Synthesis and in vitro Evaluation of Polymeric Prodrug of Ibuprofen with Amino Acid Spacer.
The present work is an agreement with simple and efficient method of improving the therapeutic efficacy of ibuprofen by masking its acidic moiety. It aims to reduce gastrointestinal side effects by controlling the rate, duration and site of release. This is achieved by synthesis and evaluation of polymeric prodrug of ibuprofen with natural polymer sodium alginate. The synthesis was supported by N-protected serine as spacer due to chemical incompatibility of drug and polymer. Synthesized prodrug was characterized for confirmation of said structures. The in-vitro dissolution profile of ibuprofen-alginate prodrug showed that the release of the drug is significantly higher in case of pH 7.2 buffer as compared to ibuprofen, which might be due to ester group adjacent to drug get hydrolyzed. The hydrolysis was found to be with faster rate in alkaline media than that of in acidic media.
Department of Pharmaceutical Chemistry, R.C. Patel Institute of Pharmaceutical Education and Research, Shirpur, (425 405) India. vivek.redasani@gmail.com.
Vivekkumar K
VK
Redasani
Sanjay B
SB
Bari
D000464:Alginates / Q000138:chemical synthesis; D000700:Analgesics / Q000009:adverse effects / Q000627:therapeutic use*; D065546:Drug Liberation; D005744:Gastric Acid / Q000737:chemistry; D065569:Gastrointestinal Absorption / Q000502:physiology; D020723:Glucuronic Acid / Q000138:chemical synthesis; D006603:Hexuronic Acids / Q000138:chemical synthesis; D006801:Humans; D006863:Hydrogen-Ion Concentration; D006868:Hydrolysis; D007052:Ibuprofen / Q000009:adverse effects / Q000627:therapeutic use*; D010146:Pain / Q000188:drug therapy*; D011108:Polymers / Q000138:chemical synthesis; D011355:Prodrugs / Q000138:chemical synthesis
D000464:Alginates; D000700:Analgesics; D006603:Hexuronic Acids; D011108:Polymers; D011355:Prodrugs; D020723:Glucuronic Acid; D007052:Ibuprofen