Gel-like preparation for local anesthesia

FIELD: medicine, urology.

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

EFFECT: higher efficiency of application.

1 cl, 1 dwg, 7 ex

 

The invention relates to the field of medicine, namely to means external application in the field of urology.

Know means "Cathedral" ("Cathejell")containing 0.05 g of chlorhexidine dihydrochloride in 100 g of gel, as well Cathejell with lidocaine containing 0.05 g of chlorhexidine dihydrochloride, and 2 g of lidocaine 100 g of gel, manufactured by the pharmaceutical company "Montavit", Austria, representing a sterile, water-soluble gel for external use in a sterile package having dielectric properties, antiseptic and local anesthetic pharmacological action and intended for catherization urethra, endoscopic studies, minor gynaecological procedures (Register of medicines of Russia. Encyclopedia of drugs: annual. the compilation. VIP. M., 2003. S).

The disadvantages of the known tools "Cathedral" are: lack of moving (lubricating) properties, weak transport effect of physiologically active principle, no anti-inflammatory action.

Known also Giganten (Digenten) - combined gel preparation containing gentamicin sulfate, lidocaine hydrochloride, atony (antiseptic), used for local anesthesia and asepsis gynecological research, cytourethroscopes (Mashkovsky PPM Lech is only means. 2 th Ed. 13-E. Kharkov: Torching. 1997. Vol.2. S).

A disadvantage of the known means is used as an antiseptic etoniya, which refers to bischetvertichnoe ammonium bases, has a higher bactericidal activity against streptococci, staphylococci, and it is mainly used externally. Upon contact with mucous membranes can cause severe irritation, less effective against wide range of bacteria. In addition, the tool has poor elastic properties, which can lead to traumatic catheter insertion.

Thus, the authors was to develop a tool that would have increased sliding (lubricating) and elastic effect and provide the most efficient transport across the mucosa of active ingredients (anti-inflammatory, antispasmodic, antiseptic), would be non-toxic, did not show undesirable side effects, it is convenient to use.

The problem is solved by applying funds for research and treatment in urology, containing the gel-forming biopolymer, disinfectant (antiseptic) component, lidocaine, gentamicin and water, which contains as a gelling biopolymer - hydroxyethyl cellulose, as a detoxifying whom Ananta - benzalconi chloride, in the following ratio of components (wt.%):

hydroxyethylcellulose0.80-1.20
benzalconi chloride (50%)0.04-0.06
lidocaine0.90-1.10
gentamicin0.08-0.12
waterrest
100

The tool may include papaverine in the amount of 0.08 to 1.20 wt.% from the total.

At the present time of patent and technical literature is not known composition of the funds for research and treatment in urology, which contains these components in the proposed qualitative and quantitative value.

The proposed tool for research and treatment in urology, containing the gel-forming biopolymer, disinfectant (antiseptic) component, lidocaine, gentamicin, and water, can be obtained as follows. In the reactor of stainless steel, equipped with a propeller stirrer, load lidocaine (0.90-1.10 wt.%), gentamicin (0.08-0.12 wt.%), benzalconi chloride (0.04-0.06 wt.%) and water to 100 wt.%, bring the mixture to a degree of homogeneity. With active stirring contribute hydroxyethyl cellulose (0.80-1.20 wt.%) until a homogeneous suspension and then until thick mass is. Mass stand for 12 hours. The finished product is packaged.

If the product contains papaverine in the amount of 0.80-1.20 wt.% of the total, it is added to the initial mixture, which is then brought to a degree of homogeneity.

The hydroxyethyl cellulose used as gelling biopolymer, is a substance of natural origin, predictable effect on the human body, able to degrade, becoming involved in the natural metabolic chain, provides a high transport capacity of physiologically active ingredients and has no unwanted side effects. The content of gelling less than 0.80 wt.% does not provide sufficient elastic and sliding properties of the proposed tools. When the content is more than 1.20 wt.% deteriorating transport function of the gel slows down the process of absorption of active ingredients. In addition, there are technological difficulties in obtaining gel, and it is difficult to uniform mixing of the solution and packaging of the finished product.

