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Aqueous solutions of pyrilamine, cimetidine, and histamine were instilled into the eyes of albino rabbits and drug levels determined as a function of time in the cornea, conjunctiva, aqueous humor, and iris-ciliary body. For all three drugs, less than 1% of the applied dose penetrates to the aqueous humor. Moreover, cimetidine and histamine are significantly less bioavailable than pyrilamine. Both cimetidine and histamine appear to bind to precorneal mucin and thus exhibit binding to conjunctival tissue with subsequent low penetration into the cornea and prolonged peak times in the aqueous humor. In addition, both drugs show binding to the iris-ciliary body as well. The influence of solution pH on the penetration of these compounds was also investigated, and a factor of two increase in aqueous levels was noted for the pH range 5-8, which encompasses the pKa's for these compounds.

Aqueous ragweed pollen extracts (20,000 PNU/ml or 78,000 PNU/ml) lose 50% of their Antigen E content within 5 months of storage at 4 degrees C. Glycerinated extracts and lyophilized ragweed pollen extracts retain their Antigen E content for over 15 months with little or no loss. The preservative phenol in aqueous extracts is destructive to Antigen E probably by protein denaturation. The stability of ragweed extracts as measured by Antigen E content is markedly enhanced with little loss after 15 month storage at 4 degrees C, when the extract is prepared as an alum precipitated suspension.

The topical antifungal agent naftifine has shown considerable potency against a broad spectrum of dermatophytes. In this study, an in vitro penetration test in human cadaver skin and an in vivo tape-stripping test were used to evaluate the penetration and antifungal activity of naftifine gel 1 percent and naftifine cream 1 percent compared with other antifungal agents. In both models, Trichophyton rubrum and T. mentagrophytes were the fungal species. Results show that naftifine gel 1 percent and naftifine cream 1 percent, in vitro and in vivo, penetrate the stratum corneum in concentrations that inhibit the growth of both fungal species. Following penetration in vitro, naftifine gel and cream were significantly more active against T. rubrum than econazole nitrate cream 1 percent. Following penetration in vivo, naftifine gel and cream were as active as econazole nitrate cream 1 percent and clotrimazole cream 1 percent against T. rubrum and T. mentagrophytes.

A simple, relatively fast, coulometric method to determine both the surface-moisture and bound-moisture content of a wide variety of lyophilized, allergenic extracts has been developed. The method has been found suitable for the detection of residual-moisture levels in both lyophilized protein and carbohydrate samples. Isothermal rate-changes in moisture desorption, normalized with respect to sample size and plotted versus time, yield desorption curves which are characteristic of several individual classes of lyophilized materials. The method, when compared to the Official Loss on Drying Procedure for Lyophilized Biologicals, has proven to be faster (1.5 hr.) and more sensitive, with increased specificity and accuracy.