RU2217127C1 - Sulfur-containing gel and method for scabies treatment - Google Patents

Abstract

FIELD: medicine, dermatology, pharmacy. SUBSTANCE: gel contains sulfur as an active substance and hydro- philic base that represents gel of rare-cross-linked acrylic polymer with content of sulfur 5.0-33.0 weight%. Composite can contain additionally glycerol or polyethyleneoxide-400 and also laevomycetin as a preserving agent or mixture of nipagin and nipasol in the ratio 3: 1. Scabies is treated by application of gel once on each skin site for 4-5 days without replacing underwear and bed linen and the gel is washed off with warm water and wear is changed. EFFECT: improved treatment method. 6 cl, 1 tbl, 2 ex

Description

 The invention relates to pharmacy and medicine and relates to acaricidal agents that can be used to treat skin diseases, including scabies.

 In connection with population migration, an increase in the number of patients with immunodeficiencies and other factors, in recent years, the incidence among the population, including children, of parasitic dermatoses, in particular scabies caused by the scabies tick Sarcoptes scabiei [Sokolova TV, Fedorovskaya R .F., Lange A.B. Scabies. - M. Medicine, 1989].

 In the treatment of various skin diseases: scabies, psoriasis, seborrhea, sycosis, etc., sulfur preparations are most widely used in domestic clinical practice.

 The current requirements for contraceptive preparations are the speed and reliability of the acaricidal effect, the absence of irritating effects on the skin, and stability during long-term storage. In the concentrations used to treat scabies (10-33%), sulfur has a pronounced keratolytic effect, which contributes to its better access to the pathogen [Skin and sexually transmitted diseases: A guide for doctors. / Edited by Yu.K. Skripkina, V.N. Mordovtseva. - M .: Medicine, 1999. S. 426-436].

 Known ointments are sulfuric simple, sulfur-tar, sulfur-naphthalan, Wilkinson ointment and a number of others [Mashkovsky M.D. Medicines At 2 hours 12th ed. Part II. - M .: Medicine, 1993]. A more complex sulfuric ointment with antipruritic effect is known. It includes sulfur, nipagin, nipazole, mink oil, ethyl alcohol, emulsion wax, citral, perfume, glycerin and water [Patent 2112505 of the Russian Federation, IPC 6 A 61 K 9/06, 33/04, 47/44. Sulfuric ointment] . Known drug sulfodecortem - an ointment containing precipitated sulfur 10 g, hydrocortisone acetate 0.4 g, medical vaseline, lanolin, stearic acid, etc. up to 100 g [Mashkovsky MD Medicines At 2 hours 12th ed. Part II. - M .: Medicine, 1993. S. 484]. The ointment is rubbed in a thin layer 2 times a day for 5-14 days. If necessary, repeat the treatment after 5-7 days. With the appearance of erythema and itching, the drug is canceled.

 All of these drugs have a common drawback. Their ointment bases are hydrophobic, interfere with the gas and heat transfer of the skin and cause allergic reactions, especially in children, their use is often accompanied by complications, mainly dermatitis of varying severity.

 Hydrophilic copolymers of acrylic acid and polyfunctional crosslinking agents are widely used as carriers of various drugs. Rare cross-linked acrylic polymers (RAP) are produced abroad under the name carbopol - 934, 940, 941, 2020, etc. They easily form viscous and transparent gels. RAP gels have several advantages over various ointment bases: they provide high bioavailability, prolonging effect and ease of use, they are non-toxic, do not undergo hydrolysis and oxidation, and are resistant to environmental factors [G. Bashura, O. Klimenko, Mshushko Z.N., Bashura A.G., Lyapunov N.A., Alyushin M.T. Surfactants and macromolecular compounds in the technology of dosage forms // Medicines. Economics, technology, prospects for obtaining: Overview. inform. - M.: VNIISENTI, 1988. V. 12. S.52; Overview: Medicine and Health Care // Pharmacy and Pharmacology. 1982. 6. S. 39-46]. Rare cross-linked acrylic polymers are included in the British, American, French and International Pharmacopoeias under the name "carbomers."

 In recent years, domestic rare-crosslinked acrylic polymers, such as arespol, MARS, have been developed, and the possibility of obtaining arespol gels and their technological properties has been studied. Using arespol, a number of drugs have been developed [Alekseev K.V., Lee V.N., Demishev V.N. et al. Rare cross-linked acrylic polymers in pharmacy // Pharmacy. 1987. 5. P.15-18; Alekseev K.V., Starodubova M.V., Slyusar O. I. Arespol - a new excipient in the technology of ointments // VII Russian National Congress "Man and Medicine": Abstracts. - M., 2000. P.598; Astrakhanova M.M., Starodubova M.V., Alekseeva K.V., Elagina I.A. New anti-inflammatory drugs for external use // VI Congress "Man and Medicine": Abstracts. - M., 1999. P.383; Kudryakova E.A., Moldaver B.L., Marchenko L.G., Tsvetkova Yu.A. Investigation of the possibility of producing gels of the new domestic rare-cross-linked acrylic polymer "Arespol" // Sat. Proceedings of the NIIF. T.39. S.212-217; Mayorova A.V., Alekseev K.V., Suslina S.N. The experience of using the rare crosslinked acrylic polymer Arespol as a part of new dermatological preparations // Mat. scientific practice. conf. "Actual issues of cosmetology." - St. Petersburg, 2000. S.80].

