Journal of Pharmaceutical Technology

Yazarlar: Tilbe ÇEVİKELLİ, Deniz ONAN, Umay Merve GÜVEN, Esra DEMİRTÜRK

Konular:Farmakoloji ve Eczacılık

Anahtar Kelimeler:Microemulsion,Theophylline,Asthma Therapy,Controlled Release,Drug Delivery System

Özet: Theophylline is widely used as a bronchodilator drug in asthma and chronic obstructive lung disease because it is effective and inexpensive. Theophylline blood concentrations should be monitored since its therapeutic index is narrow, its optimum blood levels range from 10 to 20 µg/mL; its serious side effects take place over 20 µg/mL; its efficacy falls below 10 µg/mL blood concentrations. The aim of the present study is to formulate and characterize oil-in-water microemulsion systems for oral delivery of theophylline. Microemulsion formulations represent an interesting delivery vehicle for poorly water-soluble drugs, allowing for improving their solubility and dissolution properties. A simple and reliable UV-Spectrophotometric method was developed and validated for the determination of theophylline in the concentration range of 25-150 µg/mL. In vitro drug release profile showed that after 1 hour, 40% of the drug released through the formulation in Simulated Intestinal Fluid (SIF) at pH 6.8 as a release medium and the microemulsion formulations released more than 75% of the drug during the 5 hours study period. The globule size of drug-loaded formulations was in the range of 203.6 ± 0.2 nm. Results confirmed that the proposed microemulsion formulation containing theophylline could improve and control the drug release profile in comparison to the conventional dosage form.

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