Used as a disinfectant (antiseptic) component benzalconi chloride is highly soluble in water and alcohols. Well tolerated by the skin and mucous membranes. Has microbiostatic and bactericidal action on gram-positive, in large doses - gramatically the e bacteria and Candida. The mechanism of antimicrobial action is the same as the cationic surfactants, however, it is less irritating to the mucous membranes. In addition to antiseptic that has a deodorizing effect (Krasilnikov A.P. Reference antiseptic. Minsk: High school. 1995. P.71). The lower limit (of 0.04 wt.%) sufficient for the manifestation of antiseptic effect, and furthermore, does not violate the desired gel structure. The upper limit (0.06 wt.%) due to the number, which does not have undesirable effects on the human body, and also does not violate the desired gel structure. Used as an anesthetic (local anesthetic) component lidocaine - strong local anesthetic agent, causing all kinds of local anesthesia for lubricating mucous membranes applied in the form of 1-2% solution (Mashkovsky PPM Medicines. 2 th Ed. 13-E. Kharkov: Torching. 1997. T.1. S). The lower limit (about 0.90 wt.%) sufficient for the manifestation of local anesthetic effect. The upper limit (1,10 wt.%) due to the number, which enables efficient transport of a component through the mucous membranes and does not have undesirable effects on the human body.

Used as an anti-inflammatory component gentamicin is an antibiotic of the aminoglycoside. Used in various infectious diseases, you are the bathrooms sensitive to the microorganism, effective for urinary tract infections. One of the main treatments for severe septic infections, has a broad spectrum of action, in some cases, the lack of effective activity of other antibiotics (Mashkovsky PPM Medicines. 2 th Ed. 13-E. Kharkov: Torching. 1997. Vol.2. S). The lower limit (0.08 wt.%) sufficient for the manifestation of anti-inflammatory effect. The upper limit (1,12 wt.%) due to the number, which does not have undesirable effects on the human body. The claimed content of gentamicin in combination with other components of the proposed tool provides efficient transport through the mucous membranes of the upper urinary tract, kidney, localizing the inflammatory process.

Used in appropriate cases as an antispasmodic component papaverine - myotropic spasmolytic agent, class of alkaloids. Lowers the tone and reduces contractile activity of smooth muscles, has vasodilator and antispasmodic action (Mashkovsky PPM Medicines. 2 th Ed. 13-E. Kharkov: Torching. 1997. T.1. C.430). The lower limit (to 0.80 wt.%) sufficient for the manifestation of spasmolytic action. The upper limit (1.20 wt.%) due to the number, which does not have undesirable effects on the human body. Declare soda is the content of papaverine ensures efficient transport through the mucous membranes of the lower urinary tract calling their relaxation, while in the upper urinary tract support muscle tone, which is especially important in the post-operative action and much more effective than the introduction antispasmodic component intravenously.

The proposed solution is illustrated by the following examples.

Example 1. In the reactor of stainless steel, equipped with a propeller stirrer, load lidocaine 90.00 g (0.90 wt.%), gentamicin 8.00 g (0.08 wt.%), benzalconi chloride 4.00 g (0.04 wt.%) and water 9818.00 g (98.18 wt.%), bring the mixture to a degree of homogeneity. With active stirring contribute hydroxyethyl cellulose 80 g (0.80 wt.%) until a homogeneous suspension and then until thick mass. Mass stand for 12 hours. The finished product is packaged.

Example 2. In the reactor of stainless steel, equipped with a propeller stirrer, load lidocaine 110.00 g (1.10 wt.%), gentamicin 12.00 g (0.12 wt.%), benzalconi chloride 6.00 g (0.06 wt.%) and water 9752.00 g (97.52 wt.%), bring the mixture to a degree of homogeneity. With active stirring contribute hydroxyethyl cellulose 120.00 g (1.20 wt.%) until a homogeneous suspension and then until thick mass. Mass stand for 12 hours. The finished product is packaged.

Example 3. In the reactor of stainless steel, equipped with a propeller stirrer, load lidocaine 110.00 g (1.10 wt.%), gentamicin 12.00 g (0.12 m is S.%), benzalconi chloride 6.00 g (0.06 wt.%), papaverine 80.00 g (0.80 wt.%) and water 9672.00 g (96.72 wt.%), bring the mixture to a degree of homogeneity. With active stirring contribute hydroxyethyl cellulose 120.00 g (1.20 wt.%) until a homogeneous suspension and then until thick mass. Mass stand for 12 hours. The finished product is packaged.

Example 4. In the reactor of stainless steel, equipped with a propeller stirrer, load lidocaine 90.00 g (0.90 wt.%), gentamicin 8.00 g (0.08 wt.%), benzalconi chloride 4.00 g (0.04 wt.%), papaverine 120.00 g (1.20 wt.%) and water 9658.00 g (96.58 wt.%), bring the mixture to a degree of homogeneity. With active stirring contribute hydroxyethyl cellulose 120.00 g (1.20 wt.%) until a homogeneous suspension and then until thick mass. Mass stand for 12 hours. The finished product is packaged.

