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At least 19 recordsLinked to original sources
PubMed1991

The effect of topical administration of indomethacin on symptoms in corneal scars and edema.

We conducted a masked randomized study of 50 patients to evaluate the effect of administration of topical indomethacin 1% suspension on symptoms in corneal scars, edema, infiltrates, and erosions. Patients with symptoms (photophobia, pain, itching, burning sensation, foreign-body sensation, and tearing) were treated with topically administered indomethacin 1% or placebo and monitored for eight weeks. The severity of the complaints was rated and the scores were evaluated (Wilcoxon rank-sum test). Of the 25 patients treated with indomethacin, 21 (84%) had improvement in symptoms and the severity of each of the symptoms was significantly decreased. Of the 25 patients treated with placebo, one (4%) had improvement in symptoms without statistical change of the severity of the symptoms. However, when the placebo-treated patients received indomethacin drops, the symptoms were significantly decreased (P less than .002). This study suggests that topical administration of indomethacin 1% may reduce ocular symptoms in patients with corneal scars, edema, or erosions.

Administration, Topical↗
PubMed1991

The effect of sodium hyaluronate on the migration of rabbit corneal epithelium. II. The effect of topical administration.

The effect of topically administered sodium hyaluronate (Na-HA) on the healing of corneal epithelial defect was investigated using rabbit eyes. The corneal epithelium was removed surgically or with iodine vapor or n-heptanol, and saline was administered to one eye as the control, and 0.1% or 0.25% Na-HA with a molecular weight of 87.3 x 10(4) to the other eye once daily. The area of epithelial defect was measured once daily before a topical administration, and the healing rate of epithelial defect was calculated. When the corneal epithelium was removed with iodine vapor, a topical administration of 0.1% or 0.25% Na-HA did not significantly accelerate the epithelial healing. But when removed surgically or with n-heptanol, the healing rates of the corneas treated with 0.25% Na-HA significantly exceeded those of the control eyes. When the epithelium was removed surgically, treatment with 0.1% Na-HA also significantly accelerated the healing. To determine why the effect of Na-HA differed in these three models with the epithelial defect, the amount of fibronectin (FN) produced by the cornea were investigated. The amount of FN produced was determined from the concentration of FN in the medium obtained after incubation of the corneo-scleral section with corneal epithelial defect, and the amount of Na-HA retained on that cornea was estimated from radioactivity detected in tears and cornea after a topical administration of 14C-labeled Na-HA (14C-Na-HA). The corneo-scleral section whose corneal epithelium had been removed surgically, or with n-heptanol, produced a significantly larger amount of FN than that whose corneal epithelium had been removed with iodine vapor. In addition, the amount of 14C-Na-HA retained on the cornea of the first or second model also significantly exceeded that on the cornea of the third model. The topical administration of Na-HA would thus appear to accelerate the healing of the epithelial defect producing a larger amount of FN or retaining a larger amount of Na-HA.

Administration, Topical↗
PubMed1989

Cyclosporine pharmacokinetics in cats following topical ocular administration.

Topical ocular administration of two forms of cyclosporine were studied in the cat. Both forms were able to produce measurable whole-blood levels capable of suppressing in vitro lymphocyte stimulation. The kinetics of cyclosporine following administration of either oral solution or cyclosporine in olive oil were variable, with peak concentrations ranging from 450 to 1033 ng/ml and 288 to 648 ng/ml, respectively. Absorption lag time ranged from 0 to 1.34 hr for oral solution, and 0.27 to 1.2 hr for cyclosporine in olive oil. The half-life of elimination ranged from 2.41 to 10.04 hr, and 3.09 to 15.75 hr, respectively. When compared with the commercially available oral solution, cyclosporine dissolved in olive oil was better tolerated during administration. Topical ocular administration of cyclosporine in cats offers a possible alternative method of treatment for individuals intolerant of oral administration. Topical ocular administration might also replace the need for intravenous administration of cyclosporine during perioperative periods or during periods of vomiting and nausea associated with rejection or other illnesses. Due to individual variation in absorption and elimination of topically applied cyclosporine, dosages in each cat must be determined by monitoring blood, plasma, or serum levels.

