Increased antitumor activity, intratumor paclitaxel concentrations, and endothelial cell transport of cremophor-free, albumin-bound paclitaxel, ABI-007, compared with cremophor-based paclitaxel.

ABI-007, an albumin-bound, 130-nm particle form of paclitaxel, was developed to avoid Cremophor/ethanol-associated toxicities in Cremophor-based paclitaxel (Taxol) and to exploit albumin receptor-mediated endothelial transport. We studied the antitumor activity, intratumoral paclitaxel accumulation, and endothelial transport for ABI-007 and Cremophor-based paclitaxel. Antitumor activity and mortality were assessed in nude mice bearing human tumor xenografts [lung (H522), breast (MX-1), ovarian (SK-OV-3), prostate (PC-3), and colon (HT29)] treated with ABI-007 or Cremophor-based paclitaxel.

Comparative preclinical and clinical pharmacokinetics of a cremophor-free, nanoparticle albumin-bound paclitaxel (ABI-007) and paclitaxel formulated in Cremophor (Taxol).

Purpose: To compare the preclinical and clinical pharmacokinetic properties of paclitaxel formulated as a Cremophor-free, albumin-bound nanoparticle (ABI-007) and formulated in Cremophor-ethanol (Taxol).

Experimental Design: ABI-007 and Taxol were given i.v.

Molecular mass distribution of sodium alginate by high-performance size-exclusion chromatography.

A sensitive high-performance size-exclusion chromatography (HPSEC) method with simple UV detection was developed for the molecular mass analysis of sodium alginate. It was used to evaluate alginates of varying molecular mass and the results were compared with the viscosity measurements. This HPSEC method was sensitive to serve as the stability indicating method for alginate after storage under different conditions.

Pharmacokinetics and safety of single rising doses of ofloxacin in healthy volunteers.

The pharmacokinetics, safety, and disposition of the new antimicrobial fluoroquinolone ofloxacin were evaluated after oral administration in 14 healthy, male volunteers in a double-blind, placebo-controlled study. Ofloxacin was administered as 100-, 300-, and 600-mg doses separated by 1 week. Plasma and urine concentrations after each administration were measured using a sensitive and specific high-performance liquid chromatographic procedure.

The bioavailability of ofloxacin from several formulations.

The bioavailability of ofloxacin after a single dose of one of two tablet formulations (200 or 400 mg) or a liquid formulation (1.67 mg/ml) was investigated in 24 healthy male volunteers in an open randomized, crossover design study with a 5-day wash-out period between doses. Plasma concentrations of ofloxacin were determined at various times after administration by a sensitive and specific High Pressure Liquid Chromatography (HPLC) method.

Safety of multiple doses of ofloxacin in healthy volunteers.

A safety profile of ofloxacin, a new fluoroquinolone antibiotic, was assessed in twelve healthy male volunteers. Ofloxacin was dosed at 400 mg twice daily over a 10-day course of treatment. This evaluation included chemistry and haematologic profiles, neurologic evaluations, ophthalmologic examinations, audiometric testing, and electrocardiogram before, during and the end of the study.

The effect of food or milk on the absorption kinetics of ofloxacin.

We have studied the effects of food or milk on the absorption of ofloxacin in 21 healthy male volunteers in a three-way crossover design. Milk did not alter the rate or extent of absorption of ofloxacin or its elimination. Food altered the onset and/or rate of absorption, but not the extent of absorption or the elimination rate.

Clinical experience with ofloxacin in sexually transmitted disease.

Experience with ofloxacin in the United States in the treatment of sexually transmitted diseases is reviewed. In one study, a single oral dose of either 400 mg or 600 mg eradicated Neisseria gonorrhoeae in all 43 evaluable patients. In another multicenter study a seven-day course of ofloxacin 300 mg b.