AICTE SPONSORED INTERNATIONAL SEMINAR ON HERBALS AND NATURAL PRODUCTS FOR LIVER AND PANCREATIC DISORDERS

Synthesis and Pharmacological Evaluation of Gastro-sparing Mutual Prodrug of Aceclofenac with Glucosamine

Suneela S. Dhaneshwar * 1, Sanal Dev1, B.Rathi2 and S. L. Bodhankar2
1 Department of Pharmaceutical Chemistry, Bharati Vidyapeeth University, Poona College of Pharmacy,
Erandwane, Pune, India.
2 Department of Pharmacology, Bharati Vidyapeeth University, Poona College of Pharmacy, Erandwane, Pune, India.
*Author for correspondence: Dr. Suneela Dhaneshwar E-mail: suneeladhaneshwar@rediffmail.com

InPharm Communique Vol 2, No 3 | 17

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ABSTARCT 

Aceclofenac is a nonsteroidal antiinflammatory drug that is used to relieve pain and inflammation in arthritic conditions like osteoarthritis, rheumatoid arthritis and ankylosing spodylitis. Aceclofenac is known to induce erosion and ulcers in the gastrointestinal tract but in contrast to other nonsteroidal anti-inflammatory agents, it has shown stimulatory effects on cartilage matrix synthesis. In order to lower the ulcerogenic potential and enhance effectiveness of aceclofenac as antiarthritic agent, a mutual prodrug was synthesized with neutraceutical carrier D-glucosamine that has shown to stimulate the biosynthesis of glucosaminoglycans and hyaluronic acid backbone needed for the formation of the proteoglycans found in the structural matrix of joints. The study showed that the prodrug not only lowered the ulcerogenic potential of aceclofenac but also enhanced its analgesic, antiinflammatory and antiarthritic activities thus proving the utility of D-glucosamine as an effective carrier in mutual prodrug synthesis. Key words Aceclofenac, anti-arthritic, anti-inflammatory, glucosamine, gastrosparing, mutual prodrug.

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Laboratory Synthesis Of Fenoverine

 Fenoverine Synthesis

 

MW: 459.57 MF: C26H25N3O3S

LD50 Fenoverine: 2874 mg/kg (M, p.o.)

IUPAC NAME Fenoverine:  10- [[4- (1 ,3- benzo dioxol- 5- yl methyl)- 1- piperazinyl ]acetyl]- 10 H- pheno thiazine

Reference 

French patent:  2092639

 

Laboratory Synthesis Of Fenbufen

Fenbufen Synthesis

SYNTHESIS

Tomeufeik, A.; et al. (American Cyanamid Co.); Compositions containing substituted benzoylpropionic acids and method of use to treat inflammation and pain. 

REFERENCE 

1. Fenbufen. Drugs Fut 1976, 1, 1, 21

2. DE 2147111; FR 2107848; GB 1320076; US 3784701 

   MW: 254.29 MF: C16H14O3
   LD50 Fenbufen : 795 mg/kg (M, p.o.);200 mg/kg (R, p.o.)