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DISINTEGRANTS AND THEIR INFLUENCE ON THE DISSOLUTION OF SUBSTANCES OF BIOPHARMACEUTICAL CLASSIFICATION SYSTEM CLASSES

Abstract

The characteristic of disintegrants used in technology of solid dosage forms is reviewed. The effect on release of substances of different classes from the tablets according to the biopharmaceutical classification system is presented. The characteristic of disintegrants used in technology of solid dosage forms is reviewed. The mechanisms of their action and methods of compounding into tablets, as well as factors that must be considered when choosing the optimal disintegrant, are given. The results of studies on the effectiveness of various disintegrants (crospovidone, croscarmellose sodium, sodium starch glycollate, etc.) on the release of active substances of different classes according to the biopharmaceutical classification system from tablets are discussed. A promising use of co-disintegrating agents in the technology of tablets of substances of class II BCS is highlighted. Examples of disintegrants of natural origin (mucus) used in tablets dispersed in the oral cavity are given.

About the Authors

I. E. Smekhova
Saint-Petersburg State Chemical and Pharmaceutical University
Russian Federation


V. A. Vainshtein
Saint-Petersburg State Chemical and Pharmaceutical University
Russian Federation


Y. M. Ladutko
Saint-Petersburg State Chemical and Pharmaceutical University
Russian Federation


O. V. Druzhininskaya
Saint-Petersburg State Chemical and Pharmaceutical University
Russian Federation


N. N. Tureckova
Saint-Petersburg State Chemical and Pharmaceutical University
Russian Federation


References

1. Sandeep N., Gupta M.M. Immediate Drug Release Dosage Form: A Review // Journal of Drug Delivery & Therapeutics. 2013. V. 3(2). P. 155-161.

2. Ramenskaya G. V., Savchenko A. Yu., Shokhin I. E., Kotlova M. A., Kulinich Yu. I., Vasilenko G. F., Kukes V. G. Biopharmaceutical classification of essential medicines // Pharmacy. 2011. № 5. P. 3-11].

3. Svistunov A. A., Ramenskaya G. V., Shokhin I. E. Dissolution test in pharmaceutical practice. Modern approaches, concepts and biopharmaceutical aspects // Remedium. 2011. № 11. P. 79-80.

4. Alekseev K. V., Tihonova N. V., Blynskaja E. V., Karbusheva E. Ju., Turchinskaja K. G., Miheeva A. S., Alekseev V. K., Uvarov N. A. Technology of increasing the biological and pharmaceutical accessibility of medicinal substances // J. New Medical Technologies. 2012. T. XIX. № 4. P. 43-47.

5. Demina N. B. Biopharmaceutical classification system as a tool for the development of drug formulations and their designs // Drug Development & Registration. 2017. № 2(19). P. 56-60.

6. Aleeva G. N., Zhuravleva M. V., Hafiz’janova R. H. The role of auxiliary components in ensuring pharmaceutical and therapeutic properties of drugs (a review) // Pharmaceutical Chemistry Journal. 2009. T. 43. № 4. P. 51-56.

7. Walsh J., Cram A., Woertz K., Breitkreutz J., Winzenburg G., Turner R., Tuleu C. Playing hide and seek with poorly tasting paediatric medicines: Do not forget the excipients// Advanced Drug Delivery Reviews. 2014. V. 73. P. 14-33.

8. Vadlamudi M. K., Dhanaraj S. Significance of excipients to enhance the bioavailability of poorly water-soluble drugs in oral solid dosage forms: A Review // IOP Conference Series: Materials Science and Engineering. 2017. V. 263. 022023. P. 1-16.

9. Voskobojnikova I. V., Avakjan S. B., Sokol’skaja T. A., Tjuljaev I. I., Bagirova V. L., Kolhir V. K., Sakovich G. S. Use of superdisintegrants in solid dosage forms // Pharmacy. 2005. № 2. P. 35-37.

10. Setkina S. B., Hishova O. M. Biopharmaceutical aspects of drug technology and ways of modification of bioavailability // Vestnik VGMU. 2014. T. 13. № 4. P. 162-172.

11. Kaur V., Mehara N. A Review on: Importance of Superdisintegrants on Immediate Release Tablets // International Journal of Research and ScientificInnovation. 2016. V. III(II). Р. 39-43.

12. Qureshi M. S., Zafar F., Ali H., Hameed K., Mallick N., Khan S., Baloch S. A. Superdisintegrant on disintegrant and dissolution; A review on influence // Professional Med J. 2016. V. 23(10). P. 1167-1170.

13. Desai P. M., Liew C. V., Heng P. W. S. Review of Disintegrants and the Disintegration Phenomena // Journal of Pharmaceutical Sciences. 2016. V. 105(9). Р. 2545-2555.

14. Deshmukh H., Chandrashekhar S., Nagesh C., Anmol M., Shridhar U. Superdisintegrants: A Recent Investigation and Current Approach // Asian Journal of Pharma and Technology. 2012. V. 2(1). P. 19-25.

15. Nasir A., Gohar U. F., Ahmad B. A Review Article On: Superdisintegrants // International Research Journal of Pharmaceutical Sciences. 2017. V. 8. P. 1-11.

16. Carter J. C. The role of disintegrants in solid oral dosage manufacturing. 2009. Carter Pharmaceutical Consulting Inc. Available at: http://www. carterpharmaceuticalconsulting.com/articles/The-role-of-disintergrants.html (accessed 11.06.2018).

17. Pahwa R., Gupta N. Superdisintegrants in the development of orally disintegrating tablets: a review // International Journal of Pharmaceutical Sciences and Research. 2011. V. 2(11). P. 2767-2780.

