Pharmaceutical composition for treating inflammatory diseases and eye cornea injuries

FIELD: medicine.

SUBSTANCE: composition has sulfated glycosaminoglycanes in physiologic saline of sodium salts. Sodium salt of keratan sulfate and sodium salt of chondroitin sulfate are taken as the sulfated glycosaminoglycanes in known ingredients proportion.

EFFECT: enhanced effectiveness of treatment; reduced glycosaminoglycanes consumption.

5 cl

 

The invention relates to medicine, more precisely to pharmacology, and can be used in ophthalmology for the treatment of diseases and injuries of the cornea: erosion and non-penetrating wounds of the cornea, conjunctiva and sclera, penetrating wound of the cornea and sclera, after surgical treatment, the epithelial-endothelina dystrophy of the cornea, burns to the cornea, conjunctiva, sclera, keratitis and keratokonyuktivitah.

Known for eye drops that contain the active substance mixture of glycosaminoglycans in an amount of 0.1 wt.% in physiological solution, isolated from human placenta (RF patent 2216331, MKI7A 61 K 31/726, a 61 K 9/08 A 61 F 9/00, a 61 P 27/00). These glycosaminoglycans are a mixture consisting of hyaluronic acid (46-57%) and heparin with heparansulfate (2-7%). Known eye drops "Vision-1"containing sulfated glycosaminoglycans derived cellulose, buffer salts and water (patent RF 2114587, MKI6A 61 F 9/00, a 61 K 31/715) and serve to protect the cornea from damage during phacoemulsification. Known eye drops "Balaban"containing sulfated glycosaminoglycans, sodium chloride, one - and disubstituted phosphates of sodium and water (patent RF 2128975, MKI 6 A 61 F 9/90).

The disadvantage of eye drops is not sufficiently rapid onset anticad the positive effect. Rapid onset antiexudative effect is extremely necessary in the treatment of traumatic injuries of the eye, in the treatment of inflammatory diseases, the pathogenesis of which swelling plays a role in the trigger mechanism. Removal of edema, in combination with an additional therapeutic measures provides a more rapid onset of therapeutic effect, normalize blood circulation and nutrition of tissues of the eye.

The objective of the invention is the creation of eye drops with a pronounced and rapid onset antiexudative effect and stimulate the recovery of the transparent corneal stroma in injuries and diseases of the eye.

The closest in technical essence to the claimed technical solution are eye drops containing a water-soluble mixture of glycosaminoglycans isolated from the cornea of the eye of cattle, in which glycosaminoglycans taken in an amount of 0.1 to 1.0 wt.%, the rest of saline (RF patent 2062079, MKI6A 61 F 9/06). The disadvantage of these drops is that they do not have sufficient specific actions on reparative processes in the cornea, as in their composition separately there are no specific biological stimulants, and also apparently because they contain a mixture of different glycosaminoglycans, satih ineffective in number, and not dosed offer a combination of sodium salt of keratomalacia, and sodium salt of chondroitin sulfate.

The technical result of the claimed invention is the reduction of treatment time in inflammatory eye diseases and traumatic injuries it due to the clear antiexudative action, and an earlier onset stimulation of reparative and metabolic processes and thus reduce the number of complications. In addition, the present invention allows the use of smaller doses of glycosaminoglycans in comparison with the known technical solution that provides cheaper medicines.

The technical problem is solved by the fact that the eye drops contain the active means of sulfated glycosaminoglycans in physiological solution of sodium salts, as of sulfated glycosaminoglycans contain the sodium salt of keratomalacia, and the sodium salt of chondroitin sulfate, in the following ratio, wt.%: sodium salt of createsurface of 0.002 to 0.2, the sodium salt of chondroitin sulfate 0,006-0,1, saline - rest.

Glycosaminoglycans are a major component of connective tissue. A number of well-studied diseases (hyperglobulinaemia, monopoles haridasa) are associated with increased excretion of various glycosaminoglycans, attached to the peptides. Themselves glycosaminoglycans, except createsurface, built of alternating residues hexuronate acid and 2-amino-2-deoxyhexose, and the last N-azetilirovanny, often O-sulfated, and sometimes N-sulfated. To glycosaminoglycans include hyaluronic acid, chondroitin sulfate, dermatooncology, heparin, Kermanshah, heparansulfate. Kermanshah, unlike other glycosaminoglycans, does not contain residues hexuronate acids. Its molecule consists of repeating disaccharide glycosides of links, including a residue of D-galactose and 2-acetamido-D-glucose-6-sulfate. Known createsurface containing other neutral sugars, such as D-mannose, L-fucose, and sialic acid.

