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AAPS PharmSciTech. 2006 March; 7(1): E118–E124.
Published online 2006 February 24. doi:  10.1208/pt070117
PMCID: PMC2750724

Intragastric floating drug delivery system of cefuroxime axetil: In vitro evaluation

Abstract

This investigation describes the development of an intragastric drug-delivery system for cefuroxime axetil. The 32 full factorial design was employed to evaluate contribution of hydroxypropyl methyl cellulose (HPMC) K4M/HPMC K100 LV ratio (polymer blend) and sodium lauryl sulfate (SLS) on drug release from HPMC matrices. Tablets were prepared using direct compression technique. Formulations were evaluated for in vitro buoyancy and drug release study using United States Pharmacopeia (USP) 24 paddletype dissolution apparatus using 0.1N HCl as a dissolution medium. Multiple regression analysis was performed for factorial design batches to evaluate the response. All formulations had floating lag times below 2 minutes and constantly floated on dissolution medium for more than 8 hours. It was found that polymer blend and SLS significantly affect the time required for 50% of drug release, percentage drug release at 12 hours, release rate constant, and diffusion exponent (P<.05). Also linear relationships were obtained between the amount of HPMC K100 LV and diffusion exponent as well as release rate constant. Kinetic treatment to dissolution profiles revealed drug release ranges from anomalous transport to case 1 transport, which was mainly dependent on both the independent variables.

KeyWords: hydroxypropyl methylcellulose (HPMC), sodium lauryl sulfate (SLS), factorial design, floating tablets

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.
1. McEvoy GK, editor. Cephalosporins: cefuroxime sodium and cefuroxime axetil. Bethesda, MD: American Society of Hospital Pharmacists Inc; 2003. pp. 223–231.
2. Wozniak T, Hicks J. Cefuroxime sodium. In: Florey K, editor. Analytical Profiles of Drug Substances. San Diego, CA: Academic Press; 1991. pp. 209–237.
3. Ridgway E, Stewart K, Rai G, Kelsey MC, Bielawska C. The pharmacokinetics of cefuroxime axetil in the sick elderly patient. J Antimicrob Chemother. 1991;27:663–668. doi: 10.1093/jac/27.5.663. [PubMed] [Cross Ref]
4. Sommers D, Van Wyk K, Schoeman H, Moncrieff J. Influence of food and reduced gastric acidity on the bioavailability of bacampicillin and cefuroxime axetil. Br J Clin Pharmacol. 1984;18:535–539. [PMC free article] [PubMed]
5. Finn A, Straugun A, Meyer M, Chubb J. Effect of dose and food on the bioavailability of cefuroxime axetil. Biopharm Drug Dispos. 1987;8:519–526. doi: 10.1002/bdd.2510080604. [PubMed] [Cross Ref]
6. McEvoy GK, editor. Cephalosporins: cefuroxime sodium and cefuroxime axetil. Bethesda, MD: American Society of Hospital Pharmacists Inc; 1994. pp. 152–159.
7. Williams P, Harding SM. The absolute bioavailability of oral cefuroxime axetil in male and female volunteers after fasting and after food. J Antimicrob Chemother. 1984;13:191–196. doi: 10.1093/jac/13.2.191. [PubMed] [Cross Ref]
8. Harding SM. Comparative pharmacokinetics of tablets and suspension. Res Clin Forums. 1990;12:23–29.
9. Mosher G, Mc-Bee LJ, Shaw David B. Esterase activity toward the diastereomers of cefuroxime axetil in the rat and the dog. Pharm Res. 1992;9:687–689. doi: 10.1023/A:1015818614282. [PubMed] [Cross Ref]
10. Kees F, Lukassek U, Naber KG, Grobecker H. Comparative investigations on the bioavailability of cefuroxime axetil. Arzneimittelforschung. 1991;41:843–846. [PubMed]
11. Profilaxis Antibiotica: Cefuroxima IV Versus Oral. Madrid, Spain: Glaxo Inc; 1994.
12. Ruiz-Balaguer N, Nacher A, Casabo VG, Merino M. Nonlinear intestinal absorption kinetics of cefuroxime axetil in rats. Antimicrob Agents Chemother. 1997;41:445–448. [PMC free article] [PubMed]
13. Adams DH, Wood MJ, Farrell ID, Fox C, Ball AP. Oral cefuroxime axetil: clinical pharmacological and comparative dose studies in urinary tract infection. J Antimicrob Chemother. 1985;16:359–366. doi: 10.1093/jac/16.3.359. [PubMed] [Cross Ref]
14. Sood A, Panchagnula R. Design of controlled release delivery systems using a modified pharmacokinetic approach: a case study for drugs having a short elimination half-life and a narrow therapeutic index. Int J Pharm. 2003;261:27–41. doi: 10.1016/S0378-5173(03)00267-9. [PubMed] [Cross Ref]
15. Hoffman A, Dananberg HD, Katzhendler I, Shuval R, Gilhar D, Friedman M. Pharmacodynamic and pharmacokinetic rational for the development of an oral controlled release amoxicillin dosage form. J Control Release. 1998;54:29–37. doi: 10.1016/S0168-3659(97)00165-X. [PubMed] [Cross Ref]
16. Yeole PG, Khan S, Patel VF. Floating drug delivery systems: need and development. Indian J Pharm Sci. 2005;67:265–272.
17. Arora S, Ali J, Ahuja A, Khar RK, Baboota S. Floating drug delivery systems: a review. AAPS Pharm Sci Tech. 2005;6:E372–E390. doi: 10.1208/pt060347. [PMC free article] [PubMed] [Cross Ref]
18. Colombo P, Bettini R, Peppas NA. Observation of swelling process and diffusion front position during swelling in HPMC matrices containing soluble drug. J Control Release. 1999;61:83–91. doi: 10.1016/S0168-3659(99)00104-2. [PubMed] [Cross Ref]
19. Methocel: Cellulose Ethers Technical Handbook. San Diego, CA, USA: Dow Chemical Co; 1996. pp. 18–20.
20. Dortunc B, Gunal N. Release of acetazolamide from swellable HPMC matrix tablets. Drug Dev Ind Pharm. 1997;23:1245–1249. doi: 10.3109/03639049709146165. [Cross Ref]

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