Administration, Topical↗
PubMed1987

Deposition of viprostol (a synthetic PGE2 vasodilator) in the skin following topical administration to laboratory animals.

1. Topical application of 14C-viprostol, a synthetic prostaglandin E2 analogue, to laboratory animals resulted in a significant depot of radioactivity in the skin at the application site in all species studied: mouse, rat, guinea pig, rabbit and monkey, with longer residence times in the larger species. 2. The location of the 14C-label in the skin in mice and monkeys was determined by microscopic autoradiography. Evaluation of the autoradiograms show rapid penetration of the drug into the skin via the hair follicles. 3. In mouse distribution of radioactivity was evident in the stratum corneum and down the hair shafts by 30 min. after dosing. By 2 h radioactivity was also observed throughout the viable epidermis; in the dermis only the hair shafts contained significant radioactivity. At 72 h after dose removal, radioactivity was evident only in the hair follicles and hair shaft. 4. In monkey the residence time of radioactivity in the skin was significantly longer than in mouse, but the general distribution pattern was similar in both species. 5. The presence of viprostol in the hair follicles and epidermal layer after topical administration is consistent with its extensive skin metabolism previously reported.

Administration, Topical↗
PubMedDate not supplied

[Plasma and tissue concentrations of biphenylacetic acid following 1 week oral fenbufen medication and topical administration of Felbinac gel on the knee joint].

In an randomised study 30 patients were treated during one week before undergoing an elective surgery of the knee joint with 1 or 2 g respectively of 3% Felbinac gel (biphenylacetic acid gel) or oral 300 mg Fenbufen thrice daily. Biphenylacetic acid (BPAA) is the therapeutically active metabolite of the non-steroid anti-inflammatory drug Fenbufen. Plasma concentrations were measured before, during therapy and at the time of the operation. During the surgery of the knee joint specimens of synovial fluid and -membrane, of cartilage, muscle and tendons as well as of the skin and the subcutaneous fatty tissue were obtained and the BPAA concentrations measured. There was a large variance of the obtained values in all groups. It seems that mainly methodical problems are responsible for this. At the time of surgery, the plasma concentrations following oral administration were with 10,080 ng/ml 20 to 50 times higher than those after topical administration. The tissue concentrations reached 1/8 to 1/2 of the plasma concentrations. The relation of tissue concentrations to plasma concentrations of BPAA was smaller in patients treated with oral administration than in patients treated with topical administration. Therefore a partial direct penetration of Felbinac into the deeper tissue compartments can be assumed. There was no significant difference in plasma-, synovial- or tissue concentrations between the two groups treated with the topical administration. The tissue concentrations were 1 to 2 orders of magnitude lower than those after oral administration. Only in the skin the concentrations were with 9160 respectively 3830 ng/g higher than those obtained after oral application (2110 ng/g).

Administration, Oral↗
PubMedDate not supplied

Effect of topical administration of antiinflammatory drugs to rats with adjuvant arthritis.

Oral or intramuscular administration of antiinflammatory agents produces numerous undesirable side effects. This work explores the hypothesis that topical administration of such agents directly to the site of inflammation would have beneficial antiinflammatory effects. Topical administration of steroidal and nonsteroidal antiinflammatory drugs to rats with adjuvant arthritis was as effective as oral or intramuscular administration. Peak blood levels of radioactivity following administration of equal doses of hydrocortisone-3H were considerably lower after topical administration than after oral administration.

Administration, Oral↗
PubMed1991

Effects of topical administration of timolol maleate on intraocular pressure and pupil size in dogs.

