Skip to main content
PMC home page
AAPS PharmSciTech logoLink to AAPS PharmSciTech
. 2006 Sep 22;7(3):E178–E183. doi: 10.1208/pt070378

Once-daily tablet formulation and in vitro release evaluation of cefpodoxime using hydroxypropyl methylcellulose: A technical note

Hamid A Merchant 1, Harris M Shoaib 1,✉, Jaweria Tazeen 1, Rabia I Yousuf 1
PMCID: PMC2750520  PMID: 17025258

Summary and Conclusions

Decreasing the dose frequency of cefpodoxime proxetil increases patient compliance; patients prefer to take the drug once daily. It also improves the rate of bacterial killing and hastens the cure from the indications, and therefore increases compliance. The hydrophilic matrix of HPMC controlled the cefpodoxime proxetil release effectively for 24 hours; hence, the formulation can be considered as a once-daily sustained-release tablet of cefpodoxime proxetil. The formulation showed acceptable pharmacotechnical properties and assay requirements. In vitro dissolution studies indicated a sustained-release pattern throughout 24 hours of the study that was comparable to the theoretical release profile. Drug release kinetics indicated that drug release was best explained by Higuchi’s equation, as these plots showed the highest linearity (r2=0.9734), but a close relationship was also noted with zero-order kinetics (r2=0.9708). Korsmeyer’s plots indicated ann value of 0.57, which was indicative of an anomalous diffusion mechanism or diffusion coupled with erosion; hence, the drug release was controlled by more than one process. Hixson-Crowell plots indicated a change in surface area and diameter of the tablets with the progressive dissolution of the matrix as a function of time.

Keywords: Cefpodoxime proxetil, hydroxypropyl methylcellulose (HPMC), hydrophilic matrix tablets, in vitro sustained drug release, once-daily tablet, Cefpo SR

Full Text

The Full Text of this article is available as a PDF (179.8 KB).

References

  • 1.Alderman DA. A review of cellulose ethers in hydrophillic matrices for oral controlled-release dosage forms. Int J Pharm Tech Prod Mfr. 1984;5:1–9. [Google Scholar]
  • 2.Dow Chemical Company. Using methocel cellulose ethers for controlled release of drugs in hydrophillic matrix systems. Available at: http://www.dow.com/PublishedLiterature/dh_01e7/09002fl3801e718c. pdf?filepath=methocel/pdfs/noreg/198-02075.pdf&fromPage=GetDoc. Accessed: August 24, 2006.
  • 3.Dollery C. Therapeutic Drugs. Edinburgh, Scotland: Churchill Livingstone; 1999. pp. C113–C117. [Google Scholar]
  • 4.Todd WM. Cefpodoxime proxetil: a comprehensive review. Int J Antimicrob Agents. 1994;4:37–62. doi: 10.1016/0924-8579(94)90062-0. [DOI] [PubMed] [Google Scholar]
  • 5.Sader HS, Jones RN, Washington JA, et al. Diagn Microbiol Infect Dis. 1993;17:143–150. doi: 10.1016/0732-8893(93)90025-3. [DOI] [PubMed] [Google Scholar]
  • 6.Orelox. Electronic medicines compendium, Aventis Pharma Ltd. Available at: http://emc.medicines.org.uk/emc/assets/c/html/displaydoc. asp?documentid=8940. Accessed: January 8, 2005.
  • 7.Saathoff N, Lode H, Neider K, et al. Pharmacokinetics of cefpodoxime proxetil and interactions with an antacid and an H2 receptor antagonist. Antimicrob Agents Chemother. 1992;36:796–800. doi: 10.1128/aac.36.4.796. [DOI] [PMC free article] [PubMed] [Google Scholar]
  • 8.Wai-Yip Lee T, Robinson RJ. Controlled drug delivery systems. In: Gennaro AR, editor. Remington: The Science and Practice of Pharmacy. 20th ed. Philadelphia, PA: University of Sciences in Philadelphia; 2000. pp. 903–929. [Google Scholar]
  • 9.Vantin. Pharmacia & Upjohn Company, Pharmacia Corporation. Available at: http://www.pfizer.com/download/uspi_vantin.pdf. Accessed: August 24, 2006.
  • 10.Martindale . The Extra Pharmacopoeia. 31st ed. London, UK: Royal Pharmaceutical Society; 1996. pp. 193–193. [Google Scholar]
  • 11.VIVAPHARM, cellulose-based polymer for film-coating and sustained release application. Available at: http://www.jrspharma.de. Accessed: January 8, 2005.
  • 12.British Pharmacopoeia (B.P.). London, UK: Stationary Office London; 2004.
  • 13.United States Pharmacopeia-27. Rockville, MD: US Pharmacopeial Convention; 2004:377–379. Also pp778–780.
  • 14.Qiu Y, Garren J, Samara E, et al. Once-a-day controlled-release dosage form of divalproex sodium II: development of a predictive in-vitro drug release method. J Pharm Sci. 2003;92:2317–2325. doi: 10.1002/jps.10486. [DOI] [PubMed] [Google Scholar]
  • 15.Hadjiioannou TP, Christian GD, Koupparis MA. Quantitative Calculations in Pharmaceutical Practice and Research. New York, NY: VCH Publishers Inc; 1993. pp. 345–348. [Google Scholar]
  • 16.Bourne DW. Pharmacokinetics. In: Banker GS, Rhodes CT, editors. Modern Pharmaceutics. 4th ed. New York, NY: Marcel Dekker Inc; 2002. pp. 67–92. [Google Scholar]
  • 17.Higuchi T. Mechanism of sustained action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J Pharm Sci. 1963;52:1145–1149. doi: 10.1002/jps.2600521210. [DOI] [PubMed] [Google Scholar]
  • 18.Hixson AW, Crowell JH. Dependence of reaction velocity upon surface and agitation: I-theoretical consideration. Ind Eng Chem. 1931;23:923–931. doi: 10.1021/ie50260a018. [DOI] [Google Scholar]
  • 19.Korsmeyer RW, Gurny R, Doelker E, Buri P, Peppas NA. Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm. 1983;15:25–35. doi: 10.1016/0378-5173(83)90064-9. [DOI] [PubMed] [Google Scholar]
  • 20.Siepmann J, Peppas NA. Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC) Adv Drug Deliv Rev. 2001;48:139–157. doi: 10.1016/S0169-409X(01)00112-0. [DOI] [PubMed] [Google Scholar]
  • 21.Saravanan M, Nataraj KS, Ganesh KS. Hydroxypropyl methylcellulose based cephalexin extended release tablets: influence of tablet formulation, hardness and storage on in-vitro release kinetics. Chem Pharm Bull (Tokyo) 2003;51:978–983. doi: 10.1248/cpb.51.978. [DOI] [PubMed] [Google Scholar]
  • 22.Sood A, Panchagnula R. Drug release evaluation of diltiazem CR preparations. Int J Pharm. 1998;175:95–107. doi: 10.1016/S0378-5173(98)00268-3. [DOI] [Google Scholar]
  • 23.Reddy KR, Mutalik S, Reddy S. Once-daily sustained-release matrix tablets of nicorandil: formulation and in vitro evaluation. AAPS PharmSciTech. 2003;4:E61–E61. doi: 10.1208/pt040461. [DOI] [PMC free article] [PubMed] [Google Scholar]
  • 24.Fassihi RA, Ritschel WA. Multiple layer, direct compression controlled release system: in vitro and in vivo evaluation. J. Pharm Sci. 1993;82:750–754. doi: 10.1002/jps.2600820715. [DOI] [PubMed] [Google Scholar]

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

RESOURCES