Sulfated glycosaminoglycans stimulate repair processes and normalizes metabolism in the cornea of the human eye, have the ability to reduce inflammatory and exudative reaction.

To the sulfated glycosaminoglycans (sgag) corneal stroma are Kermanshah, chondroitin sulfate, heparansulfate, heparin. Sulfated glycosaminoglycans stimulate carcity corneal stroma damage, normalizes water-salt metabolism and contribute to the restoration of clear corneal stroma, which makes their use in medicinal the media.

We found that sgag taken in different quantities and different ratios, different provide a therapeutic effect. The most rapid removal of pericardial tissue reaction of the eye occurred in the use of the sodium salt of keratomalacia in the amount of 0.002 to 0.2 wt.%, and sodium salt of chondroitin sulfate 0,006-0.1 wt.%. We discovered therapeutic effect was reached when using both small and large doses each of glycosaminoglycans, which indicates, apparently about the presence of a synergistic effect. Dosage createsurface below 0.002 wt.% and chondroitin sulphate below 0,006 provided a sharp decrease antiexudative effect. The use of doses above the upper values createsurface and chondroitin sulfate did not give a noticeable gain antiexudative effect.

This unexpected therapeutic effect can be explained by the fact that the glycosaminoglycans have a different chemical structure and the onset we have indicated therapeutic effect is important not only their quantitative content, but also their synergistic action.

Example 1. Extraction of the crystalline lens in the eye of the rabbit. In the course of surgery the surgical field was repeatedly treated by instillation of a solution of the following composition, wt.%:

sodium salt of createsurface 0,004

the sodium salt of chondroitin sulfate 0,006

sodium chloride 0,85

physiological salt solution of sodium else

Examination of the eye through the day. The cornea is transparent. It takes no. Intraocular pressure was normal.

Example 2. Experimentally produced non-penetrating wound of the cornea of the rabbit. Many times 6-8 times a day, was made instillation of a solution of the following content:

sodium salt of createsurface 0,006

the sodium salt of chondroitin sulfate 0,06

sodium chloride 0,91

physiological salt solution of sodium else

Examination of the eye through the day: eyes calm. It takes no. Partial epithelialization on day 3, epithelialization of the slit on the 6th day. Slight corneal opacity in the area of the wound. Exudate not.

Example 3. Non-penetrating wound of the cornea of the right eye of the rabbit. Six times a day eye installed the solution of the following composition:

sodium salt of createsurface 0,08

the sodium salt of chondroitin sulfate 0,02

sodium chloride 0,95

physiological salt solution of sodium else

Examination of the eye through the day: eyes calm. It takes no. Partial epithelialization on day 3, epithelialization of the incision on the 8th day. Slight corneal opacity in the area of injury. Long-term histological and electron-microscopical is the first study changes in the structure of the corneal stroma is not revealed.

Example 4. Non-penetrating wound of the cornea of the right eye of the rabbit.

Six times a day eye installed the solution of the following composition:

sodium salt of createsurface 0,02

the sodium salt of chondroitin sulfate 0,1

sodium chloride 0,95

physiological salt solution of sodium else

Examination of the eye through the day: eyes calm. It takes no. Partial epithelialization on day 3, epithelialization of the slit on the 6th day. Slight corneal opacity in the area of injury. Histological, electron microscopic study of long-term any pathological changes in the stroma of the cornea is not revealed.

Thus, the proposed solution can prevent the onset of exudative reactions during surgery and to speed the healing process of full restoration of the structure of the cornea.

1. Pharmaceutical composition for the treatment of inflammatory diseases and injuries of the cornea, including sulfated glycosaminoglycans in physiological solution of sodium salts, characterized in that the composition as of sulfated glycosaminoglycans contains the sodium salt of createsurface and the sodium salt of chondroitin sulfate in the following ratio, wt.%:

Sodium salt of createsurface0.002-0.2
The sodium salt of chondroitin sulfate0.006-0.1
Physiological salt solution sodiumRest

2. The pharmaceutical composition according to claim 1, characterized in that as a physiological solution of sodium salts using an aqueous solution 0,85-0,95%sodium chloride.

3. The pharmaceutical composition according to claim 1, characterized in that as a physiological salt solution sodium use isotonic solution of sodium chloride in phosphate buffer with pH 6.8 and 7.6.

4. The pharmaceutical composition according to claim 1, characterized in that as a physiological salt solution sodium use isotonic sodium chloride solution in borate buffer with a pH of 6.8 to 7.6.

5. The pharmaceutical composition according to claim 1, characterized in that as a physiological salt solution sodium use isotonic solution of sodium chloride in acetate-borate buffer with a pH of 6.8 to 7.6.



 

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