Viscoelastic for protection of intraocular eye tissues

FIELD: medicine.

SUBSTANCE: claimed viscoelastic based on 1.5-2.5 % methylcellulose contains additionally 0.0125-0.025 % dipivephrin hydrochloride solution and 0.0005-0.01 % of benzalconium chloride as stabilizer.

EFFECT: viscoelastic for prevention of eye tissues during intraocular interferences.

2 ex

 

The invention relates to medicine, in particular to ophthalmology, and can be used for intraocular operations to protect the intraocular tissues from surgical trauma and reduce complications.

It is known the use of viscoelastics on the basis of methylcellulose in intraocular surgeries, such as cataract extraction and phacoemulsification to protect the inner tissues of the eye, especially the corneal endothelium (Vaspourakan, Laika, ophthalmic surgery, 1997, No. 1, p.56-61). However, using even the most effective of viscoelastics vizitiu, which includes methyl cellulose, dissolved in saline solution with phosphate buffer, has certain disadvantages. In particular, it is not rare early postoperative period is complicated by increased intraocular pressure resulting from mechanical obstruction of the trabecular network viscoelastic that in some cases contributes to the development of secondary glaucoma in the long term. In addition, the use of viscoelastics of methylcellulose does not significantly reduce the development of postoperative hemorrhagic complications, in particular givemy.

We set ourselves the goal of reducing the number of operative and postoperative complications.

To solve this problem is proposed viscoelastic on the basis of methylcellulose, EXT is niteline contains dipivefrine hydrochloride and as a stabilizer - benzalkonium chloride is in the following ratio of components, %:

methylcellulose1.5 to 2.5
dipivefrine hydrochlorideof 0.0125-0,025
benzalkonium chloride0,0005-0,001
phosphate buffer solution at physiologicalrest

Viscoelastic prepared from methyl cellulose, resulting from the polymerization of modified monomers of glucose, which under stirring dissolved in saline, balanced phosphate buffer.

The proposed viscoelastic prepared as follows.

Take an accurately weighed sample of dipivefrin hydrochloride 0,01875 g and benzalkonium chloride 0.00075 grams, is dissolved in 100 ml of physiological solution containing phosphate buffer (0.05 M solution of potassium phosphate dogsleding and sodium phosphate one-deputizing) and contribute 2.0 g of methylcellulose, which under stirring gradually dissolved over night at room temperature. Finally 1 ml of viscoelastic contains 0.02 g of methylcellulose, dipivefrine hydrochloride 0,1875 mg benzalkonium chloride 0,0075 mg and 1 ml phosphate buffer saline solution. The viscosity of the obtained viscoelastic is 4000 PA/sec, which is determined by viscometric. Ready viscosus is IR filtered through a membrane filter, pour into bottles and sterilized by autoclaving (at 0.5 ATM. and 110°C for 30 min).

The proposed viscoelastic when introduced into the anterior chamber during cataract extraction surgery effectively protects the intraocular tissue (corneal endothelium and other) during surgical manipulations, provides a significant reduction in bleeding complications and postoperative intraocular pressure due to the pharmacological action of adrenaline produced during biotransformation of dipivefrin. In particular, the vasoconstrictor effect of epinephrine reduces the development of given. As a sympathomimetic dipivefrin stimulates alpha and beta receptors of the ciliary processes, reducing production and increasing the outflow of aqueous humor, thereby normalizing the intraocular pressure after cataract extraction, if the latter is complicated by postoperative hypertension. In addition, due to the potentiating action of atropine used pupil dilation during cataract extraction, a more efficient and stable maintaining mydriasis during this surgery. Practically, it is important that the lipophilic properties of dipivefrin hundreds of times higher than that of adrenaline that gives you the ability to apply it in a much smaller con is intratech, than adrenaline, and thereby significantly improve portability and reduce the incidence of side effects.

The proposed viscoelastic in front of the camera 3 rabbits (6 eyes) with cataract extraction in the experiment revealed no irritating or toxic effects with the most careful postoperative biomicroscopy and ophthalmoscopy within two months.

The proposed viscoelastic used by introducing it into the anterior chamber of the eye.

