Synthesis, kinetics and pharmacological evaluation of mefenamic acid mutual prodrug.

نویسندگان

  • Kamal Shah
  • Sushant K Shrivastava
  • Pradeep Mishra
چکیده

A novel mutual prodrug (MA-P) consisting of mefenamic acid (MA) and paracetamol (P) has been synthesized as a gastrosparing NSAID, devoid of ulcerogenic side effects. The structure of synthesized drug was confirmed by elemental analysis, infrared spectroscopy, 1H NMR spectroscopy and mass spectrometry.The kinetics of ester hydrolysis was studied by HPLC at pH 2, pH 7.4 as well as in human plasma. The pharmacological activities (anti-inflammatory, analgesic and ulcerogenic) were evaluated for the synthesized drug. The ulcerogenic reduction in terms of gastric wall mucosa, hexosamine and total proteins were also measured in glandular stomach of rats. The results indicated that MA-P ester has better ulcer index than the parent drug.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Synthesis and Pharmacological Evaluation of Cyclodextrin Conjugate Prodrug of Mefenamic acid

In the present investigation mefenamic acid prodrug of ß-cyclodextrins was synthesized. The primary hydroxy group of ß-cyclodextrins was used to block the acid group. The synthesis involved a series of protection and deprotection reaction. The ester was evaluated for stability in simulated gastric and intestinal fluid. The hydrolysis of cyclodextrin conjugate in colon is confirmed by the hydrol...

متن کامل

Design, Synthesis, and Biological Evaluation of Mutual Prodrugs of Some Selected NSAIDs

Non-steroidal Anti-inflammatory drugs (Aceclofenac, Mefenamic acid) have conjugated with different antioxidants such as Thymol, Menthol which having antiulcerogenic activity with the NSAIDsantioxidant mutual prodrug gastro sparing NSAIDs devoid of Ulcerogenic side effects. Two mutual Prodrugs have synthesized in which NSAIDs have been conjugated with different antioxidants by a glycolic acid sp...

متن کامل

Synthesis and evaluation of a prodrug of 5-aminosalicylic acid for the treatment of ulcerative colitis

Objective(s): This study is aimed to design and synthesize a prodrug of 5-aminosalicylic acid and evaluate its ameliorative effect on experimental ulcerative colitis (UC).Materials and Methods: 5-Aminosalicylic acid-alanine (5-ASA-ALA) was synthesized and characterized. Its stability study was conducted in rat plasma and in the gastroint...

متن کامل

Synthesis of a novel PEGylated colon-specific azo-based 4- aminosalicylic acid prodrug

Objective(s): 4-aminosalicylic acid (4-ASA) is an isomer of mesalazine that has recently been shown to be effective against inflammatory bowel disease (IBD), and more specifically, ulcerative colitis. However, the majority of orally administered 4-ASA is readily and extensively absorbed from the stomach and small intestine, so only a small amount is transported to the ...

متن کامل

Mutual Prodrugs - a Swot Analysis

Mutual prodrug is a form of prodrug in which two pharmacologically active agents are attached to each other in such a way that each drug acts as a promoiety/carrier for each other and vice versa. The association may be “synergistic” if the carrier shows the same biological action as that of parent drug or may provide “additional” benefit if it shows new pharmacological action which is lacking i...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:
  • Acta poloniae pharmaceutica

دوره 70 5  شماره 

صفحات  -

تاریخ انتشار 2013