Pregled i kritička analiza matematičkih pristupa za karakterizaciju praškova i višečestičnih sistema u razvoju lekova

  • Ivana Vasiljević Univerzitet u Beogradu – Farmaceutski fakultet, Katedra za farmaceutsku tehnologiju i kozmetologiju
  • Erna Turković Univerzitet u Beogradu – Farmaceutski fakultet, Katedra za farmaceutsku tehnologiju i kozmetologiju
  • Ivana Aleksić Univerzitet u Beogradu – Farmaceutski fakultet, Katedra za farmaceutsku tehnologiju i kozmetologiju
  • Jelena Parojčić Univerzitet u Beogradu – Farmaceutski fakultet, Katedra za farmaceutsku tehnologiju i kozmetologiju
DOI: https://doi.org/10.5937/arhfarm72-40961
Ključne reči: proizvodnja lekova, čvrsti farmaceutski oblici, zatezna čvrstina, protočnost, klasifikacija materijala

Sažetak


Poznavanje uticaja svojstava materijala i procesnih parametara na karakteristike čvrstih farmaceutskih oblika predstavlja osnovu Quality-by-design pristupa razvoju lekova. Kako bi bio olakšan razvoj formulacije i izbor proizvodne tehnologije, više istraživačkih grupa opisalo je matematičke pristupe, koji se zasnivaju na čestičnim karakteristikama čestica, osobinama praška i ponašanju materijala pri kompresiji. U ovom radu prikazana su teorijska razmatranja i kritički pregled matematičkih pristupa razvijenih za karakterizaciju praškova i višečestičnih sistema. Ovi matematički pristupi su, generalno, razvijeni  za karakterizaciju materijala pogodnih za direktnu kompresiju. Međutim, u nekim slučajevima se razmatraju i druge tehnologije, kao što su suva i vlažna granulacija. Među opisanim karakteristikama materijala, zatezna čvrstina se izdvaja kao jedna od najznačajnijih za procenu mehaničkih svojstava kompakta. Potrebno je ispitati i protočnost materijala. Takođe, veličina i oblik čestica, gustina materijala i profili koji opisuju kompresibilnost, kompaktibilnost i tabletabilnost materijala prepoznati su kao karakteristike koje značajno utiču na razvoj čvrstih farmaceutskih oblika. Primena matematičkih pristupa u karakterizaciji praškova i višečestičnih sistema može doprineti mehanističkom razumevanju svojstava materijala i olakšati razvoj i optimizaciju čvrstih farmaceutskih oblika lekova. Međutim, ključno je odabrati odgovarajući pristup, zavisno od željenih karakteristika finalnog preparata, kako bi sva kritična svojstva materijala bila ispitana i kritički razmotrena.

Reference

1.     Lionberger RA. FDA critical path initiatives: Opportunities for generic drug development. AAPS Journal. 2008;10:103–9.

2.          Leane M, Pitt K, Reynolds G, Anwar J, Charlton S, Crean A, et al. A proposal for a drug product Manufacturing Classification System (MCS) for oral solid dosage forms. Pharm Dev Technol. 2015;20:12–21.

3.          Pérez P, Suñé-Negre JM, Miñarro M, Roig M, Fuster R, García-Montoya E, et al. A new expert systems (SeDeM Diagram) for control batch powder formulation and preformulation drug products. Eur J Pharm Biopharm. 2006;64(3):351–9.

4.          Sun CC. A classification system for tableting behaviors of binary powder mixtures. Asian J Pharm Sci. 2016;11(4):486–91.

5.          Osamura T, Takeuchi Y, Onodera R, Kitamura M, Takahashi Y, Tahara K, et al. Characterization of tableting properties measured with a multi-functional compaction instrument for several pharmaceutical excipients and actual tablet formulations. Int J Pharm. 2016;510(1):195–202.

6.          Dai S, Xu B, Zhang Z, Yu J, Wang F, Shi X, Qiao Y. et al. A compression behavior classification system of pharmaceutical powders for accelerating direct compression tablet formulation design. Int J Pharm. 2019;572:118742.

7.          Leane, M, Pitt K, Reynolds G. and Manufacturing Classification System (MCS) Working Group. A proposal for a drug product Manufacturing Classification System (MCS) for oral solid dosage forms. Pharm Dev Technol. 2015; 20(1):12-21.

8.          Hancock B. Identifying Candidates for Direct Compression Using Material-Sparing Formulation Tools. Paper presented at: AAPS Annual Meeting; 2004 Nov 7-11; Baltimore, USA.

9.          McCormick D. Evolutions in Direct Compression. Pharmaceutical Technology. 2005;29(4):52–62.

10.       Rohrs BR, Amidon GE, Meury RH, Secreast PJ, King HM, Skoug CJ. et al. Particle size limits to meet USP content uniformity criteria for tablets and capsules. J Pharm Sci. 2006;95:1049–1059.

