A novel sustained release delivery system of ciprofloxacin for the eye was developed. The system consists of a viscosity enhancer (carbopol gel or hydroxypropylmethylcellulose solution) plus a penetration enhancer (dodecylmaltoside) to overcome penetration barriers and loss due to wash-out and thus achieve the desired ciprofloxacin ocular absorption. The present studies were designed to assess the ocular penetration and bioavailability of ciprofloxacin in sustained release formulations. In vitro studies in rabbits indicated an approximate 10-fold increase in drug penetration through the rabbit cornea using the penetration enhancer, dodecylmaltoside. In vivo bioavailability studies demonstrate that these formulations provided a long drug duration in the cornea. After administration of a single topical dose of ciprofloxacin (0.3%/30 microL), corneal levels greater than the Minimum Inhibitory Concentration (MIC90) (0.5 microg/g) were observed through eight hours. These sustained release formulations delivered 10-fold more drug into the aqueous humor than the standard solution formulation. Maximum ciprofloxacin concentrations in the aqueous humor (0.5-0.7 microg/mL) were attained between one and two hours after dosing. Using these sustained release formulations, ciprofloxacin can penetrate to the anterior chamber of the eye in concentrations that are inhibitory for most gram-negative and gram-positive organisms. These topical ocular formulations have prophylactic utility for prevention of post-surgical infection, offering greater efficacy and safety than currently available treatments.
brate has no significant effect on mouse serum cholesterol under these conditions. Although the mechanism of action of l19 has not been elucidated, it does not appear to have any significant effect on the incorporation of mevalonate into cholesterol.(19) The generic name of 1, formerly designated DH 581, is probucol.
Several features suggest that hydrogels may have potential advantages as an intraocular lens material. The IOGEL lens is a single piece hydrogel composed of 38% poly HEMA. Clinical experience with the IOGEL lens in Australia has been published, and the safety and efficacy of the lens is currently being investigated in a multicenter trial in Europe, the U.S.A., Canada, Australia, and Japan. This is the first large-scale study of a hydrogel implant. The IOGEL lens clinical study was initiated in May 1986 in Europe, in September 1986 in the U.S.A., and in November 1986 in Canada and Australia. The enrollment progress in May 1987 showed that 501 cases had been implanted in Europe, Canada, and Australia and 100 cases in the U.S.A. The visual acuity outcome is equivalent to that reported in the literature. Patients in the multinational trial achieved 20/40 or better in 86% of cases and in 96% of cases excluding unrelated pathologies. Although hydrogels have only had limited use in the clinical situation, the results of this study suggest that the IOGEL lens is a viable alternative to polymethylmethacrylate lens implants.
Parabens are the most frequently used preservative in dermatological medications. Some allergies have been reported to parabens, but these risks must be considered with respect to the benefits of parabens in concentrations used as preservatives in dermatological formulations. Considering the alternatives to parabens in preservatives and placing perspective on the reported allergies we still find parabens to be a useful preservative with minimal risk relative to its benefits.
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