Drug particle shape and size control: A necessary factor for high-quality drug production

Emshanova, S. V.; Sadchikova, N. P.; Зуев, А. П.

doi:10.1007/s11094-007-0010-9

Cited by 6 publications

(3 citation statements)

References 4 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…For many years, the particle size of pharmaceutical substances has been considered a key parameter that provides the full range of their properties as drugs [28][29][30][31]. Therefore, it is not surprising that this parameter was carefully controlled at various stages of work with drugs-from their research development to industrial production.…”

Section: Evaluation Of the Biological Propertiesmentioning

confidence: 99%

Crystal Habits and Biological Properties of N-(4-Trifluoromethylphenyl)-4-Hydroxy-2,2-Dioxo-1H-2λ6,1-Benzothiazine-3-Carboxamide

et al. 2019

View full text Add to dashboard Cite

In order to study polymorphic modifications of N-(4-trifluoromethylphenyl)-4-hydroxy-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamide, which is of interest as a promising analgesic, its three colorless crystal forms with different habitus have been obtained: sticks of ethyl acetate, plates of meta-xylene and blocks of ortho-xylene. However, the X-ray diffraction analysis has shown that all the forms studied have the identical molecular and crystal structure in spite of such significant differences in appearance. Moreover, pharmacological tests have revealed significant differences in the analgesic activity in these samples (a total of five experimental models were used: “acetic-acid-induced writhing”, “hot plate”, “thermal irritation of the tail tip” (tail-flick), “tail electric stimulation” and “neuropathic pain”), acute toxicity and the ability to cause gastric damage. As a result, only the plate crystal form of N-(4-trifluoromethylphenyl)-4-hydroxy-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamide is recommended for further studies. Thus, it has been proven that the habitus of crystals is an important characteristic of the drug substance and is able to have a noticeable effect on its biological properties. Changes in habitus should be considered as a guide to the mandatory verification of at least the basic pharmacological parameters of the new form regardless of whether the molecular and crystal structure changes.

show abstract

Section: Evaluation Of the Biological Propertiesmentioning

confidence: 99%

Crystal Habits and Biological Properties of N-(4-Trifluoromethylphenyl)-4-Hydroxy-2,2-Dioxo-1H-2λ6,1-Benzothiazine-3-Carboxamide

et al. 2019

View full text Add to dashboard Cite

show abstract

“…В условиях стремительного развития науки и техники большой практический интерес представляют физико-химические методы анализа, позволяющие проводить измерение размеров молекул и малых частиц. Анализ размеров малых частиц имеет важное значение для многих отраслей современной промышленности -медицины и фармацевтики, пищевой промышленности и космической индустрии [1][2][3][4][5][6][7].…”

Section: Introductionunclassified

Determination of Optimal Modes for Measuring the Size of Colloidal Particles by Photon-Correlation Spectroscopy and Acoustic Spectroscopy

Ясная¹,

Blinov²,

Блинова³

et al. 2020

Physical and Chemical Aspects of the Study of Clusters, Nanostructures and Nanomaterials

View full text Add to dashboard Cite

В данной работе представлены результаты измерения размера коллоидных частиц SiO двумя методами - фотонно-корреляционной спектроскопией динамического рассеяния света и акустической спектроскопией. Математическая обработка экспериментальных данных с помощью программного обеспечения спектрометров «Photocor-Complex» и «DT-1202» позволила получить гистограммы распределения по размерам коллоидных частиц диоксида кремния в стандартном образце. Впервые установлено, что оптимальными параметрами для измерения размера коллоидных частиц SiO методом фотонно-корреляционной спектроскопии являются концентрация вещества менее 1 %, угол положения фотодетектора 90° и количество измерений в цикле 50 - 100, а акустической спектроскопии - концентрация 1 %. This paper presents the results of measuring the size of colloidal SiO particles by two methods - photon-correlation spectroscopy of dynamic light scattering and acoustic spectroscopy. Mathematical processing of experimental data using the software of the Photocor-Complex and DT-1202 spectrometers made it possible to obtain of the size distribution histograms for silicon dioxide colloidal particles in a standard sample. For the first time it has been established that the optimal parameters for measuring the size of colloidal SiO particles by the photon-correlation spectroscopy are the substance concentration less than 1 %, the photodetector position angle of 90 degrees and the number of measurements in a cycle of 100 -150, and for the acoustic spectroscopy - 1 % substance concentration.

show abstract

“…Microscopic analysis of the obtained granules showed that granules of composition 1 had poor characteristics at all alcohol concentrations, their shape was far from spherical, which could lead to deterioration of flowability of the obtained granules and have a negative impact on drug appearance [14] (Figures 1, 2).…”

mentioning

confidence: 99%

Development of a New Dosage Form of Naproxen

Lebedeva¹,

Valeeva²,

Zabolotnaya³

et al. 2017

Sovrem Tehnol Med

View full text Add to dashboard Cite

The aim of the study was to create a new dosage form of naproxen -granules for rapid dissolution in the oral cavity, also to develop their optimum composition and drug formulation.Materials and Methods. The active ingredient: naproxen substance; excipients: lactose monohydrate, mannitol 100 SD (fillers), polyvinylpyrrolidone Kollidon CL (a disintegrant), sodium hydrogen carbonate and citric acid (gas-forming agent).Moisture-activated dry granulation with subsequent addition of citric acid was used to produce granules. Alcohol in different concentrations (5, 10, 20, and 30%) served as granulating liquid.Results. There has been developed the composition and drug manufacturing technology of the new dosage form of naproxengranules for rapid dissolution in the oral cavity. It has been established experimentally that granules obtained with the use of 20% alcohol have the most favorable technological characteristics. Quality assessment was carried out in accordance with the State Pharmacopoeia XIII.Conclusion. There has been obtained a new easy-to-use dosage form of naproxen with a high safety profile.

show abstract

Drug particle shape and size control: A necessary factor for high-quality drug production

Cited by 6 publications

References 4 publications

Crystal Habits and Biological Properties of N-(4-Trifluoromethylphenyl)-4-Hydroxy-2,2-Dioxo-1H-2λ6,1-Benzothiazine-3-Carboxamide

Crystal Habits and Biological Properties of N-(4-Trifluoromethylphenyl)-4-Hydroxy-2,2-Dioxo-1H-2λ6,1-Benzothiazine-3-Carboxamide

Determination of Optimal Modes for Measuring the Size of Colloidal Particles by Photon-Correlation Spectroscopy and Acoustic Spectroscopy

Development of a New Dosage Form of Naproxen

Contact Info

Product

Resources

About