Pharmaceutical composition for preventive maintenance of development and treatment of initial stage of age cataract (versions)

FIELD: medicine.

SUBSTANCE: invention concerns pharmaceutical compositions for preventive maintenance of development and treatment of an initial stage of an age cataract. The pharmaceutical composition (versions) contains the active beginning an admixture of two short-chain peptides and the suitable pharmaceutical carrier. In the first version - admixture of D-pantethine and N-acetylcarnosin at the following concentration of components: D-pantethine-not less than 0.001%, N-acetylcarnosin - not less than 0.001%, a normal saline solution - to 100%. In the second version - admixture D-pantethine and L-carnosin at the following concentration of components: D-pantethine - not less than 0.001%, L-carnosin - not less than 0.001%, a normal saline solution - to 100%.

EFFECT: high efficiency of the offered pharmaceutical composition is caused by that the components entering into composition; selectively protect different fibers of the lens of an eye.

2 cl, 7 dwg

 

The invention relates to the field of medicine, veterinary medicine and pharmacology, specifically to the composition to prevent the development and treatment of the initial stages of age-related cataracts.

According to who, the share of cataract accounts for 47.8% of all ocular pathology [World Health Organization Fact Sheet No. 282; WHO November 2004; available at www.who.int/mediacentre/factsheets/fs282/en/index.html]. Although surgical methods for the treatment of this pathology is well designed, adverse effects have also been observed and described in detail in the article [Malyugin B. E. cataract Surgery and intraocular correction afakii: achievements, problems and prospects, journal of ophthalmology, No. 1, pp.37-41, 2006.]. In this regard, the actual challenge remains finding conservative methods of prevention of the development and treatment of cataract, i.e. search anticatarrhal drugs.

The lens of the eye of man and of vertebrates consists of 90% alpha-, beta - and gamma γ-crystalline. The content of these proteins in the lens is approximately the same, but they differ significantly in structure and molecular weight. Alpha crystalline are chaperones and protect beta - and gamma-crystalline, which are the most sensitive to damage. It is believed that with age the protective properties of the alpha-crystalline weaken and associated with this the development of senile cataract.

Of obvious concern is their different denaturing factors for example, ultraviolet (UV) radiation or high temperatures that can cause aggregation cristallino. As a result of aggregation are large light-diffusing conglomerates, which lead to clouding of the lens, that is, to the development of cataracts.

Known means, created on the basis of short-chain peptides: either D-pantethine or L-carnosine, or its derivative N - acetylcarnosine, for which patents have been obtained on anticataract drugs.

As well known aqueous solutions of N-acetylcarnosine, its derivatives or salts and method of prevention and treatment of cataract with their application (international application WO 2004/028536 A1, IPC7AC 31/4164, publ. 08.04.2004).

Chemical retardation or the treatment of cataract development inhibitors separation of the phases is known from U.S. patent number US 5091421 Chemical prevention or reversal of cataract by phase separation inhibitors", IPC7A61K 31/40, 31/66, publ. 25.02.1992).

The main disadvantage of the known pharmaceutical compositions for treatment of the initial stages of age-related cataracts is that they are not sufficiently effective.

The closest analogue for the proposed pharmaceutical compositions are eye drops containing short-chain peptide L-carnosine, hydrochloric acid and water, anti-clouding of the eye lens and used for treatment of nachinauschaia age-related cataract (patent RU 2071316 C1, IPC7AC 9/00, 31/415, publ. 10.01.1997). This drug is used in the form of a 1-5% aqueous solution of carnosine. The product contains:

carnosine - 1,0-5,0 g,

the concentrated hydrochloric acid to a pH of 6.5 to 7.2,

water to 100 ml.

The disadvantage of the closest analogue is a pharmaceutical composition for the prevention of the development and treatment of the initial stages of age-related cataract is its lack of effectiveness. In addition, it is known that an aqueous solution on the basis of only one of carnosine not effectively penetrates into the lens. If you enter such a solution in the form of instillation in the eye, watery moisture on the path from the cornea to the lens it will be destroyed by the enzyme carnosinase. This forms a histidine, which is easily converted into histamine is a mediator of allergic reactions, providing for the introduction from outside the same effect as any allergen [Mark A. Babizhayev, Anatoly I. Deyev, Valentina N. Yermakova, Valerii V. Remenshchikov and Johan Bours, "Revival of the Lens Transparency with N-Acetylcarnosine", Current Drug Therapy, v.1, p.91-116, 2006].

Object of the present invention is more efficient than the known ones that are suitable for preventing or slowing down the process of clouding of the lens of the eye, i.e. to prevent the development and to ensure the initial stage of age-related cataracts.

