JOURNAL OF THE CZECH PHARMACEUTICAL SOCIETY AND THE SLOVAK PHARMACEUTICAL SOCIETY

Čes. slov. farm. 2020, 69(3):112-120 | DOI: 10.36290/csf.2020.018

Medicinal products with controlled drug release for local therapy of inflammatory bowel diseases from perspective of pharmaceutical technology

Kateřina Kubová
Ústav farmaceutické technologie, Farmaceutická fakulta, Masarykova univerzita, Brno

The aim of this article is to introduce the basic design of used medicinal products with controlled drug release for the treatment of inflammatory bowel diseases and to clarify their behaviour in gastrointestinal tract from the perspective of pharmaceutical technology. Specifically, it focuses on pharmaceutical drugs containing 5-aminosalicylic acid (Asacol®, Pentasa®, Salofalk®) and budesonide (Budenofalk®, Cortiment®, Entocort®). As a part of this paper, basic recommendations and practical information that can be used in clinical practice are also given.

Keywords: tablets; pellets; inflammatory bowel diseases; colon targeting; delayed drug release; pH-dependent polymers; capsules; granules; matrix; coating

Received: May 27, 2020; Accepted: June 16, 2020; Published: March 1, 2020  Show citation

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Kubová K. Medicinal products with controlled drug release for local therapy of inflammatory bowel diseases from perspective of pharmaceutical technology. Čes. slov. farm. 2020;69(3):112-120. doi: 10.36290/csf.2020.018.
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    References

