Abstract
Poly (l-lactic acid) (PLLA) microspheres loaded with ampicillin sodium (AMP-Na), β-lactam antibiotic, were prepared by a w/o/w multiple emulsion-solvent evaporation method. The amounts of each component in three phases (inner water phase, organic phase, and outer water phase) were carefully examined in the preparation of PLLA microspheres. The stirring rate, another preparation parameter, was also investigated for study on the effect of mechanical stress on the drug loading and morphology of PLLA microspheres. Most of the preparation parameters had a great influence on the drug loading, surface morphology and size distribution of PLLA microspheres. PLLA microspheres with 15.89 w/w% drug loading were subjected to thein vitro release experiment. The release of ampicillin sodium was constant at a rate of 1.68 μg/ml/day per 1 mg of microspheres for 18 days after a 4 days initial burst effect.
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References Cited
Alex, R. and Bodmeier, R., Encapsulation of water soluble drugs by a modified solvent evaporation method. I. Effect of process and formulation variables on drug entrapment.J. Microencapsulation, 7, 3, 347–355 (1990).
Arshady, R., Microspheres and microcapsules, a survey of manufacturing techniques: Part III: Solvent evaporation.Poly Eng. Sci., 30 (15), 915–924 (1990).
Benita, S., Characterization of drug-loaded Poly (d,l-lactide) microspheres.J. Pharm. Sci., 73, 1721–1724 (1984).
Bodmeier, R. and McGinity, J. W., Polylactic acid microspheres containing quinidine base and qunidine sulfate prepared by the solvent evaporation technique. I. Methods and morphology.J. Microencapsulation, 4, 4, 279–288 (1987).
Chemical Abstracts, 74,6412k, Spectrophotometric determination of oxacillin and ampicillin (1971).
Jeffery, H., Davis, S. S., and O’Hagan, D. T., The preparation and characterization of poly(lactide-coglycolide) microparticles I: Oil-in-water emulsion solvent evaporation.Inter. J. Pharm., 77, 169–175 (1991).
Ogawa, Y., Yamamoto, M., Okada, H., Yashiki, T., and Shimamoto, T., A new technique to efficiently entrap leuprolide acetate into microcapsules of polylactic acid or copoly (lactic/glycolic) acid.Chem. Pharm. Bull., 36 (3), 1095–1103 (1988).
Park, K. N., Shalaby, W. S. W., and Park, H. S.,Biodegradable Hydrogels for Drug Delivery. Chapter 6. Chemically-induced degradation. Technomic Publishing Company, Inc., Lancaster, Basel, pp. 141–152 (1993).
Spenlehauer, G., Veillard, M., and Benoit, J. P., Formation and characterization of cisplatin loaded poly (d,l-lactide) microspheres for chemoembolization.J. Pharm. Sci., 75 (8), 750–755 (1986).
Swarbrick, J., Drug and The Pharmaceutical Sciences, Vol. 45, R. Langer and M, Chasin, Biodegradable Polymers as Drug Delivery Systerns, Lewis D H, Chapter 1. Controlled release of bioactive agents from lactide/glycolide polymers. Marcel Dekker, Inc., New York, pp. 1–42 (1990).
Takenaka, H., Kawashima, Y., Chikamatsu, Y., and Ando, Y., Reactivity and stability of microencapsulated placental alkaline phosphatase.Chem. Pharm. Bull., 30 (2), 695–701 (1982).
Wada, R., Hyon, S. H., and Ikada, Y., Lactic acid oligomer microspheres containing hydrophilic drugs.J. Pharm. Sci., 79, 10, 919–924 (1990).
Wang, H. T., Schmitt, E., Flanagan, D. R., and Linhardt, R. J., Influence of formulation methods on thein vitro controlled release of protein from poly (ester) microspheres.J. Controlled Release, 17, 23–32 (1991).
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Kim, J.H., Kwon, I.C., Kim, Y.H. et al. Preparation of biodegradable microspheres containing water-soluble drug, β-lactam antibiotic. Arch. Pharm. Res. 19, 30–35 (1996). https://doi.org/10.1007/BF02976816
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DOI: https://doi.org/10.1007/BF02976816