The problem is solved in that the proposed pharmaceutical whom azizia to prevent the development and treatment of the initial stages of age-related cataracts, as the closest analogue that contains at least one short-chain peptide.

New in the proposed pharmaceutical composition is that it contains as active principle a mixture of two short-chain peptides and a suitable pharmaceutical carrier. In the first embodiment is a mixture of D-pantethine and N-acetylcarnosine with the following concentrations of components:

D-one - not less than 0.001%,

N-acetylcarnosine - not less than 0.001%,

saline solution up to 100%.

The second variant is a mixture of D-pantethine and L-carnosine in the following concentrations of components:

D-one - not less than 0.001%,

L-carnosine is not less than 0.001%,

saline solution up to 100%.

The content of the active agent in the composition is from 0.002% to 10%, and the content of each of the short-chain peptides is from 0.001% to 5%. The carrier may be a liquid material acting as a carrier, excipient, or medium for the active ingredient. An example of a suitable carrier is saline.

Increase efficiency anticatarrhal properties of the two proposed variants of the pharmaceutical composition in comparison with the known compounds based on the identified authors of a new mechanism of action of the active principle established pharmaceutical compositions.

Predominant drug fourmeau is for this composition can be drops, and the proposed method of their use installations in the eye. Another possible way to use variations of the composition may be intraperitoneal injection.

The authors have tested the proposed variants of the composition in the laboratory in vitro and in experimental animals in vivo at various concentrations of the active principle. The lowest concentration is determined by the boundary manifestations of a positive effect, and the maximum concentration and potential toxicity of drugs and high viscosity solution.

Below are the components included in the formulations of the pharmaceutical compositions of:

1) in the first embodiment, a mixture of short-chain peptides:

N-acetylcarnosine General formula:

and D-pantethine General formula:

2) in the second embodiment, a mixture of short-chain peptides of L-carnosine General formula

and D-pantethine, which are pharmaceutical compositions for the prevention of the development and treatment of the initial stages of age-related cataracts.

Obtained in tests of the proposed compositions in vitro and in vivo experimental dependences shown in figures 1-7.

Figure 1 shows the dose dependence of the scattered power in the solution of the beta-crystalline samples of the CSOs radiation (λ=633 nm) of ultraviolet (UV) dose when added to the solution of various short-chain peptides.

Figure 2 presents the dose dependence of the scattered power in the solution of the mixture of alpha and beta γ-crystalline trial of radiation from UV dose when added to the solution of various short-chain peptides and the proposed composition.

Figure 3 presents the dependence of the rate of cataract development (points) in the lens in different groups of experimental animals - rats (control group; UV-irradiated; UV-irradiated, which received the composition in the form of eye drops) from the time of observation (number of evaluations).

Figure 4 presents the dependence of the rate of cataract development (points) in the lens in different groups of experimental animals - rats (control group; UV-irradiated; UV-irradiated, which received the composition in the form of intraperitoneal injection at a concentration of 150 mg/kg) time of observation (number of evaluations).

Figure 5 presents the dependence of the rate of cataract development (points) in the lens in different groups of experimental animals - rats (control group; UV-irradiated; UV-irradiated, which received the composition in the form of intraperitoneal injection at a concentration of 25 mg/kg) time of observation (number of evaluations).

Figure 6 presents the dependence of the rate of cataract development (points) in front of the cortical layers of the lens in different groups of experimental animals - rats (control group; the f-irradiated; UV-irradiated, which received the composition in the form of eye drops; UV-irradiated, which received the composition in the form of intraperitoneal injection at a concentration of 25 mg/kg or 150 mg/kg) time of observation (days).

Figure 7 presents the dependence of the rate of cataract development (points) in the nuclear medium the lens layers in different groups of experimental animals - rats (control group; UV-irradiated; UV-irradiated, which received the composition in the form of eye drops; UV-irradiated, which received the composition in the form of intraperitoneal injection at a concentration of 25 mg/kg or 150 mg/kg) time of observation (days).

High efficiency of the proposed pharmaceutical compositions (options) to prevent the development and treatment of the initial stages of age-related cataract is due to the fact that their components, as determined by the authors selectively protect different proteins of the eye lens.

The authors found that L-carnosine and N-acetylcarnosine significantly slow down the aggregation of beta-crystalline, while the influence of D-pantethine on the aggregation of beta-crystalline virtually absent (see figure 1). However, D -, one slows photoaggregation mixture of beta - and alpha γ-crystalline and a mixture of beta-, alpha - and gamma γ-crystalline by maintaining superanabolon (protective) properties of alpha-crystalline (see figure 2). At the core is ve of these studies the authors have chosen composition of short-chain peptides, with supernoodles activity.

