Pharmaceutical composition for treating vaginal candidiasis and method for preparing it

FIELD: medicine.

SUBSTANCE: as an active substance, the composition contains butoconazol, a base that is a combination of a hydrophobic ingredient, a hydrophilic ingredient and an emulsifier, and also a gel-forming polymer. Hydroxypropylstarch phosphate is preferentially used as the gel-forming polymer. A method for preparing the declared composition consists in the fact that a mixture of butoconazol with a portion of the hydrophilic ingredient, the hydrophobic ingredient and emulsifier is added with a dispersion of the gel-forming polymer in the rest of the hydrophilic ingredient; the produced mixture is agitated homogenously with a preserving agent added where it might be necessary.

EFFECT: new pharmaceutical composition is characterised by a high level of antifungal activity, stability both at a storage temperature, and at a use temperature, and good pack extrusion.

14 cl, 2 tbl, 10 ex

 

The invention relates to the field of medicine and relates to pharmaceutical compositions in the form of vaginal cream containing highly effective agent antifungal action, and is suitable for the treatment of gynecological diseases.

Vaginal candidiasis (VC) is one of the most common diseases, affecting up to 75% of women of childbearing age. Widespread vaginal candidiasis associated with exposure to women of various factors of the external environment, change the environment, the wide use of antibiotics and their interaction, which reduces the immunological activity of the organism.

The drugs used in the treatment of VK, designed for both local and/or systemic use.

Systemic antifungal therapy is prescribed in case of severe clinical picture VK, chronic disease, resistance to local therapy with human immunodeficiency virus (HIV). The most effective drugs for systemic effects are azole compounds fluconazole and Itraconazole.

In uncomplicated VK used drugs for systemic effects (fluconazole 150 mg Itraconazole 200 mg 2 times a day for 3 days).

In cases of complicated course VK course of therapy should be to increase the half, however, the duration of use of drugs local action should be 14 days. Systemic antimycotics in all cases of recurrent VK are recommended as the primary therapy.

In recent years there has been a decrease in the sensitivity of conditionally pathogenic microorganisms to antimycotics. In this regard, new pathogenetically substantiated methods of treatment of VK and mixed bacterial-fungal infections of the vagina, including local use of antiseptics. Although becoming more popular, self-treatment systemic antimycotics, local therapy remains the most popular and safe treatment method.

Among the currently available antifungal agents topical application include vaginal suppositories/beads or tablets, as well as special vaginal creams. The choice of drug in each particular case should depend on the severity of the clinical course of vaginal candidiasis, extinctio, comorbidities predisposing factors.

Active ingredients include, as a rule, imidazole or polyene antimycotics. The latter include different drugs nystatin and natamycin. Among the imidazoles of the most frequently used drugs clotrimazole. In addition, there are in the original form of miconazole, econazole, isoconazole, omoconazole and other derivatives of imidazole. The imidazoles remain the drugs of choice for the treatment of vaginal candidiasis. However, it is recognized that 50% of patients discontinue treatment after experiencing relief of symptoms. To improve adherence to treatment, doctors have developed a tendency to reduce the time of use of the medicinal product and, as a result, treatment of miconazole nitrate and clotrimazole were shortened from the original 14 days to 7 and 3 days.

Butoconazole nitrate is of interest because of its very acceptable safety profile and proven clinical efficacy. Butoconazole nitrate - derived imidazole, has fungicidal activity against Candida, Trichophyton, Microsporum, Epidermophyton and some gram-positive bacteria. The most effective Candida. Blocking in cell membrane formation of ergosterol from lanosterol, increases the permeability of the membrane, leading to lysis of the cells of the fungus. The tests showed broad-spectrum antifungal activity: he consistently showed high activity against the most important eight species of Candida that are not related to the class albicans. Butoconazole surpassed currently in the imidazoles (miconazole, clotrimazole, ketoconazole, terconazole) when Engibarov the NII growth of C. albicans and pathogenic species of Candida, not related to the genus albicans.

