystals and solid dispersions have been successfully produced via the SAS process, where the solid-state properties of APIs can be well designed by controlling the operating parameters. The underlying mechanisms on the manipulation of solid-state properties are discussed, with the help of on-line monitoring and computational techniques. With continuous researching, SAS process will give a large contribution to the scalable and continuous manufacturing of desired SMS in the near future.

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ChemInform Abstract: Polymeric Amorphous Solid Dispersions: A Review of Amorphization, Crystallization, Stabilization, Solid-State Characterization, and Aqueous Solubilization of Biopharmaceutical Classification System Class II Drugs

ChemInform ◽

10.1002/chin.201642262 ◽

2016 ◽

Vol 47 (42) ◽

Author(s):

Shrawan Baghel ◽

Helen Cathcart ◽

Niall J. O'Reilly

Keyword(s):

Solid State ◽

Classification System ◽

Solid Dispersions ◽

Amorphous Solid ◽

Class Ii ◽

Amorphous Solid Dispersions ◽

Biopharmaceutical Classification System ◽

Solid State Characterization

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New metastable form of glibenclamide prepared by redispersion from ternary solid dispersions containing polyvinylpyrrolidone-K30 and sodium lauryl sulfate

Drug Development and Industrial Pharmacy ◽

10.3109/03639045.2015.1029938 ◽

2015 ◽

Vol 42 (1) ◽

pp. 70-79 ◽

Cited By ~ 4

Author(s):

Thanu Thongnopkoon ◽

Satit Puttipipatkhachorn

Keyword(s):

Sodium Lauryl Sulfate ◽

Solid Dispersions ◽

Lauryl Sulfate ◽

Metastable Form ◽

Ternary Solid Dispersions

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Solid-State NMR Investigation of Drug-Excipient Interactions and Phase Behavior in Indomethacin-Eudragit E Amorphous Solid Dispersions

Pharmaceutical Research ◽

10.1007/s11095-018-2364-y ◽

2018 ◽

Vol 35 (3) ◽

Cited By ~ 9

Author(s):

Joseph W. Lubach ◽

Jonathan Hau

Keyword(s):

Solid State ◽

Phase Behavior ◽

Solid State Nmr ◽

Solid Dispersions ◽

Amorphous Solid ◽

Amorphous Solid Dispersions ◽

Eudragit E ◽

Excipient Interactions

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Effect of Drug–Polymer Interactions through Hypromellose Acetate Succinate Substituents on the Physical Stability on Solid Dispersions Studied by Fourier-Transform Infrared and Solid-State Nuclear Magnetic Resonance

Molecular Pharmaceutics ◽

10.1021/acs.molpharmaceut.9b00301 ◽

2019 ◽

Vol 16 (6) ◽

pp. 2785-2794 ◽

Cited By ~ 9

Author(s):

Yuya Ishizuka ◽

Keisuke Ueda ◽

Hitomi Okada ◽

Junpei Takeda ◽

Masatoshi Karashima ◽

...

Keyword(s):

Nuclear Magnetic Resonance ◽

Fourier Transform ◽

Solid State ◽

Magnetic Resonance ◽

Solid Dispersions ◽

Physical Stability ◽

Fourier Transform Infrared ◽

Polymer Interactions ◽

Hypromellose Acetate Succinate ◽

Nuclear Magnetic

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Different BCS Class II Drug-Gelucire Solid Dispersions Prepared by Spray Congealing: Evaluation of Solid State Properties and In Vitro Performances

Pharmaceutics ◽

10.3390/pharmaceutics12060548 ◽

2020 ◽

Vol 12 (6) ◽

pp. 548 ◽

Cited By ~ 1

Author(s):

Serena Bertoni ◽

Beatrice Albertini ◽

Nadia Passerini

Keyword(s):

Solid State ◽

Drug Carrier ◽

Solid Dispersions ◽

Class Ii ◽

Water Soluble ◽

Drug Dissolution ◽

Crystalline Solid ◽

Dissolution Behavior ◽

Bcs Class Ii

Delivery of poorly water soluble active pharmaceutical ingredients (APIs) by semi-crystalline solid dispersions prepared by spray congealing in form of microparticles (MPs) is an emerging method to increase their oral bioavailability. In this study, solid dispersions based on hydrophilic Gelucires® (Gelucire® 50/13 and Gelucire® 48/16 in different ratio) of three BCS class II model compounds (carbamazepine, CBZ, tolbutamide, TBM, and cinnarizine, CIN) having different physicochemical properties (logP, pKa, Tm) were produced by spray congealing process. The obtained MPs were investigated in terms of morphology, particles size, drug content, solid state properties, drug-carrier interactions, solubility, and dissolution performances. The solid-state characterization showed that the properties of the incorporated drug had a profound influence on the structure of the obtained solid dispersion: CBZ recrystallized in a different polymorphic form, TBM crystallinity was significantly reduced as a result of specific interactions with the carrier, while smaller crystals were observed in case of CIN. The in vitro tests suggested that the drug solubility was mainly influenced by carrier composition, while the drug dissolution behavior was affected by the API solid state in the MPs after the spray congealing process. Among the tested APIs, TBM-Gelucire dispersions showed the highest enhancement in drug dissolution as a result of the reduced drug crystallinity.

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