Ocular Activity

In the early stages of class 4 involvement, treatment with small doses of prednisone may be initiated when control of the hyperthyroidism or adequate therapy of hypothyroidism has not arrested the ocular activity. Improvement in motility usually occurs within 4 to 12 weeks. Many patients experience enough subsequent improvement in ocular motihty so that severe class... 

SM Sarwai. MA Kassem, MA Aitia, M El-Mahdy. The rormulaiion-perforniancc relationship of multiple emulsions and ocular activity. J Controlled Rel 32 259-268 (1994). 

MA Kassem, SM Safwai, MA Aiiia. M El-Mahdy. Influence of the phase volume ratio of multiple emulsions on the ocular activity of prednisolone. STP Pharma 5 309-315 0 995). 

Vagal effects, salivation/A blood pressure, dry mouth/4- ocular accommodation Vagal effects, salivation adrenergic/A blood pressure/facilitates D1 stim Hyperreactivity/facilitates a-activation... 

An ophthalmic suspension should use the drug in a microfine form usually 95% or more of the particles have a diameter of 10 pm or less. This is to ensure that the particles do not cause irritation of the sensitive ocular tissues and that a uniform dosage is delivered to the eye. Since a suspension is made up of solid particles, it is at least theoretically possible that they may provide a reservoir in the cul-de-sac for slightly prolonged activity. However, it appears that this is not so, since the drug particles are extremely small, and with the rapid tear turnover rate they are washed out of the eye relatively quickly. 

Although usually considered to be inactive ingredients in ophthalmic formulations added because they impart viscosity, many of these polymers function as ocular lubricants. They are marketed as the active ingredients in OTC ocular lubricants used to provide relief from dry eye conditions. The regulatory requirements for these OTC products are found in the FDA Code of Federal Regulations (21CFR349.12), and their formulations are presented in the Twelfth Edition of the APhA Handbook of Nonprescription Drugs. 

The anhydrous petrolatum base may be made more miscible with water through the use of an anhydrous liquid lanolin derivative. Drugs can be incorporated into such a base in aqueous solution if desired. Poly-oxyl 40 stearate and polyethylene glycol 300 are used in an anti-infective ointment to solubilize the active principle in the base so that the ointment can be sterilized by aseptic filtration. The cosmetic-type bases, such as the oil-in-water (o/w) emulsion bases popular in dermatology, should not be used in the eye, nor should liquid emulsions, owing to the ocular irritation produced by the soaps and surfactants used to form the emulsion. 

Morimoto et al. [33] demonstrated that the ocular absorption of hydrophilic compounds over a wide range of molecular weights could be increased by 2 and 10 mM sodium taurocholate and sodium taurodeoxycholate in a dose-dependent manner. The compounds were glutathione (307 Da), 6-carboxyfluorescein (376 Da), FTTC-dextran (4 kDa), and insulin (5.7 kDa). Of the two bile salts, sodium taurodeoxycholate was more effective. At 10 mM, this bile salt increased the permeability of 6-carboxyfluorescein from 0.02% to 11%, glutathione from 0.08% to 6%, FITC-dextran from 0% to 0.07%, and insulin from 0.06% to 3.8%. Sodium taurocholate, on the other hand, increased the permeability to 0.13%, 0.38%, 0.0011%, and 0.14%, respectively. Taurodeoxycholate was more effective than taurocholate in the nasal epithelium as well [202], This difference in activities can possibly be attributed to their micelle-forming capability, which is higher for taurodeoxycholate, a dihydroxy bile salt [190],... 

PM Hughes, AK Mitra. (1993). Effect of acylation on the ocular disposition of acyclovir. II Corneal permeability and anti-HSV 1 activity of 2 -esters in rabbit epithelial keratitis. J Ocular Pharmacol 9 299-309. 

It is well known that 1,10-phenanthrolines are highly active ironchelating agents. The parent compound itself has recently been shown to increase HIF-la levels in ocular tissue and to suppress 02-mediated epithelial cell proliferation when administered to mice [29]. A quantitative assay was developed to measure transcriptional potency of certain HIF stabilizers via an HRE-mediated (3-lactamase production in which the EC50 of 1,10-phenanthroline was measured to be approximately 8 pM. In addition, VEGF was dose-dependently produced in mouse embryonic fibroblasts by 1,10-phenanthroline with an EC50 of... 

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