Combined ophthalmic preparation presented in form of eye drops and containing polyhexamethylene guanidine and taurine

FIELD: medicine.

SUBSTANCE: preparation comprises branched polyhexamethylene guanidine in the form of hydrochloride, taurine, a promoting ingredient, additives and water. The promoting ingredient is specified in succinic acid or its pharmaceutically acceptable salt, while the additives are specified in a group consisting of physiologically acceptable alkaline or acidic agents and a salt tonic agent specified in physiologically acceptable sodium or potassium salts or mixtures thereof.

EFFECT: more effective therapeutic effectiveness for pathological conditions of the eyes, and a potential comorbid bacterial infection.

3 cl, 3 tbl, 4 ex

 

The technical field to which the invention relates.

The invention relates to pharmacology and ophthalmology. More specifically, it provides the drug in the form of eye drops for the treatment of pathological conditions of the eye, such as ocular hypertension and cataracts, as well as acting as a reparative remedy for the injuries of the cornea, especially complicated by bacterial infections. The drug in accordance with the invention may find application as an additional tool in preparing patients for surgery by cataract and anti-complications of bacterial origin in the postoperative period.

The level of technology

In its broadest sense, the term "cataract" determine any change in optical homogeneity or decrease the transparency of the eye lens. In the etiology of cataract involved many factors, such as heredity, aging, diabetes, Smoking, nutrition, the cumulative effect of x-ray and UV radiation and the endocrine and/or enzymatic equilibrium in the body.

These factors negatively affect the processes and electrolyte metabolism, which, in particular, leads to disruption of cellular osmoregulation and adversely alters the permeability of cell membranes of the cornea and retina. In the publication Cops is s, Century, Vislobokova I.I., manav VV // Biology. - 1989. - Ser. So 3. No. 1. Pp.62-66, it was shown that taurine normalizes and electrolyte metabolism. Also in the literature there is evidence of normalization of protein, carbohydrate and hormone metabolism in the introduction taurine. These factors contributed to the introduction of taurine in ophthalmic practice from the second half of the 1970-ies.

Ocular hypertension is not a disease as such, but is a pathological condition of elevated intraocular pressure, which normally is within 10-21 mm Hg Persistent or recurrent ocular hypertension can cause not only the development of glaucoma, but also lead to other injuries of the eye, leading to vision loss, such as occlusion of the retinal vein and nglaucomatous the destruction layer of the optic nerve fibers [D.S. Minckler "Histology of optic nerve damage in ocular hypertension and early glaucoma". Surv. Ophthalmol. Vol.33 (April 1989). P.401-411].

There is information about what instillation solutions taurine positively affect gematologicheskii barrier and significantly reduce intraocular pressure (IOP). In article Bunin YA, Yartseva H., Kolesnikova Y.A., Yermakova VN, Yakovlev A.A., Berdnikovoy T.A., Komleva N.A. "the Effect of taurine on intraocular pressure and the blood-ophthalmic barrier (experimental study)" [GP is. the oft. No. 1 (1978). S-24] on the model of prostaglandin hypertension in rabbits have shown that instillation of 4% solution of taurine delay time increased IOP and statistically reduces 2-5 mm Hg IOP experienced eyes during the whole experiment. Similar results were obtained in models of salt hypertension in the eyes of rhesus monkeys. Thus, taurine has a hypotensive effect on the intraocular pressure, which may be due to inhibition of secretion of aqueous humor.

Mechanical injury of the cornea, especially those produced in the absence of proper medical care (e.g., natural disasters, military actions, expeditions and other), usually accompanied by bacterial infections that can have irreversible effects on the eye until his loss.

Preparing the patient for ophthalmic surgery, particularly cataract, requires eradication of bacterial infections that can cause postoperative complications, especially in the case of older paniotov or patients with diabetes mellitus (S. Suto, M. Morinaga, T. Yagi, S. Tsuji, Toshida H. "Conjunctival sac bacterial flora isolated prior to cataract surgery. Infect. Drug Resist. No.5 (2012). P.37-41). In the first place should be maximally reduced the degree of contamination of the typical agents of conjunctivitis and blepharitis. Therefore, there is a need is to be in ophthalmic preparations with a wide profile of antibacterial activity, with hypotensive and reparative action.

