Document Detail

Product development studies of amino acid conjugate of Aceclofenac.
MedLine Citation:
PMID:  19450228     Owner:  NLM     Status:  MEDLINE    
The prodrugs designed by classical approach increase lipophilicity of the drug, which decreases the water solubility thus decreasing the concentration gradient, which controls drug absorption. To overcome the limitations of traditional prodrug approach, water soluble prodrugs can be designed by adding selected amino acid to the drug moiety that are the substrates for the enzyme located at the intestinal brush border thus overcoming pharmaceutical problem without compromising bioavailability. ACaa (Amino acid conjugate of Aceclofenac) was synthesized by conjugation with l-phenylalanine by conventional coupling method using N, N-dicyclohexylcarbodiimide and ACaa was characterized by melting point, TLC, photomicrograph, UV, FT-IR, FT-NMR, MS-FAB, XRD and DSC. As a part of product development study ACaa was subjected to studies like In-vivo in albino rats and in-vitro like ACaa reversion to AC (Aceclofenac) in aqueous buffers of pH 1.21, 2.38. 3.10, 6.22 and 7.41, at a constant concentration (0.05M), ionic strength (micro = 0.5) and at a temperature of 37 degrees C +/- 0.5 degrees C, ACaa showed negligible reversion (2.15 %) up to 24 hrs study at acidic pH thus suggesting stability in acidic environment of stomach, the rate of reversion increased as pH of medium increased. pH- partition profile, pH- solubility profile and micromeritic studies were also carried out in comparison to pure drug. The solubility and lipophilicity of ACaa exhibited higher values at all pH range when compared to AC. The micromeritic properties also evaluated in terms of particle shape and size, IQCS and kurtosis. Resulting IQCS value approached zero thus suggesting reducing in the degree of skewness.
Ajay Pal Singh; Wafa Mossa Ramadan; Rajiv Dahiya; A S Sarpal; Kamla Pathak
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Current drug delivery     Volume:  6     ISSN:  1567-2018     ISO Abbreviation:  -     Publication Date:  2009 Apr 
Date Detail:
Created Date:  2009-05-19     Completed Date:  2009-06-26     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101208455     Medline TA:  Curr Drug Deliv     Country:  United Arab Emirates    
Other Details:
Languages:  eng     Pagination:  208-16     Citation Subset:  IM    
Department of Pharmaceutics, Faculty of Pharmacy, Al-Arab Medical University, Benghazi, Libya, P.O. 5341, Libya.
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MeSH Terms
Anti-Inflammatory Agents, Non-Steroidal / chemistry,  pharmacology,  toxicity
Biological Availability
Calorimetry, Differential Scanning
Chromatography, Thin Layer
Diclofenac / analogs & derivatives*,  chemistry,  pharmacology,  toxicity
Hydrogen-Ion Concentration
Mass Spectrometry
Particle Size
Phenylalanine / chemistry*
Prodrugs / chemical synthesis,  chemistry*,  pharmacology,  toxicity
Rats, Inbred Strains
Spectrophotometry, Ultraviolet
Spectroscopy, Fourier Transform Infrared
Stomach / drug effects,  pathology
Transition Temperature
X-Ray Diffraction
Reg. No./Substance:
0/Anti-Inflammatory Agents, Non-Steroidal; 0/Prodrugs; 15307-86-5/Diclofenac; 63-91-2/Phenylalanine; 89796-99-6/aceclofenac

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