Effects of topical administration of a single dose of timolol maleate on intraocular pressure (IOP) and pupil diameter were evaluated in normotensive eyes of 11 clinically normal dogs over 12 hours (7:00 AM to 7:00 PM). Mean (+/- SEM) normal IOP was 15.5 (+/- 1.1) mm of Hg and diurnal fluctuation was observed, with the highest IOP seen in the morning. Mean normal pupil diameter was 8.5 (+/- 0.3) mm. Topical treatment with 0.5% timolol resulted in reduction of IOP in the treated and nontreated eyes. Mean reduction of IOP in the treated eye was 2.5 mm of Hg, a reduction of 16.1%, with maximal reduction of 3.7 mm of Hg. Mean reduction of IOP in the nontreated eye was 1.4 mm of Hg, a reduction of 9.0%. The treated eye had reduced pupil diameter at 30 minutes after treatment, which persisted throughout the 12 hours of the study. Mean reduction of pupil diameter in the treated eye was 2.9 mm, a reduction of 34.1%. In addition, a contralateral effect on pupil diameter was seen in the nontreated eye, with mean reduction of 1.2 mm, a reduction of 14.1%. Topical administration of timolol maleate resulted in reduction of IOP and pupil diameter in treated and contralateral eyes, thus supporting the use of timolol for treatment of glaucoma in dogs. Miosis indicates possible beta-adrenergic inhibition or alpha-adrenergic activation of the sphincter muscle. beta-Adrenergic blockade would then result in miosis.

Administration, Topical↗
PubMed1991

Effects of topical administration of timolol maleate on intraocular pressure and pupil size in cats.

Effects of topical administration of a single dose of timolol maleate, a nonselective beta-adrenergic blocking agent, on intraocular pressure (IOP) and pupil diameter were evaluated in the normotensive eyes of 10 clinically normal cats over 12 hours. Mean (+/- SEM) normal IOP was 17.1 (+/- 1.1) mm of Hg and diurnal fluctuation was observed, with the highest IOP seen in the evening. Mean (+/- SEM) normal pupil diameter was 10.1 (+/- 0.5) mm. Topical treatment with 0.5% timolol resulted in reduction of IOP in treated and nontreated eyes. This effect was time-dependent and was first observed at 6 hours after treatment. Mean reduction of IOP was 22.3% in the treated eye and 16.3% in the nontreated eye. The treated eye had reduced pupil diameter at 30 minutes after treatment, and miosis persisted throughout the 12 hours of the study. Mean reduction of pupil diameter was 38.7%. A contralateral effect on pupil diameter was not seen in the nontreated eye. Topical administration of timolol maleate results in a reduction of IOP in treated and contralateral eyes, which supports the use of timolol for treatment of glaucoma in cats. In addition, the treated eye becomes miotic. This effect may indicate beta-adrenergic inhibition or alpha-adrenergic activation of the iris sphincter muscle. beta-Adrenergic blockade would then result in miosis.

Administration, Topical↗
PubMed1991

Reduced severity of oxygen-induced retinopathy in the newborn rat after topical administration of timolol maleate. A preliminary study.

The effects of timolol maleate on intraocular pressure (IOP) and the severity of retinopathy induced by exposure to 80% oxygen were studied in newborn Wistar rats. One drop of timolol maleate (0.25%) instilled in each eye twice a day for the first ten days of life substantially reduced intraocular pressure without significantly modifying arterial pressure. Forty percent of the ratlings treated in this way failed to develop oxygen-induced retinopathy (OIR) after exposure to 80% oxygen for the first five days of life; in the other 60% OIR was less severe than that seen in an identically oxygenated group that did not receive timolol. The authors hypothesize that the pharmacologically induced reduction in IOP may have attenuated the effects of the high concentrations of oxygen on the immature retinal vessels by improving the ocular perfusion pressure. The possibility that timolol maleate also exerts a direct action on the caliber of these vessels cannot be excluded.

Administration, Topical↗
PubMed1988

Effect of topical administration of vancomycin versus chlorhexidine on alpha-hemolytic streptococci in oral cavity.

In a crossover study the effect of local vancomycin (paste containing 0.5% vancomycin applied to the gums three times a day for 7 days) versus chlorhexidine mouth rinsing (0.2% chlorhexidine solution twice a day for 7 days) on alpha-hemolytic streptococci in the oral cavity was investigated in eight volunteers. Mixed saliva and dental plaque samples were collected for microbiologic analysis before administration, during treatment, and after withdrawal of the agents. The numbers of different alpha-hemolytic streptococci were determined in the samples. The total numbers of Streptococcus mitior, Streptococcus mutans, and Streptococcus sanguis were significantly reduced by the vancomycin treatment compared with the chlorhexidine treatment (p less than 0.05) after 2 days of administration. Two days after the treatment was stopped the numbers of alpha-hemolytic streptococci had returned to pretreatment levels. Local prophylaxis with vancomycin as a complement to systemic antimicrobial prophylaxis may therefore be useful in the prevention of infective endocarditis.