The prior art various ophthalmic preparations containing taurine. In the application OR (publ. 11.06.1997) revealed eye drops to accelerate the regeneration of the cornea after injury, containing 0.5 to 3.0% taurine, sodium chloride, potassium chloride and sodium bicarbonate having a pH of from 5.5 to 8.0 and the osmotic pressure of from 250 to 450 mOsm.

The disadvantage of these drugs taurine is their susceptibility to colonization by pathogens during storage of the opened packaging, which makes the application of inefficient and unsafe.

In the patent RU 2127099 (publ. 10.03.1999) revealed eye drops containing (in wt.%):

sodium succinate shestibalny1,91
sodium citrate 5.5-water0,40
sorbitol0,80
sodium chloride0,31
L-glutamic acid,0,015
Riboflavin is mononucleotides0,02
benzalkonium chloride0,014
glucose0,30
taurine0,4
distilled water for injectionrest

The use of drops can improve energy metabolism in the cells of the anterior and posterior epithelium of the cornea, and keratoplastic under any process that violates this exchange.

In the patent RU 2404768 (publ. 10.03.1999) revealed eye drops for the prevention and treatment of cataract, containing:

taurine1,5-1,9 g
carnosine1,5-1,9 g
glutathionenot less than 0.01 g
the low molecular weight dextran
microdispersionsthe 10.5-15.0 g
benzalkonium chloride0,005-0,02 g
purified waterto 100 ml

In the patent RU 2295331 (publ. 20.03.2007) disclosed reparative eye drops and antiglaucoma action, containing:

taurine4 g
cyanocobalamin0.025 g
dextran5.0 g
benzalkonium chloride0.01 g
purified waterto 100 ml

The use of benzalkonium chloride as a preservative and helps to reduce the degree of contamination of microbial products after the introduction of the open packaging, but the preservatives of this type have a strong local irritant and allergen that is their fault. There is therefore a need for new effective and safe drugs for the treatment of cataract.

Disclosure of inventions

As a result of extensive studies, the authors of the present invention have found that the disadvantages of the known prior art can be overcome by creating a combined ophthalmic drug in the form of eye drops containing polyhexamethylene guanidine and taurine and additionally comprising sodium succinate.

Thus, the present invention is aimed at expanding Arsenal of medicines, provides ophthalmic drug in the form of droplets containing a combination of act the main components, the promoting component, auxiliary substances and water, in which the combination of active components composed of branched, guanidine of the formula (I)

n1n2and n3equal 1-3, a z is equal to 0.15-1,10 molecular weight distribution MW/Mnfrom 5.4 to 9.3 when the mass-average molecular mass MWin the range of from about 3800 to 6300 and srednetsenovoj molecular mass Mnin the range of from about 600 to 1100, present in the form of hydrochloride, and taurine;

the promoting component selected from succinic acid or its pharmaceutically acceptable salts, with the following content of components (in wt.%):

hydrochloride, guanidine0,03-0,5
taurine1,0-5,0
the promoting component0,5-2,0

excipients selected from the group consisting of physiologically portable alkaline or acid agents present in amounts required to maintain the pH of the preparation is in the range of from 6.0 to 7.8, and salt tonic agent selected from physiologically-tolerated salts of sodium or potassium is their mixtures, present in an amount to provide toychest drug comparable to onicescu natural tear fluid of a healthy person.

Preferably in ophthalmic drug is physiologically tolerable acid agent is hydrochloric acid present in the amount required to ensure the pH of the drug 6,0±0,1.

Also preferably in ophthalmic drug is physiologically tolerable alkali agent is a mixture of potassium dihydrophosphate and megahydrological sodium present in amounts required to maintain the pH of the preparation is in the range from 7.2 to 7.7.