The advantages created by the authors of the drug and the results of its tests, have shown a positive effect in slowing UV-induced cataract in rats, described in the works:

1) Sostav L.V., Shuttles E.V., Sapogova NV, Bityurin NM, V.V. Nemov, Karpov PU, D. Sheremet, Polunin G.S., Avetisov SE, Ostrovsky M.A. investigation of the influence supernoodles (protective) activity of short-chain peptides on the rate of UV-induced excimer laser aggregation of beta-crystalline // Vestnik of ophthalmology, (accepted for publication).

2) Avetisov SE, Polunin G.S., Sheremet, D., Makarov I.A., Fedorov A.A., Karpov PU, Muranov C.O, Timofeev, A., Kostov L.V., Shuttles E.V., Bityurin NM, Sapogova NV, V.V. Nemov, Boldyrev A.A., Ostrovsky M.A. study of the effects of a mixture of di - and Tetra-peptides on the "extended" model ultravioletabsorbing cataract in rats // journal of ophthalmology, (accepted for publication)

The proposed composition more effectively inhibit the aggregation mixture cristallino forming the lens of the eye, than L-carnosine, N-acetylcarnosine or D, one separately (figure 1,2). On the basis of each of these substances were previously proposed anticataract drugs [see the above-mentioned patents analogues: EN 2071316; US 5091421; WO 2004/028536], but compared with L-carnosine or N-ACE what incarnation the effectiveness of the proposed compositions above 1.5 times, as compared with D-pantethine - 2.5 times.

Preclinical trials of the proposed variants of the composition in rats showed no acute or chronic toxicity, allergenic, irritant, mutagenic and teratogenic effects, and tolerability of high doses of drugs. According to the classification of these songs belong to harmless substances.

The invention is carried out as follows.

On the influence of the pharmaceutical composition on the slow aggregation cristallino forming the lens of the eye, evident in the following examples carried out in laboratory conditions in vitro and in experimental animals in vivo.

Example 1.

Proteins of the lens of the eye of the bull alpha-, beta - and gamma-crystalline, as well as D -, one acquired in the company "Sigma", USA). L-carnosine and N-acetylcarnosine were acquired in the firm "Hamari Chemicals Ltd.", (Japan).

Proteins in the amount of 0.5 mg/ml dissolved in phosphate buf-ore (0.1 M NaCl, 10 mm Na2NRA4, 3 mm To2NRA4pH of 7.2) and was passed through membrane filters with a pore size of 0.45 μm and 0.22 μm (firm Sartorius, Germany). For removing insoluble impurities test tube with the solution was centrifuged for 15 minutes at room temperature with the acceleration of 5000 g. In the study of mixtures cristallino L - and alpha-crystallin ispolzovalis a 1:1 ratio.

As the source of UV radiation was used pulsed excimer XeCl laser LPX-200 (firm "Lambda Physik, Germany), the wavelength of which is λ=308 nm.

Used mode of laser irradiation, the closest thing to the lighting conditions of the lens natural light. The experiments were carried out at a temperature of (22±1)°C, and heating of the solution during irradiation did not exceed 2°C. the Degree of aggregation of the protein was estimated by the amount dispersed in the solution power of the test radiation HeNe laser (λ=633 nm). The height of the quartz cuvette was 10 mm, the length along the beam HeNe and Has lasers - 10 mm and 5 mm, respectively. To study the dynamics of protein aggregation was measured according to P(D) power P scattering in a solution of protein a trial of radiation with λ=633 nm on the value of UV exposure D (i.e. the dose of UV radiation in j/cm2). The parameter characterizing the rate of aggregation is the exposure to UV-irradiation (dose), which begins the growth of the light scattering test radiation in solution. This parameter we denote as D*.

Effects on susceptibility to UV radiation beta-crystalline same concentrations of D-pantethine, L-carnosine, or N-acetylcarnosine separately is shown in figure 1. From the experimental curves shows that L-carnosine and N-acetylcarnosine significantly slow f is toaggregate beta-crystalline, moreover, the reduction in aggregation of these peptides with the same accuracy of measurement error, and the addition of D-antenna almost does not reduce D*, then there is no effect on the rate of aggregation of beta-crystalline.

Example 2.

