Pharmaceutical and technological characteristics of the fractional composition and grinding of the 3,6,9-triazatricyclotetradecane derivative

Abstract


Introduction. Bulk powders provide reliable process operations for producing pharmaceuticals based on them, such as filling and unloading from bins, as well as filling capsules and tablet press dies. In pharmaceutical production, powdered materials are subject to a variety of significant technological processes, which can result in significant changes in the physical properties of the particles, affecting their flowability. To maintain consistent product quality and effectively manage bulk material processes, it is necessary to consider the mechanisms underlying flowability and the critical process parameters at each stage of production. Understanding the key characteristic — the flowability of powdered materials — at virtually all stages of production determines the effectiveness of fluidization, mixing, milling, granulation, and tableting processes. The aim of this study is to investigate the pharmaceutical and technological characteristics of the fractional composition and grindability of a 3,6,9-triazatricyclotetradecane derivative. Materials and Methods. Standardized pharmacopoeial methods were used as experimental research tools, allowing for the description of various aspects of powder flow properties. The obtained research results were statistically substantiated, ensuring the validity of the obtained results. Results. A 3,6,9-triazatricyclotetradecane derivative was shown to exhibit poor flowability, representing a powder fraction with a particle size range greater than 94 μm but less than 355 μm. According to the established data, the powder fraction consists primarily of particles in the size range from 180 μm to 94 μm, which characterizes it as a finely dispersed powder. Classic powder classification terms in accordance with OFS.1.4.2.0032 were deemed inapplicable, and fineness was defined as a percentage of the powder mass passing through a sieve of a given size. Based on the results of a natural angle of repose study, flowability was characterized as "very poor". The compressibility and Hausner coefficients ranged from 28 to 31 and 1.43 to 1.46, respectively, characterizing the 3,6,9-triazatricyclotetradecane derivative as a poorly flowing substance. Conclusion. The experimental data obtained provide the foundation for further pharmaceutical development of the composition and technology for producing drugs based on the 3,6,9-triazatricyclotetradecane derivative.

About the authors

Alexandra M. Kulikova

I. M. Sechenov First Moscow State Medical (Sechenov University), Moscow, Russia

Email: aleksandrakulikova2023@mail.ru

Galina E. Brkich

I. M. Sechenov First Moscow State Medical (Sechenov University), Moscow, Russia

Email: brkich_g_e@staff.sechenov.ru

Andrey O. Kuznetsov

I. M. Sechenov First Moscow State Medical (Sechenov University), Moscow, Russia

Email: kuznetsov_a_o@staff.sechenov.ru

References

  1. Emery E., Oliver J., Pugsley T., Sharma J., Zhou J. Flowability of moist pharmaceutical powders. Powder Technol. 2009;189:409—415. doi: 10.1016/j.powtec.2008.06.017
  2. Enferad S., Petit J., Gaiani C., Falk V., Burgain J., Kiesgen De Richter S., Jenny M. Effect of particle size and formulation on powder rheology. Part. Sci. Technol. 2021;39:362—370. doi: 10.1080/02726351.2020.1738605
  3. Worku Z. A., Kumar D., Gomes J. V. et al. Modelling and understanding powder flow properties and compactability of selected active pharmaceutical ingredients, excipients and physical mixtures from critical material properties. Int. J. Pharm. 2017;531:191—204. doi: 10.1016/j.ijpharm.2017.08.063
  4. Juliano P., Barbosa-Cánovas G. V. Food powders flowability characterization: theory, methods, and applications. Annu. Rev. Food Sci. Technol. 2010;1:211—239. doi: 10.1146/annurev.food.102308.124155
  5. Kunnath K., Huang Z., Chen L., Zheng K., Davé R. Improved properties of fine active pharmaceutical ingredient powder blends and tablets at high drug loading via dry particle coating. Int. J. Pharm. 2018;543:288—299. doi: 10.1016/j.ijpharm.2018.04.002
  6. Tomasetta I., Barletta D., Poletto M. Correlation of powder flow properties to interparticle interactions at ambient and high temperatures. Particuology. 2014;12:90—99. doi: 10.1016/j.partic.2013.02.002
  7. Tomas J., Kleinschmidt S. Improvement of flowability of fine cohesive powders by flow additives. Chem. Eng. Technol. 2009;32:1470—1483. doi: 10.1002/ceat.200900173
  8. Shah D. S., Moravkar K. K., Jha D. K. et al. A concise summary of powder processing methodologies for flow enhancement. Heliyon. 2023;9(6):e16498. doi: 10.1016/j.heliyon.2023.e16498
  9. Yu W., Muteki K., Zhang L., Kim G. Prediction of bulk powder flow performance using comprehensive particle size and particle shape distributions. J. Pharm. Sci. 2011;100:284—293. doi: 10.1002/jps.22254
  10. Lavrov M. I., Karlov D. S., Palyulin V. A. et al. Novel positive allosteric modulator of AMPA-receptors based on tricyclic scaffold. Mendeleev Commun. 2018;28(3):311—313. doi: 10.1016/j.mencom.2018.05.028

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