11.       Yalkowsky SH, Bolton S. Particle size and content uniformity. Pharm Res. 1990;7:962–966.

 

12.       Leane M, Pitt K, Reynolds GK, Dawson N, Ziegler I, Szepes A, et al. Manufacturing classification system in the real world: factors influencing manufacturing process choices for filed commercial oral solid dosage formulations, case studies from industry and considerations for continuous processing. Pharm Dev Technol. 2018;23:964–77.

13.       Leane M, Pitt K. Adoption of the MCS concept in the pharmaceutical industry. Paper presented at: 12th World Meeting on Pharmaceutics, Biopharmaceutics and Pharmaceutical Technology; 2021 May 11-14; virtual meeting.

14.       Dai S, Xu B, Shi G, Liu J, Zhang Z, Shi X, et al. SeDeM expert system for directly compressed tablet formulation: A review and new perspectives. Powder Technol. 2019;342:517–27.

15.       Suñé-Negre JM, Pérez-Lozano P, Miñarro M, Roig M, Fuster R, Hernández C, et al. Application of the SeDeM Diagram and a new mathematical equation in the design of direct compression tablet formulation. Eur J Pharm Biopharm. 2008;69(3):1029–39.

16.       Aguilar-Díaz JE, García-Montoya E, Pérez-Lozano P, Suñe-Negre JM, Miñarro M, Ticó JR. The use of the SeDeM Diagram expert system to determine the suitability of diluents-disintegrants for direct compression and their use in formulation of ODT. Eur J Pharm Biopharm. 2009;73(3):414–23.

17.       Suñé-Negre JM, Roig M, Fuster R, Hernández C, Ruhí R, García-Montoya E, et al. New classification of directly compressible (DC) excipients in function of the SeDeM Diagarm Expert System. Int J Pharm. 2014;470(1–2):15–27.

18.       Scholtz JC, Steenekamp JH, Hamman JH, Tiedt LR. The SeDeM Expert Diagram System: Its performance and predictability in direct compressible formulations containing novel excipients and different types of active ingredients. Powder Technol. 2017;312:222–36.

19.       Aguilar-Díaz JE, García-Montoya E, Suñe-Negre JM, Pérez-Lozano P, Miñarro M, Ticó JR. Predicting orally disintegrating tablets formulations of ibuprophen tablets: An application of the new SeDeM-ODT expert system. Eur J Pharm Biopharm. 2012;80(3):638–48.

20.       FDA. Guidance for Industry Orally Disintegrating Tablets. 2008.

21.       Sipos E, Oltean AR, Szabó ZI, Rédai EM, Nagy GD. Application of SeDeM expert systems in preformulation studies of pediatric ibuprofen ODT tablets. Acta Pharm. 2017;67(2):237–46.

22.       Khan A, Majeedullah, Qayum M, Ahmad L, Ahmad Khan S, Abbas M. Optimization of diluents on the basis of SeDeM-ODT expert system for formulation development of ODTs of glimepiride. Adv Powder Technol. 2022;33(2):103389.

23.       Rao MRP, Sapate S, Sonawane A. Pharmacotechnical Evaluation by SeDeM Expert System to Develop Orodispersible Tablets. AAPS PharmSciTech. 2022;23(5):1-14.

24.       Zieschang L, Klein M, Jung N, Krämer J, Windbergs M. Formulation development of medicated chewing gum tablets by direct compression using the SeDeM-Diagram-Expert-System. Eur J Pharm Biopharm. 2019;144:68–78.

25.       Shah DS, Jha DK, Gurram S, Suñé-Pou M, Garcia-Montoya E, Amin PD. A new SeDeM-SLA expert system for screening of solid carriers for the preparation of solidified liquids: A case of citronella oil. Powder Technol. 2021;382:605–18.

26.       Mamidi HK, Mishra SM, Rohera BD. Application of modified SeDeM expert diagram system for selection of direct compression excipient for liquisolid formulation of Neusilin® US2. J Drug Deliv Sci Tech. 2021;64:102506.

27.       Leuenberger H. The compressibility and compactibility of powder systems. Int J Pharm. 1982;12:41–55.

28.       Galdón E, Casas M, Gayango M, Caraballo I. First study of the evolution of the SeDeM expert system parameters based on percolation theory: Monitoring of their critical behavior. Eur J Pharm Biopharm. 2016;109:158–64.

29.       Gülbağ S, Yılmaz Usta D, Gültekin HE, Oktay AN, Demirtaş Ö, Karaküçük A, et al. New perspective to develop memantine orally disintegrating tablet formulations: SeDeM expert system. Pharm Dev Technol. 2018;23(5):512–9.

30.       Pitt K, Heasley M. Determination of the tensile strength of elongated tablets. Powder Technol. 2013;238:169–75.