Figure 2 shows the change of speed of photoaggregation mixture of alpha - and beta γ-crystalline adding the same concentration of D-pantethine or L-carnosine, or N-acetylcarnosine, and only one of the proposed compositions, namely the mixture of D-pantethine N-acetylcarnosine, because the influence of the other songs are equally accurate to measurement error. From the comparison of exposures in which begins the scattering of the probe beam in the solution mixture of alpha - and beta γ-crystalline and adding to the solution of the peptides or compositions, clearly visible best protective effect of the proposed compositions compared with the effects of L-carnosine, N-acetylcarnosine or D-pantethine separately.

Examples 1 and 2 show a selective effect of short-chain peptides on the rate of photoaggregation cristallino. If L-carnosine or N-acetylcarnosine directly inhibit the aggregation of beta-crystalline, D -, one slows down the aggregation mixture of beta - and alpha γ-crystalline, i.e. supports the chaperone (protective) activity of alpha-crystalline. On the basis of these results were established PR is alagaesia composition: mixture of the D-pantethine N-acetylcarnosine or a mixture of D-pantethine with L-carnosine, more slow photoaggregation cristallino eye lens than L-carnosine, or N-acetylcarnosine, or D, one separately.

Example 3.

Studies anticatarrhal the impact of the proposed compositions in experiments in vivo on the development of UV-induced cataract in rats. The experiment was conducted on 33 rats male species Wistar (66 eyes) aged from 20 to 23 days with body weight 39-41, the follow-up Period was 10 months (43 weeks). All animals were divided randomly into 5 groups.

The first group consisted of 8 animals, which initiated the formation of UV-cataract, but did not enter the proposed composition (drugs).

The second (control) group consisted of 7 rats that were not exposed to UV radiation and did not receive the drugs.

In the 3rd group (6 animals, 12 eyes) irradiated animals received drugs in the form of installations in the eyes of a 5% solution of each peptide from the proposed combinations.

In the 4th group (6 animals, 12 eyes) irradiated animals received drugs in the form of intraperitoneal injection at a dose of 25 mg/kg of each peptide from the proposed combinations.

In the 5th group (6 animals, 12 eyes) irradiated animals received the composition of the peptides in the form of intraperitoneal injection at a dose of 150 mg/kg of each peptide from the proposed combinations.

Installation and NutriBar the bus injections were performed once every day during the whole observation period (10 months).

Initiating the development of UV cataract was performed using two UV quartz irradiators FMR-K-01 "Sun" (λ=280-400 nm), located at a distance of 0.3 m above the cage with the animals. Radiation sessions with a duration of 16 minutes was carried out through the day. For wavelengths 313 and 366 nm radiation intensity irradiators by Parker and Hatchard stood at 23.7±4,41and 21.5±4,0 j/(s·m2), respectively. (1Data are presented as M±σ, where M is the average intensity value, σ - standard deviation.)

Subjective assessment of the dynamics of development of cataract was performed using the method of expert estimations on digital photos of the lens. The study was carried out with three independent expert. In the analysis of photographs used their own scale scoring.

Biomicroscopic study of the lenses (the method of expert estimates) allowed to reveal the dynamics of the formation of cataract in animals studied groups during the experiment. So, after the first evaluation, conducted one month after the beginning of irradiation, were statistically significant differences between the 1st (exposure) and 2 (control) group. The reliability of differences persisted throughout the observation period. By the end of the experiment in the irradiated group was observed the formation of a medium of expression the particular homogeneous oblicovochnogo cataract, more intense in the nuclear layers (cataract 5 points), while in the control group lens to a much greater extent retained its opacity (cataract 2-3 points).

The main groups treated with the proposed composition of the background UV radiation, dynamics of increase of opacities in the lens was not the same (see figure 3, 4, 5). The earliest statistically significant differences compared with irradiated (1st) group originated in the 4th and 5th groups (exposure and introduction respectively 25 mg/kg and 150 mg/kg of the drug intraperitoneally) already in the 2nd month of the experiment. However, by the end of the experiment on day 313 more pronounced anticanonically effect of the proposed compositions was obtained in group 3 (irradiation and installation preparation). At last observation cataract in this group corresponded to 2-3 points. In group 4 at the end of the experiment cataract valued at 3 points, 5 group by 3-4 points.

Example 4.

Objective assessment of the dynamics of development of lens opacities was carried out by microdensitometry biomicroscopic sections of the lens. Biomicroscopy was performed at the slit lamp SL-75 (Opton, Germany) at an angle of inclination of the light source 45° and the open aperture of 0.1 mm Studies were performed monthly. The study was carried out by quantitative assessment of the severity of the haze in front cortical the s layers, in the anterior, middle and posterior thirds of the nucleus and posterior cortical layers of the lens.

