RU2118523C1 - Ophthalmological agent used for glaucoma treatment mainly - Google Patents

Abstract

FIELD: medicine, ophthalmology. SUBSTANCE: invention proposes an ophthalmological agent that has biologically active substance and distilled water. Agent has thymol as a biologically active substance at amount from 0.01 to 1.0 wt. -%. Agent can contain additionally menthol and anesthesin taken at equal ratio to thymol. Agent named as thymenthol is used in the form of eye drops for treatment of elderly patients with chronic glaucoma. Agent has the following composition, wt.-%: thymol 0.25; menthol 0.25, and distilled water - the rest. Agent can be used for treatment of patients with glaucoma and acute and chronic infections of anterior eye chamber and for prophylaxis of progressive myopia. The use of preparation provides stable decrease of intraocular pressure. EFFECT: enhanced effectiveness of an agent. 7 cl, 2 ex

Description

 The invention relates to medicine and pharmacology, in particular to the manufacture of eye drops and their use.

 It is known to use biologically active substances from the group of cholinomimetics, anticholinesterase substances and sympatholytic substances to obtain antihypertensive ophthalmic preparations. (Mashkovsky M. D. Medicines, vol. 2.-M .: Medicine, 1977, p. 449-450). However, ophthalmic preparations based on these substances do not have universality.

 The closest analogue of the claimed funds are eye drops containing pilocarpine (See USSR author's certificate N 1803101, A 61 K 9/08, 1993).

Drops contain components in the following ratio, wt.%:
Pilocarpine Hydrochloride - 10.0
Catamine AB (preservative) - 10.0 ml
Sodium chloride - 8.0
Purified water - Up to 1000 ml
Drops are prepared by dissolving pilocarpine hydrochloride in water, adding an isotonizing agent and a preservative, followed by sterilization of the solution.

 The use of the described analogue, like other cholinomimetics, worsens accommodation and reduces visual acuity. The drug is not universal and requires the appointment in combination with other compensating drugs.

 The creation of a new drug solves the problem of obtaining an ophthalmic agent with a wide spectrum of action, which provides a hypotensive effect in combination with other types of therapeutic effects in the treatment of eye diseases. Since the most pronounced therapeutic effect (technical result of the invention) from the use of the new drug is a persistent decrease in intraocular pressure, its primary purpose is the treatment of glaucoma.

 The name "TYMENTOL" is selected for the new drug. (The abbreviated name of its variants is “MTN” and “MTA”).

 In a wide range of therapeutic effects of timenthol, three directions can be distinguished.

 1. The first and preferred direction is the treatment of different types of glaucoma. The main manifestation of the action of timentol when instilled into the conjunctival sac is the directly hypotensive effect.

 Strong hypotensive activity of timentol manifests itself in primary wide-angle glaucoma and in glaucoma with a closed and narrow chamber angle. The drug can also be used for acute glaucoma. Timentol causes moderate myosis, facilitates the outflow of aqueous humor, and steadily reduces intraocular pressure. Unlike cholinomimetics (pilocarpine, etc.), timentol does not impair accommodation, increases visual acuity and the ability to see in poor lighting.

 2. The second direction in the spectrum of action of timentol is the treatment of acute and chronic infections of the anterior chamber of the eye in the presence of the so-called low-virulent flora. Timentol is effective in keratitis, adenoviral and allergic conjunctivitis and similar diseases, contributing to the active regeneration of affected tissues.

 3. The third direction of use of timentol is the treatment of progressive myopia, myotic choreitis, opacification of the vitreous body, degenerative eye lesions and traumatic retinal detachment.

 Essentially, the preparation of timentol is a solution in distilled water of thymol in an amount of 0.0001-0.001 g / l, which corresponds to its concentration of 0.01-1.0 wt.%. In this range, the concentration of thymol in solution of 0.1-0.5 wt.% Is more optimal. It is preferable to use drops with a thymol content of 0.25 wt.%.

 To increase the hypotensive efficacy of the drug, menthol is additionally introduced into it in an amount of 0.01-1.0 wt.%. This version of the drug is called "Timentol-M". (MTN).

In a preferred embodiment, timentol-M contains components in the following ratio, wt.%:
Thymol - 0.1-0.5
Menthol - 0.1-0.5
Distilled Water - Else
In this case, thymol and menthol are introduced in a ratio of 1: 1.

