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Clathrate Hydrates of Organic Solvents as Auxiliary Intermediates in Pharmaceutical Research and Development: Improving Dissolution Behaviour of a New Anti-Tuberculosis Drug, Perchlozon.
Ogienko, Andrey G; Myz, Svetlana A; Nefedov, Andrey A; Ogienko, Anna A; Adamova, Tatyana P; Voronkova, Olga M; Amosova, Svetlana V; Trofimov, Boris A; Boldyrev, Vladimir V; Boldyreva, Elena V.
  • Ogienko AG; Faculty of Natural Sciences, Novosibirsk State University, 630090 Novosibirsk, Russia.
  • Myz SA; LLC "SP IIC", 630049 Novosibirsk, Russia.
  • Nefedov AA; LLC "SP IIC", 630049 Novosibirsk, Russia.
  • Ogienko AA; Faculty of Natural Sciences, Novosibirsk State University, 630090 Novosibirsk, Russia.
  • Adamova TP; N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 630090 Novosibirsk, Russia.
  • Voronkova OM; Institute of Molecular and Cellular Biology, Siberian Branch of the Russian Academy of Sciences, 630090 Novosibirsk, Russia.
  • Amosova SV; A.V. Nikolaev Institute of Inorganic Chemistry, Siberian Branch of the Russian Academy of Sciences, 630090 Novosibirsk, Russia.
  • Trofimov BA; LLC "SP IIC", 630049 Novosibirsk, Russia.
  • Boldyrev VV; A.E. Favorsky Irkutsk Institute of Chemistry, Siberian Branch of the Russian Academy of Sciences, 664033 Irkutsk, Russia.
  • Boldyreva EV; A.E. Favorsky Irkutsk Institute of Chemistry, Siberian Branch of the Russian Academy of Sciences, 664033 Irkutsk, Russia.
Pharmaceutics ; 14(3)2022 Feb 24.
Article in English | MEDLINE | ID: covidwho-1765809
ABSTRACT
There is an urgent need for new drugs to overcome the challenge of the ever-growing drug resistance towards tuberculosis. A new, highly efficient anti-tuberculosis drug, Perchlozone (thioureidoiminomethylpyridinium perchlorate, Pz), is only available in an oral dosage form, though injectable forms and inhalation solutions could be better alternatives, offering higher bioavailability. To produce such forms, nano- and micro-particles of APIs would need to be prepared as dispersions with carriers. We use this case study to illustrate the principles of selecting solvents and excipients when preparing such formulations. We justify the choice of water-THF (19.1 wt % THF) as solvent and mannitol as carrier to prepare formulations of Pz-a poorly soluble compound-that are suitable for injection or inhalation. The formulations could be prepared by conventional freeze-drying in vials, making the proposed method suitable for industrial scaling. A similar strategy for selecting the organic solvent and the excipient can be applied to other compounds with low water solubility.
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Full text: Available Collection: International databases Database: MEDLINE Language: English Year: 2022 Document Type: Article Affiliation country: Pharmaceutics14030495

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Full text: Available Collection: International databases Database: MEDLINE Language: English Year: 2022 Document Type: Article Affiliation country: Pharmaceutics14030495