In the patent RU 2320322 described system vaginal drug delivery with almost neutral pH value, including emulsion with almost neutral pH value, containing globules having two phases: an internal water-soluble phase and an external water-insoluble phase or film. The delivery system includes a therapeutically active drug, which is an antifungal agent selected from the group consisting of butoconazole nitrate, clotrimazole, ketoconazole nitrate, miconazole, polyene antifungal agents, and others. However, the known composition is characterized by a rather complex manufacturing technology.

In the patent of Russian Federation № 2379027 described composition, which represent the emulsion with a high content of dispersed phase comprising an active substance, 4.0 wt.% or less of propylene glycol, one or more of pharmaceutically acceptable excipients that promote release of the active substance in the vaginal cavity. Specifically described delivery system in the form of cream with nitrate butoconazole (2%). Known composition intended for the treatment of fungal infections of the vaginal cavity of a woman. As an example, the delivery system described composition, which includes an active ingredient (butoconazole nitrate), guide opony component (mineral oil, microcrystalline wax, hydrophobic silicon dioxide), hydrophilic component (propylene glycol, water, an aqueous solution of sorbitol), emulsifier (glycerylmonostearate, polyglyceryl-3-oleate), preservative (methylparaben, propylparaben).

In the patent document US 20110251141 described pharmaceutical composition, comprising a combination of an antifungal component butoconazole or its salts and other active ingredient (clindamycin phosphate, metronidazole). As auxiliary ingredients known composition comprises a hydrophobic component (mineral oil, microcrystalline wax), hydrophilic component (water, aqueous solution of sorbitol), emulsifier (glycerylmonostearate, PEG-30 dipolyhydroxystearate), preservative (methylparaben, propylparaben). However, the known compositions do not provide sufficient prolongation of action of the active ingredient of butoconazole nitrate, how this is achieved is known composition of butoconazole [Reference Vidal. Drugs in Russia: a Handbook. M: Attraversare, 2007, S. 1003, drug Ginovart]. In the known composition of the prolongation of action of the drug is achieved hydrophobic base that provides high adhesion (stickiness) to the walls of the vagina, resulting in the cream it does not follow in a few days. However, this arrangement has the significant negative aspects: first, the drug is very difficult to wash from the vagina; secondly, butoconazole is this basis in suspension; this requires the use of micronized powder butoconazole, otherwise the suspension has large particle size 100-250 μm, and the drug does not always withstand the test of homogeneity for Gasfurnace; thirdly, it is very difficult to wash from such compositions production equipment.

The purpose of this invention is to provide pharmaceutical compositions in the form of vaginal cream containing substance antifungal action (butoconazole nitrate), modified on the basis of ensuring the effectiveness and duration of action of the drug, as well as the development of a method of obtaining a composition.

To solve this problem is proposed pharmaceutical composition comprising as active ingredient butoconazole or its salt in an effective amount, and the basis, which is a combination of hydrophobic and hydrophilic components and emulsifier, characterized in that it contains additional gel-forming polymer and does not contain another active ingredient.

Butoconazole belongs to the group of imidazoles. It has fungicidal activity against Candida, Trichophyton, Microsporum, Epidermophyton and some gram-positive bacteria. In before Occitania embodiment, the composition includes butoconazole in the form of nitrate. Preferably the composition contains 2 g/100 g of the composition of butoconazole.

In a preferred embodiment, the composition has the following ratio of components, g/100 g composition:

Butoconazole nitrate1,0-3,0,
Gelling polymerthe 2.0-14,0
BaseRest

As a polymer-gel-use a derivative of cellulose, such as methylcellulose, hydroxypropylcellulose, hypromellose, carboxymethylcellulose, sodium carboxymethylcellulose, hydroxyethylcellulose or modified starch, such as hydroxypropylmethyl phosphate, or different reconstitue acrylic polymers (carbopol) - "Carbopol the homopolymers", "Carbopol copolymers and Pemulen". "Carbopol the homopolymers" - polymers of acrylic acid with allilohreos or allinterfaces. "Carbopol copolymers and Pemulen" - polymers of acrylic acid, modified long chain (C10-C30) alkylacrylate and sewn with allinterfaces, preferably gel-forming polymer in number, g/100 g composition: 3-12. It is preferable to use as a gelling agent of Hydra is ciprofibrate phosphate in the amount preferably g/100 g composition: 6-9.