 Closest to the proposed solution is a simple sulfuric ointment containing sulfur precipitated at a concentration of 33% and a consistent emulsion base water / petrolatum (petrolatum 6 hours, water 3 hours, emulsifier T-2 1 hour) [Mashkovsky M. D. Medicinal facilities. In 2 h. 12th ed. Ч, II. - M .: Medicine, 1993. S. 484]. This drug has inherent disadvantages common to ointments on hydrophobic bases - after applying the ointment, dermatitis and eczema often develop, in addition, the ointment is characterized by an unpleasant odor, it is difficult to remove from the skin and stains clothes.

 The objective of the invention is to create a new composition of acaricidal action on a hydrophilic basis, i.e. devoid of the above disadvantages, expanding the range of funds for this purpose.

 The objective of the invention is also the development of a method for the treatment of scabies using the claimed gel.

 The tasks are carried out by the proposed composition with sulfur on a hydrophilic gel base with RAP with a sulfur content of 5.0-33.0 wt.% And the method of its application.

 Gelling components are RAP, selected from the group of arespol, MARS, carbopol. Sodium hydroxide is contained as a neutralizing agent. The composition includes water and optionally preventing drying of glycerin or polyethylene oxide (PEO) 400 and, as preservatives, chloramphenicol or a mixture of nipagin and nipazole 3: 1 in the general following ratio of ingredients, weight. %: sulfur 5.0-33.0; carbopol or arerespol, or MARS 0.2-2.0; NaOH solution to pH 5.0-8.0; PEO 400 or glycerol 0.1-15.0; chloramphenicol 0.25-1.0 or a 3: 1 mixture of nipagin and nipazole 0.1-0.3; water is the rest.

 Treatment of patients with uncomplicated scabies is carried out according to the general method: once daily rubbing the ointment into the skin for 4-5 days without changing underwear and bedding, followed by a shower (bath), boiling and changing underwear and bedding.

 Local use of the drug does not have an allergic effect and does not cause dermatitis. Their treatment is practically relapse-free.

 The sulfur gel is prepared using the following technology. Arespol (MARS, carbopol) is added with stirring to the calculated amount of purified water, then sodium hydroxide solution is added and mixed until a uniform transparent gel is obtained. The sulfur is triturated with about half the amount of gel, then the remaining gel is added in portions and mixed until a homogeneous mass is formed.

 The invention is illustrated by the following examples of formulations (see table).

 The obtained gels are characterized by satisfactory consistent properties (spreadability and extrusion), thixotropic properties, colloidal and thermal stability.

 A comparative study of the pharmacological action on guinea pigs showed the absence of a locally irritating and allergenic effect of a gel with sulfur based on RAP and revealed a pronounced local irritating effect of the prototype - a simple sulfuric ointment based on a water / petroleum jelly-based emulsion.

 The obtained gels with sulfur on a hydrophilic basis have been tested in the clinic of skin diseases of St. Petersburg. State Medical Academy. I.I. Mechnikova (St. Petersburg State Medical Academy).

 Under supervision was 21 patients with scabies, including 6 children aged 6 to 14 years. For adults, 20% was used, and for children, 10%, gel-based sulfuric ointment.

 12 patients got scabies for the first time; in 9 patients who were previously treated on an outpatient basis in polyclinics and high-pressure centers, relapses of the disease, complicated by dermatitis, occurred. In 16 patients, an itch mite was found.

 The treatment of patients with uncomplicated scabies was carried out according to the general method: daily rubbing the ointment into the skin for 4-5 days without changing underwear and bedding, followed by a shower (bath) and changing underwear and bedding. At the same time, an examination was carried out of persons who were in contact with patients who, if necessary, had also been treated accordingly.

 Treatment of patients with scabies complicated by dermatitis began with the elimination (treatment) of dermatitis with the usual anti-inflammatory drugs (agitated suspensions, indifferent creams, pastes, antihistamines, etc.) followed by the use of 20% hydrophilic sulfur ointment. In adult patients who first became ill with scabies, 20% gel ointment on a gel basis was used immediately after diagnosis. Children used 10% ointment.

 All patients tolerated the treatment well. In no case were dermatological complications and side effects noted. Clinical manifestations of scabies resolved after 5-7 days; in 6 patients, the so-called post-itchy pruritus was observed within 6-9 days. No relapses were noted.

