Solid state transformations in consequence of electrospraying – A novel polymorphic form of piroxicam

“…The same group even reported that piroxicam was converted to a previously unknown crystal structure after electrospraying. 20 The previously mentioned studies highlight the complexity of electrospraying in preparing amorphous SDs. It could be anticipated because amorphous materials are thermodynamically unstable and inherently have a tendency to crystallize.…”

Section: Process-related Problems Using Electrospraying For Amorphous Sdmentioning

confidence: 98%

“…Therefore in several studies, a supplementary configuration of nozzleering and needle can be introduced. [16][17][18][19][20][21][22] This configuration, commonly called corona neutralizer, is connected to a separate high voltage source and consists of a discharging stainless steel ring or needle, placed opposite to or concentrically around the nozzle. The charged droplets produced from the nozzle will be discharged when they come across the region of these neutralizers.…”

Section: The Basic Principles Of Electrosprayingmentioning

confidence: 99%

Pharmaceutical Applications of Electrospraying

Nguyen

Clasen

Mooter

2016

Journal of Pharmaceutical Sciences

153

128

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The electrohydrodynamic atomization technique, or simply called electrospraying, has been extensively studied for biomedical as well as for pharmaceutical applications over the past years. The simplicity, flexibility, and efficiency of producing particles at the microscale or nanoscale, with tailored size, shape, morphology, and microstructure, make electrospraying to become one of the most promising and well-practiced approaches to be applied in many biomedical and pharmaceutical fields, from improving the bioavailability of poorly aqueous soluble drugs, preparing targeted drug delivery systems, and controllable drug release systems to delivering sensitive therapeutic agents such as protein-based drugs or even living cells. Nevertheless, some issues still remain with respect to low throughput as well as the complex interplay between a great number of processing and formulation factors. A comprehensive understanding of these fundamental aspects is essential for the successful application of electrospraying for the production of particulate formulations with desired properties.

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“…But the quantitative content of phases (judging by the change in the intensity of the peaks) is very different. It is possible that this factor had a decisive impact on the analgesic effect of the crystalline forms of amide (2).…”

Section: Issn 2308-8303mentioning

confidence: 99%

“…And if the original interest in such objects was caused solely by curiosity of researchers, but by the accumulation of information about the diversity of the properties of polymorphic substances it gradually became practical. This area of crystallography has found especially bright and productive reflection in medicinal chemistry [1][2][3][4][5]. As it turned out, polymorphism of drugs is capable to change their characteristics radically, and now no serious pharmaceutical manufacturer can ignore the problem [6][7][8][9].…”

mentioning

confidence: 99%

Polymorphism and the analgesic activity of N-(3-pyridylmethyl)-4-hydroxy-2-oxo-1,2,5,6,7,8-hexahydroquinoline-3-carboxamide

Украинец

Mospanova

Bereznyakova

et al. 2015

J. org. pharm. chem.

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selected by the results of the primary pharmacological screening as the leading structure has revealed a significant change in anesthetic properties in different samples of this compound. Since the substance under study was not soluble in water, and animals received it orally as a thin aqueous suspension, the most likely cause of the effect observed was thought to be the changes in the crystalline structure of N- (3pyridylmethyl)-4-hydroxy-2-oxo-1,2,5,6,7,8-hexahydroquinoline-3-carboxamide occurring in it under the influence of external factors. This assumption has been fully confirmed by the thorough microscopic investigation of high -and low-active samples, as well as more objective data, the methods of powder and single crystal X-ray diffraction analysis. Thus, in particular, it has been found that with all the variety of crystalline and amorphous forms included in the samples studied their qualitative composition appeared to be quite similar. At the same time the quantitative content of some of the phases varies greatly, and obviously, it was the factor determining the size of the analgesic effect.ПОЛІМОРФІЗМ ТА АНАЛГЕТИЧНА , відібраного за результатами первинного фармакологічного скринінгу як структури-лідера, виявило суттєву зміну знеболюючих властивостей у різних зразків цієї сполуки. Оскільки досліджувана речовина нерозчинна у воді і піддослідним тваринам вводилась перорально у вигляді тонкої водної суспензії, то найбільш ймовірною причиною виявленого ефекту визнали зміни кристалічної будови N-(3-піридилметил)-4-гідрокси-2-оксо-1,2,5,6,7,8-гексагідрохінолін-3-карбоксаміду, які відбуваються у ньому під впливом зовнішніх факторів. Це припущення повністю підтвердилось ретельним мікроскопічним дослідженням високо-та низькоактивного зразків, а також більш об'єктивними даними, одержаними методами порошкового і монокристалічного рентгеноструктурного аналізу. Так, зокрема, встановлено, що при всьому розмаїтті кристалічних та аморфних форм, що входять у досліджувані зразки, їх якісний склад виявився доволі схожим. В той же час кількісний вміст деяких фаз сильно розрізняється, що, очевидно, й послужило визначальним фактором для величини аналгетичного ефекту. ПОЛИМОРФИЗМ И АНАЛЬГЕТИЧЕСКАЯ , отобранного по результатам первичного фармакологического скрининга в качестве структуры-лидера, выявило существенное изменение обезболивающих свойств у разных образцов этого соединения. Поскольку испытуемое вещество не растворимо в воде и подопытным животным вводилось перорально в виде тонкой водной суспензии, то наиболее вероятной причиной обнаруженного эффекта посчитали изменения кристаллического строения N-(3-пиридилметил)-4гидрокси-2-оксо-1,2,5,6,7,8-гексагидрохинолин-3-карбоксамида, происходящие в нем под воздействием внешних факторов. Это предположение полностью подтвердилось тщательным микроскопическим исследованием высоко-и низкоактивного образцов, а также более объективными данными, полученными методами порошкового и монокристаллического рентгеноструктурного анализа. Так, в частности, установлено, что при всем многообр...

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Solid state transformations in consequence of electrospraying – A novel polymorphic form of piroxicam

Cited by 37 publications

References 33 publications

Controlled release of drugs in electrosprayed nanoparticles for bone tissue engineering

Controlled release of drugs in electrosprayed nanoparticles for bone tissue engineering

Pharmaceutical Applications of Electrospraying

Polymorphism and the analgesic activity of N-(3-pyridylmethyl)-4-hydroxy-2-oxo-1,2,5,6,7,8-hexahydroquinoline-3-carboxamide

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