Example 1. Patient M., aged 52, was admitted with a diagnosis of almost complete complicated cataract of the left eye. Data of examination: visual acuity of 0.01 not corrects. Intraocular pressure measured at pneumotonometry, 19 mm Hg Data electroholography: Poto 20.0; - 0,28; F - 1,52; KB - 92. Gonioscopy: the anterior chamber angle is open, pigmentation trabeculae weak. Objective: the appendages of the eye is not changed. The cornea is transparent. Front camera is of medium depth. The pupil is round, lens diffuse cloudy. More deep superficial environment is not ophthalmoscopically.

Under local instillations and retro-bulbar anesthesia, the patient produced cataract extraction with implantation of posterior chamber intraocular lens and cell proposed viscoelastic. Equipment operation: diamond blade is made of puncture of the cornea 13 hours. Through him in front is the Amer introduced a 1% solution mezatona (0.1 ml). After pupil dilation anterior lens capsule opened cystotomy. The corneal incision is continued up to 10 hours. The core of the lens is displayed by sliding. Produced lavage and aspiration of cataract masses. Using a syringe with a curved cannula into the anterior chamber introduced the proposed viscoelastic in the amount of 0.3 ml (containing 2.5% methylcellulose, 0.025% dipivefrin hydrochloride, 0,001% benzalkonium chloride in isoosmotic phosphate buffer). Then in the capsular bag entered posterior chamber IOL. Her alignment is performed using the hook. The anterior capsule of the crystalline lens in the optical zone of the cut. Front camera rinsed with saline. On the corneal incision superimposed continuous seam. Under the conjunctiva put 0.5 ml of 0.4% solution of dexasone and 0.5 ml of gentamicin (20 mg). Complications during and after surgery were observed.

The patient was discharged on the 6th day field operations with a slightly irritated eye, normal pressure (12 mm Hg - pneumotonometry) and visual acuity equal to 1.0. Control patient survey nine months after the operation showed that the visual acuity of the operated eye was kept at the same level - 1.0, intraocular pressure was equal to 17 mm Hg (pneumotonometry), hydrodynamic parameters in the normal range.

Example 2. Patient R., 72 years old, was admitted for an operation with the automotive technician is zoom: Mature cataract of the left eye.

Upon admission to the hospital: eyes calm, transparent cornea, anterior chamber, the average depth, pupil round, his reaction to light is weak. The lens diffuse cloudy. Details of the fundus not ophthalmoscopically.

Acuity of light perception with the correct projection light. The intraocular pressure on pneumotonometry - 19 mm Hg Data electroholography: Pabout- 14,0; - 0,38; F - 1,12; CB - 80. If gonioscopy celebrated open anterior chamber angle with slight pigmentation trabeculae.

Produced cataract extraction with implantation of posterior chamber intraocular lens and the introduction in front of the camera eye of the proposed viscoelastic. After injection of 0.1 ml of 1% mezatona in the anterior chamber through the paracentesis 13 hours and subsequent expansion of the pupil anterior chamber was opened cystotomy. Performed corneal incision from 13 to 10 hours. The core of the lens is displayed by sliding. After washing and aspiration lenticular masses in front of the camera entered the proposed viscoelastic in the amount of 0.2 ml (containing 1.5% methylcellulose, of 0.0125% of dipivefrin hydrochloride, 0,0005% benzalkonium chloride in isoosmotic phosphate buffer) and produced by the implantation of a posterior chamber artificial lens with partial excision of the anterior capsule. Front camera rinsed with saline. The corneal incision is sutured continuous seam is m Upon termination of operations under the conjunctiva of the operated eye put 0.5 ml of gentamicin, and 0.5 ml of 0.4% solution of dexasone. The surgery went without complications. Postoperative complications were also not observed.

On the 7th day after the operation the patient was discharged from hospital. Visual acuity of the operated eye at discharge to 0.9, IOP of 14 mm Hg During the control examination the patient after 6 months visual acuity of 1.0, hydrodynamic performance - without a pathology.