One of the main technical results of the present invention is to accelerate the recovery of the corneal tissue at injury, complicated by attached bacterial infection. Another technical result is to improve the flow of cataract. Another technical result is the ability to reduce drug load allergenic antibiotics in the preparation of the patient for ophthalmic surgery, for example, on cataract.

A comparative study of drug action "Taufon, eye drops 4%, and the drug in accordance with the invention in a model of traumatic cataract in rabbits revealed the advantage of pre the proposed drug in comparison with the known, expressed in a smaller area and intensity of turbidity damaged portion of the lens. In the research process was found not to have any side effects, as well as signs of intolerance and allergic steps of the proposed drug.

Thus, the authors confirm the achievement of the claimed technical result of the invention.

The implementation of the invention

Hereinafter the invention will be illustrated by examples of its implementation.

Example 1. Preparation of eye drops, not containing buffer mixture

Under aseptic conditions in suspension a sterile container load pyrogen-free distilled water, taken in the amount of 80-85% of the volume of the finished product. Under stirring in water dissolve 0.05 g of polyhexamethylene guanidine hydrochloride (phmg-GC), and 1.00 g of taurine, from 2.00 g of sodium succinate and 0.70 g of sodium chloride, after which the pH of the solution is brought to a value of 6.0±0,1 addition of 0.1 M hydrochloric acid. The mass of the mixture is brought up to 100.00 g of the addition of pyrogen-free distilled water.

Sterilization of the solution is carried out at 120°C for 10-12 minutes, after which the finished drug portions 5 ml Packed in sterile vials from high-pressure polyethylene with a dropper, supplied screw-on lids and placed in the box with the indication information is then, necessary for the identification and application.

Example 2. Preparation of eye drops with a buffer mixture

Under aseptic conditions in suspension a sterile container load pyrogen-free distilled water, taken in the amount of 85-90% of the volume of the finished product, which is heated to 60°C. With stirring in hot water dissolving 0.03 g of potassium dihydrophosphate, 0.27 g of monohydrogenphosphate sodium and 0.50 g of sodium succinate. The resulting solution was cooled to 25°C and bring in it when mixing 0.50 g pgmg-GC, 5,00 g of taurine and 0.1 g of sodium chloride. The mixture is stirred until complete dissolution of the components.

Spend sterilizing filtration through a filter with shut-off capacity of 0.2 μm, portions of 2 ml aseptically Packed in vials of high-pressure polyethylene with a dropper, supplied screw caps and placed in boxes with the information necessary for the identification and application.

Example 3. The study of therapeutic action on the model of traumatic cataract in rabbits

The study was conducted on 24 rabbits breed "White giant" average weight of 4.75 kg by the age of 4-5 months with a model of traumatic cataract, divided into groups of 6 animals (n in table 2).

After medical Misa called twice instillation in the conjunctival cavity 1%solution of pilocarpine Hydra is chloride with an interval of 15 minutes, produce laser coagulation of the pigment portion of the pupil localization coagulates 1,5-2,0 mm outwards from the optical center of the lens in the Meridian 8-10 h, causing a traumatic cataract. The iris of each eye put 15-40 coagulates. The parameters of laser radiation pulse energy of 1.6 to 2.2 W, pulse duration of 0.6 seconds.

In accordance with the objectives of the study all animals are divided into 4 groups (table 1).

Table 1
GroupThe drug and dosage
1The preparation in accordance with example 1; 1 mg/kg rabbit 1 time per day subkonyunktivalno for 10 days
2The preparation in accordance with example 2; 1 mg/kg rabbit 1 time per day subkonyunktivalno for 10 days
3"Taurine, eye drops 4%", 1 mg/kg rabbit 1 time per day subkonyunktivalno for 10 days
4Water for injection of 0.3 ml rabbit 1 time per day subkonyunktivalno for 10 days

In the first week biomicroscopy of the eye lens and the study of its p is srcnode spend every day, and further - weekly in transmitted light using a slit lamp SL-2B and head binocular microscope (NBO-2) using the Ophthalmoscope lenses of different optical power.

