Home | Articles
Published on:June 2021
Indian Journal of Pharmaceutical Education and Research, 2021; 55(2s):s414-s427
Original Article | doi:10.5530/ijper.55.2s.113

Development of Colon Targeting Tablet of a JAK Inhibitor to Combat Chronic Ulcerative Colitis: A Novel Approach for Local Drug Delivery

Authors and affiliation (s):

Vakar1, Rupa Mazumder1,*, Swarupanjali Padhi1, Kirpa Shanker Tiwari2, Parikh Kinjal3

1Department of Pharmaceutics, Noida Institute of Engineering and Technology (Pharmacy Institute), 19 Knowledge Park – II, Institutional Area, Greater Noida, Uttar Pradesh, INDIA.

2Sun Pharmaceutical Industries Limited, Sarhaul, Sector – 18, Gurugram, Haryana, INDIA.

3Faculty of Pharmacy, The Maharaja Sayajirao University of Baroda, Kalabhavan, Vadodara, Gujarat, INDIA.


Background: Tofacitinib, a pan-Janus kinase (JAK) inhibitor, initially used for the treatment of rheumatoid arthritis, was later found to have robust efficacy in Phase 2 and Phase 3 ulcerative colitis clinical trials. It had been approved by FDA for its use in the treatment of moderate to severe ulcerative colitis, in 2018. Objectives: The main objective of the present work was to develop a new colonic drug delivery system for tofacitinib using combined approaches of formulating an extended release matrix tablet along with a pH sensitive polymer coating of Eudragit® S100. Methods: The core tablets of tofacitinib were prepared by wet granulation method containing sodium carboxymethyl cellulose (CMC) as rate controlling polymer. Formulation variables used in the matrix system and pH dependent coating were optimized. Results: Negligible drug release was obtained in 0.1 N HCl and 6.4 pH phosphate buffer media, where as in 7.2 pH phosphate buffer media, the drug release increased up to 94.2±2.0%. Minimum concentration of sodium CMC was 11% (w/w) to ensure6 h’s extended release of drug from the matrix tablet. While, the minimum functional coating percentage, was found to be 13% in order to obtain an adequate lag time. Conclusion: The study showed that, the lag time of the drug release was highly affected by the coating percentage of Eudragit S 100 and product temperature during coating. After the lag time, extended drug release was observed, and rate of drug release was found to be depended on the concentrations of sodium CMC used in the core tablet. The final colon targeted formulation showed no change in either its physical appearance, drug content or in dissolution pattern even after three months of storage at 40±2°C/75±5% RH.

Key words: Colon targeted matrix tablet, Controlled release, Lag period, Ulcerative colitis, Tofacitinib, JAK inhibitor, Immunosuppressant.



Impact Factor

IJPER - An Official Publication of Association of Pharmaceutical Teachers of India is pleased to announce continued growth in the 2019 Release of Journal Citation Reports (source: 2018 Web of Science Data).


Impact Factor® as reported in the 2018 Journal Citation Reports® (Clarivate Analytics, 2019): 0.425

The Official Journal of Association of Pharmaceutical Teachers of India (APTI)
(Registered under Registration of Societies Act XXI of 1860 No. 122 of 1966-1967, Lucknow)

Indian Journal of Pharmaceutical Education and Research (IJPER) [ISSN-0019-5464] is the official journal of Association of Pharmaceutical Teachers of India (APTI) and is being published since 1967.


IJPER uses reference linking service using Digital Object Identifiers (DOI) by Crossref. Articles from the year 2013 are being assigned DOIs for its permanent URLs