The introduction of the gel-forming polymer promotes the formation of stable cream as when the storage temperature (25°C) and temperature (37°C). When selected this concentration provides the necessary rheological properties of the creams and maintaining consistency even when the temperature is raised to 40°C. at the same time ensures the stability of the composition during storage and good extrusion finished dosage forms of packaging (tubes), which is very important for ease of use for patients.

As the basis of the carrier features a modified hydrophilic base, represented by emulsion 1 kind, which in combination with a water-soluble polymer provides a gel-like consistency at body temperature and bioadhesion of the drug to the mucosa of the vagina that prevents leakage. Preferably the base has the following composition, g/100 g composition:

Hydrophobic component3,0-of 17.0
The hydrophilic componentto 50.0 to 90.0
Emulsifier3,0-15,0

As the hydrophobic component in the composition predpochtite is correctly applied isopropylmyristate, which is a solvent butoconazole, more preferably in the amount of 6-9 g/100 g of the composition, can also be used isopropylpalmitate, cetostearyl of isononanoate may be used instead of, or in conjunction with them the following excipients: octil the dodecanol, ethylhexyl octanoate, Cocoyl kapiokurt, oleyl the oleate.

As the hydrophilic component preferably uses a combination of propylene glycol and water, which more preferably contains a pH corrector. Alternatively, you can also use other polyhydric alcohols such as glycols, for example butyleneglycol, glycerin, macrogol, in particular the oxides of the General formula H(O-CH2-CH2)nOH, preferably the oxides with an average molecular weight 375-6000, more preferably with an average molecular weight of 1000-4000, or mixtures of these compounds. For adjusting the pH are the hydroxides of alkali metals, preferably sodium hydroxide, can also be used amines, such as trometamol or diethylamine.

The preferred ratio of components of the hydrophilic component, g/100 g composition:

Propylene glycol2,0-15,0
The pH corrector to pH 3.5 to 6.5
Purified water48,0 - 75,0

Preferably the pH of the composition is in the range of 4.5 to 6.5, so butoconazole is in the composition in dissolved form, which ensures a uniform distribution in the mass, and improves the effectiveness of its action.

To ensure the colloidal stability of the emulsion in the composition are introduced emulsifying agents 1 and 2 kinds, the total content is more preferably ranges from 3.7 to 12.3 g/100 g of the composition. Thus preferably uses of macrogol 20 cetosteatil ether and cetosteatil alcohol in the following ratio, g/100 g composition:

Of macrogol 20 cetosteatil ether1-3,5
Cetosteatil alcohol4,7-6,8

In a preferred embodiment of the invention the composition comprises a preservative. One of the conditions that determine the quality and safety of medicines for local use, is the effectiveness of antimicrobial preservatives. As antimicrobial preservatives used methyl parahydroxybenzoate, sodium propyl parahydroxybenzoate, Phenoxyethanol in an amount of from 0.3 to 1.0 g/100 g of the composition. Preferably the dryer is xethanol in the amount of 0.45-0.9 g/100 g of the composition. Preferably in combination with Ethylhexylglycerin, which increases the antimicrobial activity of Phenoxyethanol. Preferably in the ratio of 9:1.

The claimed ratio of ingredients found experimentally and is the best.

The proposed pharmaceutical composition is in the form of soft medicinal forms, preferably in the form of cream on emulgelooe basis, and represents a complex dispersed system, which is simultaneously emulsion (oil/water) and the solution (with respect to the active ingredient). The proposed composition is characterized by a homogeneous distribution and a minimum particle size of the hydrophobic component of the emulsion.