Using the proposed viscoelastic was operated in 8 patients (10 eyes) with age and complicated cataract (basic group). For comparison with known viscoelastic on the basis of methylcellulose - visition has been operated on 12 people (12 eyes) with age and complicated cataract (control group). The compared groups were comparable in age and sex of patients, and the frequency of common comorbidities. It should be noted that all the patients and control group in the pre-operative examination was excluded primary glaucoma. Term follow-up of patients after surgery is 6 to 9 months.

In the main group, where cataract extraction, including with implantation of a posterior chamber intraocular lens was performed using the proposed viscoelastic, during the operation of the complications were not observed is camping. Whereas in the control group in 2 cases (16.7 per cent) was observed hyphema. In one case, the occurrence of givemy was associated with a lack of pupil dilation. Here it is pertinent to note that the width of the pupil in the main group during the operation, an average of 1.2 mm was greater than in the control.

In the early postoperative period in the main group of hemorrhagic complications were observed. In any case, in the early postoperative period was not marked hypertension, and in the late secondary glaucoma. Whereas in the control group in 2 cases (16.7 per cent) in the early postoperative period was observed hyphema, which was eliminated in the assigned resolving treatment. In 3 cases (25,0%) in the early postoperative period was recorded hypertension (32 -50 mm Hg - pneumotonometry), which was cropped local anti-hypertensive therapy and the use of diakarba. In the long term after surgery in 1 patient (8.3 per cent), has developed secondary glaucoma, which required surgical treatment.

Thus, the use of the proposed viscoelastic when cataract extraction, including the use of IOL, contributes to a significant reduction in bleeding complications and hypertension in the early postoperative period and secondary glaucoma in later.

Viscosus the IR to protect the inner tissues of the eye, containing methylcellulose, phosphate buffer, characterized in that it further comprises dipivefrine hydrochloride and benzalkonium chloride in the following ratio, wt.%:

Methylcellulose1.5 to 2.5
Dipivefrine hydrochlorideof 0.0125-0,025
Benzalkonium chloride0,0005-0,001
Saline
containing phosphate bufferrest



 

Same patents:

FIELD: pharmaceutical chemistry.

SUBSTANCE: invention deals with creating pharmaceutical compositions containing bile acids and methods of treatment using these compositions. For this purpose, invention provides transparent aqueous solution containing bile acid or its compounds, polysaccharide, and water. Amounts of the two formers are selected so that they remain in solution at all values within selected pH range. Administration of such a composition increases level of enterohepatic bile acid in body, including blood, and also increases absorption of bile acid. Addition of various drug to composition allows effective treatment of corresponding diseases.

EFFECT: improved transportation to body tissues of bile acids both as individual therapeutic agents and as drug forms.

47 cl, 11 dwg, 16 tbl, 18 ex

FIELD: medicine, ophthalmology, chemico-pharmaceutical industry.

SUBSTANCE: the suggested pharmaceutical composition is indicated for local application and contains an inhibitor angiotensin converting enzyme as an active substance and target additions, moreover, the content of active substance corresponds to about 1-20 mg/ml. The composition suggested could be designed as eye drops, spay, gels, solution for local injections. As target additions one should apply water that contains a buffer agent, an isotonic mixtures, a conservant and a prolongator. Additionally, this composition contains preparations chosen out of the following groups: antibiotics, macro- and microelements, vitamins, adrenoblocking agents. The innovation provides anti-ischemic action, improves reparative processes and accelerates the processes of healing.

EFFECT: higher efficiency.

3 cl, 7 ex

FIELD: veterinary medicine.

SUBSTANCE: composition comprises solution for per os introducible to animals. The solution contains Phenasal and additives. Phenasal is applied as solution of its salt in aprotonic bipolar hydroxyl-containing solvents and bases.

EFFECT: high therapeutic activity; reduced Phenasal consumption; enhanced effectiveness of treatment.

4 cl, 2 tbl

Haemostatic agent // 2275201

FIELD: pharmaceutical industry, in particular haemostatic agent.

SUBSTANCE: claimed agent represents aqueous solution, containing 2-150 g of zinc polyacrylate, 10-100 g sodium alginate and 1-30 of acetic acid in 1 l of distilled water. Agent of present invention being in contact with blood and tissues provides film formation 30 s.