In addition, all rabbits immediately after cataract simulation, as well as after 1 and 2 months of therapy compared drugs are photography nature of cataract using the apparatus "Retcam-2" (production of Massive Research, USA). The results of dynamic monitoring of rabbits entered in a special registration card.

After 30 minutes of laser treatment of pigmented border of the pupil in the ground causing the laser coagulates acquires a milky white color. On the second day of the experiment, the pupil acquires former size and exposes the Department of the lens subjected to laser radiation. It is an area of intensive clouding of the capsule and anterior cortical lens layers in a u shape (projection pigmented rims constricted pupil at the time of laser irradiation). This thin plot of turbidity, follow the contour of the edge of the pupil, surrounded by a halo subcapsular vacuoles and sites growing dimness, not extending more than 1.5 mm from the basic "outline" of the dimness.

Starting from the third or fourth day pomot is of the considered sections of the lens reaches the maximum intensity, depth and area and stabilized. The trend to reverse (very minor) traumatic cataract development gains since the 30th day of the experiment. However, even after 60 days of treatment of the studied drugs in any case not showed complete regression of cataract.

Size of the lens opacity is determined using a micrometer grid imposed on the full-sized image of the lens performed using apparatus "Retcam-2", by the formula

S=N+n/2,

where S is the area of opacity mm2; N is the number of millimeter squares, fully "employed" turbidity, n is the number of millimeter squares, partially "employed" by the dimness.

The severity of lens opacity assessed on a four point scale: 0 for full transparency of the lens; "1" - a gentle blackvideo turbidity; "2" - pronounced turbidity, which still guess weakened the fundus of the eye reflex; "3" - intense dense cataract in the absence in his projection of the fundus of the eye reflex. Due to the fact that cataract heterogeneous, calculate the average coefficient of turbidity by multiplying the intensity of the turbidity in each plot on its area, followed by summing and dividing by the total area of the dimness.

The results of the dynamic observation of the clouding of the second lens in rabbits in groups, shown in table 1, are presented in table 2.

Table 2
GroupnThe monitoring phase
30 days60 day
Size, mm2SeveritySize, mm2Severity
164,8±0,62,3±0,34,1±0,62,1±0,3
264,1±0,52,0±0,43,7±0,51,9±0,2
366,1±0,62,9±0,25,2±0,62,3±0,3
466,4±0,73,1±0,36,1±0,527±0,3

The drug in accordance with examples 1 and 2 of the invention according to a survey on the 30th day of the experiment were statistically significantly more effective than drug "Taufon, eye drops 4%". In the control group 4 size, depth and intensity of turbidity remained more stable than in animals treated with therapy.

According to the results of further observations of rabbits, conducted in the period from 30 to 60-day experiment, installed more noticeable stabilization and deceleration of the development of opacities in the lens (area, depth and intensity of turbidity), especially in group 2, treated with drug therapy in accordance with examples 1 and 2 of the invention.

Example 4. The definition of the spectrum bactericidal efficacy in vitro and minimum bacteriostatic (overwhelming growth) concentration (MBC)

Spectrum bactericidal efficacy in the experience of in vitro characterized by suspension polymerization in accordance with the guidance of P 4.2.2643-10 "laboratory Methods of research and testing of disinfectants to assess their effectiveness and safety. Explore 0.05% solution of hydrochloride, guanidine of the formula (I) (G-pgmg) and preparations prepared in accordance with examples 1 and 2 of the invention.

Minimum bacteriostatic (IPC) concentration determination is Aut micromethods serial twofold dilutions in medium Mueller-Hinton (Oxoid) in accordance with the normative document "guidelines for determining the sensitivity of microorganisms to antibiotics" (MUK 4.2 1890-04).