The introduction part of butoconazole is provided by the simultaneous achievement of antifungal and antibacterial action. As already noted, butoconazole is present in the composition in dissolved form, which ensures a uniform distribution in the mass, and improves the effectiveness of therapeutic action.

Pharmacological studies have shown that the proposed composition on the effectiveness of therapeutic action is not inferior to the Comparators. The results of the study of antimicrobial activity of the claimed cream butoconazole method of diffusion in agar are shown in table 1.

Table 1
The test microorganismThe diameter of the zones of growth inhibition (mm)
S. aureus was ATSS 6538 Por 10.60±0,11
S. aureus 192511,05±0,10
S. aureus 172210,10±0,04
S. aureus 6209,70±0,04
S. saprophyticus ATCC 1530511,08±0,10
M. luteus ATCC 934111,40±0,13
C. xerosis 191112,15±0,14
C. albicans ATCC 885-653to 20.88±0,06
C. tropicalis Vkhu-547/Y-100319,80±0,27
C. pseudotropicalis Vkhu-601/3322,43±0,29
C. parapsilosis Vkhu-488/1022,58±0,24
C. neoformans Vkhu-881/Wcmu-75317,03±0,08

Antifungal effect of the claimed composition was observed for all strains of yeast-like fungi, used in experimental research.

Studied acute whom I subacute toxicity, irritant and sensitizing effect of this composition with butoconazole nitrate.

The results of studies of acute toxicity indicate that when intravaginal the way the administration to female rats at a dose of 12.0 g/kg developed the composition has no toxic effect on the General condition and the dynamics of body weight of the animals, does not cause changes of biochemical parameters of blood serum does not change the relative weight of internal organs of rats.

The results obtained in the subacute experiment (within two weeks), indicate that intravaginal introduction developed compositions rats at doses of 2.0 g/kg 4.0 g/kg no toxic effect on the General condition, behavior, weight gain of animals on electrophysiological activity of the myocardium, peripheral blood, the functional state of the Central nervous system, liver and kidneys of rats.

According to the results of pathomorphological studies have shown that the cream butoconazole in subacute exposure does not change, such factors as the relative weight of internal organs of rats. After exposure to the investigational product no morphological signs of damage of vital organs of animals.

The vaginal cream 2% did not show local irritating action that podtverzdeniye, and has no sensitizing effect.

The choice of ingredients and their ratio significantly affects the way of obtaining the drug.

The method of obtaining the claimed compositions is that to the mixture of butoconazole with a part of the hydrophilic component, a hydrophobic component and the emulsifier are added to the dispersion of the gelling polymer in the remaining part of the hydrophilic component and the resulting mixture is stirred until smooth, adding in the appropriate preservative. In a preferred variant of the method the solution butoconazole prepared in emulsion obtained by adding emulsifiers and a hydrophobic component to the mixture of butoconazole and propylene glycol. It is preferable to adjust the pH of the resulting emulsion to prevent crystallization of the active substance in the manufacturing process and storage.

A typical example. Active ingredient (butoconazole nitrate) mixed with propylene glycol at a temperature of 65-75°C and add the emulsifier (a combination of macrogol 20 cetosteatil ether and cetosteatil alcohol), a hydrophobic component (isopropylmyristate), if necessary, adjust the pH (10% solution of sodium hydroxide), mix thoroughly and add to the dispersion of the gelling polymer (hydroxypropylmethyl phosphate in water), homogen serout. Then add the preservative, homogenize and cool the resulting cream to room temperature. Get a homogeneous cream white or almost white, which is Packed in tubes.

