Pharmaceutical composition with antidepressant activity
(57) Abstract:The composition includes, by weight. %: as the active substance - ()-fluoxetine 8,5-30,0, as auxiliary substances microcrystalline cellulose is 60.0 to 90.0, Aerosil 0.5 to 10.0 and a salt of stearic acid 0.1 to 1.5. Preferably the composition is in the form of hard gelatin capsules. A new pharmaceutical composition with antidepressant activity easily releases the active substance and stable during long term storage. 1 C.p. f-crystals, 2 tab. The invention relates to medicine, specifically to pharmaceutical compositions for the treatment of depressions of different etiology and severity of bulimic neurosis (to reduce appetite), obsessive-compulsive disorders.Fluoxetine (or) N-methyl--[4-(trifluoromethyl)phenoxy]phenylpropylamine hydrochloride), an antidepressant belonging to the group of selective inhibitors of neuronal serotonin uptake [Mashkovsky M. D. Medicines, T. 1, ed. 13th, Kharkov: Torsing, 1997, S. 102]. Being selective and reversible inhibitor of the reuptake of serotonin, fluoxetine improves your mood, eliminates the feeling of fear and tension, disformal, containing as active substances 3 aryloxy-3-phenylpropylamine, including fluoxetine, in the amount of 1-50 mg per single dose (U.S. patent N 4194009, 1980). The composition may be in the form of solid dosage forms (tablets, capsules or solution. However, the specific composition of auxiliary substances not listed.In the international application WO 93/09769, 1993, describes a pharmaceutical composition (prototype), which is made in the form of capsules and includes, in wt.%:
Active substance - 8,0-16,0
Lactose - 44,6-52,6
Corn starch - 15,0,
Magnesium stearate - 0,4
As active substances the product contains an optical isomer S (+)-fluoxetine, which is not absolutely identical in show pharmacological effect ()-fluoxetine, a mixture of R and S isomers.In addition, the application of the composition on the basis of the optically inactive fluoxetine inactive ingredients in the specified qualitative and quantitative ratio, mainly starch, hinders the absorption rate of the active substance from the dosage form.The task of the invention is to provide pharmaceutical compositions with an optimal combination of auxiliary substances is against the specified task is the new pharmaceutical composition with antidepressant activity easily releases the active substance and stable during storage.This technical result is achieved by the fact that the proposed pharmaceutical composition comprising as active substances ()-fluoxetine and as excipients salt of stearic acid, also contains microcrystalline cellulose and are presented in the following ingredients, wt.%:
()-Fluoxetine - 8,5-30,0
Microcrystalline cellulose is 60.0 to 90.0,
Aerosil - 0.5 to 10.0,
Salt stearine acid is 0.1 to 1.5,
The claimed ratio of ingredients is best found experimentally. As a salt of stearic acid can be used stearates of calcium, magnesium, zinc or other metals. Due to the claimed invention, the dosage form is capable of releasing into the environment dissolution of more than 96% of active substance per 45 min (Gasfurnace XI edition (GF XI) - not less than 75.0 per cent). Raspadaemost new members - 4-6 min (GF XI - not more than 20 min). The inventive composition has a high stability after 2 years of storage the content of impurities does not exceed 1.0% (from massiv.Pharmacokinetic study of a new composition were conducted in healthy volunteers aged 20-55 years with body mass 45-85 kg in the absence of chronic diseases and allergies to ()-fluoxetine. All subjects were previously exposed to General examination and research. Subjects previously (within 2 weeks) did not receive similar drugs and did not take other medicines during the study. Each volunteer in the morning on an empty stomach took 2 capsules of the drug (40 mg, calculated on the basis of ()- fluoxetine) who drank 100 ml of water at room temperature. Found that the new composition of bioequivalence known, the concentration of the ()-fluoxetine in blood within 1 hour after administration of equivalent doses of the active substances was proposed composition 65% higher than the comparison drug.The proposed pharmaceutical composition is in the form of solid dosage forms, preferably in the form of capsules, which allows you to mask the unpleasant bitter taste of the active substance and provides simplicity and ease of filling and subsequent use of the drug patients.Obtaining the inventive pharmaceutical composition may be the and ingredients optionally sieving the mixture and subsequent kapsulirovaniem.The obtained pharmaceutical composition complies with the requirements of the global Fund XI (in appearance, raspadaemosti, dissolution, uniformity of dosage, microbiological purity and other parameters), stable in storage and has a shelf life of at least 2 years.The invention is illustrated by the following examples (see table 1):
Example 1. In a clean, dry mixer sequentially load the previously sifted powders ()-fluoxetine (22,36 g of 18.6 wt.%), microcrystalline cellulose (90,5 g, 75,4 wt.%), Aerosil (6.0 g, 5.0 wt.%) and stearate (1.2 g, 1.0 wt.%) and mix thoroughly until smooth, then capsulebuy in hard gelatin capsules.The obtained capsules meet the requirements of the pharmaceutical agent. The results of the analysis are presented in table 2.Examples 2-4 perform similarly (table 1). The obtained capsules meet the requirements of the pharmaceutical agent. 1. Pharmaceutical composition with antidepressant activity, comprising as active substance fluoxetine and as excipients salt of stearic is as fluoxetine - ()-fluoxetine in the following ingredients, wt.%:
