Ophthalmic solution, application

The USP has numerous requirements, e.g., ophthalmic solutions [need be] essentially free from foreign particles, suitably compounded and packaged for instillation into the eye, or ophthalmic suspensions [need contain] solid particles dispersed in liquid vehicle intended for application to the eye [1]. Ophthalmic suspensions are required to be made with the insoluble drug in a micronized form to prevent irritation or scratching of the cornea. A finished ophthalmic ointment must be free from large particles and must meet the requirements for leakage and for metal particles under ophthalmic ointments . These and other requirements will be discussed further in subsequent sections. 

C. Parenteral or ophthalmic solutions Solutions used for injection (parenteral) or application to the eye (ophthalmic). Excipients include ... 

A 34-year-old woman with primary open-angle glaucoma began topical application of travoprost ophthalmic solution (0.004%, 1 drop/day) and 30 minutes later developed abdominal cramp that lasted for 2 hours. The same symptoms appeared on 3 days after drug administration. The pain disappeared after travoprost withdrawal. 

Sodium borate is used in pharmaceutical applications similarly to boric acid (see Boric Acid). It has been used externally as a mild astringent and as an emulsifying agent in creams. It has also been used in lozenges, mouthwashes, otic preparations (0.3% w/v), and ophthalmic solutions (0.03-1.0% w/v). Sodium borate has additionally been investigated in the prevention of crystal formation in freeze-dried solutions. Preparations of sodium borate in honey have historically been used as paints for the throat, tongue, and mouth, but such use is now inadvisable because of concerns about toxicity in such applications, see Section 14. Sodium borate is also used in cosmetics such as moisturizers, deodorants, and shampoos. 

All povidone types have applications in ophthalmic solutions [83-86,102, 267, 354]. Povidone K 17, povidone K 25 and povidone K 30 are usually used in eye drops while the higher-molecular type, povidone K 90, is preferred for contact lens solutions [87,88,203,382]. It is usually added to these dosage forms in concentrations between 2% and 10% and performs the functions shown in Table 101. 

Takada, H., Mori, H., Yamazaki, R, Goto, S., and Niwa, C. (1998) Photostability testing of various ophthalmic solutions and its application for medication instructions, Byoin Yakugaku, 24, 601-610. 

While ophthalmic solutions are by far the most preferred dosage forms, ophthalmic ointments are still being marketed for night time applications and where prolonged therapeutic actions are required. 

Dionex Corporation (2008) Dionex Application Note No. 194 Determination of Carbachol in Ophthalmic Solutions Using Reagent-Free Ion Chromatography System. Dionex Corporation (now part of Thermo Fisher Scientific), Sunnyvale,... 

It is concluded from these results that one year application of 0.3%OFLX ophthalmic solution to dogs causes neither ocular toxicity nor systemic adverse effect. 

In the present study, we examined ocular toxicity of ofloxacin ophthalmic solution (3 times daily for one year application) in beagle dogs with pigmented eyes. In order to investigate the effects of melanin-bound ofloxacin on retinal function and the effect of ofloxacin on central nerve system, electroretinogram (ERG) was recorded and behavior of dogs was observed during test periods. 

Azelastine ophthalmic solutions were tested in 3 albino rabbits (White Himalayan) each per concentration. The concentrations used were 0.01%, 0.05%, 0.1%, and 0.5%. A single application of one drop into the conjunctival sac of one eye per animal was given. 

The contralateral eye remained untreated as control. Measurements of the corneal sensitivity were performed before treatment as well as 1,5, 10,15, 20,25, 30,40, 50, 60,70, and 80 minutes after the treatment. Additionally Azelastine ophthalmic solutions with concentrations of 0.05% or 0.1% were tested after single application in pigmented Fauve de Bourgogne rabbits. 

According to the results of the experimental studies and to the findings of Harris et al. the acute, transient reduction of the comeal sensitivity only in rabbits was considered not to be prohibitive for the further development of Azelastine ophthalmic solutions. Clinical phase I studies were performed, where special consideration was given to the measurement of the comeal sensitivity. As in rabbits also in man the positive reference test dmg proxymetacaine hydrochloride was able to induce a distinct and measurable local anesthesia with a fast onset of action and a duration of approximately 15-30 minutes. Azelastine ophthalmic solutions at concentrations of 0.05% and/or 0.1%, however, did not produce any changes of the comeal sensitivity after both single or repeated applications. Concerning these results it must especially be noted, that in human volunteers the more sensitive pa-... 

Although this chapter is directed toward ophthalmic products, it is largely applicable to parenteral and even nonsterile products (solutions, emulsions, and suspensions). The choice of preservative is limited to only a few chemicals that have been found, over the years, to be safe and effective for this purpose. These are benzalkonium chloride, thimerosal, methyl- and propylparaben, phenylethanol, chlorhexidine,... 

In the eye, hypertonic solutions may cause drawing of water towards the site of application whereas hypotonic solutions may cause water to move from the topical application site through the tissues of the eye. When instilled into the eye, isotonic solutions cause no contraction or swelling of the tissues with which they come in contact, and cause no discomfort. Therefore, it is very important to adjust the isotonicity of topical ophthalmic products. Isotonic adjustments are also important for nasal and aural preparations, parenteral products, and irrigating solutions. In a given product, all the... 

Topical anesthesia of nose and throat, abolish laryngeal and esophageal reflexes prior to diagnostic procedure Topical Direct application of a 0.25% or 0.5% topical solution or by oral inhalation of a nebulized 0.5% solution. Total dose should not exceed 20 mg. Mild pain, burning and/or pruritus associated with herpes labialis (cold sores or fever blisters) Topical Apply to the affected area no more than 3-4 times a day. Ophthalmic anesthesia Topical 1-2 drops of a 0.5% solution. 

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