Specific examples of carrying out the invention is presented in table 2. In examples 4-6 as a gel-forming polymer is used hydroxypropylmethylcellulose, in the examples 7,8 - carboxymethylcellulose and in examples 9-10 - hydroxypropylcellulose. In examples 2, 7 as a hydrophobic component used isopropyl, in examples 3 and 9 - cetostearyl isoneof in example 4 - combination of isopropylmyristate and octyldodecanol in equal proportion. In example 2, instead of the propylene glycol used butyleneglycol and as proof pH potassium hydroxide in example 3 polyethylene glycol (polyethylene oxide 6000) and in example 4 as a pH corrector use trometamol. Obtained according to examples 1, 2, 3, 4 pharmaceutical composition meets regulatory requirements (in appearance, homogeneity, microbiological purity and other parameters), stable in storage and has a shelf life of over 2 years.

Table 2
IngredientsContent, g/100 g of the composition is
Examples
12345
Butoconazole nitrate2,01,02,03,02,2
Gelling polymer8,02,014,013,06,0
Hydrophobic component3,06,0of 17.08,09,0
The hydrophilic component78,082,551,070,174,22
Emulsifier8,08,016,0 5,57,8
Preservative1,00,5-0,40,78
IngredientsContent, g/100 g of the composition
Examples
678910
Butoconazole nitrate1,851,02,052,152
Gelling polymer8,82,013,06,87,7
Hydrophobic component6,54,08,38,77,8
The hydrophilic component 73.8690,082,8268,1873,83
Emulsifier8,13,07,88,18,0
Preservative0,89-0,670,50,67

1. Pharmaceutical composition in the form of soft medicinal forms, which comprises as active ingredient butoconazole or its salt in an effective amount and basis, which is a combination of a hydrophobic component, a hydrophilic component and an emulsifier, characterized in that it further comprises a gelling polymer and does not contain another active ingredient.

2. The pharmaceutical composition under item 1, characterized in that it contains as active ingredient butoconazole nitrate.

3. The pharmaceutical composition according to p. 2, characterized in that it contains the ingredients in the following ratio, g/100 g composition:

Butoconazole nitrate 1,0-3,0,
Gelling polymerthe 2.0-14,0
BaseRest

4. The pharmaceutical composition according to p. 3, characterized in that it contains ingredients framework in the following ratio, g/100 g composition:

Hydrophobic component3,0-of 17.0
The hydrophilic componentto 50.0 to 90.0
Emulsifier3,0-16,0

5. The pharmaceutical composition according to p. 4, characterized in that it contains as a hydrophilic component propylene glycol, water and the pH corrector.

6. The pharmaceutical composition according to p. 5, characterized in that it contains propylene glycol, water and the pH corrector in the following ratio, g/100 g composition:

Propylene glycol2,0-15,0
Purified water48,0-75,0
The pH correctorTo pH 3.0 to 6.5

7. The pharmaceutical composition according to p. 6, characterized in that it contains as the hydrophobic component is isopropylmyristate.

8. The pharmaceutical composition according to p. 7, characterized in that it contains as an emulsifier combination of macrogol 20 cetosteatil ether and cetosteatil alcohol.

9. The pharmaceutical composition according to p. 8, characterized in that it contains macrogol 20 cetosteatil ether and cetosteatil alcohol in the following ratio, g/100 g composition:

Of macrogol 20 cetosteatil ether1-3,5
Cetosteatil alcohol4,7-6,8

10. The pharmaceutical composition under item 1, characterized in that it additionally contains a preservative.

11. The pharmaceutical composition according to p. 10, characterized in that it contains as preservatives combination of Phenoxyethanol and Ethylhexylglycerin.

12. The pharmaceutical composition according to p. 11, characterized in that it contains Phenoxyethanol and Ethylhexylglycerin in the ratio of 9:1.

13. A method of obtaining a composition, characterized in PP.1-12, according to which a mixture of butoconazole with a part of the hydrophilic component, a hydrophobic component and the emulsifier are added to the dispersion of the gelling polymer in the remaining part of the hydrophilic component and the resulting mixture is stirred until smooth, adding more if needed conservative is so

14. The method according to p. 13, whereby butoconazole nitrate is mixed with propylene glycol and emulsion butoconazole nitrate receive in the presence of a pH corrector.