 Examples of treatment.

 1. Patient V., 38 years old, a builder, complained of severe itching of the entire skin, especially at night. Itself suggests that he has scabies, which he contracted while on a long business trip to Siberia. Not treated. Objectively: skin lesions are common. Typical seropapular elements are found on the skin of the body, mainly in the lower abdomen, genitals, back, upper limbs.

 Microscopic examination revealed an itch mite in the scales of the elements. The treatment was prescribed with 20% gel-based sulfuric ointment according to the method described above. Already by 3-4 days, the itching decreased sharply, and soon completely stopped. After 7-8 days, all scabies resolved. The patient for two months was twice invited for follow-up examinations. No manifestations of scabies were detected. The treatment was well tolerated. Dermatological complications were not noted. Almost healthy. Family members are healthy.

 2. Patient Zh. 37, a janitor, complained of widespread itching, especially in the evening and at night. Sick for about two months. In the KVD at the place of residence, a diagnosis of scabies was established. At the same time as the mother, her daughter, 9, fell ill. Treatment with the usual 20% sulfuric ointment was prescribed. Itching gradually decreased, and scabies were resolved. But on day 3-5, both patients had common erythematous, scaly elements, in large folds with wetting phenomena. Diagnosed with posthumous dermatitis. Treatment with sulfuric ointment based on water / petrolatum was discontinued, desensitizing agents, calcium gluconate, lotions in the foci of weeping, a zinc bolt on the skin of the body were prescribed. Gradually, the appearance of dermatitis resolved. But after 2 weeks, the mother and her daughter again had itchy elements on the hands, lower body, and genitals.

 With these phenomena, both patients were examined at the clinic of skin diseases of St. Petersburg State Medical Academy named after Mechnikov.

 The diagnosis was established: relapse of scabies (incomplete treatment after the initial treatment), posthumous resolving dermatitis. Microscopic examination revealed an itch mite in the skin tissue elements.

 She was prescribed treatment with sulfur-based ointment on a gel basis (mother 20% and her daughter 10%) according to the above method. Itching decreased by 3-4 days, scabies resolved on 6-7 days. With double control examinations, no manifestations of scabies and its complications were detected. A series of preventive measures at the place of residence.

 Thus, 20% and 10% sulfuric ointment, made on a new non-vaseline base containing RAP, is a very effective anti-scab product and has significant (principal) advantages compared to the usual 20% sulfuric ointment prepared on the basis of petroleum jelly. According to observations, the new composition of the ointment is undoubtedly more effective compared to a 20% benzyl benzoate emulsion.

 Hydrophilic-based sulfuric ointment has a number of related advantages: it does not have an unpleasant odor, it does not stain clothes, which are easily washed after use using ordinary detergents.

 The cost-effectiveness of the new drug is currently being determined.

Thus, for the treatment of scabies, a gel with sulfur based on crosslinked acrylic polymers is proposed, which
- has a pronounced acaricidal effect;
- does not have a locally irritating and allergic effect;
- does not cause dermatitis;
- characterized by satisfactory consistent thixotropic properties, colloidal and thermal stability;
- convenient to use;
- It can be made at pharmaceutical enterprises and in pharmacies.

 As a result of testing the gel and the method of its use at the Department of Dermatology of the II Mechnikov St. Petersburg State Medical Academy in the treatment of scabies in adults and children, it was found that the treatment with the claimed composition is practically relapse-free, has no local irritating and allergic effects. After application of the gel, the occurrence of dermatitis was not observed in both adults and children in any case.

Claims (6)

1. A composition having acaricidal action, containing sulfur as an active substance and a base, characterized in that the base is hydrophilic and is a gel of a cross-linked acrylic polymer, and the sulfur content is 5.0-33.0 wt.%. 2. The composition according to claim 1, characterized in that the hydrophilic gel base includes a rare cross-linked acrylic polymer, a solution of sodium hydroxide and water in the following ratio, wt.%: Arespol, or MARS, or carbopol 0.2-2.0 A solution of NaOH aqueous To pH 5.0-8.0 Water Else 3. The composition according to any one of claims 1 and 2, characterized in that it further comprises glycerol or PEO 400 in an amount of 0.1-15.0 wt.%. 4. The composition according to any one of claims 1 to 3, characterized in that it further comprises chloramphenicol as a preservative in an amount of 0.25-1.0 wt.%. 5. The composition according to any one of claims 1 to 3, characterized in that it further comprises as a preservative a mixture of nipagin and nipazole 3: 1 in an amount of 0.1-0.3 wt.%. 6. A method of treating scabies by applying a composition containing sulfur to the skin, characterized in that they rub the composition according to any one of claims 1-5 once daily for 4-5 days without changing underwear and bed linen, and then wash it off with warm water , and linen is changed to disinfected.

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