Primjena ciklodekstrina u razvoju parenteralnih pripravaka

master's thesis

• Title (english): The use of cyclodextrins in the development of parenteral formulations
• Author: Josipa Vidović
• Mentor: Mario Jug (mentor)
• Committee member: Mario Jug (predsjednik povjerenstva)
• Committee member: Sanda Vladimir-Knežević (član povjerenstva)
• Committee member: Jasmina Lovrić (član povjerenstva)
• Granter: University of Zagreb; Faculty of Pharmacy and Biochemistry; (Department of pharmaceutical technology); Zagreb
• Defense date and country: 2020-02-20, Croatia
• Scientific / art field, discipline and subdiscipline: BIOMEDICINE AND HEALTHCARE; Pharmacy; Pharmacy

Abstract

Razvoj novih i inovativnih lijekova za liječenje različitih bolesti, koji su učinkoviti i sigurni za primjenu veliki je izazov. Primjena kombinatorijalne kemije i molekulskog modeliranja u razvoju novih lijekova rezultirali su potencijalnim novim lijekovima izražene lipofilnosti i visoke molekulske mase te posljedično slabe topljivosti u vodi. Upravo je ograničena topljivost vodeći razvoj odbacivanja novih struktura, jer rezultira niskom bioraspoloživosti i suboptimalnim učinkom ispitivanog lijeka. Ciklodekstrini su ciklički oligosaharidi koji se u farmaceutskoj tehnologiji koriste kao pomoćne tvari za maskiranje neugodnog okusa i mirisa lijeka te za poboljšanje topljivosti i posljedično bioraspoloživosti lijekova. Danas su na tržištu prisutne formulacije lijekova s ciklodekstrinima namijenjene za različite puteve primjene, uključujući i pripravke za parenteralnu primjenu. Obzirom da parenteralna primjena ima određene prednosti naspram drugih načina primjene u tijeku je razvoj i provođenje kliničkih ispitivanja brojnih parenteralnih formulacija koje sadrže ciklodekstrine. S obzirom na povoljne rezultate ispitivanja te sigurnost primjene takvih formulacija može se u skorije vrijeme očekivati značajan porast broja takvih formulacija u svakodnevnoj kliničkoj praksi. U ovom radu prikazane su prednosti i nedostatci uporabe ciklodekstrina u razvoju parenteralnih pripravaka. U tu svrhu razmatrani su rezultati kliničkih studija formulacija koje su nedavno registrirane ili su u naprednim fazama kliničkih ispitivanja. Gledajući superiorne terapijske rezultate, kao što su brži nastup djelovanja uz smanjenje broja i intenziteta nuspojava, može se očekivati značajan porast broja parenteralnih formulacija u kliničkoj praksi u skoroj budućnosti.

Abstract (english)

It is a great challenge to develop new and innovative medicines for the treatment of a variety of diseases, which are effective and safe to administer. The use of combinatorial chemistry and molecular modelling in the development of new drugs has resulted in molecules with pronounced lipophilicity and high molecular weight, and consequently poor solubility in water. The poor solubility of new drug entities has been recognized as one of the most important factors that lead to rejections of such new structures, as they show low bioavailability and suboptimal therapeutic effect. Cyclodextrins are cyclic oligosaccharides used in pharmaceutical technology as multifunctional excipients able to mask the unpleasant taste and odor of a drug and to improve their solubility and consequently bioavailability. Cyclodextrin-based drug formulations currently available on the market are intended for various routes of administration, including parenteral administration. Parenteral administration provides certain advantages over other routes of administration, so the development and clinical trials of parenteral formulations containing cyclodextrins are in the pipeline of numerous pharmaceutical companies. The favorable efficiency and the safety of currently available formulations may lead to a significant increase in the number of such formulations in daily clinical practice in the near future. This paper outlines the advantages and disadvantages of cyclodextrin used in the development of parenteral preparations. To this end, the results of clinical studies of formulations that have recently been registered or are in advanced stages of clinical trials have been considered. Looking at superior therapeutic outcomes, including the faster onset of action accompanied by reduced number and intensity of side effects, a significant increase in the number of parenteral formulations in clinical practice can be expected in the near future.

• Keywords: ciklodekstrini; parenteralni pripravci
• Keywords (english): cyclodextrins; parenteral preparations
• Language: croatian
• URN:NBN: urn:nbn:hr:163:371078
• Study programme: Title: Pharmacy; Study programme type: university; Study level: integrated undergraduate and graduate; Academic / professional title: magistar/magistra farmacije (magistar/magistra farmacije)
• Type of resource: Text
• File origin: Born digital
• Access conditions: Open access
• Created on: 2022-08-26 11:56:35