Topical administration solution

An oximine (i.e., a substituted oxime) analogue of alprenoxime was examined in an attempt to overcome the problem of low stability in aqueous solution. To this end, the methoxime analogue of alprenolol (11.74, R = Me) was prepared and evaluated [109]. Stability in solution was greatly improved at neutral pH. Topical administration to rabbits produced a decrease in intraocular pressure that had the same onset and intensity as that produced by alprenolol, but that lasted longer. Alprenolol was, indeed, formed in eye tissues as a metabolite, with the peak concentration reached 30 min after topical administration of the methoxime. 

Application of the liquid to animal skin caused moderate irritation. Chronic topical administration of a 5% solution to mice did not cause skin tumors or any visible skin reaction. In the eyes, glycidol produced severe irritation despite the severity of primary injury, no blindness or permanent defects in the cornea, lens, or iris resulted from the applications. 

In 2-week and 13-week toxicity studies topical administration of MEKP (as a 45% solution in dimethyl phthalate) to both rats and mice resulted in a spectrum of necrotic, inflammatory, and regenerative skin lesions limited to the application site. Lesions considered secondary to the dermal lesions included increased hematopoiesis in the spleen in rats and mice and increased myeloid hyperplasia of the bone marrow in mice. 

Dorzolamide hydrochloride is commercially available as a 2% ophthalmic solution. In man, it is well tolerated, and topical administration into the... 

It is given by oral, rectal or topical administration (50-150 mg/day, maximal daily dose 200 mg) as well as an ophthalmic solution. 

After topical administration of an ophthalmic drug solution, the drug has to cross a succession of anatomical barriers before reaching the systemic circulation. These barriers (as shown in Figure 25.1) can be commonly classified as precorneal and corneal barriers [3]. 

The topical administration of solutions to the eye is often an unpleasant procedure associated with significant burning, stinging, lacrimation, and emotional trepidation. 

Polyoxyl 35 castor oil is mainly used as an emulsifing and solubilizing agent, and is particularly suitable for the production of aqueous liquid preparations containing volatile oils, fat-soluble vitamins, and other hydrophobic substances. Cremophor EL emulsifies or solubilizes the fat-soluble vitamins A, D, E, and K in aqueous solutions for oral and topical administration. In 1 mL of a 25% v/v aqueous polyoxyl 35 castor oil (Cremophor EL) solution it is possible to incorporate approximately 10 mg of vitamin A palmitate approximately 10 mg of vitamin D approximately 120 mg of vitamin E acetate or approximately 120 mg of vitamin Kj. 

Undecylenic acid is one of the better fatty acids for use as a fungicide, although cure rates are low. It can be used in concentrations up to 10% in solutions, ointments, powders, and emulsions for topical administration. The preparation should never be applied to mucous membranes because it is a. severe irritant. Undecylenic acid has been one of the agents traditionally used for athlete s foot (tinea pedis). Cure rates are low. however. 

If a patient with bronchial hyperreactivity requires /3-blocker therapy, one of the selective /3i-blockers (e.g., acehutolol, atenolol, metoprolol, or pindolol) should be used at the lowest possible dose. Celiprolol and betaxolol appear to possess greater cardioselectiv-ity than currently marketed drugs. " Fatal status asthmaticus has occurred with the topical administration of the nonselective timolol maleate ophthalmic solution for the treatment of open-angle glaucoma. Early investigations with ophthalmic hetaxolol suggest that it is well tolerated even in timolol-sensitive asthmatics. - ... 

It is also apparent that little effort is made to optimize the vehicle for topically administered sensitizers (e.g., dermal, oral cavity). For such applications, one is frequently presented to simple aqueous solutions of ethanol or DMSO. Topical preparations thereby offer a challenge to the formulation expert. Application to the oral cavity and larynx would benefit from bioadhesive formulations to increase the contact time between sensitizer and tissue. A well-designed vehicle could allow topical administration of sensitizers to tumors located close to the skin surface and thus offer an alternative to the present systemic administration. 

Bacitracin is mainly used for topical application. A great variety of ointments, solutions, troches and tablets are available for local application. For broadening of the antimicrobial spectrum it is very often combined with other antibiotics such as neomycin, penicillin, tyrothricin and polymixin. Topical administration is used against infections of the skin, eye, ear and throat, with little incidence of sensitization. Good results have been obtained in the prophylactic and active treatment of infected burns - . Inhalation has been reported for susceptible respiratory tract infections. Bacitracin appears to have some antihelminthic activity. ... 

Use In alcoholic solutions for topical administration for chilblains, rheumatism, etc. The desensitizing activity on neurons is utilized in neurobiological research. As e.g. Dolenon , C. is applied in therapy of pain and diabetic polyneuropathy. 

Walters T, Rinehart M, Krebs W, Holdbrook M. Tear concentration and safety of levofloxacin ophthalmic solution 1.5% compared with ofloxacin ophthalmic solution 0.3% after topical administration in healthy adult volunteers. Cornea 2010 29 263-8. 

To prove the relevance of the acute, transient comeal hypoesthesia or even anesthesia found in rabbits after topical administration of Azelastine ophthalmic solutions, testing was additionally performed in Beagle dogs. In contrast to rabbits no indication of any acute or general reduction of the comeal sensitivity was noted in the Beagle dogs. 

Another application of nano-emulsions in the pharmaceutical field is in ocular administration (a topical administration). Nano-emulsions are used as ocular delivery systems to sustain the pharmacological effect of drugs in comparison with their respective aqueous solutions [133]. 

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