Preparation of Ophthalmic Solutions: Modern Concepts: I. Atropine Sulphate

Kedvessy, G; Grosz, Stephen; Szepesy, A.

doi:10.1136/bjo.34.4.228

Cited by 2 publications

(2 citation statements)

References 6 publications

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“…Later, a preparation of 0.2 mL 0.5% with edetate-containing BAC solution 0.1% (pH 4.6) and 0.49 g NaCl 0.9% and 10 mL was added to the national formulation collection (NRF 15.34, pH 4.83). A formulation containing boric acid, thiomersal stock solution, and hypromellose was originally chosen by one pharmacy because the preservative was more effective in the pH range [ 26 ].…”

Section: Discussionmentioning

confidence: 99%

“…Dutch colleagues have indicated the ingredients of the drops they prescribe: benzalkonium chloride (BAC) as preservative, sodium edetate, boric acid, and purified water. The stability of atropine depends on the formulation [ 26 ]. Although the bioavailability and intraocular pharmacokinetics of atropine are well characterized [ 27 ], little is known about its precise penetration of the cornea.…”

Section: Introductionmentioning

confidence: 99%

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Corneal Penetration of Low-Dose Atropine Eye Drops

Austermann

Schaeffel

Mathis

et al. 2021

JCM

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Major studies demonstrating the inhibition of myopia in children and juveniles by low-dose atropine eye drops provide little information on the manufacturing process and the exact composition of the atropine dilutions. However, corneal penetration might significantly vary depending on preservatives, such as benzalkonium chloride (BAC), and the atropine concentration. Since there is a trade-off between side effects, stability, and optimal effects of atropine on myopia, it is important to gain better knowledge about intraocular atropine concentrations. We performed an ex vivo study to determine corneal penetration for different formulations. Atropine drops (0.01%) of different formulations were obtained from pharmacies and applied to the cornea of freshly enucleated pig eyes. After 10 min, a sample of aqueous humor was taken and atropine concentrations were determined after liquid–liquid extraction followed by high-performance liquid chromatography–tandem mass spectrometry (LC-MS/MS). The variability that originated from variations in applied drop size exceeded the differences between preserved and preservative-free formulations. The atropine concentration in the anterior chamber measured after 10 min was only 3.8 × 10−8 of its concentration in the applied eye drops, corresponding to 502.4 pM. Obviously, the preservative did not facilitate corneal penetration, at least ex vivo. In the aqueous humor of children’s eyes, similar concentrations, including higher variability, may be expected in the lower therapeutic window of pharmacodynamic action.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Corneal Penetration of Low-Dose Atropine Eye Drops

Austermann

Schaeffel

Mathis

et al. 2021

JCM

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On the Maintenance of Sterility in Eye-Drops

Klein

Millwood

Walther

1954

Journal of Pharmacy and Pharmacology

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Conclusion and Summary A number of substances were tested against Ps. pyocyanea (Ps. œruginosa) and their bactericidal concentration determined. The quaternary ammonium compounds, although bactericidal, are not recommended because of their effect on the cornea. The mercurial compounds:—thiomersalate 0·005 per cent, and phenylmercuric acetate and nitrate 0·005 per cent., are safe, and are recommended for eserine and sodium fluorescein, which are the most liable to pyocyanea contamination, also for methylcellulose eye‐drops, which are liable to contamination by moulds. These compounds are not only powerful bactericides but are also fungicides. Chlorbutol in saturated solution (about 0·8 per cent.) is safe and recommended, but owing to the fact that the solution cannot be heated without detriment to the preservative its use needs great care. Chlorcresol 0·1 per cent, is safe, but in that concentration it causes smarting, and 0·03 per cent, kills pyocyanea within 24 hours. The p‐hydroxybenzoates in 0·1 per cent, solution are reliable for most of the eye‐drops used except fluorescein. Phenylethyl alcohol is safe in 0·5 per cent, concentration but much quicker in its action at 0·6 per cent., and further clinical trials are needed with this promising preservative. For cortisone eye‐drops 0·9 per cent, of benzyl alcohol, the one used in the original solution, is recommended. Eye‐drops used in hospital wards, outpatient departments and factory medical rooms, should be prepared with bactericidal preservatives, but for eye‐drops used by individual patients, a bacteriostatic agent may be permissible. However, for reasons of safety and to make it as foolproof as possible a uniform procedure using a bactericidal preservative is recommended. Up to now the National Formulary has recommended the use of bacteriostatic agents only. In view of the increasing incidence of eye infections reported by different authorities from many parts of the world, more stringent standards seem desirable.

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Preparation of Ophthalmic Solutions: Modern Concepts: I. Atropine Sulphate

Cited by 2 publications

References 6 publications

Corneal Penetration of Low-Dose Atropine Eye Drops

Corneal Penetration of Low-Dose Atropine Eye Drops

On the Maintenance of Sterility in Eye-Drops

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