PMCCPMCCPMCC

Search tips
Search criteria 

Advanced

 
Logo of aapspharmspringer.comThis journalToc AlertsSubmit OnlineOpen Choice
 
AAPS PharmSciTech. 2002 September; 3(3): 83–89.
Published online 2015 February 19. doi:  10.1007/BF02830625
PMCID: PMC2784056

Influence of complex solubility on formulations based on lambda carrageenan and basic drugs

Abstract

The purpose of the present work was to compare the behavior of some drug/carrageenan complexes having different solubility in water, in a controlled release formulation. Diltiazem HCl, bupropion HCl, metoprolol tartrate, and tramadol HCl were used as model drugs. The complexes were characterized by means of solubility measurements, release test at constant surface area, and water uptake measurements, and the results were related to their performance in controlled release formulations. For the more soluble complexes (involving metoprolol and tramadol) the occurrence of gelation after hydration was observed, while diltiazem complex apparently did not gellify; bupropion behavior was intermediate. A correspondence was found between the observed differences in complex solubility and hydration-gelation behavior and the drug release profiles. For all the drugs considered, the release was completed in about 10 to 12 hours, but different kinetics were observed depending on the solubility of the complexes. All the considered complexes seem suitable for controlled release purposes, although the data obtained show the relevance of the complex solubility to drug release profiles.

Full Text

The Full Text of this article is available as a PDF (111K).

Selected References

These references are in PubMed. This may not be the complete list of references from this article.
1. Kalinkova GN. Studies of beneficial interactions between active medicaments and excipients in pharmaceutical formulations. Int J Pharm. 1999;187:1–15. doi: 10.1016/S0378-5173(99)00176-3. [PubMed] [Cross Ref]
2. Nujoma YN, Kim C.J. A designer's polymer as an oral drug carrier (tablet) with pseudo-zero-order release kinetics. J Pharm Sci. 2002;85:1091–1095. doi: 10.1021/js960030t. [PubMed] [Cross Ref]
3. Konar N, Kim C.J. Drug release from drug-polyanion complex tablets: poly(acrylomido-2-methyl-1-propanesulfonate sodium-co-methyl methacrylate) J Control Release. 1999;57:141–150. doi: 10.1016/S0168-3659(98)00112-6. [PubMed] [Cross Ref]
4. FMC Corporation, Pharmaceutical Division, Philadelphia, PA, USA. Marine colloids carrageenan. Technical bulletin, 1993.
5. Bonferoni MC, Rossi S, Tamayo M, Pedraz JL, Dominguez Gil A, Caramella C. On the employment of lambda carrageenan in a matrix system, I: sensitivity to dissolution medium and comparison with Na carboxymethylcellulose and xanthan gum. J Control Release. 1993;26:119–127. doi: 10.1016/0168-3659(93)90111-H. [Cross Ref]
6. Bonferoni MC, Rossi S, Ferrari F, Bertoni M, Bolhuis GK, Caramella C. On the employment of lambda carrageenan in a matrix system. III: optimization of a lambda carrageenan-HPMC hydrophilic matrix. J Control Release. 1998;51:231–239. doi: 10.1016/S0168-3659(97)00175-2. [PubMed] [Cross Ref]
7. Bonferoni MC, Rossi S, Ferrari F, Bettinetti GP, Caramella C. Characterization of a diltiazem-lambda carrageenan complex. Int J Pharm. 2000;200:207–216. doi: 10.1016/S0378-5173(00)00389-6. [PubMed] [Cross Ref]
8. Bonferoni MC, Rossi S, Ferrari F, Caramella C. Development of a once-a-day tablet formulation based on a diltiazem/carrageenan interaction product. In: Proceedings of the 2nd World Meeting APGI/APV. Paris. 25/28 May (1998). Pag 153–154.
9. Caramella C, Bonferoni MC, Patent application PCT/EP/98/06864.
10. Bonferoni MC, Rossi S. Ferrari F, Sorrenti M, Caramella C. Characterization of interaction products between carrageenan and some basic drugs. In: Proceedings of the 2nd World Meeting APGI/APV, Paris, 25/28 May (1998). Pag 71–72.
11. Klotz IM, Walker FM, Pivan RB. The binding of organic ions by proteins. J Am Chem Soc. 1946;68:1486–1490. doi: 10.1021/ja01212a030. [PubMed] [Cross Ref]
12. Ferrari F, Rossi S, Bertoni M, Caramella C, Geddo M. Modelling of water penetration into fast disintegrating tablets. STP Pharma Sci. 1991;1(2):137–144.
13. Peppas NA. Analysis of Fickian and non-Fickian drug release from polymers. Pharm Acta Helv. 1985;60:110–111. [PubMed]
14. Bonferoni MC, Rossi S. Ferrari F, Stavik E, Pena Romero A, Caramella C. Factorial analysis of the influence of dissolution medium on drug release from carrageenan-diltiazem complexes. AAPS Pharm Sci Tech. 2000;1. Available at [PMC free article] [PubMed]
15. Bonferoni MC, Rossi S, Tamayo M, Pedraz JL, Dominguez Gil A, Caramella C. On the employment of lambda carrageenan in a matrix system. II: lambda carrageenan and hydroxypropylmethylcellulose mixtures. J Control Release. 1994;30:175–182. doi: 10.1016/0168-3659(94)90264-X. [Cross Ref]

Articles from AAPS PharmSciTech are provided here courtesy of American Association of Pharmaceutical Scientists