| Product development studies of amino acid conjugate of Aceclofenac. | |
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MedLine Citation:
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PMID: 19450228 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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Ajay Pal Singh; Wafa Mossa Ramadan; Rajiv Dahiya; A S Sarpal; Kamla Pathak |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Current drug delivery Volume: 6 ISSN: 1567-2018 ISO Abbreviation: - Publication Date: 2009 Apr |
Date Detail:
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Created Date: 2009-05-19 Completed Date: 2009-06-26 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 101208455 Medline TA: Curr Drug Deliv Country: United Arab Emirates |
Other Details:
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Languages: eng Pagination: 208-16 Citation Subset: IM |
Affiliation:
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Department of Pharmaceutics, Faculty of Pharmacy, Al-Arab Medical University, Benghazi, Libya, P.O. 5341, Libya. ajaykansana@yahoo.co.in |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Anti-Inflammatory Agents, Non-Steroidal / chemistry, pharmacology, toxicity Biological Availability Calorimetry, Differential Scanning Chromatography, Thin Layer Crystallography Diclofenac / analogs & derivatives*, chemistry, pharmacology, toxicity Female Hydrogen-Ion Concentration Hydrophobicity Male Mass Spectrometry Particle Size Phenylalanine / chemistry* Prodrugs / chemical synthesis, chemistry*, pharmacology, toxicity Rats Rats, Inbred Strains Solubility Spectrophotometry, Ultraviolet Spectroscopy, Fourier Transform Infrared Stomach / drug effects, pathology Transition Temperature X-Ray Diffraction |
| Chemical | |
Reg. No./Substance:
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0/Anti-Inflammatory Agents, Non-Steroidal; 0/Prodrugs; 15307-86-5/Diclofenac; 63-91-2/Phenylalanine; 89796-99-6/aceclofenac |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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