Pharmaceutical composition for anesthesia in ophthalmology

 

(57) Abstract:

The invention relates to medicine, namely to ophthalmology, and can be used for abdominal eye operations for in-vessel anesthesia and pain with non-invasive surgical and diagnostic manipulations on the front segment of the eye. The invention is characterized by the fact that the pharmaceutical composition for anesthesia in ophthalmology, including local anesthetic, according to the invention further comprises viscoelastic and heparin in the following ratio, wt.%: a local anesthetic is 0.01 to 4.0; heparin - 5-500 u/ml; viscoelastic - else, while an additional may include carnosine in concentrations of 0.01 to 2.0%. Viscoelastic contains 0,1-3,0% sodium hyaluronate, and/or 0.1 to 6.0% chondroitin sulphate, and/or 0.1 to 6.0% by foresterie derivative of cellulose in isotonic saline solution at pH 7,0-7,5 or pharmaceutical composition contains as viscoelastic solution with a pH of 7.2 to 7.4 in the following ratio, wt.%: alkyl-and/or carboxylic-, and/or hydroxyalkyl - derived cellulose - 0,21-6,0; sodium chloride - 0,85-0,95; one-deputizing sodium phosphate - 0,0025-0,0040, disubstituted phosphate sodium - importnode operations and expanding Arsenal of medicines, applicable in case of ophthalmic interventions. 3 C.p. f-crystals.

The invention relates to medicine, namely to ophthalmology, and can be used for abdominal eye operations (including extraction (phacoemulsification) cataract with IOL implantation) to the internal chamber of anesthesia and pain with non-invasive surgical and diagnostic manipulations on the front segment of the eye (the removal of stitches, pneumatici, radial keratotomy, lamellar and interlamellar keratoplasty, penetrating deep sclerectomy, etc. and gonioscopy, binocular ophthalmoscopy in patients with severe corneal syndrome).

Known drug, a local anesthetic for cell anesthesia when performing cataract extraction with IOL implantation (Koch P. S. Anterior chamber irrigation with unpreserved 1% lidocaine for anesthesia during cataract surgery. J. Cataract Refractive Syrg 1997; 23, 551-554). During surgery in the anterior chamber of the eye is introduced an aqueous solution of lidocaine 1% without preservative in the amount of 0.25 - 0.5 ml of this pair - and retro-bulbar injection of anesthetic is not performed.

The disadvantage of applying a local anesthetic as proposed is that at certain stages operas, spiracy and irrigation during phacoemulsification and leaching lenticular masses), the anesthetic is washed out of the eye, the patient begins to feel pain. This often requires repeated administration of lidocaine. While there is always the possibility that an aqueous solution of lidocaine can get to the rear segment of the eyeball (especially when the integrity of the anterior hyaloid membrane) and have toxic effects on the optic nerve.

The task of the invention is to achieve effective and long-lasting anesthesia throughout the surgical and diagnostic procedures.

The technical result is to decrease the number of complications during surgical operations and diagnostic procedures, as well as increasing the comfort level and pain management of the patient throughout the surgery or procedure.

The technical result is achieved in that a pharmaceutical composition for anesthesia in ophthalmology, including local anestis, according to the invention further comprises viscoelastic and heparin in the following ratio, wt.%:

A local anesthetic is 0.01 to 4.0

The heparin units/ml - 5 - 500

Viscoelastometer contains carnosine at a concentration of 0.01 to 2,0%.

The pharmaceutical composition may contain as viscoelastic 0,1 - 3,0% sodium hyaluronate, and/or 0.1 - 6.0% chondroitin sulphate, and/or 0.1 - 6.0% of water-soluble derivatives of cellulose in isotonic saline solution with a pH of 7.0 and 7.5.

Another option of the invention is one in which the pharmaceutical composition contains as viscoelastic solution with a pH of 7.2 - 7.4 Vision-1, obtained according to the patent of Russian Federation N 2114587 in the following ratio, wt.%:

Alkyl-and/or carboxylic-, and/or hydroxyalkylated cellulose - 0,21 - 6,0

Sodium chloride - 0,85 - 0,95

One-deputizing sodium phosphate - 0,0025 - 0,0040

Disubstituted phosphate sodium - 0,0115 - 0,0135

Glycosaminoglycans - 0,0051 - 0,080

Purified water - the Rest

The viscoelastics is viscous solutions of various substances: methylcellulose derivatives - Occucoat (Eye of the World, V. 2, N 3, p. 62, 1997), Vision 1 (RF patent N 2114587), sodium hyaluronate - Provisc, Healon (J. Cataract Refract Surg 1998, 24, 1130-1135), chondroitin-sulfate sodium - Viscoat (J. Cataract Refract Surg 1998, 24, 678-683). The main purpose of using viscoelastics is to protect the corneal endothelium from injury during the operation.

An advantage of the claimed pharmaceutical compositions for the treatment of pain in italmatic in the environment occurs gradually, for quite a long time, because the used amount of 0.1 to 1.0 ml is in the anterior chamber of the eye (protecting the corneal endothelium from surgical trauma and enveloping the iris) throughout the operation. This leads to the fact that the anesthetic is much slower washed out of the eye tissues, and therefore with fewer anesthetic provides an effective and long lasting pain relief.

As a local anesthetic can be used lidocaine (xylocain), tetracaine and other drugs from the group of local anesthetics.

The concentration of local anesthetic (in wt.%: 0.01 to 4.0) is due to the fact that the lower concentration has no analgesic action, and higher damages the endothelium of the cornea and has a toxic effect on nerve fibers.

Heparin is proteoglycan, widely used in medicine. Has antiexudative effect, which is especially important when surgical interventions. The concentration of heparin was found experimentally. To this end in the anterior chamber of the eye of rabbits of the Chinchilla breed was introduced the claimed pharmaceutical composition containing different amounts of heparin. Biomicroscopic the minor exudative reaction in the anterior chamber. When the concentration of heparin from 5 to 500 u/ml eye remained calm, the optical medium of the eye is transparent, corneal edema is absent. When the concentration of heparin above 500 IU/ml is observed weakly severe bleeding.

Carnosine - getidentity dipeptide, a natural product of metabolism. Is a natural antioxidant, tread water membrane and the lipid phase of biological membranes, the stabilizer of protein structures. The boundaries of the carnosine concentration was determined experimentally. To this end, the rabbits of the Chinchilla breed was replaced by the moisture of the anterior chamber of the claimed pharmaceutical composition. When the concentration of carnosine from 0.01 to 2.0% biomicroscopic a day after the introduction of corneal edema was absent, the loss of endothelial cells was not more than 4% of the original number. When the concentration of carnosine is less than 0.01%, the loss of endothelial cells was 7%. When the concentration of carnosine more than 2.0% in some cases 15 minutes after injection was observed narrowing of the pupil, that is, undesirable side reactions.

Thus, the proposed pharmaceutical composition for anesthesia in ophthalmology is a comprehensive drug, with prodolzhitelnostyu eyes, and antiexudative effect.

The pharmaceutical composition was prepared as follows. Sodium hyaluronate and/or chondroitin sulphate, and/or water-soluble derivative of cellulose dissolved in isotonic saline solution with a pH of 7.0 and 7.5, centrifuged to remove insoluble fraction decanted. The solution is filtered. As viscoelastic in the pharmaceutical composition can be used Visiton 1. Further according to the invention add heparin and anesthetic. The stirred solution, again filtered under sterile conditions and filled vials or syringes.

In the pharmaceutical composition may further be introduced carnosine. It is added after the introduction of the anesthetic.

When used as viscoelastic solutions of cellulose derivatives, a pharmaceutical composition may be sterilized by autoclaving.

Pharmaceutical composition for anesthesia in ophthalmology "Viscoelastic" is used when performing abdominal eye operations (extraction [phacoemulsification] cataract with IOL implantation, vitrectomy, penetrating keratoplasty and other operations), and injected intraoperatively in the anterior chamber of the eye. P is ebolivia can be used for non-invasive surgical and diagnostic manipulations on the front segment of the eye (the removal of stitches, pneumatici, radial keratotomy, lamellar and interlamellar keratoplasty, penetrating deep sclerectomy, etc. and gonioscopy, binocular ophthalmoscopy in patients with severe corneal syndrome). For this viscoelastic applied to the cornea or instilled into the conjunctival cavity of the eye.

Example 1. Patient S. 74 years old with a diagnosis of left eye: Mature, complicated cataract, open-angle operated glaucoma. During surgery, extracapsular cataract extraction with IOL implantation, the patient produced analgesia proposed pharmaceutical composition. In front of the camera eye was administered pharmaceutical composition in an amount of 1.0 ml in the following ratio, wt.%:

Xylocain - 1,0

Heparin - 500 IU/ml

6,0% Chondroitin-sulfate - Rest

During surgery, the patient pain or pain is not felt. The postoperative period was without complications. Loss of endothelial cells is not privysila 5-6% in the observation period up to 6 months after surgery.

Example 2. A patient 52 years with a diagnosis of left eye: immature complicated cataract, myopia of an average degree of diabetic retinopathy. The General is with IOL implantation, the patient produced analgesia proposed pharmaceutical composition is injected into the anterior chamber of the eye in the amount of 0.5 ml in the following ratio, wt.%:

Xylocain - 1,0

Heparin - 200 u/ml

Carnosine - 2,0

a 3.0% Solution of sodium hyaluronate - Rest

During surgery, the patient pain or pain is not felt. The postoperative period was without complications. Loss of endothelial cells is not privysila 5-6% in the observation period up to 6 months after surgery.

Example 3. Patient N. 22 years old with a diagnosis of left eye: immature innate tadakamalla cataract. Patients performed phacoemulsification (aspiration) cataract with IOL implantation. During the irrigation capsulorhexis and aspiration of cataract with IOL implantation was used proposed pharmaceutical composition with a low viscosity. In front of the camera eye as irrigation fluid was administered pharmaceutical composition in an amount of 150 ml in the following ratio, wt.%:

Xylocain and - 0,01

Heparin - 5 u/ml

Carnosine - 0,01

0,1% Methylhydroxyethylcellulose - Rest

During surgery, the patient pain or disease is 5-6% in the observation period up to 6 months after surgery.

Example 4. Patient R. 35 years with a diagnosis of left eye traumatic retinal detachment, myopia moderate, severe photophobia. Before binocular ophthalmoscopy he was produced analgesia proposed pharmaceutical composition. The patient's cornea was applied pharmaceutical composition in an amount of 0.3 ml in the following ratio, wt.%:

Tetracaine - 4,0

Heparin - 500 IU/ml

0.1% Chondroitin-sulfate - Rest

During the examination the patient significant discomfort from bright light did not feel that helped to make him careful ophthalmoscopy. The cornea was not dried up.

Example 5. Patient, 65 years of age with a diagnosis of right eye narrow-angle compensated glaucoma. Before gonioscopy to the contact surface of gonioscopy and in the conjunctival cavity caused to the proposed pharmaceutical composition for pain relief in the amount of 0.3 ml in the following ratio, wt.%:

Tetracaine - 4,0

Heparin - 500 IU/ml

0.1% Chondroitin-sulfate - Rest

During the examination the patient significant discomfort from bright light and contact with gonioscope did not feel that helped prod">

Example 6. Patient C. for 30 years with a diagnosis of left eye: keratoconus III degree. During surgery, penetrating keratoplasty, the patient produced analgesia proposed pharmaceutical composition. In front of the camera eye was administered pharmaceutical composition in an amount of 1.0 ml in the following ratio, wt.%:

Xylocain - 0,5

Heparin - 200 u/ml

6,0% Hydroxypropylcellulose - Rest

During surgery, the patient pain or pain is not felt. The postoperative period was without complications. In the observation period up to 1 year after surgery, the transplant of the cornea remained clear.

Example 7. Under item 4 of the formula. Patient S. 65 years with a diagnosis of left eye: immature complicated cataract, senile miosis. During surgery, extracapsular cataract extraction with IOL implantation, the patient produced analgesia proposed pharmaceutical composition. In front of the camera eye was administered pharmaceutical composition in an amount of 1 ml in the following ratio, wt.%:

Xylocain - 1,0

Heparin - 500 IU/ml

Carnosine - 2,0

Vision 1 - Rest

Thus Visiton 1 contains the following sotoshi sodium phosphate - 0,0030

Disubstituted phosphate sodium - 0,0144

Glycosaminoglycans - 0,080

Purified water - the Rest

During surgery, the patient pain or pain is not felt. The postoperative period was without complications. Loss of endothelial cells is not privysila 5-6% in the observation period up to 6 months after surgery.

1. Pharmaceutical composition for anesthesia in ophthalmology, including local anesthetic, characterized in that it further comprises viscoelastic and heparin in the following ratio of components:

Local anesthetic, wt.% of 0.01 to 4.0

The heparin units/ml - 5 - 500

Viscoelastic, wt.% - Rest

2. The pharmaceutical composition under item 1, characterized in that it additionally contains carnosine in concentrations of 0.01 to 2.0%.

3. The pharmaceutical composition according to paragraphs.1 and 2, characterized in that as viscoelastic use of 0.1 to 3.0% sodium hyaluronate, and/or 0.1 to 6.0% chondroitin sulphate, and/or 0.1 to 6.0% water-soluble derivatives of cellulose in isotonic saline solution with a pH of 7.2 and 7.5.

4. The pharmaceutical composition according to paragraphs.1 and 2, characterized in that as viscoelastic use a solution with a pH of 7.2 to 7.4, including alkyl-and/or carboxy is hydrated sodium phosphate, glycosaminoglycans, purified water in the following ratio, wt.%:

Alkyl-and/or carboxylic-, and/or hydroxyalkylated cellulose - 0,21 - 6,0

Sodium chloride - 0,85 - 0,95

One-deputizing sodium phosphate - 0,0025 - 0,0040

Disubstituted phosphate sodium - 0,0115 - 0,0135

Glycosaminoglycans - 0,0051 - 0,080

Purified water - the Rest

 

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