EFFECT: haemostatic agent of improves quality.

FIELD: pharmaceutical industry, in particular agent for treatment of joint diseases in form of injections.

SUBSTANCE: claimed agent contains glucoseamine salt, preservative, non-ionic surfactant, in particular oleic acid and polyoxyethylated sorbitan monoether, and water.

EFFECT: agent for treatment of joint diseases of improved effectiveness combining chondroprotevtive action with high pharmacokinetic properties and biological availability.

3 cl, 3 tbl, 4 ex

FIELD: medicine.

SUBSTANCE: remedy has saccharides like chondroitin sulfate (0.5-20.0% by mass) and salt of glycosamine (1.0-25.0% by mass), preservative (0.1-2.0% by mass), nonionogenic substance like monoester of oleic acid and polyoxyethylized sorbitan (1.0-5.0% by mass), and water (the rest).

EFFECT: increased active substances bioavailability and diffusion rate into articulation zone.

3 cl, 3 tbl

FIELD: medicine, in particular preparation of quick closing insulin preparations for treatment of diabetus mellitus.

SUBSTANCE: claimed method includes preparation of solutions containing insulin and ancillary substances, blending thereof, sterilizing filtration and bottling into flacks. Previously buffer solution containing 2.35-2.45 mg of disubstituted sodium phosphate; 2.25-3.0 mg m-cresol, and 15-17 mg of glycerol as calculated to 100 U of insulin is prepared, then insulin solution is prepared at 3.1-3.3 and added to buffer solution. Solutions are blended at agitation for 10-20 min, pH is adjusted to 7.2-7.4 and water is added up to finish insulin concentration of 100 IU/ml.

EFFECT: human gene engineered insulin of prolonged storage time without losses of physical, chemical and biological properties.

2 ex, 1 tbl

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to therapy of topical suppurative-inflammatory processes. Agent represents an aqueous isoosmotic solution comprising 0.25% of novocaine, 1% of cefazolin sodium salt and 0.77% of sodium chloride. Invention provides the development of optimal conditions for safety mechanical moving of agent in intercellular space under positive hydrodynamic pressure in the permanent state from the injection point in direction to side of deeply localized pathological focus and eliminates the pain component of the inflammatory response.

EFFECT: valuable medicinal properties of agent.

2 ex

FIELD: medicine, transfusion, infusion therapy.

SUBSTANCE: invention proposes antioxidant representing hydroxyethylated starch or pullulan chemically modified with steric-hindranced phenol. Fragment of steric-hindranced phenol represents β-(4-hydroxy-3,5-di-tert.-butylphenyl)-propionyl or β-(4-hydroxy-3,5-di-tert.-butylphenyl)-α-(N-benzoylamino)-acryloyl and its content is from 2 wt.-% up to limit solubility of polymer in water and doesn't exceed 10 wt.-% for modified hydroxyethylated starch and 12 wt.-% for modified pullulan. Plasma substitute showing antioxidant and antiradical activity represents indicated polymeric antioxidant in physiological solution or Ringer-Lock solution in plasma substitute based on the corresponding non-modified polymer. Also, invention describes a method for maintenance the level of arterial pressure and processes of antioxidant protection of body under condition of acute blood loss by using the indicated plasma substitute. As compared with analogs, new plasma substitute shows two kinds of activity: antioxidant and antiradical that are sufficient for operative increase of arterial pressure and its stabilization at the level of physiological norm, and for decreasing amount of free radicals and enhancing antioxidant protection of body in acute massive blood loss.

EFFECT: valuable medicinal properties of agents.

5 cl, 6 tbl, 4 ex

FIELD: organic chemistry, pharmacy.