Administration, Topical↗
PubMed1989

Determination of the developmental toxicity potential of butoxypropanol in rabbits after topical administration.

The developmental toxicity (embryofetotoxicity or teratogenicity) and maternal toxicity of butoxypropanol, a propylene glycol ether, was evaluated in New Zealand White rabbits. Dosages of 0 (water), 10, 40 or 100 mg/kg/day, selected on the basis of the water solubility of butoxypropanol and the results of a pilot study, were administered percutaneously to groups of artificially inseminated (Day 0) female rabbits on Days 7 through 18 of gestation. The dosage volume was 2 ml/kg. The control group contained 17 does and each test group contained 19 does. Does were observed for signs of test substance effect on abortion or premature delivery, body weight, and feed consumption. On Day 29, they were euthanized and examined for pregnancy, number and placement of implantations, early and late resorptions, and live fetuses. Pregnancy occurred in 15 control does (88%) and in 16 does in each test group (84%). There were no statistically significant differences between test and control groups for maternal body weight gain, feed consumption, number of corpora lutea per ovary, implantations, live fetuses, early and late resorptions, fetal body weights, gender, or gross external changes. There were no visceral or skeletal fetal alterations at any dose tested. No signs of maternal toxicity were observed; however, mild erythema occurred at the site of application at the 100 mg/kg/day dose level. The developmental no-effect level was greater than 100 mg/kg/day.

Administration, Topical↗
PubMed1991

Gas chromatographic-mass spectrometric determination of two new antimycotic agents, 1-[(5-chloro-2-benzofuranyl)(2-chlorophenyl)methyl]-1H-imidazole and 1-[(5-bromo-2-benzofuranyl)phenylmethyl]-1H-imidazole, in rabbit plasma following topical administration: a preliminary comparison with bifonazole.

A method for the analysis of the antimycotic drugs 1-[(5-chloro-2-benzofuranyl)(2-chlorophenyl)methyl]-1H-imidazole, 1-[(5-bromo-2-benzofuranyl)phenylmethyl]-1H-imidazole and bifonazole in rabbit plasma, employing gas chromatography-mass spectrometry with selected-ion monitoring, was developed. The procedure involved single-step purification of the biological matrix via liquid-liquid extraction on Extrelut columns and use of a carrier substance to minimize the negative effects of adsorption sites during the gas chromatographic process. The limits of detection ranged from 0.1 to 1.4 ng/ml, starting from a 200-microliter sample. The method was applied to a preliminary evaluation of percutaneous absorption of both drugs in the rabbit after a single administration, in comparison with bifonazole.

Administration, Topical↗
PubMed1992

Mitomycin concentration in rabbit and human ocular tissues after topical administration.

The authors measured mitomycin C (MMC) concentrations in ocular tissues with high-performance liquid chromatography. Mitomycin C concentration after a single subconjunctival injection of the drug in rabbit eyes showed a rapid decrease with a half-life of 0.18 to 0.30 hours for the conjunctiva and 0.20 to 0.45 hours for the sclera at the injection site. Irrigating the ocular surface with 200 ml of saline after MMC application reduced the initial drug concentration to one fifth in the sclera and to one fifteenth in the conjunctiva but did not change the half-life. The MMC concentration in human trabeculectomy specimens obtained immediately after MMC application (0.2 mg/0.5 ml) and irrigation was 5.4 to 12.0 micrograms/g with a mean of 8.4 micrograms/g, a level similar to that in the rabbit sclera immediately after the irrigation after administration of the same MMC dose. These results indicate that MMC disappears rapidly from the ocular tissues and that irrigating the tissues significantly reduces the tissue concentration of MMC.

Administration, Topical↗
PubMed1989

Otrivine-antistin-pupil, corneal and conjunctival responses to topical administration.

The ocular effects of Otrivine-Antistin eyedrops have been measured in a placebo controlled single-blind study in sixteen healthy volunteers. The drops produced mild sympathomimetic responses in the eye but had no effect on corneal sensitivity or on intraocular pressure. The evidence indicates that use of Otrivine-Antistin imposes no risk to the subject.

Administration, Topical↗