    1. Ludwig A., van Ooteghem M., Delva A. Disintegration of hard gelatin capsules, part 1: Composition and structure of the capsule wall. Pharm. Ind. 1979; 41, 796-798.
    2. Dvořáčková K. Principy uvolňování léčiv z perorálních matricových tablet obsahujících hypromelosu. Chem. Listy 2009; 103(1), 66-72.
    3. Colombo P., Bettini B., Santi P., Peppas N. A. Swellable matrices for controlled drug delivery: gel-layer behaviour, mechanisms and optimal performance. Pharm. Sci. Tech. Today 2000; 3(6), 198-204. Go to original source... Go to PubMed...
    4. Bruschi M. L. Strategies to modify the drug release from pharmaceutical systems. 1. vydání. Cambridge: Woodhead Publishing 2015.
    5. Philip A. K., Philip B. Colon targeted drug delivery systems: a review on primary and novel approaches. Oman Med. J. 2010; 25(2), 79-87. Go to original source... Go to PubMed...
    6. Shimono N., Takatori T., Ueda M., Mori M., Higashi Y., Nakamura Y. Chitosan dispersed system for colon-specific drug delivery. Int. J. Pharm. 2002; 245(1-2), 45-54. Go to original source... Go to PubMed...
    7. Singh B. N. Modified-release solid formulations for colonic delivery. Recent. Pat. Drug Deliv. Formul. 2007; 1, 53-63. Go to original source... Go to PubMed...
    8. Segregur D., Flanagan T., Mann J., Moir A., Karlsson E. M., Hoch M., Carlile D., Sayah-Jeanne S., Dressman J. Impact of acid-reducing agents on gastrointestinal physiology and design of biorelevant dissolution tests to reflect these changes. J. Pharm. Sci. 2019; 108(11), 3461-3477. Go to original source... Go to PubMed...
    9. Nugent S. G. Intestinal luminal pH in inflammatory bowel disease: possible determinants and implications for therapy with aminosalicylates and other drugs. Gut 2020; 48(4), 571-577. Go to original source... Go to PubMed...
    10. Naiserová M., Kubová K., Vysloužil J., Bernatoniene J., Brokalakis I., Vetchý D. (Meth)acrylates copolymers of Eudragit® type in oral tablet technology. Čes. slov. Farm. 2019; 68, 183-197. Go to original source...
    11. Maurer J. M., Schellekens R. C., van Rieke H. M., Wanke C., Iordanov V., Stellaard F., Wutzke K. D., Dijkstra G., van der Zee M., Woerdenbag H., Frijlink H. W., Kosterink J. G. Gastrointestinal pH and transit time profiling in healthy volunteers using the intellicap system confirms ileo-colonic release of colopulse tablets. PloS One 2015; 10(7); e0129076. https://dx.plos.org/10.1371/journal.pone.0129076 (12. 8. 2019) Go to original source... Go to PubMed...
    12. Sinha V. R., Kumria R. Microbially triggered drug delivery to the colon. Eur. J. Pharm. Sci. 2003; 18(1), 3-18. Go to original source... Go to PubMed...
    13. Park K., Shalaby W. S., Park H. (eds.) Biodegradation. In: Biodegradable hydrogels for drug delivery, USA: Technomic publishing company 1993; 13-34. Go to original source...
    14. Rajpurohit H., Sharma P., Sharma S., Bhandari A. Polymers for colon targeted drug delivery. Indian J. Pharm Sci. 2010; 72(6), 689-696. Go to original source... Go to PubMed...
    15. Freire C., Podczeck F., Veiga F., Sousa J. Starch-based coatings for colon-specific delivery. Part II: Physicochemical properties and in vitro drug release from high amylose maize starch films. Eur. J. Pharm. Biopharm. 2009; 72(3), 587-594. Go to original source... Go to PubMed...
    16. Mohanty, S., Panigrahi A. K. Multiparticulate drug delivery system for colon targeting. Int. J. Pharm. Pharm. Sci. 2015; 7(3), 433-436.
    17. Thakral S. N., Thakral N. K., Majumdar D. K. Eudragit®: a technology evaluation. Expert Opin. Drug Del. 2012; 10(1), 131-149. Go to original source... Go to PubMed...
    18. Madu S. J., Azubuike C. P., Okubanjo O., Mohammed A., Emeje O. M. Physicochemical and disintegrant properties of sodium carboxymethyl starch derived from Borassus aethiopum (Arecaceae) shoot. J. Polym. Res. 2018; 5(8), 167. Go to original source...
