 |
[email protected] |
 |
3275638434 |
 |
 |
| Paper Publishing WeChat |
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License
Improvement of Oral Efficacy of Erythromycin Ethyl Succinate using Stearic Acid-Myrj-52-based SLM’s
Uduma Eke Osonwa, Stephen Olaribigbe Majekodunmi, Emmanuella OnyechiN and Harrison Thaddeus Gugu
Full-Text PDF
XML 1268 Views
DOI:10.17265/1934-7375/2017.01.006
Solid lipid microparticles of erythromycin ethyl succinate were prepared using solvent evaporation method to improve its bioavailability and efficacy. The solvent was allowed to evaporate after which the various entrapments were determined; the best entrapment was used in the in vivo studies to determine the bioavailability and efficacy. This study was done with albino mice. The best entrapment obtained was 83% with a loading capacity of 2.9% (Batch D) and was used in comparison with the unformulated drug to check for the in vivo efficacy. The results show higher efficacy with the formulated drug than with the pure drug both in vitro and in vivo. The in vitro test results were better despite that some enzymes which need to act on the solid lipid microparticles were not present in the in vitro assay and could lead to a reduction in the release of the drugs. In conclusion, there was improvement in efficacy, and hence bioavailability.
Erythromycin ethyl succinate, solidlipid, microparticles, oral bioavailability, improved activity
[1] Shaji, J., and Joshi, V. 2005. “Self-micro Emulsifying Drug Delivery System for Improving Bioavailability of Hydrophobic Drugs and Its Potential to Give Sustain Release Dosage Form.” Ind. J. Pharm Educ. 9: (3): 45-61.
[2] Kanazawa, M., Shimohata, T., Tanaka, K., et al. 2007. “Clinical Features of Patients with Myasthenia Gravis Associated with Autoimmune Diseases. ” Eur J Neurol. 14 (12):1403-4.
[3] Bittner, B., and Mountfield, R. J. 2002. “Intravenous Administration of Poorly Soluble New Drug Entities in Early Drug Discovery: The Potential Impact of Formulation on Pharmacokinetic Parameters.” Curr. Opin. Drug Discov. Dev. 5: 59-71.
[4] Yu, B. G., Okano, T. K., Kataoka, T. K., and Kwon, G. 1998. “Polymeric Micelles for Drug Delivery: Solubilization and Haemolytic Activity of Amphotericin.” J. Control Release. 53: 131-6.
[5] Meyer, M. C. 1998. “Bioavailability of Drugs and Bioequivalence.” In Encyclopedia of Pharmaceutical Technology, edited by Swarbrick, I. and Boylan, I. C., Vol. 2. New York: Marcel Dekker Inc., 33-58.
[6] Shargil, L., and Yu, B. G. 1999. Applied Biopharmaceuitcs. Vol. 2. Appleton-Century Crofts, Norwalk, C.T., 193-203.
[7] Martin, A. 2003. Physical Pharmacy. 5th Ed. Lippincott Williams and Wilkins, A. Walters Kluwer Co., Philadelphia, 410-8.
[8] Carstensen, J. T. 1998. Pharmaceutical Preformulation. Taylor and Francis Inc., USA., ISBN: 9781566766906, 14-47.
[9] Brahmankar, D. M., and Jaiswal, S. B. 2009 “Text Book of Biopharmaceutics and Pharmacokinetics.” 2nd ed. Vallabh Prakashan, Delhi, India. 349-357.
[10] Rinaki, E., Valsam, I. G., and Macheras, P. 2003 “The Power Law Can Describe the ‘Entire’ Drug Release Curve from HPMC-Based Matrix Tablets: A Hypothesis.” Int. J. Pharm. 255 (1-2): 199-207.
[11] Lindenberng, M., Kopp, S., and Dressman, J. B. 2004. “Classification of Orally Administered Drugs on the World Health Organization Model List of Essential Medicines according to the Biopharmaceutics Classification System.” Eur. J. Pharm. Biopharm. 58 (2): 265-78.
[12] Chaudhary, A., Nagaich, U., Gulati, N., Sharma, V. K., and Khosa, R. L. 2012. “Enhancement of Solubilization and Bioavailability of Poorly Soluble Drugs by Physical and Chemical Modifications: A Recent Review.” Journal of Advanced Pharmacy Education & Research 2 (1): 32-67.
[13] Alfred, M. et al. 1993. Physical Pharmacy. 4th ed. B.I. Publication, Pvt. Ltd., 212-50.
[14] Shargel, L., and Yu, A. B. 1999. Applied Biopharmaceutics & Pharmacokinetics. New York, McGraw-Hill, 4th ed. ISBN 0-8385-0278-4.
[15] Gogate, M. S. 1986. ”Erythromycin Monograph.” In Chemical Stability of Pharmaceuticals: A Handbook for Pharmacists. 2nd ed. (K. A. Connors, G. L. Amidon, V. J. Stella, eds.). New York: John Wiley and Sons, 457-63.
[16] Okore, V. C. 2009. Principles of Pharmaceutical Microbiology “Antibioticassay and Tests”. Ephrata publishers No. 12 Orba road, Nsukka, Enugu state, Nigeria, 197-9.