Preparations with a concentration of active ingredient 1000 μg/ml, prepared in pyrogen-free distilled water, diluted to 128 µg/ml of culture medium. Studies performed in 96-well tablets for immunological studies. Prepare a series of twofold dilutions of study drug in the environment II Mueller-Hinton (Oxoid) in a volume of 50 μl. For microorganisms, poorly growing on ordinary nutrient media, in the above medium was added 5% defibrinating sheep blood.

The inoculate bacterial cultures from isolated colonies are prepared in the form of a suspension according to the standard turbidity of Mcfarland (0,5) in physiological solution. The suspension is diluted in the environment II Mueller-Hinton concentrations up to 108CFU/ml of the Prepared suspension contribute to the wells of plates (50 μl/well) and prepare a dilution in the concentration range from 128 to 0,0003 mg/ml Inoculated tablets incubated for 18 hours at 37°C. the Lowest concentration of the study drug, at which no visible growth of microorganisms, is an estimate of the IPC.

To determine the IPC Candida albicans isolated from colonies of preparing a suspension in a nutrient medium Saburo standard turbidity of Mcfarland (0,5), which corresponds to 106CFU/ml for fungal cultures. A series of twofold dilutions of the drugs are prepared in an environment Saburo in on what JaME 100 ml. After inoculation of yeast tablets incubated for 48 hours at 30°C.

The results of the action at the IPC series serial twofold dilutions are presented in table 3.

Table 3
The microorganism (Strain)Mr. pgmgMedication
Example 1Example 2
Eschenchia coli (ATSS 27952)248
Proteus mirabilis (5)114
Staphylococcus aureus (ATCC 29213, sensitive to methicillin)248
Staphylococcus aureus (ATSS 43300 methicillin-resistant)244
Candida albicans (ATSS 24433)4816
Streptococcus oralis (1105007)1 24
Streptococcus pyogenes (151023)288

The data obtained indicate that the proposed drug has a higher activity compared with the solution pgmg-GC.

1. Ophthalmic drug in the form of droplets containing a combination of active components, the promoting component, auxiliary substances and water, wherein the combination of active components composed of branched, guanidine of the formula (I)

n1n2and n3equal 1-3, a z is equal to 0.15-1,10 molecular weight distribution MW/Mnfrom 5.4 to 9.3 when the mass-average molecular mass MWin the range of from about 3800 to 6300 and srednetsenovoj molecular mass Mnin the range of from about 600 to 1100, present in the form of hydrochloride, and taurine;
the promoting component selected from succinic acid or its pharmaceutically acceptable salts, with the following content of components (in wt.%):

hydrochloride, guanidine0,03-0,5
taurine1,0-5,0
the promoting component0,5-2,0

excipients selected from the group consisting of physiologically portable alkaline or acid agents present in amounts required to maintain the pH of the preparation is in the range of from 6.0 to 7.8, and salt tonic agent selected from physiologically-tolerated salts of sodium or potassium and mixtures thereof, present in an amount to provide toychest drug comparable to onicescu natural tear fluid of a healthy person.

2. Ophthalmic preparation according to claim 1, characterized in that the physiologically tolerable acid agent is hydrochloric acid present in the amount required to ensure the pH of the drug 6,0±0,1.

3. Ophthalmic preparation according to claim 1, characterized in that the physiologically tolerable alkali agent is a mixture of potassium dihydrophosphate and megahydrological sodium present in amounts required to maintain the pH of the preparation is in the range from 7.2 to 7.7.



 

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8 cl, 13 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, particularly dermatology, namely to a film coating solution for the removal of pathological nail keratoderma, containing: 10 to 20% of urea, 8 to 12% of the film coating polymer Eudragit E100, 45 to 50% of ethanol, 1 to 5% of propylene glycol, 0.5 to 1% of diethylphthalate, and water up to 100%.

EFFECT: invention provides preparing a transparent film coating high-urea solution.

5 cl, 4 ex

FIELD: medicine.