The optimal ratio of components for timentol-M is the following, wt.%:
Thymol - 0.25
Menthol - 0.25
Distilled Water - Else
The shelf life of the preparations of timentol and timentol-M is up to a year under normal conditions at room temperature.

 To further increase the effectiveness of the drug in acute eye lesions, anesthetics are additionally introduced into the composition. This version of the drug is called "Timentol-A".

Timentol-A contains components in the following ratio, wt.%:
Thymol - 0.1-1.0
Menthol - 0.1-1.0
Anestezin - 0.1-1.0
Distilled Water - Else
The ratio of the amount of thymol, menthol and anesthesin in the solution is 1: 1: 1. It is preferable to use the drug timentol-A at a content of 0.5 wt. % thymol, 0.5 wt.% menthol and 0.5 wt.% anestezin. Shelf life of timentol-A is up to 6 months under normal conditions.

 A method of obtaining the preparation of timentol and its variants described above involves dissolving in distilled water the starting components of thymol and menthol, produced by the industry in the form of powders. When dissolving, heating, the use of solvents and other operations that can change the nature or biological activity of thymol and menthol are not allowed. The low solubility of these components does not prevent the preparation of dilute solutions with the claimed low concentration of thymol and menthol in the usual way.

 The invention can be illustrated by the following examples.

Example 1. The preparations of timentol and timentol-M were used in the form of eye drops for three times a day during the treatment of chronic forms of glaucoma in patients of an older age group. A group of 40 people was examined, to whom the drug was prescribed in the form of eye drops of the following composition, wt.%:
Thymol - 0.25
Menthol - 0.25
Distilled Water - Else
An adverse reaction was not detected in any patient. The intraocular pressure was measured 5 minutes after instillation, 20 minutes, 24 hours and 1 week after instillation. A decrease in intraocular pressure was noted in 25 patients with open-angle glaucoma and in 14 patients with glaucoma in aphaktic eyes. When studying the effect of the drugs timentol and timentol-M, a complete absence of toxic reactions, allergic and other adverse reactions was noted.

Example 2. The drug timentol-A was used in the treatment of a patient with traumatic brain injury and hypertonicity in the left eye. Eye drops of the following composition were used, wt.%:
Thymol - 0.5
Menthol - 0.5
Anestezin - 0.5
Distilled Water - Else
Twice instillation of the drug. A sharp decrease in intraocular pressure was noted 12 minutes after instillation into the conjunctival sac.

 According to the results of clinical trials, a positive effect was revealed from the use of timentol preparations and its variants in the treatment and re-examination of most patients.

Claims (3)

1. Ophthalmic agent, mainly for the treatment of glaucoma, containing a biologically active substance and distilled water, characterized in that it contains thymol as a biologically active substance in the following ratio of components, wt.%:
Thymol - 0.01 - 1.0
Distilled Water - Else
2. The tool according to claim 1, characterized in that it contains components in the following ratio, wt.%:
Thymol - 0.1 - 0.5
Distilled Water - Else
3. The tool according to claim 1, characterized in that it contains components in the following ratio, wt.%:
Thymol - 0.25
Distilled Water - Else
4. The tool according to p. 1, characterized in that it additionally contains menthol in the following ratio of components, wt.%:
Thymol - 0.01 - 1.0
Menthol - 0.01 - 1.0
Distilled Water - Else
moreover, the ratio of thymol and menthol is 1: 1. 5. The tool according to claim 4, characterized in that it contains components in the following ratio, wt.%:
Thymol - 0.1 - 0.5
Menthol - 0.1 - 0.5
Distilled Water - Else
with a ratio of thymol and menthol 1: 1. 6. The tool according to claim 4, characterized in that it contains components in the following ratio, wt.%:
Thymol - 0.25
Menthol - 0.25
Distilled Water - Else
7. The tool according to p. 1, characterized in that it further comprises anestezin and menthol in the following ratio of components, wt.%:
Thymol - 0.1 - 1.0
Menthol - 0.1 - 1.0
Anestezin - 0.1 - 1.0
Distilled Water - Else
moreover, the ratio of thymol, menthol and anestezin is 1: 1: 1.