SUBSTANCE: invention relates to a medicinal agent representing solution of the compound N-[O-(p-pivaloyloxybenzenesulfonylamino)benzoyl]glycine of the formula (I):

in common with at least one regulator of pH value chosen from the group consisting of trisodium phosphate hydrate, sodium hydroxide and potassium hydroxide in the amount providing pH 7.0-9.0. Proposed medicinal agent represents injection formulation and designated for treatment of state with the proposed compound that is an inhibitor of enzyme elastase and improves the disease state. Also, invention relates to the ready medicinal formulation of this agent representing the injection formulation prepared by drying and freezing out. Invention provides acceptable solubility and stability of the compound (I) in solution and as a component of ready injection medicinal formulations.

EFFECT: improved and valuable pharmaceutical properties of medicinal formulation.

15 cl, 6 tbl, 1 dwg, 6 ex

FIELD: pharmaceutical industry.

SUBSTANCE: invention provides pharmaceutical composition useful as anticonvulsive drug to prevent and treat epileptic attacks. Drug is prepared in the form of oxcarbazepine-containing suspension, which, after shake, shows viscosity between 5 and 52 vPa-s. In its preferred embodiment, thixotropic oral suspension contains 5 g/ml oxcarbazepine. In another embodiment, oxcarbazepine suspension includes mixture of carboxymethylcellulose and microcrystalline cellulose in amount between 1.25 and 1.95 g/ml based on total volume of composition. In a still other embodiment, suspension contains oxcarbazepine and less than 0.5 g/ml hydroxyethylcellulose.

EFFECT: avoided lumping during storage period while preserving satisfactory flow characteristics, stability, and good tolerance at oral administration.

13 cl, 3 ex

FIELD: medicine.

SUBSTANCE: the suggested peroral preparation of controlled release contains 2-amino-3-cyano-5-(2-fluorophenyl)-4-methylpyrrole as an active ingredient. T is applied for treating pollakiuria and incontinence of urine. Application of the suggested preparation provides better quality of life in a patient who should follow certain schedule and scheme of therapy without any excessive increase in the level of medicinal preparation in blood plasma due to controlling the rate for preparation's release in vivo and, also, due to decreased frequency in the intake of the suggested medicinal preparation.

EFFECT: higher efficiency of therapy.

16 cl, 4 dwg, 10 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to a pharmaceutical composition made mainly as solid medicinal formulations and comprising therapeutically effective amount of gliclazide and the special additive in the amount 4.65-6.70 mass. p. per mass unit of active substance. The additive comprises hydroxypropylmethylcellulose, microcrystalline cellulose, aerosil and stearate taken in the following ratio of components, mass. p. per 1 m. p. of active substance: hydroxypropylmethylcellulose, 2.50-3.50; microcrystalline cellulose, 2.12-3.00; aerosil, 0.01-0.05, and stearate, 0.02-0.15. Proposed pharmaceutical composition provides the sustained-release of gliclazide and high bioavailability of active substance, a simple method for its preparing as compared with solid medicinal formulation of gliclazide known from the prior art.

EFFECT: improved and valuable properties of composition.

3 cl, 2 tbl, 3 ex

FIELD: medicine, endocrinology, pharmaceutical technology, pharmacy.

SUBSTANCE: invention relates to nateglynide-containing preparation used in treatment of diabetes mellitus that comprises nateglynide as an active component and a carrier wherein nateglynide in amorphous form and indicated carrier represents hydrophilic material. Amorphous property of crystalline nateglynide is provided by the following methods: 1) by dissolving nateglynide crystals in pharmacologically acceptable solvent in common with hydrophilic materials taken among the group consisting of water-soluble polymers, water-swelling polymers, sugar alcohols and salts followed by granulation in fluidized layer, granulation by stirring at high rate, drying by spraying and process for coat applying for granulation of amorphous nateglynide; 2) by mixing nateglynide crystals with hydrophilic materials taken among the group of water-soluble polymers, water-swelling polymers, sugar alcohols and salts and the following application of the high shift force to the prepared mixture; 3) by mixing nateglynide crystals with hydrophilic materials taken among the group of water-soluble polymers, water-swelling polymers, sugar alcohols and salts and the following plasticizing the prepared mixture in melt by heating and milling at cooling; 4) by dissolving nateglynide crystals in pharmacologically acceptable liquid additives wherein liquid additives represent water-soluble polymers that are liquid at 37°C. Using amorphous nateglynide allows preparing the nateglynide preparation with immediate release wherein the dissolving rate of medicinal agents is high and without crystalline transition during preparing or preserving preparations.

