Pharmaceutical composition containing hyaluronidase and liposomes for external application |
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IPC classes for russian patent Pharmaceutical composition containing hyaluronidase and liposomes for external application (RU 2417097):
 Anti-inflammatory and antibacterial drug / 2413527
Invention refers to chemical-pharmaceutical industry, namely to development of an anti-inflammatory and antibacterial drug representing a dry polyextract containing dry extracts of the following herbal raw material: Indian kidney tea (leaves), bearberry (leaves), knotgrass (herb), pot marigold (blossom), Ural licorice (root).
 Fermented milk or vegetable proteins, containing receptor ligand, and their application / 2403051
Invention relates to medicine and can be used for manufacturing product for treatment or prevention of benign hypertrophy of prostate and/or erectile dysfunction in mammals. Product is obtained by fermentation of food material, which contains animal milk, in presence of at least one strain of Lactobacilli. Obtained milk serum is used for treatment or prevention of said pathology.
 Method of treating chronic prostatitis / 2400269
Invention relates to medicine and can be used for treatment of chronic prostatitis. For this purpose at the background of intake of medications acoustic therapy of prostate with weak-focused shock-wave acoustic pulses is carried out. Amplitude of pressure is within the range 5-90 bar with pulse duration not longer than 2 mcs. Size of focal area of focusing does not exceed 50 mm, depth of shock wave penetration being 150 mm.
 Alpha-aminoamide derivatives used for treating lower urinary tract disorders / 2395504
Invention relates to use of a therapeutic agent which is an α-amino-amide compound of formula (I):
 Nonsteroid modulators of androgen receptor, method of production, pharmeceutical composition thereof and use / 2378250
Invention relates to novel nonsteroid synthetic derivatives with the following structures or their pharmaceutically acceptable salts:
Method of chronic prostatitus treatment / 2370256
Invention relates to medicine, namely - to urology. On background of traditional treatment carried out is influence on prostate gland by chaotically changing magnetic field. Influence is rectal, with frequency 1 - 2000 Hz, strength 15-20 E. Duration of session 10-15 minutes. Preliminarily 1-2 hours earlier biologically active points selected from line E27, E28, E29, E30, R11, R12, R13, R14, VC2, VC3, VC4, V28, V31, V32, V33, V34, VG4 are influenced. Influence is performed by current of negative polarity, with intensity 50-100 mcA, voltage 9 V, after that suppository Vitaprost is introduced rectally.
 C-6 modified indazolyl pyrrolotriazines / 2356903
Described are C-6 modified indazolyl pyrrolotriaxolines of formula I
Method of vesicular prostate complex disease treatment involving cryotherapy / 2349291
Invention concerns medicine, urology, and can be applied in vesicular prostate complex disease treatment. It involves placing patient into cryothermic chamber and exposed to heat carrier vapour based on liquid nitrogen for 2-3 minutes. Temperature within -140°C to -180°C is maintained inside the chamber. Cryotherapy course includes 10 daily sessions by one per day. Cryotherapy course is applied in conservative complex therapy of disease in decadent exacerbation or instable remission phase.
Treatment method for chronic prostatitis / 2344853
Method includes: exposure to LED radiation and constant magnetic field, on prostate gland projection per rectum; balneotherapy; magnetotherapy on pubis, sacrum, and perineum. Additionally, peat applications, sodium chloride bathes, rectal sapropelic tampons, and exposure to sinusoid modulated current are conducted. Treatment is conducted during periods from March to April and from October to November. Peat applications are conducted on "pantie" area, from 9 to 12 o'clock, at temperature 38-40°C, during 20 to 30 minutes, every other day. Peat applications are alternated with sodium chloride bathes, from 14 to 16 o'clock, at temperature 37-38°C, during 10 to 12 minutes. On first 10-12 days period, rectal exposition to blue and infrared LED radiation combined with magnetic field is conducted on prostate gland projection, during 10 to 12 minutes daily. On next 10-12 days period, rectal magnetised sapropelic tampon exposition is conducted, tampon volume being 140 to 160 ml, at temperature 37-38°C, during 20 to 30 minutes. Simultaneously, sinusoid modulated current is applied by perineal-sacral technique. Treatment course length is 21 to 24 days.
Means for treatment of chronic prostatitis / 2342940
Means for treatment of chronic prostatitis contains the active substance including a complex of water-soluble peptides, allocated from prostate gland of livestock, and glycine in the ratio 1 : 2; the carrier including dimethyl sulfoxide and a softener, thus it is executed in the form of an ointment, the carrier contains an emulsive basis including softener, distilled monoglycerides and purified water, and in addition contains preservative.
Immunocorrective agent for treating diseases of viral aetiology / 2411039
Invention refers to pharmacology and medicine. Substance of the invention consists that an immunocorrective drug exhibiting an intense specific antiviral activity for treating diseases of viral aetiology contains human recombinant interferon alpha and/or beta, and/or gamma, an antioxidant complex of tocopherol acetate or its derivative, including water-soluble ones, and ascorbic acid salts, calcium pantothenate, antiviral ingredients, as well as pharmaceutical aids and excipients in certain ratios in 1 g of the drug. As antiviral ingredients, the drug contains arbidol and its derivatives, remantadin, oseltamivir, ribavirin, inosine pranobex (isoprinosine), glycyrrhizic acid and its derivatives, nucleosides of a group - famvir, valacyclovir, ganciclovir, valganciclovir, foscarnet, cidofovir, lobucavir, sorivudine, brivudine, antiretroviral - lamivudine, zidovudine, lopinavir, stavudine. The agent is presented in rectal and vaginal suppositories, gel, ointment, liquid.
Drug preparation tilorone in suppositories / 2411032
Invention refers to a pharmaceutical industry, and concerns making a preparation Tilorone in the form of rectal suppositories 125 mg, being an antiviral immunostimulant.
 Food additive for supply of nutritional mineral substances / 2409991
Food additive characterised by the minerals it contains being a component of a salt hydrate melt in the form of ions, the said nutrient substances represented by at least calcium; the salt hydrates melt is amorphously hardening and is represented by a salt-water system with water content in the food additive corresponding to the most hydrated ion coordination number. The food additive is used as admixture during production of food products, chewing gum, beverages, toothpaste, mouth wash liquids and oral cavity hygiene products. The nutrient mineral substances are easily digestible due to their containment in the additive in ion form.
Method of treating chronic prostatitis / 2408378
Invention refers to medicine, namely to urology, and can be used for treating chronic bacterial non-Chlamidia prostatitis. That is ensured by the integrated treatment that involves antibacterial therapy and administration of Interferon A in the form of ointments or suppositories. The therapeutic course is 7 days to be repeated in a week.
 Application of octenidine dihydrochloride in semisolid preparations / 2408372
There is offered application of octenidine dihydrochloride for making a semisolid pharmaceutical compositions for wound repair, treatment of atopic dermatitis, infected eczema, dermatomycosis, vaginal infections, acne, herpes and/or control of pathogenic germs resistant to many medicinal preparations where the composition contains 0.005 to 5 wt % of octenidine dihydrochloride, propylene glycol, hydroxypropyl cellulose and water.
Homoeopathic suppositories for treating genital disorders / 2402346
Invention refers to pharmaceutical industry, particularly to homoeopathic suppositories. Homoeopathic suppositories contain black walnut oil, walnut oil, homoeopathic oily extract of sea-buckthorn, melilot herb, sage herb, acacia blossom taken in equal portion, homoeopathic essence of black walnut, oily extract of Peloid mud of the Tambukan lake and a base taken in a certain ratio.
Pharmaceutical composition for treating urogenital infections / 2401102
Offered pharmaceutical composition for treating urogenital infections in a unit dosage form contains antiseptics, a biologically active additive, an ingredient for natural vaginal acidity, an antifungal agent, an anesthetic and a base. Even in minimum dosage, the pharmaceutical composition exhibits an effective action for treating urogenital infections since it has a wide spectrum of antimicrobial action, such as antiseptic and antifungal, removes painful symptoms of urogenital infections, normalises a disturbed microflora and ensures a regenerative effect.
 Pharmaceutical composition for treatment of dysplastic processes of cervix / 2395281
Invention relates to field of medicine, pharmaceutical industry and deals with novel medications used for treatment of dysplastic processes of the cervix and rectum mucosa. Medication for treatment of dysplastic processes of the cervix and rectum mucosa, in form of suppository is characterised by the following: it contains 3,3'-diindolylmethane, epigallocatechin-3-gallate, as well as catalyst of epigallocatechin-3-gallate inhibiting activity with respect to DNA-methyltransferases, representing cations Mg2+ in form of pharmaceutically acceptable magnesium salt, lipophilic base, which contains hard fat, polyvinylpyrrolidone and butylhydroxyanisol and/or butylhydroxytoluol.
Complex api preparation in form of suppositories for treatment of andrological diseases and method of obtaining it / 2376978
Group of inventions relates to pharmaceutical industry, medicine and concerns composition, obtaining and application of original complex API preparation in form of rectal suppository. Claimed is complex natural preparation in form of suppository for treatment of andrologic diseases which contains ambrosia or bee-bread, cocoa butter or other fat base, preparation additionally contains homogenised larvae of queen bee with native royal jelly or lyophilised powder from homogenised drone larvae and drone jelly. Claimed is method of obtaining suppository including homogenisation of queen bee larvae and native royal jelly preliminarily frozen at temperature -21°C, and further unfrozen at +5-8°C and extracted from ovaries or lyophilisation of homogenised drone larvae and drone jelly, addition to obtained mass of crushed bee-bread or ambrosia, step-by-step mixing of said fractions with cocoa butter or other fat base until hoimogeneous suppository mass is obtained, formation of suppositories with 3.0 g weight, cooling, packing, marking. Claimed is method of treating patients with andrologic diseases by means of suppositories.
Pharmaceutical composition for treating urogenital diseases / 2375064
Invention refers to medicine and concerns production of a pharmaceutical composition for treating urogenital diseases in women. The composition contains estriol, antiseptics, particularly chlorhexidine bigluconate, or nonoxynol, or miramistin, biologically active additive, particularly Dexpanthenol, or tocopherol acetate, or camomile extract, or vegetable or animal phospholipid, or retinol palmitate, or phylloquinone, or horsetail extract, or winterbloom extract, or nettle extract, an anaesthetic, particularly lidocaine, or benzocaine, or mepivacaine, or procaine, or cinchocaine and a suppository base. As a suppository base, the composition contains vitepsol, or solid fat, or polyethylene oxide.
 Method for making sterilised powdered pancreatine / 2413532
Invention refers to pharmacology and represents a method for making pancreatine including heating of a dispersed form of pancreatine containing one or more solvents at temperature at least 85°C for 48 h to ensure total concentration of solvents in the dispersed form of pancreatine equal or less than 3.5 wt % at any moment of said heating process, while the dispersed form of pancreatine is specified from powder, pellets, micropellets, microspheres, granules and granulates.
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FIELD: medicine, pharmaceutics. SUBSTANCE: invention refers to pharmacy, namely to a pharmaceutical composition for local application, containing enzyme hyaluronidase which can be used in pharmacy for treatment and prevention of inflammatory prostate diseases, such as prostatitis. The pharmaceutical composition for local application contains as an active ingredient hyaluronidase 2.44 wt %, Tween-80 2.93 wt %, PEG-1500 91.69 wt %, liposome 2.44 wt %, and pharmaceutically acceptable carriers or excipients, such as benzydamine 0.5 wt %. EFFECT: invention provides treatment and prevention of inflammatory prostate diseases, such as prostatitis. 1 tbl, 2 ex
The present invention relates to the pharmacy, and in particular to pharmaceutical compositions for topical application in the form of suppositories containing the enzyme hyaluronidase, which can be used in pharmacy for the treatment and prevention of inflammatory diseases, such as hemorrhoids, prostatitis and paraproctitis. Known medicines for local use, used for the treatment of chronic prostatitis, contains anti-inflammatory components, which are not enzymes, for example, extracts of medicinal plants (Prostanorm CJSC "Farmville" (Russia). Known drug Tantum Verde in the form of a solution for rinsing; dispersible tablets; powder, aerosol, gel, including anti-inflammatory component benzydamine and not containing liposomes and hyaluronidase (Mashkovsky PPM Medicines. - 15-ed., added, Corr. and extra - M.: New Wave, 2006. - s). Known pharmaceutical enzyme-containing composition comprising a hyaluronidase covalently-linked with polyoxidonium (LOGIDATA, suppositories for vaginal and rectal injection of 3000 ME, OOO "NPO PETROVAX PHARM"). Described composition does not contain liposomes, which ensures rapid absorption, extension, and controlled release of the enzyme, and therefore, has no advantage is the EU ETS claimed composition. Known for immobilization of various substances in liposomes (liposomes and other nanoparticles as a means of drug delivery. Questions of medical chemistry. Kaplun A.P. No. 1, 1999, available online http://medi.ru/pbmc/8890101.htm - D1), where we offer traditional media provide mainly stabilizing the forms, unlike vistavlennij composition, providing not only stabilization, but controlled release of hyaluronidase. Known suppositories, in particular for the treatment and prevention of prostatitis, which include PEG-1500, tween-80, carriers and excipients, when this dosage form is stable for 2 years of storage (Kozlova ZH.M., etc. Creating rectal suppositories with amaranth oil. Herald of the Voronezh state University, series a: Chemistry, Biology, pharmacy, 2008, No. 1 - 3. Pharmaceutical compositions containing the enzyme hyaluronidase, and liposomes for topical application in the form of suppositories in the treatment and prevention of inflammatory diseases, such as hemorrhoids, prostatitis and paraproctitis, not described. Thus, the present invention is that for the first time to offer a pharmaceutical composition for topical application in the form of suppositories controlled release of the active substance containing the enzyme hyaluronidase and liposomes, which m which can be used for the treatment and prevention of inflammatory diseases, such as hemorrhoids, prostatitis and paraproctitis. The claimed technical result distinguishes the proposed composition from longitute that it does not contain hyaluronidase, chemically bound to a polymeric carrier - polyoxidonium, and provides physical and not chemical immobilization of the enzyme, resulting in controlled release of the active substance with an innovative mechanism of action. According to the present invention proposed a pharmaceutical composition for topical application in the form of suppositories containing as the active ingredient of 2.44 wt.% hyaluronidase, 2,93 wt.% tween-80, 91,69 wt.% PEG-1500, 2,44 wt.% liposomes and carriers or excipients, such as benzydamine 0.5 wt.%. As a preferred embodiment of the claimed invention proposed pharmaceutical composition in suppository specified above, optionally containing one or more anti-inflammatory ingredient. Most preferred is a pharmaceutical composition in the form of suppositories containing hyaluronidase as an active ingredient, benzydamine as an anti-inflammatory ingredient and pharmaceutically acceptable carriers and excipients, in the following ratio, wt.%:
The active ingredient of the claimed pharmaceutical compositions in the form of suppositories are liposomes and the enzyme hyaluronidase. Hyaluronidase has a specific ability to depolymerizing hyaluronic acid to glucosamine and glucuronic acid, increases the permeability of the tissues and facilitates the movement of fluids in the interstitial spaces (Mashkovsky PPM Medicines, Moscow, New Wave, 2006, str-661). Liposomes in the stated concentration can encapsulate all components of suppositories, the concentration of which is comparable with the concentration of liposomes (range: 0.5-2,93 wt.%), excluding, thus, the glycol, the concentration of which lies within 91,19-93,50 wt.%. Encapsulation in liposomes components suppositories provides stabilization and rapid penetration through cell membranes of cells at the injection suppositories, unlike covalently-linked with polyoxidonium hyaluronidase. For the preparation of compositions used in isout drug enzyme preparation "Hyaluronidase". The drug is derived from bovine testis by extraction of the crushed material, followed by purification and freeze drying. Lyophilized powder "Lydasum" is used in the form of injectable medicine for the treatment of contractures of the muscles in the eye practice to ensure a more subtle scarring of the affected cornea in the treatment of keratitis. With the aim of expanding the range of actions in pharmaceutical compositions for topical application in the form of suppositories offered benzydamine, which provides not only a holding action, but also inhibits the synthesis of prostaglandins, they are effective in bacterial and fungal infections. Hyaluronidase in the form of these drugs is not used for the treatment and prevention of inflammatory diseases of the prostate gland due to its difficulty of absorption through intact mucous and low level of consumer properties, as well as lack of stability at a moisture content of over 10% and in solution, with the loss of enzyme activity during the day. Suddenly discovered that the hyaluronidase and liposomes can be incorporated into a stable pharmaceutical composition in the form of suppositories for local use to preserve the activity of hyaluronidase in a long time. Pharmaceutical is th composition in the form of suppositories of the present invention are generally made by using common methods, using solid or liquid pharmaceutically acceptable carriers or excipients selected from emulsifiers, dispersing agents, preservatives, flavoring agents, pH regulators, polymeric carriers and other excipients, which are suitable for preparation of compositions for local application. Additional advantages of the specified composition are the introduction of the suppositories benzydamine, its ability to quickly penetrate through the mucous membrane and, accordingly, usability, and ease of dispensing. The rapid penetration through the mucosa due to the binding of hyaluronidase with liposomes, able to encapsulate the active substance. In addition, the active ingredients can be used in combination with benzydamine, providing an additional advantage of the claimed composition. The claimed pharmaceutical composition in suppository is stable in relation to the activity of hyaluronidase and its constituent active components during long-term storage, which is achieved by immobilization of hyaluronidase on the liposomes contained in the specified composition. The activity of the claimed compositions is due to the activity of its constituent agents. Discovered that the pharmaceutical composition is I for local application in the form of suppositories, containing hyaluronidase 2,44 wt.%, is stable in relation to the activity of the enzyme when it is long-term storage, while the activity of this enzyme prepared in the form of a solution, decreases rapidly. Therefore, the claimed composition can be used for the effective treatment and prevention of inflammatory diseases. The present invention is illustrated by the following examples. EXAMPLE 1 Pharmaceutical composition in the form of suppositories on the basis of hyaluronidase, benzydamine has the following composition:
The above composition is prepared by the following method. In liposomes dissolve benzydamine and hyaluronidase, the resulting solution is stirred. In the resulting solution contribute melt PEG-1500 and tween-80, having a temperature of 38°C, mix, mold and cooled. EXAMPLE 2 Pharmaceutical composition in the form of suppositories on the basis of hyaluronidase has the following is the structure:
The above composition is prepared as in EXAMPLE 1, wherein is included excluded benzydamine. Evaluation of stability of hyaluronidase in compositions for local application Since the main drawback of enzymes is their instability during long-term storage of finished dosage forms based on them within the expiration date was the comparative assessment of the preservation of enzyme activity during storage in solution and in the form of a composition for topical use (for example, suppositories). The hyaluronidase activity was determined by the following method. Per unit of the enzymatic activity of hyaluronidase take that amount of enzyme that releases 0.001 microequivalent glucosamine for one minute under given conditions determine. The suppository is dissolved in 5 ml of acetate buffer solution. Two tubes (experimental sample) add 0.1 ml of the investigated solution and 0.2 ml of acetate buffer solution. In a third test tube (entry checkpoints for important locations the I sample) add 0.3 ml of acetate buffer solution. The tubes are placed in a thermostat at a temperature of 37±0.1°C and incubated for 5 minutes, then all of the tubes in series, with an interval of 30 seconds (stopwatch) was added to 0.2 ml of substrate solution. The mixture is incubated for 15 minutes (stopwatch) in a thermostat at a temperature of 37±0,1°C. After incubation, all tubes for 5 minutes, placed in a bath of ice. Cooled samples sequentially with an interval of 30 seconds (stopwatch) add calculated titer of 0.8 M solution of potassium tetraborate and 3 minutes (stopwatch) placed in a boiling water bath. Then the tubes for 5 minutes, placed in a bath of ice. In chilled tubes poured in 3 ml of diluted reagent Ehrlich and incubated in a thermostat at a temperature of 37±0.1°C for 20 minutes (stopwatch). After incubation, the sample is cooled to room temperature and measure the optical density of solutions (experimental samples) on the spectrophotometer at a wavelength of 586 nm in a cell with a layer thickness of 10 mm as the reference solution using a control sample. Simultaneously measure the optical density of the solution of N-acetyl-D - glucosamine, to which 0.5 ml of a solution of N-acetyl-D-glucosamine was added to the titer calculated amount of 0.8 M solution of potassium tetraborate, placed in a boiling water bath for 3 minutes (stopwatch), and further progress is jut, as explained above. As the reference solution using a control sample. The results are shown in the following table.
As can be seen from the table, the introduction of the enzymes in the composition for local application allows to obtain a stable pharmaceutical composition for topical application in the form of suppositories in the treatment and prevention of inflammatory diseases of the prostate. Despite the fact that with the introduction of the enzymes in the composition of these songs is a minor loss of enzyme activity, with further storage for 2 years, enzymes do not alter their activity due to physical stabilizes and labile structure of the enzyme used by nanoneedles. Pharmaceutical composition for topical application, which can be used in inflammatory diseases of the prostate, in the form of suppositories containing as the active ingredient of 2.44 wt.% hyaluronidase, 2,93 wt.% tween-80, 91,69 wt.% PEG-1500, 2,44 wt.% liposomes and carriers or excipients, such as benzydamine 0.5 wt.%.
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