Comparison of lubricant (moving) actions proposed means and the famous "Katedrala" experimental as follows, and as the criteria used, the duration of the moisture retention gel. Funds applied to an inert carrier (plastic plate) and control the water content at certain time intervals by weighing methods. Thus was obtained a comparative profile of moisture loss for the means of two compositions: "Catedral", selected as a prototype, and the tool pre the proposed composition (wt.%: hydroxyethylcellulose - 0.80, benzalconi chloride (50%) - 0.04, lidocaine - 0.90, gentamicin - 0.08, water - 98.18). It is shown that within, for example, 25 hours in the tool proposed composition is about 80% water, the rate of water loss for Cathedral significantly higher (see drawing).

Example 6. Patient R., aged 45, was admitted with a diagnosis of stone n/3 of the left ureter. Was made transureteral lithotripsy, in which the instrument was processed by the proposed tool, the tool was introduced into the ureter on the side of the operation in the volume of 2 ml. Marked more easy in comparison with the "Catedrales", the introduction of the tool into the ureter on the side of the operation. It was possible to reduce the number of analgesics 1/4 by reducing the morbidity of the introduction of the tool and analgesic effect tools. The operation was performed without parenterale antibiotics.

Example 7. Patient M., 37 years old, was admitted with a diagnosis of stone/3 of the right ureter. Conducted transureteral lithotripsy, the proposed remedy was processed by the tool. In addition, the tool was introduced into the ureter on the side of the operation in a volume of 2.5 ml by treatment achieved more easy and comfortable for the patient, the introduction of the tool into the ureter on the side of the operation, a reduced amount of analgesic drug by 25% by reducing injuries is lichnosti the introduction of the tool and analgetic action of the tool. The operation was performed without parenterale antibiotics.

Thus, the proposed tool for research and treatment in urology has improved properties, namely high penetrating ability of active ingredients (anti-inflammatory, antispasmodic, antiseptic), moving (lubricating) and elastic effect, non-toxic, has no unwanted side effects. In addition, doctors and patients had good appearance money and easy to use for consistency, no odor.

The proposed tool can be used as an effective tool for the treatment of inflammatory, traumatic and postoperative diseases in urology and gynecology.

Part of the funds does not include components that are prohibited in the media, intended to come into contact with mucous.

1. The local anaesthetic in the form of a gel containing a gel base, lidocaine hydrochloride, antiseptic component benzalconi chloride and water, characterized in that it additionally contains gentamicin, and as a gel base - hydroxyethyl cellulose biopolymer, in the following ratio, wt.%:

0,80-1,20
Hydroxyethylcellulose
Benzalconi chloride (50%)0,04-0,06
Lidocaine hydrochloride0,90-1,10
Gentamicin0,08-0,12
WaterThe rest is up to 100

2. The tool according to claim 1, characterized in that it further comprises papaverine in the number of 0.80-1.20 wt.% from the total.



 

Same patents:

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to the propofol anesthetic composition suitable for parenteral administration. The composition comprises propofol in the concentration from 1 mg/ml to 20 mg/ml, d-alpha-tocopheryl polyethylene glycol-1000 succinate (TPGS) in the concentration from 10 mg/ml to 200 mg/ml, and water. The mass ratio of propofol to TPGS is at least 1:10. The composition is sterilized by final sterilization in autoclave. The present composition overcomes shortcomings of the ready preparative formulation in the emulsion form, namely, it provides the stable clear product in storage under regulated temperature conditions, i. e . in cooling.

EFFECT: improved and valuable pharmaceutical properties of composition.

11 cl, 7 ex

FIELD: organic chemistry, polymers, medicine.

SUBSTANCE: invention describes lidocaine polyacrylate eliciting the prolonged topical anesthetic effect of the general formula: wherein n means (number of links) = 50-70; means a link of polyacrylic acid; means N,N-diethylaminoacetic acid 2,4-dimethylanilide.

EFFECT: valuable medicinal properties of compound.