()-Fluoxetine - 8,5 - 30,0
Microcrystalline cellulose is 60.0 to 90.0
Aerosil - 0,5 - 10,0
Salt of stearic acid is 0.1 to 1.5
2. The pharmaceutical composition under item 1, characterized in that it is made in the form of hard gelatin capsules.
FIELD: medicine, gastroenterology, pharmacy.
SUBSTANCE: invention relates to a pharmaceutical composition used in treatment of changed gastroenteric contracting capability. The composition comprises tegaserod and co-agent taken among the group including prucaloprid, fluoxetine, fedotosine, baclofen, octreotide, omeprazol and ranitidine. The combination provides attainment of synergetic effect.
EFFECT: improved and valuable medicinal properties of composition.
7 cl, 3 ex
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to using a pharmaceutical preparation comprising beta-blocking agent in the maintenance dose less 50 mg, in particular, in the range from 25 mg to 47 mg in mixture with a pharmaceutically acceptable adjuvant, vehicle or carrier. The preparation is used in treatment of atherosclerosis and diseases associated with thereof. Invention provides decreasing dose of the preparation.
EFFECT: improved using method.
6 cl, 3 tbl, 1 ex
SUBSTANCE: invention proposes pharmaceutical compositions consisting of multiple particles with sustained-release of serotonin reuptake selective inhibitor (SRSI) with membrane cover comprising ammonium-methacrylate copolymer, or compositions comprising SRSI particles mixture, or compositions comprising SRSI particles mixture in form of sustained-release of SRSI, Also, invention relates to method for treatment of depression involving administration of these compositions. In particular, SRSI represents fluoxetine, fluvoxamine, sertraline or their salt. Proposed compositions provide a less index of fluctuations that reflects lower values of maximal concentrations of substance in plasma blood after multiple administrations, safety and good tolerance also.
EFFECT: improved medicinal and pharmaceutical properties of compositions.
11 cl, 5 dwg, 26 tbl, 6 ex
FIELD: medicine, narcology, biochemistry, pharmacy.
SUBSTANCE: invention proposes using the combination of dextromethorphan and the second medicine (quinidine, yohimbin, haloperdol, adjmaline, lobeline, pipamperon, fluoxetine, labetalol, chlorpromazine, domperidone, nortryptiline, quinine, oxyprenolol, propranolol, timolol, methaprolol, diphenhydramine, papaverine, mexiletine or their salts or isomers) for removing addiction to opiates, opioids or synthetic narcotics with exception cocaine and barbiturates (help in refusal in their using) or in case of chronic using antidepressant and corresponding treatment methods. The proposed combination of drugs reduces pain and relieves the withdrawal syndrome on the background of reducing morphine dose (antidepressant) up to the complete removing their intake.
EFFECT: enhanced effectiveness and valuable medicinal properties of medicine combinations.
54 cl, 2 ex
FIELD: medicine, pharmacology.
SUBSTANCE: the present innovation deals with correcting affected erythropoiesis in case of severe hypoxia. One should fulfill subcutaneous single injection of propranolol for laboratory mice on the 2nd d after hypoxia modeling at the dosage of 5 mg/kg. The innovation enables to improve the dynamics for reconstructing cellularity and qualitative values of erythroid source of blood formation, increase the number of erythrocytes in peripheral blood at decreasing the production of their pathological forms due to preventing the lesion of commitment precursor cells of erythropoiesis in post-hypoxic period.
EFFECT: higher efficiency of correction.
3 ex, 3 tbl
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to tablet containing cetirizine and pseudoephedrine used in treatment of allergic disorders. Invention relates to a tablet comprising two separate layers. Invention relates to combinations of two pharmaceutical substances representing cetirizine and pseudoephedrine prepared in the weight ratio pseudoephedrine to cetirizine = 12-30. Pseudoephedrine-containing segment comprises inert pharmaceutical excipients and an alkalinizing agent. Pharmacokinetics patterns of cetirizine and pseudoephedrine are similar practically with pharmacokinetic pattern of medicinal preparations containing each of these components taken separately in the same doses. Invention provides the development of combination of pharmaceutical substances useful in treatment being without adverse effects.
EFFECT: improved and valuable medicinal properties of tablet.
44 cl, 5 tbl, 3 ex