Transnasal microemulsions containing diazepam
SUBSTANCE: invention relates to medications and concerns microemulsion for transnasal diazepam introduction, including carrier, which contains water, fatty acid ester, hydrophilic surface-active substance, polar solvent and alcohol, fatty acid and water are contained in carrier in approximately equal amounts, contained amount of alcohol exceeding amount of each of surface-active substance and polar solvent. Also described is method of transnasal diazepam introduction to patient who needs it.
EFFECT: quick beginning of active substance action and improvement of absorption.
16 cl, 1 tbl
The technical field
This invention relates to pharmaceutical compositions for delivery of diazepam through the mucous.
The level of technology
Status epilepticus is a neurological disease in which the mortality ranges from 3 to 35%. The main goal of treatment is the rapid regulation of pathological activity convulsions; the longer status epilepticus is not exposed to the treatment, the harder it is to control and the greater the risk of permanent brain damage.
Thus, for the patient's critical is a clear plan, including appropriate treatment effective drugs in adequate doses, with a suitable pharmaceutical composition, as well as the attention hypoventilation and hypotension. Currently, for the treatment of epileptic status employing multiple treatment regimens. For this purpose one of the most commonly used benzodiazepine is diazepam. Intravenous administration of anticonvulsants is the fastest way to suppress epileptic convulsions. However, when intravenous administration is not desirable and is deposited, for example, due to technical difficulties such as the need for sterile equipment and qualified personnel, and because of the possible development of thrombophlebitis can be very desirable other route of administration. To the ome, intravenous administration is often associated with hypotension, cardiac arrhythmia and depression of the Central nervous system. Consequently, Moolenaar et al., Int. J. Pharm., 5: 127-137 (1986) tried to introduce people diazepam several other routes, such as intramuscular injection, in the form of oral tablets and rectal solution. It turned out that only rectal introduction provides a fairly rapid absorption and therefore can be considered as alternative IV injection method injection. However, the rectal route is very inconvenient, especially in urgent cases. In U.S. patent 4863720, Burghardt described sublingual spray pharmaceutical drug in which the drug can be a benzodiazepine, optimally containing polyethylene glycol (PEG) and ethanol, di - and/or triglyceride of fatty acids and pharmaceutically acceptable propellant.
Recently it was found that the mucous membrane of the nose is a practical way of introducing many medical substances. Vnutripuzarnoe introduction has the advantage that the drugs can be introduced easily to achieve systemic or localized effect. However, the main problem with the intranasal drug administration is the fact that most of the molecules of the drug diffuses slowly and poorly through the nasal mucous membrane and therefore desirable level terapeuticas the th agent cannot be achieved simply by transnasal administration. An additional disadvantage is that the introduction is limited to a small amount, i.e. usually you cannot enter more than approximately 150 ml per nostril. Amounts exceeding specified, will flow into the throat and proglatavetsa.
Therefore, there is a need to solvents - mediums, which dissolve the desired drug, namely diazepam in a high concentration and yet do not irritate the nasal mucosa. Intranasal absorption of a drug can be increased sovmestnim the introduction of chemical adjuvant or accelerators permeability. For example, Lau and Slattery [Lau et al., Iit. J. Pharm., 54: 171-174 (1989)] was trying to enter a benzodiazepine, such as diazepam, by dissolving it in a number of solvents: triacetin, dimethyl sulfoxide, PEG 400, Cremophor EL, Lipal-9-LA, isopropylacetate and Azone. Although many of the solvents was dissolved diazepam in desirable concentrations, they irritated mucous and could not be used for transnasal administration. It was found that Cremophor EL less all irritate the nose, but nasal absorption in the case of the use of the media was very slow (Tmax≈1,4 h) and the peak concentration was lower than after IV injection.
Transnasal solution with improved properties described in the application U.S. 09/624305. The media for this solution is an aqueous medium containing aliphatic the cue alcohol C 1-C5, glycol, such as propylene glycol, and biological surfactant selected from the salts of bile acids and lecithins. These solutions preferably contain equal amounts of alcohol and glycol. It has been found that such solutions are effective for transnasal the introduction of certain drugs, particularly benzodiazepines. Recently, