Pharmaceutical composition for prolonged anesthesia in ophthalmology "preanesthetic"

 

(57) Abstract:

The invention can be used for abdominal eye operations for prolonged cell anesthesia and pain when removing sutures, non-penetrating deep sclerectomy, diagnostic manipulations on the front segment of the eye and other Composition contains, wt%: local anesthetics short steps of 0.01 to 5.0, local anesthetics long periods of 0.01 to 5.0, isotonic buffer solution with a pH of 6.8 to 7.6 - rest. The composition may further contain heparin, mydriatic, adrenomimetic, carnosine, steroidal and non-steroidal anti-inflammatory agents, Antihemorrhagics and hemostatic agents in specified quantities. The invention allows to achieve effective and prolonged anesthesia for all surgical diagnostic procedures and in the early postoperative period. 9 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) for prolonged cell anesthesia and prolonged analgesia when n is sopexa, 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 R. S. Anterior chamber irrigation with unpreserved 1% lidocaine for anesthesia during cataract surgery. J Cataract Refractive Surg 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 of the operation, when there is a significant passage of irrigation solution through the camera eye (hydrodissection, aspiration 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 re-injection of lidocaine.

The task of the invention is to achieve effective and prolonged analgesia during in the result is a reduction in 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 and in the early postoperative period.

The technical result is achieved in that a pharmaceutical composition for prolonged anesthesia in ophthalmology "Preanesthetic" according to the invention further comprises a buffered isotonic solution with a pH of 6.8 to 7.6, and as a local anesthetic, a mixture of local anesthetics short and long-term actions in the following ratio, wt.%:

local anesthetics short steps of 0.01 to 5.0

local anesthetics long action - 0,0-1-5,0

buffered isotonic solution with a pH of 6.8 to 7.6 - rest

One variant of the invention is one in which pharmaceutical composition "Preanesthetic" additionally contains viscoelastic at a concentration of 50.0 - 99,0%.

One variant of the invention is one in which pharmaceutical composition "Preanesthetic" further comprises heparin at a concentration of 5 to 500 IU/ml

One variant of the invention is one in which pharmaceutical composition "Preanesthetic" further comprises mydriatic concentration 0.005-static" additionally contains adrenomimetic at a concentration of 0.001 - 1,0%.

One variant of the invention is one in which pharmaceutical composition "Preanesthetic" additionally contains carnosine in concentrations of 0.01 to 2.0%.

One variant of the invention is one in which pharmaceutical composition "Preanesthetic" additionally contains steroidal anti-inflammatory agents in a concentration of from 0.1 to 500 mg/ml

One variant of the invention is one in which pharmaceutical composition "Preanesthetic" additionally contains a non-steroidal anti-inflammatory agents in a concentration of 0.001-2%.

One variant of the invention is one in which pharmaceutical composition "Preanesthetic" additionally contains substances that inhibit the production of intraocular fluid in a concentration of 0.001 to 1.0%.

One variant of the invention is one in which pharmaceutical composition "Preanesthetic" additionally contains Antihemorrhagics and hemostatic agents in a concentration of 0.001 to 10.0%.

An advantage of the claimed pharmaceutical compositions for prolonged anesthesia in ophthalmology "Preanesthetic" is that in the anterior chamber of the eye or in the situation on the initial short-acting anesthetic causes rapid pain relief, but easily and quickly washed out of the tissue. Anesthesia local anesthetic long action develops more slowly but for a long time. In addition, anesthetics mixture patentiert the action of each other. Pharmaceutical composition for prolonged anesthesia in ophthalmology "Preanesthetic" contains substances according to variants of the invention to facilitate more effective interaction of anesthetics with tissues.

As local anesthetics short steps can be used lidocaine (xylocain), tetracaine and other drugs from the group of local anesthetics or combinations thereof. As local anesthetics long-term actions can be used bupivacaine (marcain) and other drugs from the group of local anesthetics or combinations thereof.

The concentration of local anesthetics short steps in wt.%: of 0.01 to 5.0 due to the fact that the lower concentration has no analgesic action, and the higher damage of the eye tissue.

The concentration of local anesthetics with prolonged activity in wt.%: of 0.01 to 5.0 due to the fact that the lower concentration has no analgesic action, and more the standard procedure should be a gradual, throughout time manipulation allocation of local anesthetics in the surrounding environment, in the proposed pharmaceutical composition "Preanesthetic" add viscoelastic.

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 surgery. Viscoelastic is viscous and therefore the allocation of the dissolved local anesthetics into the environment occurs gradually over a long enough time, because the used amount of 0.1 to 1.0 ml is in the anterior chamber of the eye and conjunctival cavity throughout the manipulation. This leads to the fact that anesthetics much more slowly washed out of the eye tissues, and therefore with fewer anesthetics results in an effective and long lasting pain relief.

The concentration of viscoelastic from 50,0 - 99,0% is selected depending on whether the viscosity of the solution proposed pharmaceutical composition "the poly is complicated disease, with a high risk of formation of exudate in the proposed pharmaceutical composition "Preanesthetic" add heparin.

Heparin is proteoglycan with antiexudative action. 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 observation twenty-four hours after injection showed that when the concentration of the heparin is less than 5 IU/ml, there is a slight exudative reaction in the anterior chamber. When the concentration of heparin from 5 u/ml 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.

In cases where for a successful surgery (cataract extraction), it is necessary to dilate the pupil, in the proposed pharmaceutical composition "Preanesthetic" add mydriatic.

As mydriatic can be used adrenaline, mezaton, atropine, phenylephrine, cyclopentolate and other drugs from the group of agonists and cholinergic antagonists.

In cases where the surgery is performed on the eye with a high risk of hemorrhagic complications, or when necessary to limit the absorption of the anesthetic into the blood stream in the proposed pharmaceutical composition "Preanesthetic" add adrenomimetic.

Adrenoceptor agonist - group of medicinal drugs that have a stimulating effect on adrenergic receptors. These include epinephrine, norepinephrine, izadrin, effedrin, tyramine, and others Interacting with the eye tissues, they cause contraction of blood vessels, which reduces blood circulation and consequently, to reduce leaching of anesthetics from tissue and lengthening their actions. In addition, the agonists have a good hemostatic effect in the injured vessels.

The concentration of adrenomimetic from 0.001 to 1.0% when the operations of the eyes due to the fact that a lower concentration stimulates the adrenergic receptors and the higher damage of the eye tissue.

In cases when the operation is accompanied by increased tissue damage in the eye, in the proposed pharmaceutical composition "Preanesthetic" add carnosine.

Carnosine - gioi 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% 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.

In cases when the operation is long and covers a large amount of eyes in the proposed pharmaceutical composition "Preanesthetic" add steroidal anti-inflammatory agents.

The concentration of steroidal anti-inflammatories (prednisone, dexasone, dexamethasone, betamethasone, and others) from 0.1 to 500 mg/ml due to the fact that the lower concentration has insufficient anti-inflammatory effect, and the higher damage of the eye tissue.

In cases when the operation is long, traumatic the teroidnyh anti-inflammatory agents.

The concentration of non-steroidal anti-inflammatories (diclofenac, flurbiprofen and others) from 0.001 to 2.0% due to the fact that the lower concentration has insufficient anti-inflammatory effect, and the higher damage of the eye tissue.

In cases where the operation is performed on eyes with a tendency to increase in intraocular pressure (typically glaucoma), in the proposed pharmaceutical composition "Preanesthetic" add substances that suppress the production of intraocular fluid, i.e., decreasing intraocular pressure.

As substances suppressing the production of intraocular fluid, the pharmaceutical composition may contain timolol, betaxolol, Clovelly, apraclonidine etc.

The concentration of a substance suppressing the production of intraocular fluid, of 0.001 to 1.0% due to the fact that the lower concentration has insufficient anti-hypertensive effect, and the higher damage of the eye tissue.

In cases where the operation is performed in eyes with reduced blood clotting and increased risk of bleeding, in the proposed pharmaceutical composition "Preanesthetic" add Antihemorrhagics and hemostatic agents in to the song can contain aminocaproic acid, chloride and calcium gluconate, fibrinogen, thrombin and other

Concentration Antihemorrhagics and hemostatic means of 0.001 to 10.0% due to the fact that the lower concentration has insufficient Antihemorrhagics and hemostatic action, and the higher damage of the eye tissue.

Thus, the proposed pharmaceutical composition for prolonged anesthesia in ophthalmology "Preanesthetic" is a complex drug that has prolonged analgesic effect, protective properties with respect to the corneal endothelium and other internal structures of the eye, as well as anti-inflammatory, antiexudative, hemostatic and anti-hypertensive effect.

Pharmaceutical composition for prolonged anesthesia in ophthalmology "Preanesthetic" can be used for 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. After surgery, she washed the irrigation solution. Pharmaceutical composition for prolonged anesthesia "Palaeogene eyes (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 purpose it is applied to the cornea or instilled into the conjunctival cavity of the eye.

Pharmaceutical composition "Preanesthetic" obtained as follows. The mixture of local anesthetics short and long-term actions are dissolved in isotonic buffer with a pH of 6.8 to 7.6, centrifuged to remove insoluble fraction decanted. The solution is filtered. Further according to the invention in the pharmaceutical composition may further be introduced viscoelastic, heparin, mydriatic, adrenomimetic, carnosine, steroidal or non-steroidal anti-inflammatory drugs, a substance inhibiting the production of intraocular fluid, and the preparation of the group Antihemorrhagics and hemostatic means or any desired combination. Heparin is not used in the same solution with drugs from the group Antihemorrhagics and hemostatic means. The stirred solution, again filtered under sterile conditions and filled vials or syringes.

Examples

Agenda photophobia. Before binocular ophthalmoscopy he was produced analgesia proposed pharmaceutical composition "Preanesthetic". The patient's cornea was applied pharmaceutical composition in an amount of 0.2 ml in the following ratio, wt.%:

tetracaine - 0,5

bupivacaine - 0,75

buffered isotonic solution with a pH of 6.8 to 7.6 - rest

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

EXAMPLE 2: a Patient 45 years with a diagnosis of left eye: immature complicated cataract, myopia of an average degree, robes edge of the pupil, diabetic retinopathy. The overall condition is complicated by insulin-dependent diabetes mellitus. 30 minutes before the operation in the conjunctival cavity of the eye was buried pharmaceutical composition "Preanesthetic" in the amount of 0.1 ml in the following ratio, wt.%:

lidocaine - 2,0

bupivacaine - 0,75

viscoelastic - 60,0

mezaton - 10,0

aminocaproic acid - 10,0

adrenaline - 1,0

diclofenac - 2,0

buffered isotonic solution with a pH of 6.8 to 7.6 - rest

During surgery phacoemulsification cataract have "Preanesthetic" is injected into the anterior chamber of the eye in the amount of 0.5 ml in the following ratio of components, wt.%:

lidocaine - 0,01

bupivacaine - 0,1

viscoelastic - 99,0

mezaton - 0,005

adrenaline - 0,001

carnosine - 2,0

buffered isotonic solution with a pH of 6.8 to 7.6 - rest

By the time of the operation was achieved with good surface anesthesia and mydriasis up to 6 mm During the surgery, the patient pain or pain is not felt. Of newly formed vessels of the iris in the manipulation of the nucleus of the lens appeared bleeding, which quickly stopped. The postoperative period was without the expressed inflammatory reaction, without givemy and other complications. Loss of endothelial cells did not exceed 8% in the observation period up to 12 months after surgery.

EXAMPLE 3: Patient K. 25 years with a diagnosis of right eye: immature innate tadakamalla cataract. 30 minutes before the operation in the conjunctival cavity of the eye was buried pharmaceutical composition "Preanesthetic" in the amount of 0.05 ml in the following ratio, wt.%:

tetracaine - 1,0

bupivacaine - 5,0

viscoelastic - 50,0

mezaton - 8,0

buffered isotonic solution with a pH of 6.8 to 7.6 - rest

Then during surgery in the anterior chamber of the eye was additionally introduced Farmaceutici - 0,1

bupivacaine - 0,1

the heparin units/ml - 5

viscoelastic - 89,0

dexason, mg/ml 0,1

buffered isotonic solution with a pH of 6.8 to 7.6 - rest

By the time of the operation was achieved with good surface anesthesia and mydriasis to 9 mm. During the surgery, the patient pain or pain is not felt. The postoperative period was without severe inflammatory reactions and other complications. Loss of endothelial cells did not exceed 6% in the observation period up to 12 months after surgery.

EXAMPLE 4: a Patient D. 73 years with a diagnosis of right eye: Mature complicated cataract. During surgery, extracapsular cataract extraction with IOL implantation, the patient produced analgesia proposed pharmaceutical composition "Preanesthetic". 30 minutes before the operation in the conjunctival cavity of the eye was buried pharmaceutical composition in an amount of 0.1 ml in the following ratio, wt.%:

lidocaine - 5,0

bupivacaine - 0,75

viscoelastic - 50,0

mezaton - 10,0

buffered isotonic solution with a pH of 6.8 to 7.6 - rest

Then during surgery in the anterior chamber of the eye was additionally administered pharmaceutical composition "R> the heparin units/ml - 500

viscoelastic - 70,0

buffered isotonic solution with a pH of 6.8 to 7.6 - rest

By the time of the operation was achieved with good surface anesthesia and mydriasis up to 8 mm During the surgery, the patient pain or pain is not felt. The postoperative period was without severe inflammatory reactions and other complications. Loss of endothelial cells did not exceed 6% in the observation period up to 12 months after surgery.

Example 5: a Patient N. 67 years old 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 the treatment of pain "Preanesthetic" in the amount of 0.3 ml in the following ratio, wt.%:

tetracaine - 0,5

bupivacaine - 0,75

the heparin units/ml - 500

viscoelastic - 65,0

buffered isotonic solution with a pH of 6.8 to 7.6 - rest

During the examination the patient significant discomfort from bright light and contact with gonioscope did not feel that helped to make him a thorough gonioscopy, and then laser iridectomy. The cornea was not damaged.

EXAMPLE 6, is the patient produced analgesia proposed pharmaceutical composition. In front of the camera eye was administered pharmaceutical composition "Preanesthetic" in the amount of 0.3 ml in the following ratio, wt.%:

lidocaine - 0,1

bupivacaine - 0,1

buffered isotonic solution with a pH of 6.8 to 7.6 - 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: Patient F. 73 years with a diagnosis of right eye: Mature swelling cataract, secondary I ab glaucoma. 30 minutes before the operation in the conjunctival cavity of the eye was buried pharmaceutical composition "Preanesthetic" in the amount of 0.1 ml in the following ratio, wt.%:

lidocaine - 2,0

bupivacaine - 0,75

viscoelastic - 65,0

timolol - 1,0

dexason, mg/ml - 500,0

buffered isotonic solution with a pH of 6.8 to 7.6 - rest

Then during surgery in the anterior chamber of the eye was additionally administered pharmaceutical composition "Preanesthetic" in the amount of 0.5 ml in the following ratio, wt.%:

lidocaine - 0,2
aminocaproic acid - 0,001

buffered isotonic solution with a pH of 6.8 to 7.6 - rest

By the time of the operation was achieved with good surface anesthesia and normal intraocular pressure. During surgery, the patient pain or pain is not felt. The postoperative period was without severe inflammatory reactions and other complications. Loss of endothelial cells did not exceed 12% in the observation period up to 12 months after surgery.

1. Pharmaceutical composition for anesthesia in ophthalmology, including local anesthetic, characterized in that it further comprises a buffered isotonic solution with a pH of 6.8 to 7.6, and as a local anesthetic, a mixture of local anesthetics short and long-term actions in the following ratio, wt.%:

Local anesthetics short steps of 0.01 to 5.0

Local anesthetics long periods of 0.01 to 5.0

Buffered isotonic solution with a pH of 6.8 to 7.6 - Rest

2. The pharmaceutical composition under item 1, characterized in that it further comprises viscoelastic at a concentration of 50.0-99,0%.

3. The pharmaceutical composition according to paragraphs.1 and 2, characterized in that it further comprises heparin in concentric mydriatic at a concentration of 0.005 to 10.0%.

5. The pharmaceutical composition according to paragraphs.1-4, characterized in that it further comprises adrenomimetic at a concentration of 0.001 to 1.0%.

6. The pharmaceutical composition according to paragraphs.1-5, characterized in that it additionally contains carnosine in concentrations of 0.01 to 2.0%.

7. The pharmaceutical composition according to paragraphs.1-6, characterized in that it further comprises a steroidal anti-inflammatory agents in a concentration of from 0.1 to 500 mg/ml

8. The pharmaceutical composition according to paragraphs.1-7, characterized in that it further comprises a non-steroidal anti-inflammatory agents in a concentration of 0.001-2%.

9. The pharmaceutical composition according to paragraphs.1-8, characterized in that it further contains substances that inhibit the production of intraocular fluid in a concentration of 0.001 to 1.0%.

10. The pharmaceutical composition according to paragraphs.1, 2 and 4-9, characterized in that it further comprises Antihemorrhagics and hemostatic agents in a concentration of 0.001 to 10.0%.

 

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