Abstract
The present investigation deals with the optimization, formulation, and characterization of oral in situ gel of spiramycin. Sodium alginate and hydroxypropyl methylcellulose were used as cross-linking and viscosifying agents, respectively. Sodium bicarbonate was used as a floating agent. In preformulation studies, the melting point, pH, and partition coefficient were found to be 133°C, 9.5, and 0.193, respectively. The drug had retention time at around 2.65 minutes in high performance liquid chromatography (HPLC). During compatibility studies of drug with all polymers, we observed that there were no changes in the FTIR spectra of a mixture of drug and polymers. All the formulations showed good pourability. Floating time and total floating time were ~30 sec and >12 hours, respectively. During in vitro drug release studies, the drug was released from the formulation around 80–100% for 12–16 hrs. In TEM analysis, we found that the drug molecules were well entrapped in the polymer and the drug was released slowly for up to 12 hrs. In these studies, we found that the concentration of sodium alginate and HPMC had significant influence on floating lag time, gelling capacity, and cumulative percentage drug release. During antimicrobial studies, we found that the formulation containing spiramycin showed good zone of inhibition against different microbial strains (Staphylococcus aureus and Escherichia coli).
Highlights
Antimicrobial therapy of an infection depends on the concentration of the antibiotic at the site of infection, which must be sufficient to inhibit growth of the offending microorganisms
We describe the formulation and evaluation of in situ oral gels of spiramycin based on the concept of pH triggered and ion activated systems
FTIR spectrum of the pure spiramycin was recorded by FTIR spectrophotometer
Summary
Antimicrobial therapy of an infection depends on the concentration of the antibiotic at the site of infection, which must be sufficient to inhibit growth of the offending microorganisms. Staphylococcus aureus is a bacterium that is a member of the Firmicutes and is frequently found in the human respiratory tract and on the skin [1, 4]. Staphylococcus aureus is not always pathogenic, it is a common cause of skin infections (e.g., boils), respiratory disease (e.g., sinusitis), and food poisoning. Staphylococcus aureus food poisoning is often caused when a food handler contaminates food products that are served or stored at room temperature or refrigerator temperature [1, 2]. Other infections caused by Staphylococcus aureus are skin and soft tissue infections such as abscesses, cellulitis, and pneumonia [3]
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