31.       Pitt KG, Webber RJ, Hill KA, Dey D, Gamlen MJ. Compression prediction accuracy from small scale compaction studies to production presses. Powder Technol. 2015;270(PB):490–3.

32.       Nordström J, Klevan I, Alderborn G. A particle rearrangement index based on the kawakita powder compression equation. J Pharm Sci. 2009;98(3):1053–63.

33.       Nordström J, Klevan I, Alderborn G. A protocol for the classification of powder compression characteristics. Eur J Pharm Biopharm. 2012;80(1):209–16.

34.       Klevan I, Nordström J, Tho I, Alderborn G. A statistical approach to evaluate the potential use of compression parameters for classification of pharmaceutical powder materials. Eur J Pharm Biopharm. 2010;75(3):425–35.

35.       Kawakita Kimio, Lüdde Karl-Helmut. Some Considerations on Powder Compresion Equations. Powder Technol. 1971;4(2):61–8.

36.       Heckel RW. Density-pressure relationship in powder compaction. Trans Met Soc, AIME. 1961;221:671–5.

37.       Ryshkewitch E. Compression strength of porous sintered alumina and zirconia. J Am Ceram Soc. 1953;36:65–8.

38.       Duckworth W. Discussion of Ryshkewitch paper. J Am Ceram Soc. 1953;36:68.

39.       Worku Z, Kumar D, Gomes J, He Y, Glennon B, Ramisetty K, 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(1):191–204.

40.       Abdul S, Chandewar AV, Jaiswal SB. A flexible technology for modified-release drugs: Multiple-unit pellet system (MUPS). J Control Release. 2010;147:2–16.

41.       Xu M, Heng PWS, Liew CV. Formulation and process strategies to minimize coat damage for compaction of coated pellets in a rotary tablet press: A mechanistic view. Int J Pharm. 2016;499(1–2):29–37.

42.       Luo G, Xu B, Zhang Y, Cui X, Li J, Shi X, et al. Scale-up of a high shear wet granulation process using a nucleation regime map approach. Particuology. 2017;31:87–94.

43.       Cui XL, Xu B, Zhang Y, Zhang N, Shi XY, Qiao YJ. Application of quality by design in granulation process for ginkgo leaf tablet (Ⅰ)： comprehensive characterization of granule properties. Zhongguo Zhong yao za zhi = Zhongguo Zhongyao Zazhi = China Journal of Chinese Materia Medica. 2017;42(6):1037–42.

44.       Khan A. Optimization of the process variables of roller compaction, on the basis of granules characteristics (flow, mechanical strength, and disintegration behavior): an application of SeDeM-ODT expert system. Drug Dev Ind Pharm. 2019;45(9):1537–46.

45.       Hamman H, Hamman J, Wessels A, Scholtz J, Steenekamp JH. Development of multiple-unit pellet system tablets by employing the SeDeM expert diagram system I: pellets with different sizes. Pharm Dev Technol. 2018;23(7):706–14.

46.       Hamman H, Hamman J, Wessels A, Scholtz J, Steenekamp J. Development of multiple-unit pellet system tablets by employing the SeDeM expert diagram system II: pellets containing different active pharmaceutical ingredients. Pharm Dev Technol. 2019;24(2):145–56.

47.       Vasiljević I, Turković E, Piller M, Zimmer A, Parojčić J. An investigation into applicability of different compression behaviour assessment approaches for multiparticulate units characterization. Powder Technol. 2021;379:526–36.

48.       Vasiljević I, Turković E, Nenadović S, Mirković M, Zimmer A, Parojčić J, et al. Investigation into liquisolid system processability based on the SeDeM Expert System approach. Int J Pharm. 2021;605: 120847.

49.       Vasiljević I, Turković E, Aleksić I, Parojčić J. An investigation into formulation factor impact on the characteristics of granules prepared by selective laser sintering. Paper presented at: 13th World Meeting on Pharmaceutics, Biopharmaceutics and Pharmaceutical Technology; 2022 Mar 28-31; Rotterdam, the Netherlands.

50.       Vasiljević I, Turković E, Piller M, Mirković M, Zimmer A, Aleksić I, et al. Processability evaluation of multiparticulate units prepared by selective laser sintering using the SeDeM Expert System approach. Int J Pharm. 2022; 629:122337.

51.       DFE pharma [Internet]. Formulation tool; 2022 [cited 2022 Dec 22]. Available from: https://dfepharma.com/formulation-tool/#/en/guided.

52.       BASF [Internet]. ZoomLabTM – Virtual Formulation Assistant; 2022 [cited 2022 Dec 22]. https://myapps.basf.com/ZoomLab/Dashboard.

Objavljeno
2022/12/29
Broj časopisa
Vol. 72 Br. Notebook 6 (2022): Arhiv za farmaciju
Rubrika
Pregledni (Revijalni) rad
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