After 10 months the animals were taken from the experiment by an overdose of chloroform anaesthesia according to the "Statement for the Use of Animals in Ophthalmic and Visual Research" [7]. The lenses also recorded and produced the half-sections according to standard methods. Optical and morphometric study anticatarrhal effect of the drugs was performed on the "Photomicroscope III (Opton, Germany) using a hardware-software complex automatic morphogenically company "Dyamorph (Dyamorph Lens").

Data microdensitometric analysis allowed us to obtain objective results biomicroscopic study (see Fig.6, 7). The animals of the 1st group (irradiation and lack of treatment) noted a progressive increase in optical density (POP) lens layers during the whole observation period, and the increase was most pronounced in the first 3 months. In terms 3-10 months from the beginning of the experiment, growth curve of optical density is the graph of a linear function. By the end of the observation period maximum values noted in POP nuclear layers (the growth rate was 117±5%). In the cortical layers of the lens, the growth rate was slightly smaller and had reached 97±3%

In the 2nd control group during the whole observation period diagnosed with a slight steady increase in POP in all the layers (the increase was 37±4%), what can be the evidence of the natural process of development of age-related lens changes in rats species Wistar. Compared to the 1st group differences in rates highly significant at each observation (p<0,001).

In groups of animals treated with the proposed composition, the dynamics of changes in the rate of optical density was as follows (see Fig.6, 7):

Group 3 (irradiation and installation preparation) - growth graph POP in cortical layers and the core of the lens is almost completely repeats the curve of the 2nd group (control). Group 4 (irradiation and the introduction of 25 mg/kg of the drug intraperitoneally) - values measure the optical density in the dynamics exceed the corresponding values in the control group. In all cases, the value of POP with a high degree of reliability is lower than in group 1 (irradiation and lack of treatment) and higher than in control (p<0,001).

Group 5 (irradiation and the introduction of 150 mg/kg of the drug intraperitoneally) - characteristic curve of POP meets the 4th group. Although the magnitude of the POP is greater than the value of this indicator in animals 4-th group, however, intergroup differences at all points statistically insignificant (p>0,05).

Thus, experiments using the developed pharmaceutical compositions performed both in the laboratory and on a pilot alive who were, showed more efficient slowdown aggregation cristallino eye lens than with the use of known drugs in its class.

1. Pharmaceutical composition for the prevention of the development and treatment of the initial stages of age-related cataracts, containing at least one short-chain peptide, characterized in that the active agent comprises a mixture of two short-chain peptides D-pantethine and N-acetylcarnosine with the following concentrations of components:

D-onenot less than 0.001%
N-acetylcarnosinenot less than 0.001%
salineup to 100%

2. Pharmaceutical composition for the prevention of the development and treatment of the initial stages of age-related cataracts, containing at least one short-chain peptide, characterized in that the active agent comprises a mixture of two short-chain peptides D-pantethine and L-carnosine in the following concentrations of components:

D-onenot less than 0.001%
L-carnosinenot less than 0.001%
salineup to 100%



 

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3 cl, 1 tbl

FIELD: medicine.

SUBSTANCE: 2 blood samples are taken with interval 3 days against complex medicinal supplement under the following scheme. Therapy of the first exfusion day is characterized with single introduction of phetabolyl 0.4 mg/kg intramuscularly, 5% vitamin B1 - 50 mg intravenously, vitamin B12 - 500γ st. units intramuscularly, 5%vitamin C - 150 mg intravenously and 10 % aminoplasmal E - 250 ml intravenously drop-by-drop. The same day and the next two days imply intramuscular injection of ferrum lek 100 mg once, sorbypher 325 mg twice a day, folic acid - 5 mg 3 times a day. For the second day exfusion is accompanying with single subcutaneous introduction of epocryne in dosage 4 thausand UNITS. Then for the third day control inspection is carried out. The second day of exfusion implies single introduction of 5% vitamin B6 - 50 mg intravenously, 5% vitamin C - 150 mg intravenously, vitamin B12 - 500γ st.units intramuscularly and 10% aminoplasmal E - 250 ml intravenously drop-by-drop. This day and in the subsequent two - three days imply intramuscular introduction of ferrum lek 100 mg once, sorbypher 325 mg twice a day, folic acid - 5 mg 3 times a day. For the second day exfusion is accompanying with single subcutaneous introduction of epocryne in dosage 4 thausand UNITS. Then for the third day control inspection is carried out again. Since the first exfusion and before autoblood preparation nutritive supplement is carried out using module protein added to mix "Berlamine Modular" 50 g twice a day daily. After exfusion autoblood is divided on erythrocyte mass and fresh frozen plasma.

EFFECT: prevention of dangerous erythropoiesis and metabolic disorders.

1 ex, 3 cl

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