DESIGN AND IN VITRO CHARACTERIZATION OF IN SITU FORMING CONTROLLED RELEASE IMPLANTS OF A NARCOTIC ANTAGONIST DRUG


Tektaş S., Serim T. M., Yüksel N., Özdemir A. N.

3rd International Gazi Pharma Symposium Series, 8 - 10 Eylül 2021, ss.147

  • Yayın Türü: Bildiri / Özet Bildiri
  • Sayfa Sayıları: ss.147
  • Ankara Üniversitesi Adresli: Evet

Özet

Opioid and alcohol addiction are one of the major health problems. Opioids account for 76% of deaths involving drug use disorders, while alcohol is responsible for about 3.6% of global deaths. Opioid antagonists block the effects of psychoactive substances and alcohol acting on µ, ᴋ, and δ opioid receptor sites by binding competitively to these receptors. Because of the extensive first-pass metabolism, the bioavailability of this group of active pharmaceutical substances is low and fluctuations in plasma concentrations occur when used orally. In addition, oral tablets have been associated with high rates of early withdrawal from treatment. For all these reasons, it would be advantageous to develop a dosage form in which the liver is bypassed, a constant plasma concentration can be achieved, and patients are not burdened with taking medication. In this study, in situ forming gel systems containing XTZ-21 have been investigated to meet all the requirements based on a gelling mechanism by solvent exchange. Resomer R 203 S as a biodegradable polymer and dimethyl sulfoxide, N-methyl pyrrolidone, poly(ethylene glycol) dimethyl ether (Mn = 250), poly(ethylene glycol) 400, benzyl alcohol, and ethyl heptanoate as solvents, were used for the preparation of formulations. The optimized formulation was determined by low burst drug release and controlled release of the drug for one month.