EFFECT: valuable pharmaceutical properties of preparation.

6 cl, 3 tbl, 9 dwg

FIELD: medicine, pharmacy.

SUBSTANCE: invention proposes a composition comprising as active components pyridoxine hydrochloride and doxylamine succinate and a disintegrating agent that provide the following dissolving pattern: 20-90% of the total amount of each component among pyridoxine hydrochloride and doxylamine succinate are dissolved in 5-120 min. The composition is made preferably as a tablet with an enterosoluble envelope. The tablet has a core comprising pyridoxine hydrochloride and doxylamine succinate, and inactive excipients also. The composition is used in treatment of nausea, vomiting being especially in pregnancy. The composition provides rapid and simultaneous release of synergetic pair of indicated active components.

EFFECT: improved and valuable properties of composition.

24 cl, 2 dwg, 9 tbl, 3 ex

FIELD: medicine, urology.

SUBSTANCE: the present innovation deals with means for external application. The suggested gel-like preparation contains hydroxyethylcellulose polymer as a gel foundation, lidocaine hydrochloride, an antiseptic component - benzalconium chloride (50%), gentamycin and water. The remedy is nontoxic and easy in application, it demonstrates no unfavorable side irritating action being of high penetrating capacity of active components.

EFFECT: higher efficiency of application.

1 cl, 1 dwg, 7 ex

FIELD: pharmaceutics.

SUBSTANCE: the suggested pharmaceutical composition at delayed release contains fluvastatin or its pharmaceutically acceptable salt hydroxypropylmethylcellulose and nonionic hydrophilic polymer. The latter is being hydroxyethylcellulose at average molecular weight ranged 90000-1300000 or hydroxypropylcellulose at average molecular weight ranged 370000-1500000 or polyethylenoxide at average molecular weight ranged 100000-500000. The suggested pharmaceutical composition is necessary to obtain peroral medicinal remedy for decreasing cholesterol level in plasma, it, also, provides the supply of fluvastatin into the body during prolonged period of time, for example, for more than 6 h and enables to minimize the possibility for premature release or "discharge" of considerable fluvastatin quantities.

EFFECT: higher efficiency.

21 cl, 6 dwg, 5 ex, 5 tbl

FIELD: pharmaceutical industry, medicine.

SUBSTANCE: invention relates to peroral immediate-released drug in solid form, containing low molecular thrombin inhibitor based on peptide with pH-depending solubility. Claimed drug has size particle less than 300 mum and contains combination of microcrystal cellulose and sodium glycolate starch in amount of more than 35 mass % (calculates as preparation mass).

EFFECT: drug with reduced dependence of thrombin inhibitor dissolution from pH and increased releasing rate from tablet.

17 cl, 3 ex, 3 dwg

The invention relates to pharmaceutical compositions comprising a stable water-insoluble complex, consisting of stable amorphous form of the therapeutically active compound dispersed on a molecular level in the water-insoluble ionic polymer

The invention relates to a solid molded dosage form for controlled release of nimesulide for oral administration

FIELD: organic chemistry, pharmacy.

SUBSTANCE: invention relates to a medicinal agent representing solution of the compound N-[O-(p-pivaloyloxybenzenesulfonylamino)benzoyl]glycine of the formula (I):

in common with at least one regulator of pH value chosen from the group consisting of trisodium phosphate hydrate, sodium hydroxide and potassium hydroxide in the amount providing pH 7.0-9.0. Proposed medicinal agent represents injection formulation and designated for treatment of state with the proposed compound that is an inhibitor of enzyme elastase and improves the disease state. Also, invention relates to the ready medicinal formulation of this agent representing the injection formulation prepared by drying and freezing out. Invention provides acceptable solubility and stability of the compound (I) in solution and as a component of ready injection medicinal formulations.

EFFECT: improved and valuable pharmaceutical properties of medicinal formulation.

15 cl, 6 tbl, 1 dwg, 6 ex

Up!