 

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8 cl, 1 dwg, 1 tbl

FIELD: biotechnology.

SUBSTANCE: aqueous composition for anaesthesia is proposed, which comprises propofol as an active agent, the PEG-660-12-hydroxystearate as a solubiliser, benzyl alcohol, or chloroethanol or parabens as preservative, the tocopherol and arginine or glycine at a specific content of components wt %. The GABA agonists can be additionally added to the composition, e.g. aminophenyl-butyric acid, local anesthetics such as lidocaine, alpha-2-adrenoceptor agonists such as xylazine. The method is proposed for implementing anaesthesia comprising administering to a patient of an effective amount of the claimed composition.

EFFECT: invention provides low toxicity of dosage form and high efficiency.

5 cl, 3 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: composition containing curcumine, an acid specified in a group consisting of citric acid, malic acid, acetic acid, tartaric acid, lactic acid, alginic acid or a mixture thereof, and an edible emulsifying agent with specific characteristics and taken in a certain amount wherein the above composition is applicable as a therapeutic agent. The composition containing curcumine, the edible emulsifying agent or a mixture thereof, the acid specified in a group consisting of citric acid, malic acid, acetic acid, tartaric acid, lactic acid, alginic acid or a mixture thereof taken in certain proportions, and additionally encapsulated into a gelatine capsule, wherein the above composition is applicable for treating or preventing an inflammation and/or diseases caused by the inflammation.

EFFECT: compositions improve the curcumine bioavailability effectively.

13 cl, 1 tbl, 6 ex

FIELD: medicine.

SUBSTANCE: hydrophilic therapeutic agent is specified in a group consisting of albuterol, bendamustine, captopril, carboplatin, ciprofloxacin, gemcitabine, ibandronate, lamivudine, metformin, niacin, oxycodone, ranitidine and sumatriptan. The composition also contains a solvent, a surfactant and a hydrophilic carrier. The above hydrophilic carrier is compatible to the therapeutic agent solution and the surfactant.

EFFECT: good stability and bioavailability compatible to that of injection formulations when administered orally.

21 cl, 2 dwg, 13 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: pharmaceutical oil-in-water emulsion contains mometasone or mometasone furoate, propylene glycol and water. The propylene glycol concentration makes from 20 to approximately 45 wt %. A mass ratio of propylene glycol and water in the oil-in-water emulsion makes from 1:1 to approximately 1:3. A portion of mometasone or mometasone furoate is found insoluble in the emulsion.

EFFECT: composition is characterised by stability and therapeutic effect.

27 cl, 6 dwg, 5 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to an herbal formulation of topical nanoemulsion for treating acne-related skin disorders. The above formulation contains an aqueous phase comprising a therapeutic agent, rose water and/or lemon juice, and an oil phase containing an essential oil, a non-ionic surfactant and an accessory surfactant. The aqueous and oil phases are related within the range of 1:1 to 1:2, while a particle size of the herbal formulation is less than 5 nm. The essential oil is presented by tea tree oil, basil oil, rosemary oil, lavender oil, jojoba oil, bergamot oil, clove oil and peppermint oil. The invention also refers to a method for preparing the herbal formulation which involves providing the aqueous and oil phases, mixing the above phases to produce a mixture to be emulsified with the non-ionic surfactant to prepare a macroemulsion. The prepared macroemulsion is mixed with ethanol to produce a nanoemulsion with a particle size less than 5 nm.

EFFECT: invention provides the herbal formulation with good penetration, prolonged effect causing no irritation.

8 cl, 4 dwg, 7 ex

FIELD: medicine.

SUBSTANCE: invention represents a drug for treating osteoarthrosis presented as a soft dosage form, containing glucosamine and methyl salicylate as active substances, and additive agents.

EFFECT: enhanced anaesthetic action and lower toxicity of methyl salicylate.

10 cl, 1 tbl, 4 ex

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