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Formation of Dispersible Taohong Siwu Tablets
Published on: February 3, 2023
Once-daily tablet formulation and in vitro release evaluation of cefpodoxime using hydroxypropyl methylcellulose: A
Hamid A Merchant1, Harris M Shoaib2, Jaweria Tazeen1
1Faculty of Pharmacy, University Road, 75270, Karachi, Pakistan.
Abstract:
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 (r 2=0.9734), but a close relationship was also noted with zero-order kinetics (r 2=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.
Insights
Developing a once-daily sustained-release tablet of cefpodoxime proxetil using HPMC enhances patient compliance and bacterial killing rates. This formulation effectively controls drug release for 24 hours, offering a promising alternative for improved therapeutic outcomes.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Pharmacokinetics
Background:
- Patient compliance with antibiotic regimens is often limited by frequent dosing schedules.
- Cefpodoxime proxetil is an effective antibiotic, but its conventional dosing may impact adherence.
- Sustained-release formulations offer potential for improved patient compliance and therapeutic efficacy.
Purpose of the Study:
- To develop and characterize a once-daily sustained-release tablet formulation of cefpodoxime proxetil.
- To evaluate the in vitro drug release profile and kinetics of the developed formulation.
- To assess the suitability of the formulation for improved patient compliance.
Main Methods:
- Formulation of cefpodoxime proxetil sustained-release tablets utilizing a hydrophilic HPMC matrix.
- Evaluation of pharmacotechnical properties including assay and tablet characteristics.
- In vitro dissolution studies conducted over 24 hours.
- Analysis of drug release kinetics using Higuchi, Korsmeyer-Peppas, and Hixson-Crowell models.
Main Results:
- The HPMC matrix effectively controlled cefpodoxime proxetil release for 24 hours, achieving a sustained-release profile.
- The formulation exhibited acceptable pharmacotechnical properties and met assay requirements.
- In vitro dissolution data closely matched theoretical release profiles, with drug release best described by Higuchi's equation (r²=0.9734).
- Korsmeyer-Pappas analysis indicated an anomalous diffusion mechanism (n=0.57), suggesting combined diffusion and erosion control.
Conclusions:
- A once-daily sustained-release tablet of cefpodoxime proxetil can be effectively developed using an HPMC matrix.
- The formulation demonstrates favorable in vitro release characteristics, supporting improved patient compliance and potentially enhanced therapeutic outcomes.
- The drug release mechanism involves a combination of diffusion and matrix erosion, providing a controlled release profile over 24 hours.
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