Isolation, Characterization and Pharmacological Evaluation of 8-chloro-3 (1-methyl-piperidene-4-yl) 5H-benzo [5, 6] Cyclohepta [1, 2b] Pyridene-11(6H)-one from Loratadine


	Journal of Pharmacy and Allied Health Sciences
	Year: 2012 \| Volume: 2 \| Issue: 1 \| Page No.: 1-11 DOI: 10.3923/jpahs.2012.1.11

Isolation, Characterization and Pharmacological Evaluation of 8-chloro-3 (1-methyl-piperidene-4-yl) 5H-benzo [5, 6] Cyclohepta [1, 2b] Pyridene-11(6H)-one from Loratadine

Rashmi Arora, Naresh Singh Gill and Susan Mathew

Abstract: The presence of impurities in the Active Pharmaceutical Ingredient (API) has always raised the curiosity of the synthetic or medicinal chemists. Thus the identification and understanding of these impurities has increased the interest of researchers and regulatory authorities all over the world. The present investigations were carried out on a process related impurity formed during the synthesis of loratadine. The impurity was isolated from an intermediate stage formed at the 9th stage of the synthesis (L-08) by column chromatography and analysed by HPLC, LC-MS, NMR and IR. The isolated compound was found to be a benzoic [5, 6] cyclohepta [1, 2b] pyridine and was identified to be a by product formed during the Grignard reaction involved in the loratadine synthesis. Further the impurity was subjected to anti-inflammatory and locomotor activity test to evaluate its pharmacological properties. The isolated compound showed potent anti-inflammatory activity, 58.6% at 5 mg kg^-1 by Carageenan induced rat paw edema. Further the isolated compound was evaluated for locomotor activity and showed significant loss of locomotor activity at 50 mg kg^-1. The present findings showed that the impurity has significant pharmacological properties and its isolation from the API is a must in order to obtain a pure compound.

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How to cite this article:

Rashmi Arora, Naresh Singh Gill and Susan Mathew, 2012. Isolation, Characterization and Pharmacological Evaluation of 8-chloro-3 (1-methyl-piperidene-4-yl) 5H-benzo [5, 6] Cyclohepta [1, 2b] Pyridene-11(6H)-one from Loratadine. Journal of Pharmacy and Allied Health Sciences, 2: 1-11.

DOI: 10.3923/jpahs.2012.1.11

URL: https://scialert.net/abstract/?doi=jpahs.2012.1.11

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