JOURNAL OF THE CZECH PHARMACEUTICAL SOCIETY AND THE SLOVAK PHARMACEUTICAL SOCIETY

Čes. slov. farm. 2014, 63(5):206-212 | DOI: 10.36290/csf.2014.039

Formulation of cores for the controlled release of glucose for prevention of hypoglycemia in diabetes patients

Aleš Franc1,*, Kateřina Dvořáčková1, Jan Muselík1, Martina Žvaková1,3, Vladimíra Slováková1, David Vetchý1, Dana Sabadková1, David Neumann2, Roman Goněc1,3
1 Veterinary and Pharmaceutical University in Brno, Faculty of Pharmacy, Department of Pharmaceutics, Brno, Czech Republic
2 University Hospital, Pediatric Clinic, Hradec Králové, Czech Republic
3 Masaryk Memorial Cancer Institute, Brno, Czech Republic

Hypoglycemic episodes are a frequent and serious complication in both types of diabetes mellitus. The risk of hypoglycemic conditions can be managed by a coated pellet dosage form, which can release glucose in a delayed regime to achieve the maximum estimated effect of antidiabetics. The pellet cores, intended for coating with ethylcellulose, were prepared consisting of four osmotically active excipients: crosscarmellose (Ac-Di-Sol®), a mixture of microcrystalline cellulose and carmellose sodium (Avicel® RC 591), carboxymethyl starch sodium (Vivastar® P 5000) and macrogol 6000, respectively. The aim of this study was to increase the glucose content in the pellets to minimize their volume and to improve the administration to the patients. The content of glucose in the pellet cores was increased from 45 to 75 or 80%, respectively, for all compositions. All pellet samples had satisfactory mechanical and flow properties required for the coating process. The highest values of sphericity were achieved in the lower mean particle size sample containing 80% of glucose, 15% of Avicel® PH 101 and 5% of carboxymethyl starch sodium and the higher mean particle size sample containing 75% of glucose and 25% of Avicel® RC 591.

Keywords: hypoglycemia; delayed release; glucose
Grants and funding:

This paper was supported by the project IGA MZ No 14479/2013 Preparation of dosage forms with controlled release of glucose to prevention of hypoglycemic states and the project IGA VFU No 61/2014/FaF Development of pH-dependent dissolution method for control of pellets with controlled release of glucose for the prevention of hypoglycemia.

Received: September 8, 2014; Accepted: September 16, 2014; Published: May 1, 2014  Show citation

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Franc A, Dvořáčková K, Muselík J, Žvaková M, Slováková V, Vetchý D, et al.. Formulation of cores for the controlled release of glucose for prevention of hypoglycemia in diabetes patients. Čes. slov. farm. 2014;63(5):206-212. doi: 10.36290/csf.2014.039.
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References

  1. American Diabetes Association Workgroup on Hypoglycaemia, 2005.
  2. Hopkins D. Exercise-induced and other daytime hypoglycemic events in patients with diabetes: prevention and treatment. Diabetes. Res. Clin. Pr. 2004; 65, 35-39. Go to original source... Go to PubMed...
  3. Frier B. M. Morbidity of hypoglycaemia in type 1 diabetes. Diabetes. Res. Clin. Pr. 2004; 65, 47-52. Go to original source... Go to PubMed...
  4. Fisher M., Heller S. R. Hypoglycaemia in clinical diabetes. Chichester, UK. 1999, 167-186.
  5. Ryan Ch. N., Gurtunca A. D. Hypoglycaemia: a complication of diabetes therapy in children. Semin. Pediatr. Neurol. 2005; 12, 163-177. Go to original source...
  6. The Estee Corp. US Patent, 5545410.
  7. Hercules Inc. US Patent, 5795606.
  8. Sabadková D., Franc A., Muselík J., Neumann D.. Pelety s riadeným uvoľňovaním glukózy k prevencii hypoglykemií, Čes. Slov. Farm. 2014; 63, 101.
  9. Franc A., Muselík J., Sabadková D., Neumann D., Minaříková I. Different size of pellets with controlled release of glucose and dissolution profiles. World meating on pharmaceutics, biopharmaceutics and pharmaceutical technology. Lisbon Portugal 31. March - 3. April 2014.
  10. Franc A., Muselík J., Sabadková D., Neumann D. Pellets with controlled release of sugar for hypoglycaemia prevention in diabetes. 9. World meating on pharmaceutics, biopharmaceutics and pharmaceutical technology. Lisbon Portugal 31. March - 3. April 2014.
  11. Rowe R. C., Sheskey P. J.. Quinn A. M. E. Handbook of pharmaceutical excipients. 6th ed. London: Pharmaceutical Press, 2009.
  12. Neumann D., Franc A., Muselík J. CS Patentová přihláška PV 2013 - 338.
  13. Rabišková, M. Technologické parametry lékových mikroforem, jejich význam a metody jejich stanovení. Čes. Slov. Farm. 1996; 45, 177-179.
  14. Celine V. L., Siang M. Ch., Heng P. W. S. Elucidation of spheroid formation with and without the extrusion step. AAPS PharmSciTech. 2007; 8, E70-E81. Go to original source... Go to PubMed...
  15. Podczeck F., Rahman S. R., Newton J. M. Evaluation of a standardised procedure to assess the shape of pellets using image analysis. Int. J. Pharm. 1999; 192, 123-138. Go to original source... Go to PubMed...
  16. Chopra R. F., Podczeck J. M., Alderborn G. The influence of pellet shape and film coating on the filling of pellets into hard shell capsules. Eur. J. Pharm. Biopharm. 2002; 53, 327-333. Go to original source... Go to PubMed...
  17. Gajdziok J., Bernatoniene J., Muselík J., Masteiková R., Dvořáčková K., Petkeviciute Z., Lazauskas R., Kalveniene Z., Bernatoniene R. The evaluation of formulations for the preparation of new formula pellets, Pharm. Dev. Technol. 2011; 16, 520-528. Go to original source... Go to PubMed...
  18. Rabišková M., Häring A., Minczingerová K., Havlásek M., Musilová P. Mikrokrystalická celulosa v perorálních lékových formách. Chem. Listy, 2007; 101, 70-77.
  19. Wlosnewski J. C., Kumpugdee-Vollrath M., Sriamornsak P. Effect of drying technique and disintegrant on physical properties and drug release behavior of microcrystalline cellulose-based pellets prepared by extrusion/spheronization. Chem. Eng. Res. Des., 2010; 88, 100-108. Go to original source...
  20. Rabišková M., Masteiková R., Chalupová Z., Dvořáčková K. Lékové formy a biofarmacie: II. Brno: Veterinární a farmaceutická univerzita 2009.




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