1 cl, 2 tbl, 1 ex

The invention relates to medicine and can be used in anesthesiology, ophthalmology, dentistry, otolaryngology, surgery
The invention relates to pharmacy

-modification of the hydrochloride of 2 - dimethylaminoethanol ether p-butylaminoethyl acid as a local anesthetic means and how you can get" target="_blank">

The invention relates to a new crystalline-modification of the hydrochloride of 2 - dimethylaminoethanol ether p-butylaminoethyl acid as a local anesthetic remedies, the way it is received, namely, that the solution of the hydrochloride of 2 - dimethylaminoethanol ether p-butylaminoethyl acid in water, in an organic solvent or their mixture is heated to boiling, it is dispersed in the refrigerant and subjected to freeze-drying

The invention relates to a new methyl-isopropyl[(3-n-propoxyphene)ethyl]amine of formula I, where R1represents n-propyl, R2is methyl, R3- isopropyl, or its pharmaceutically acceptable salts, which have the properties of a topical local anaesthetics and can be used to produce medicines used for local anesthesia

The invention relates to new pharmaceutical compositions comprising one or more local anesthetics in oil form, one or more surfactants, water and optional additives agents, taste masking, and also to a method of pain relief and to a method for producing pharmaceutical compositions
The invention relates to medicine, namely to anesthesiology

FIELD: chemical-pharmaceutical industry and technology, pharmacy.

SUBSTANCE: invention relates to a method for addition of difficultly water-soluble medicinal substances to the emulsion base. Method involves preliminary preparing solid dispersions by melting a medicinal substance and polyethylene glycol-1500 in the ratio = 1:(5-5.5) by mass at temperature no causing their destruction (90-140°C). Then solid dispersions are added to emulsion bases. Invention provides enhancing the pharmaceutical availability of difficultly water-soluble medicinal substances from soft medicinal formulations by 4-50.2 times and providing the better release due to enhanced solubility and rate of dissolving medicinal substances in preparing solid dispersions. This results to reducing dose and adverse effect of the medicinal substance on the body.

EFFECT: improved method for addition and preparing.

1 tbl, 3 dwg, 5 ex

FIELD: veterinary medicine, pharmacy.

SUBSTANCE: invention proposes ointment comprising tartaric acid, precipitated sulfur, boric acid, wax, colophony and vegetable oil taken in the definite ratios. The ointment provides healing damaged tissue of animal being without adverse effect.

EFFECT: valuable curative properties of ointment.

1 tbl

FIELD: medicine, arthrology, pharmacy.

SUBSTANCE: invention relates to agents of topical applying used in treatment of articulation diseases. Proposed agent comprises mixture of chondroitin sulfate and glucosamine salts as a saccharide, the compound taken among the group nonsteroid anti-inflammatory agents, in particular, ibuprofen or nimesulid, or piroxicam, or meloxicam, or diclofenac salt, or indometacin, or ketoprofen, dimethylsulfoxide and an ointment base taken in the definite ratio of components. Invention provides enhancing effectiveness due to the content a mixture of low-molecular and high-molecular saccharides in it that results to increasing diffusion rate of active component to the articulation zone and also the compound taken among the group of nonsteroid anti-inflammatory agents. The combined using these agents provides the curative synergetic effect.

EFFECT: improved and valuable medicinal properties of agent.

2 cl, 14 ex

FIELD: medicine, cosmetology.

SUBSTANCE: the suggested wound-healing remedy includes a gel-forming agent, an active substance and distilled (deionized) water. As the active substance it contains Mexidol (2-ethyl 6-methyl 3-oxypyrridine succinate) at the following ratio of components, weight%: gel-forming agent 0.5-5.0, stabilizing agent 0.01-0.8, conservant 0.01-1.0, Mexidol 0.01-10.0, distilled (deionized) water - the rest. The suggested remedy is highly efficient. It is of pronounced wound-healing action in 1, 2 and 3 phases of wound process. It quickly liquidates inflammatory processes, decreases painfulness, edema, considerably improves the state of affected tissues, accelerates reparative-degenerative processes and terms of epithelization. It possesses the wide spectrum of action, manifests pronounced action at treating different skin and mucosal lesions - wounds, fissures, bedsores, trophic ulcers of different genesis, surface burns of 1-3 degree, radiation lesions, it, also, removes skin microlesions that possess the nature of cosmetic defects, moreover, it improves skin structure.

EFFECT: higher efficiency of application.

2 ex

FIELD: medicine, arthrology, pharmacy.

