BIOAVAILABILITY AND OCULAR DISPOSITION OF KETOROLAC TROMETHAMINE FROM VARIOUS OPHTHALMIC PREPARATIONS | ||||
| Bulletin of Pharmaceutical Sciences Assiut University | ||||
| Article 14, Volume 30, Issue 2, December 2007, Page 275-297 PDF (531.46 K) | ||||
| Document Type: Original Article | ||||
| DOI: 10.21608/bfsa.2007.64211 | ||||
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| Authors | ||||
| Hamdy M. Abd El-Aleem1; Farouk M. Sakr1; Osama A. Soliman1; Hatem, El-Awady2; Germeen N. Salama1 | ||||
| 1Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt | ||||
| 2Ophthalmic Center, Faculty of Medicine, Mansoura University, Mansoura 35516, Egypt | ||||
| Abstract | ||||
| Ketorolac tromethamine was formulated in different ophthalmic preparations namely; eye drops, gels, ocuserts and ointments using the following carriers; sodium carboxymethyl cellulose (sod. CMC), polyvinyl alcohol (PVA), hydroxypropylmethyl cellulose (HPMC), absorption base and gelatin. The ophthalmic formulations were prepared containing 0.5% of the drug. All prepared formulae containing the drug were subjected to stability study and release characteristics. Also, the effect of these drug carriers on the uptake and ocular disposition of ketorolac tromethamine by the eye tissues of rabbits (conjunctiva, cornea, iris-ciliary body and aqueous humor) was studied. The obtained results revealed that, the released amounts from the ophthalmic preparations after six hours can be arranged in the following order; Eye drops > ocuserts > gel > ointments. Sod CMC eye drops exhibited the higher rate of release than sod CMC gel, PVA and absorption base ointments. Gelatin ocuserts exhibited the higher rate of release than HPMC ocuserts and carbopol 934 & sod CMC ocuserts. The release rate of the drug from eye drops and PVA ointment obeys first order kinetics, while, other preparations obey Higuchi diffusion model with non-Fickian kinetics. Most formulations (including eye drops) could be stored for 6 months at 25°C, 35°C, 45°C without physical or chemical degradations of the drug. However, PVA and absorption bases showed some changes in the drug content (t90 was 2.84 months for both at 45°C). The decomposition rate of ketorolac tromethamine followed the first-order degradation kinetic. The highest stable formulae are, sod CMC eye drops and gel (t90 values were, 151.9 and 91.18 months, respectively at 45°C). The highest concentration of the drug (Cmax) from all tested formulations is provided in conjunctiva followed by cornea, iris-ciliary body, then aqueous humor. The peak time for maximum drug concentration (Tmax) from sod CMC eye drops was two hours. While, that for sod CMC gel, PVA ointment and gelatin ocuserts was three hours in all tissues after the application of the tested formulations. In addition, the total availability of the drug from the tested formulations was in the following order: gelatin ocuserts > sod CMC gel > PVA ointment > sod. CMC eye drops. | ||||
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