    19. Ibekwe, V. C., Liu F., Fadda H. M., Khela M. K., Evans D. F., Parsons G. E., Basit A. W. An investigation into the in vivo performance variability of pH responsive polymers for ileo-colonic drug delivery using gamma scintigraphy in humans. J. Pharm. Sci. 2006; 95(12), 2760-2766. Go to original source... Go to PubMed...
    20. SPC Asacol 400, 800 enterosolventní tablety. http://www.sukl.cz/modules/medication/detail.php?code=0203805&tab=texts (12. 8. 2019).
    21. Kaur G., Jain S., Tiwary A. Recent approaches for colon drug delivery. Recent. Pat. Drug Deliv. Formul. 2007; 1(3), 222-229. Go to original source... Go to PubMed...
    22. Oral drug delivery technologies. Phloral®. https://healthcare.evonik.com/product/health-care/downloads/evonik-phloral-dual-action-coating-fail-safe-colonic-delivery-factsheet.pdf (12. 10. 2019).
    23. Mcconnell E. L., Fadda H. M., Basit A. W. Gut instincts: Explorations in intestinal physiology and drug delivery. Int. J. Pharma. 2008; 364(2), 213-226. Go to original source... Go to PubMed...
    24. Liu F., Moreno P., Basit A. W. A novel double-coating approach for improved pH-triggered delivery to the ileo-colonic region of the gastrointestinal tract. Eur. J. Pharm. Biopharm. 2010; 74(2), 311-315. Go to original source... Go to PubMed...
    25. Varum F., Freire A. C., Bravo R., Buser T., Goutte F., Basit A. W. Opticore: Accelerating drug release in ileo-colonic region of the gastrointestinal tract. Denver: AAPS conference 13.-17. 11. 2016. Poster presentation.
    26. SPC Asacol 1600 mg tablety s řízeným uvolňováním. http://www.sukl.cz/modules/medication/detail.php?code=0242525&tab=texts (1. 10. 2019).
    27. Karoui S. (ed.) Inflammatory bowel disease - Advances in pathogenesis and management. 1. ed. Rijeka: IntechOpen 2012. Go to original source...
    28. Richard J., Benoît J. P. Techniques de l'Ingénieur 2000; 2210, 1-20.
    29. Tenjarla S. Dissolution of commercially available mesalamine formulations at various pH levels. Drugs R D. 2015; 15(2), 211-215. Go to original source... Go to PubMed...
    30. Chuong M. C., Christensen J. M., Ayres J. W. New dissolution method for mesalamine tablets and capsules. Dissolution Technologies 2008; 15(3), 7-14. http://www.dissolutiontech.com/DTresour/200808Articles/DT200808_A01.pdf (11. 4. 2020). Go to original source...
    31. SPC Pentasa 500 mg Prolong tablety s prodlouženým uvolňováním. http://www.sukl.cz/modules/medication/detail.php?code=0247411&tab=texts (12. 3. 2020).
    32. Gisbert J. P., Gomollon F., Mate J., Pajares J. M. Role of 5-aminosalicylic acid (5-ASA) in treatment of inflammatory bowel disease: a systematic review. Dig. Dis. Sci. 2002; 47, 471-488. Go to original source... Go to PubMed...
    33. Wilhelm R., Pröls M., Greinwald R., Nacak T. Optimised high-dose mesalazine-containing tablet. WO2017072050A1. https://patents.google.com/patent/WO2017072050A1/en (30. 10. 2019).
    34. SPC Salofalk 500 enterosolventní tablety. http://www.sukl.cz/modules/medication/detail.php?kod=0075567 (9. 9. 2019).
    35. Kruis W., Greinwald R., Fingerhut T. In-vitro dissolution testing of 5-aminosalicylic acid release from pH dependent mesalazine formulations. J. Crohns Colitis 2011; 5(5), 499-500. Go to original source... Go to PubMed...
    36. Karkossa F., Klein F. A biopredictive in vitro comparison of oral locally acting mesalazine formulations by a novel dissolution model for assessing intraluminal drug release in individual subjects. J. Pharm. Sci. 2018; 107(6), 1680-1689. Go to original source... Go to PubMed...
    37. SPC Salofalk 500 mg, 1000 mg, 1500 mg, 3000 mg enterosolventní granule s prodlouženým uvolňováním. http://www.sukl.cz/modules/medication/detail.php?code=0195909&tab=texts (23. 10. 2019).
    38. Leifeld L., Pfützer R., Morgenstern J., Gibson P. R., Marakhouski Y., Greinwald R., Mueller R., Kruis W. Mesalazine granules are superior to Eudragit-L-coated mesalazine tablets for induction of remission in distal ulcerative colitis - a pooled analysis. Aliment. Pharmacol. Ther. 2011; 34, 1115-1122. Go to original source... Go to PubMed...