SUBSTANCE: agent comprises glucosamine salt as saccharide, dimethylsulfoxide, ointment base and ibuprofen or nimesulide, or piroxicam, or meloxicam, or diclofenac salt, or indometacin, or ketoprofen as a nonsteroid anti-inflammatory agent. Glucosamine hydrochloride, glucosamine sulfate sodium, potassium or calcium salt is used as glucosamine, and diclofenac potassium or sodium salt is used as diclofenac salt. New ointment shows high perfusion rate of active substances to the articulation zone and enhanced effectiveness. Invention expands assortment of agents used in treatment of articulations.

EFFECT: improved, enhanced and valuable medicinal properties of agent.

2 cl, 14 ex

FIELD: cosmetic industry, cosmetics.

SUBSTANCE: invention relates to a method for preparing a base for cosmetic agents used in skin care. Method for preparing biologically active base for cosmetic agents comprises fermentation of cultures of strains lactobacilli and bifidobacteria in hydrolyzate-milk medium containing lactulose. The ferment of lactobacilli and bifidobacteria in the amount 3-5% of nutrient medium volume is plated and fermented for 6-8 x up to formation of suspension with acidity value = 70°-100° and with titer value 1010 CFU followed by its heating at temperature 80-85°C for 10-15 min and cooling. The content of lactulose in medium is 1.5-2 wt.-%. The base prepared by proposed method provides reducing loss of biologically active substances to minimal value and allows conferring to the base high nutrient activity and producing regenerating, softening, bactericidal and anti-inflammatory effects on skin.

EFFECT: improved preparing method, improved and valuable medicinal and cosmetic properties of base.

2 cl, 1 tbl, 4 ex

FIELD: medicine, dermatology, chemical-pharmaceutical industry, pharmacy.

SUBSTANCE: invention relates to an antifungal gel pharmaceutical composition based on ketoconazole and clotrimazole that are derivatives of imidazole. The composition comprises ketoconazole or clotrimazole as an active component, polyethylene glycol-400 (PEG-400) as a solvent, carboxyvinyl polymer as a gel-forming agent, polyethylene glycol as a gel stabilizing agent, organic amine or inorganic bas as a regulator of pH and water taken in the definite ratio of components. The composition is prepared by dissolving active component in PEG-400, dispersing carboxyvinyl polymer in water, successive addition to dispersion propylene glycol as a stabilizing agent and regulator of pH and combination of prepared solution and gel followed by stirring the mixture up to preparing the gel composition with pH 5-7. Invention provides preparing antifungal composition with reduced adverse effect.

EFFECT: improved preparing method, valuable medicinal properties of composition.

2 cl, 1 tbl, 11 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to curative ointments with anti-inflammatory effect and with biostimulating properties for treatment of burns, suppurative and infected wounds of different etiology and to a method for treatment above said diseases using the ointment said. The proposed ointment comprising bee wax and greasy basis comprises colophony additionally. As greasy basis the ointment comprises butter and vegetable oil in the following ratio of components, wt.-%: bee wax, 20-30; butter, 30-40; vegetable oil, 15-25; colophony, 15-25. Method involves applying ointment by thin layer 0.5-3 mm on dense cotton fabric, its applying to damaged site, keeping and removing ointment with change of bandage 1-3 times per 24 h for 3-14 days. Method provides enhancing the therapeutic effectiveness of ointment due to significant acceleration the healing process of suppurative wounds and insidious furuncles being the ointment doesn't cause irritating effect.

EFFECT: improved and valuable medicinal properties of ointment.

2 cl, 4 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to medicinal preparations used for treatment of suppurative wounds. Invention involves applying boric acid (powder) and multi-component ointments on water-soluble base (Laevomecolum or Laevosinum) taken in the ratio 1:10 and used for treatment of suppurative wounds. Invention provides the development of agent exhibiting the expressed antibacterial, dehydrating and necrolytic effect.

EFFECT: valuable medicinal properties of agent.

2 ex

FIELD: medicine, in particular homoeopathic ointment for treatment of hemorrhoids, dermatitis and rhinitis.

SUBSTANCE: claimed ointment includes Calendula D 1, Hamamelis D 1, Aesculus D 1, and menthol as active ingredients and zinc oxide and vaseline as ointment base in specific ratio. Ointment of present invention makes it possible to improve microcirculation and cell respiration in tissues, to reduce venous engorgement, to increase immunity, to stimulate regeneration processes.

EFFECT: ointment for treatment of hemorrhoids, dermatitis and rhinitis of improved effect.

1 tbl

FIELD: pharmaceutics.

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

EFFECT: higher efficiency.

21 cl, 6 dwg, 5 ex, 5 tbl

Up!