Clathrate Hydrates of Organic Solvents as Auxiliary Intermediates in Pharmaceutical Research and Development: Improving Dissolution Behaviour of a New Anti-Tuberculosis Drug, Perchlozon | Sciact - CRIS-система Института катализа

Clathrate Hydrates of Organic Solvents as Auxiliary Intermediates in Pharmaceutical Research and Development: Improving Dissolution Behaviour of a New Anti-Tuberculosis Drug, Perchlozon Научная публикация

Журнал

Pharmaceutics
ISSN: 1999-4923

Вых. Данные

Год: 2022, Том: 14, Номер: 3, Номер статьи : 495, Страниц : 16 DOI: 10.3390/pharmaceutics14030495

Ключевые слова

formulations for inhalation; formulations for injections; freeze-drying; anti-tuberculosis drugs; clathrate hydrates

Авторы

Ogienko Andrey G. ^1,2 , Myz Svetlana A. ² , Nefedov Andrey A. ^1,3 , Ogienko Anna A. ⁴ , Adamova Tatyana P. ⁵ , Voronkova Olga M. ² , Amosova Svetlana V. ⁶ , Trofimov Boris A. ⁶ , Boldyrev Vladimir V. ^1,7 , Boldyreva Elena V. ^1,8

Организации

1	Faculty of Natural Sciences, Novosibirsk State University, 630090 Novosibirsk, Russia
2	LLC “SP IIC”, 630049 Novosibirsk, Russia
3	N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 630090 Novosibirsk, Russia
4	Institute of Molecular and Cellular Biology, Siberian Branch of the Russian Academy of Sciences, 630090 Novosibirsk, Russia
5	A.V. Nikolaev Institute of Inorganic Chemistry, Siberian Branch of the Russian Academy of Sciences, 630090 Novosibirsk, Russia
6	A.E. Favorsky Irkutsk Institute of Chemistry, Siberian Branch of the Russian Academy of Sciences, 664033 Irkutsk, Russia
7	V.V. Voevodsky Institute of Chemical Kinetics and Combustion, Siberian Branch of the Russian Academy of Sciences, 630090 Novosibirsk, Russia
8	G.K. Boreskov Institute of Catalysis, Siberian Branch of the Russian Academy of Sciences, 630090 Novosibirsk, Russia

Информация о финансировании (9)

1	Российский фонд фундаментальных исследований	17-03-00784 (АААА-А17-117040710138-5)
2	Министерство науки и высшего образования Российской Федерации (с 15 мая 2018)	0239-2021-0002
3	Министерство науки и высшего образования Российской Федерации (с 15 мая 2018)	0236-2021-0001
4	Министерство науки и высшего образования Российской Федерации (с 15 мая 2018)	075-00610-21-01 (122011900429-5) FWGZ-2021-0017
5	Федеральное агентство научных организаций России	V.44.5.6 (01201281994)
6	Фонд развития интернет-инициатив
7	Агентство стратегических инициатив	HealthNet
8	Министерство науки и высшего образования Российской Федерации (с 15 мая 2018)
9	Министерство науки и высшего образования Российской Федерации (с 15 мая 2018)	0238-2021-0005 (АААА-А21-121011490018-2)

There is an urgent need for new drugs in order to overcome the challenge of the ever growingever-growing drug resistance towards tuberculosis. A new highly efficient an-ti-tuberculosis drug, Perchlozone (thioureidoiminomethylpyridinium perchlorate, Pz) is only available as an oral dosage form, though injectable forms and inhalation solutions could be bet-ter alternatives, offering higher bioavailability. In order tTo produce such forms, nano- and mi-cro-particles of APIs 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 injections or inhalations. The formulations could be prepared by conventional freeze-drying in vials, making the pro-posed method suitable for industrial scaling. Similar A similar strategy of selecting the organic solvent and the excipient can be applied to other compounds with low water solubility.

Ogienko A.G. , Myz S.A. , Nefedov A.A. , Ogienko A.A. , Adamova T.P. , Voronkova O.M. , Amosova S.V. , Trofimov B.A. , Boldyrev V.V. , Boldyreva E.V.
Clathrate Hydrates of Organic Solvents as Auxiliary Intermediates in Pharmaceutical Research and Development: Improving Dissolution Behaviour of a New Anti-Tuberculosis Drug, Perchlozon
Pharmaceutics. 2022. V.14. N3. 495 :1-16. DOI: 10.3390/pharmaceutics14030495 WOS Scopus РИНЦ CAPlus PMID OpenAlex

Поступила в редакцию:	29 дек. 2021 г.
Принята к публикации:	21 февр. 2022 г.
Опубликована online:	24 февр. 2022 г.
Опубликована в печати:	1 мар. 2022 г.

Web of science:	WOS:000774531600001
Scopus:	2-s2.0-85125641787
РИНЦ:	48187443
Chemical Abstracts:	2022:1002369
PMID (PubMed):	35335870
OpenAlex:	W4214567811

БД	Цитирований
Scopus	2
Web of science	1
OpenAlex	1