18. Andreev P. V. Using modified starch in Russian pharmaceutical industry // Pharmaceutical Chemistry Journal. 2004. T. 38. № 8. P. 37-41.

19. Voskobojnikova I. V., Avakjan S. B., Sokol’skaja T. A., Tjuljaev I. I., Bagirova V. L., Kolhir V. K., Sakovich G. S. Modern auxiliary substances in manufacture of tablets. Use of high-molecular substances for perfection medicinal forms and optimization of technological process // Pharmaceutical Chemistry Journal. 2005. T. 39. № 1. P. 22-28.

20. Kugach V. V., Kostantin Zh. Microcrystalline cellulose in manufacture of tablets. Vestnik farmacii. 2006. № 2. P. 72-79.

21. Chang D., Chang R.-K.Review of Current Issues in Pharmaceutical Excipients // Pharmaceutical Technology. 2007. Р. 1-7.

22. Mohanachandran P. S., Sindhumol P. G., Kiran T. S. Superdisintegrants: An overview // International Journal of Pharmaceutical Sciences Review and Research. 2011. V. 6(1). P. 105-109.

23. Homjak N., Homjak E. 3-D effect of Nise®: how pharmacokinetics help to cope with pain // Farmacevt Praktik. 2017. № 03. P. 32-34.

24. Kyron T-314 (Polacrilin Potassium). Available at: http://www.corelpharmachem.com/kyron_t314.htm (accessed 11.06.2018).

25. Tencova A. I., Terjoshkina O. I., Rudakova I. P., Samylina I. A., Gus’kova T. A. Current biopharmaceutical aspects of excipients // Pharmacy. 2012. № 7. S. 3-6.

26. Shihora H., Panda S. Superdisintegrants, Utility in Dosage form: A Quick Review // Journal of Pharmaceutical Science & Bioscientific Research. 2011. V. 1(3). P. 148-153.

27. Zhao N., Augsburger L. L. The influence of swelling capacity of super disintegrants in different pH media on the dissolution of hydrochlorothiazide from directly compressed tablets // AAPS Pharm Sci-Tech. 2005. V. 6(1). P. 120-126.

28. Balasubramaniam D., Bi T. Influence of superdisintegrants on the rate of drug dissolution from oral solid dosage forms // Pharmaceutical industry. 2010. № 4(21). S. 91-99.

29. Ghenge G., Pande S. D., Ahmad A., Jejurkar L., Birari T. Development and characterisation of fast disintegrating tablet of Amlodipine besylate using mucilage of plantago ovata as a natural superdisintegrant // International Journal of Pharm Tech Research. 2011. V. 3. P. 938-945.

30. Rajesh Y. V., Balasubramaniam J., Bindu K., Sridevi R., Swetha M., Rao V. U. Impact of superdisintegrants on efavirenz release from tablet formulations // Acta Pharm. 2010. V. 60. P. 185-195.

31. Balasubramaniam J., Bee T. Influence of Superdisintegrants on the Rate of Drug Dissolution from Oral Solid Dosage Forms // Pharmaceutical Technology. 2009. V. 2009 Supplement, Issue 1. Available at: http://www.pharmtech.com/influencesuperdisintegrants-rate-drug-dissolutionoral-solid-dosage-forms (accessed 11.06.2018).

32. Forxiga (dapagliflozin). Assessment report.European Medicines Agency. 2012. Available at: http://www.ema. europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/002322/WC500136024.pdf (accessed 11.06.2018).

33. Chitra K. P., Eswaraiah M. C., Basaveswararao M. V. Effect of various superdisintegrants on immediate release formulations of SGLT2 inhibitor dapagliflozin // International Journal of Research in Applied, Natural and Social Sciences. 2017. V. 5(1). P. 61-72.

34. Ajaykumar B., Babu R., Y., Sasikanth K., Laxmi Aswini G., Srinivas D. Study on Influence of Super Disintegrants and Lubricants on the Dissolution Rate of Atenolol Tablets // Res. J. Chem. Env. Sci. 2013. V. 1(4). P. 52-55.

35. Balasubramaniam J., Bindu1 K., Rao V. U., Ray D., Haldar R., Brzeczko A. W. Effect of Superdisintegrants on Dissolution of Cationic Drugs // Dissolution Technologies. 2008. V. 15(2). Р. 18-25.

36. Gohel M. C., Parikh R. K., Brahmbhatt B. K., Shah A. R. Improving the Tablet Characteristics and Dissolution Profile of Ibuprofen by Using a Novel Coprocessed Superdisintegrant: A Technical Note // AAPS Pharm SciTech. 2007. V. 8(1). Article 13. P. E1-E6.

37. Patil C., Das S. Effect of various superdisintegrants on the drug release profile and disintegration time of Lamotrigine orally disintegrating tablets // African Journal of Pharmacy and Pharmacology. 2011. V. 5(1). P. 76-82.

38. Pahwa R., Sharma S., Rana A.S., Garg A., Singh I. Emergence of Natural Superdisintegrants in the Development of Orally Disintegrating Tablets // Indo Am. J. Pharm. Sci. 2016. V. 3(8). P. 777-787.


Review

For citations:


Smekhova I.E., Vainshtein V.A., Ladutko Y.M., Druzhininskaya O.V., Tureckova N.N. DISINTEGRANTS AND THEIR INFLUENCE ON THE DISSOLUTION OF SUBSTANCES OF BIOPHARMACEUTICAL CLASSIFICATION SYSTEM CLASSES. Drug development & registration. 2018;(4):62-72. (In Russ.)

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