alexa In vivo Evaluation of Ulcerogenic Activity of Ketorolac, its Solid Dispersion Systems, as Well as its Microcapsules in Rats
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Research & Reviews in Pharmacy and Pharmaceutical Sciences
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Research Article

In vivo Evaluation of Ulcerogenic Activity of Ketorolac, its Solid Dispersion Systems, as Well as its Microcapsules in Rats

Esmat Zien El-Deen1*, El Rashidy MA2*, Mamdouh Ghorab1, Shadeed Gad1 and Heba Yassin1

1Pharm Technology Department, Faculty of Pharmacy, Tanta University, Tanta, Egypt

2Pharmaceutics Department, Faculty of Pharmacy Suez Canal University, Ismailia, Egypt

*Corresponding Author:
Esmat Zien El-Deen
Pharm.Technology Department
Faculty of Pharmacy
Tanta University, Tanta, Egypt
E-mail: [email protected]
El Rashidy MA
Pharmaceutics Department
Faculty of Pharmacy Suez Canal University
Ismailia, Egypt
E-mail: [email protected]

Received: 04-08-2015 Accepted: 08-09-2015



Ketorolac is a potent non-steroidal analgesic drug. It is 36 times more potent than phenyl butazone, and twice as that of indomethacin. The oral administration of ketorolac is associated with high risk of adverse effects such as irritation, ulceration, bleeding of gastrointestinal tract, edema as well as peptic ulceration. These attributes make ketorolac a good candidate for controlled release dosage forms, so as to ensure slow release of the drug in the stomach. The present study reports on the formulation of ketorolac loaded Eudragit RS100, Eudragit RL100 as well as Ethyl cellulose as a controlled release drug delivery system. Solid dispersion and microencapsulation by air suspension method were the techniques of choice in order to coat the drug so as to improve bioavailability and stability and also target a drug at specific sites. The ratio of (1:3) drug to polymer from all polymers used was selected from solid dispersions systems as well as microcapsules to conduct further in vivo evaluation, since it was the best ratio which achieved significant reduction in the release of ketorolac at acidic pH of the stomach and maximal release at alkaline pH of the intestine. The effects of various formulations on ulcer index as well as ulcer incidence were studied. The obtained results indicate that microencapsulation technique was able to protect the stomach from ulcerogenic effect ketorolac compared to solid dispersion technique.


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