    39. Gruber P., Lach H. J., Otterbeck N. Budesonide pellets with a controlled release pattern and process for producing them. WO1995008323A1. https://patents.google.com/patent/WO1995008323A1/en (15. 11. 2019).
    40. Villa R., Pedrani M., Ajani M., Fossati L. Controlled release and taste masking oral pharmaceutical composition. US 8293273 B2. https://patents.google.com/patent/US9592203B2/en (3. 12. 2019).
    41. Iborra M., Alvarez-Sotomayor D., Nos P. Long-term safety and efficacy of budesonide in the treatment of ulcerative colitis. Clin. Exp. Gastroenterol. 2014; 7, 39-46. Go to original source... Go to PubMed...
    42. Klein S., Stein J., Dressman J. Site-specific delivery of anti-inflammatory drugs in the gastrointestinal tract: an in-vitro release model. J. Pharm. Pharmacol. 2005; 57(6), 709-719. Go to original source... Go to PubMed...
    43. Goyanes A., Hatton G. B., Basit A. W. A dynamic in vitro model to evaluate the intestinal release behaviour of modified-release corticosteroid products. J. Drug Deliv. Sci. Tec. 2015; 25, 36-42. Go to original source...
    44. SPC Budenofalk 3 mg enterosolventní tvrdé tobolky. http://www.sukl.cz/modules/medication/detail.php?kod=0064787 (18. 11. 2019).
    45. SPC Budenofalk UNO 9 mg enterosolventní granule. http://www.sukl.cz/modules/medication/detail.php?code=0158943&tab=texts (12. 8. 2019).
    46. Nardelli S., Pisani L. F., Tontini G. E., Vecchi M. L. MMX® technology and its applications in gastrointestinal diseases. Therap. Adv. Gastroenterol. 2017; 10(7), 545-552. Go to original source... Go to PubMed...
    47. Hillery A. M., Brayden D. J. Oral drug delivery. In: Hillery A. M., Park K. (eds.) Drug Delivery: Fundamentals & Applications, 2nd ed. London: Taylor & Francis Group, LLC 2017; 171-200. Go to original source...
    48. Thakral S., Thakral N. K., Majumdar D. K. Eudragit®: a technology evaluation. Expert Opin. Drug Deliv. 2012; 10(1), 131-149. Go to original source... Go to PubMed...
    49. Goyanes A., Chang H., Sedough D., Hatton G. B., Wang J., Buanz A., Gaisford S. Basit A. W. Fabrication of controlled-release budesonide tablets via desktop (FDM) 3D printing. Int. J. Pharm. 2015; 496(2), 414-420. Go to original source... Go to PubMed...
    50. Cortiment 9 mg tableta s prodlouženým uvolňováním. http://www.sukl.cz/modules/medication/detail.php?code=0206462&tab=texts (25. 10. 2019).
    51. Brunner M., Ziegler S., di Stefano A. F. D., Dehghanyar P., Kletter K., Tschurlovits M., Villa R., Bozzella R., Celasco G., Moro L., Rusca A., Dudczak R., Müller M. Gastrointestinal transit, release and plasma pharmacokinetics of a new oral budesonide formulation. Br. J. Clin. Pharmacol. 2006; 61(1), 31-38. Go to original source... Go to PubMed...
    52. Stegemann S. Hard gelatin capsules today - and tomorrow. https://pdfs.semanticscholar.org/12d4/148f4e7a261c0d3020c0140f7192ea361706.pdf (20. 11. 2019).
    53. Eudragit®. https://healthcare.evonik.com/sites/lists/NC/DocumentsHC/Evonik-Eudragit_brochure.pdf (11. 10. 2019).
    54. SPC Entocort 3 mg tvrdé tobolky s řízeným uvolňováním http://www.sukl.cz/modules/medication/detail.php?code=0208797&tab=texts (30. 9. 2019).
    55. Mackenzie-Smith L., Marchi P., Thorne H., Timeus S., Young R., le Calvé P. Patient preference and physician perceptions of patient preference for oral pharmaceutical formulations: results from a real-life survey. Inflamm. Bowel Dis. 2018; 3(1), 43-51. Go to original source... Go to PubMed...
    56. Keil R., Wasserbauer M., Zádorová Z., Kojecký V., Hlava Š., Šťovíček J., Chudý J., Roznětinská M., Drábek J., Kubišová N., Lochmannová J. Adherence, risk factors of non-adherence and patient's preferred treatment strategy of mesalazine in ulcerative colitis: multicentric observational study. Scand. J. Gastroenterol. 2018; 53(4), 459-465. Go to original source... Go to PubMed...
    57. Kane S., Huo D., Aikens J., Hanauer S. Medication nonadherence and the outcomes of patients with quiescent ulcerative colitis. Am. J. Med. 2003; 114(1), 39-43. Go to original source... Go to PubMed...

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