SUBSTANCE: group of inventions refers to medicine, and concerns a dosage form of insulin containing insulin, a dissolving agent, and a zinc chelator, wherein the dosage form has a pH value varying within the range more than pH 7 and pH 7.6, represents a transparent aqueous solution; it also concerns an injection dosage form of insulin; a method of treating a diabetic patient involving the injection of the above dosage form into the patient.

EFFECT: group of inventions provides higher accumulation and transport through the epithelial cells as compared to insulin in a combination of HCl and zinc chelator above.

27 cl, 11 ex, 13 dwg

FIELD: medicine.

SUBSTANCE: group concerns a prolonged delivery of a compstatin analogue, as well as an optional additional active agent when released from a microscopic gel-like inclusion formed if a liquid composition containing the compstatin analogue is introduced into an extravascular space, such as a vitreous chamber of eye in a mammalian body. The invention also refers to a method of treating an individual suffering age-related macular degeneration (ARMD).

EFFECT: improving the compstatin delivery system for the complement system inhibition required for treating ARMD.

58 cl, 4 ex, 6 tbl, 5 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmacology, pharmaceutics and medicine, more specifically to a new generation of high-stable dosage forms prepared with using the process of sublimation in a specific mode with a composition containing no stabilising agents reducing the width of therapeutic action of finished dosage form substantially. The invention concerns the pharmaceutical composition for injections and infusions containing 3-oxy- and methylpyridine derivatives and pharmaceutically acceptable salts thereof as an active ingredient, sodium chloride or potassium chloride as an additive agent, in the form a lyophilisate. The process involves the sublimation followed by the vacuum dewatering for at least 64 hours.

EFFECT: pharmaceutical composition possesses high stability for the whole shelf-life as opposed to all known pharmaceutical formulations of these compounds; it preserves pharmacological activity and enables dissolving the composition immediately before use and reducing a risk of the negative effect of the thermal sterilisation of aqueous solutions.

2 cl, 7 ex, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to medicine. A pharmaceutical formulation for the treating diseases associated with endothelial dysfunction contains an active ingredient presented by a methyl pyridine derivative - 1.0-6.0 wt %; purine - 10.0-80.0 wt % and additive agents - the rest. The active substance is presented by compounds of a group: 3 -(N,N-dimethyl carbamoyloxy)-2-ethyl-6-methylpyridinium succinate, 3-methylpyridinium succinate, 2-ethyl-6-methyl-3-hydroxypyridinium hydrochloride, 6-trichloromethyl-2-chloropyridine (nitrapyrin), 2-ethyl-6-methyl-3-hydroxypyridine succinate. Purine is presented by inosine, adenosine, hypoxanthine. The pharmaceutical formulation may be presented in the form of injections, lyophilisate, solid capsules, tablets and suppositories.

EFFECT: formulation according to the invention provides creating the stable drug dosage form which considerably exceeds the existing analogues in pharmacodynamics activity on the endothelial dysfunction and toxicological properties.

4 cl, 4 tbl, 9 ex

FIELD: chemistry.

SUBSTANCE: invention relates to biochemistry, particularly a method for specific collection of DNA molecules (DNA aptamers) with high affinity for a recombinant protein target. Said method involves synthesis of a single polypeptide chain of a recombinant protein containing a fragment of glutathione S-transferase, a protein target, a peptide sequence split by the B. Anthracis lethal factor, a peptide which is biotinylated in vitro under the action of an E.coli biotin-ligase enzyme, binding the obtained recombinant polypeptide with an oligonucleotide library and immobilising the protein on paramagnetic particles bearing glutathione, washing the paramagnetic particles with the immobilised polypeptide from unbound oligonucleotides in a liquid stream, splitting the protein target with the bound DNA aptamers from the surface of paramagnetic particles with the B. anthracis lethal factor, separating and amplifying the DNA sequence with affinity to the recombinant protein target in a polymerase chain reaction and obtaining a set of single-chain DNA aptamers that are specific to the protein target.

EFFECT: invention provides efficient production of DNA aptamers with high affinity for recombinant protein targets.

4 dwg, 4 ex

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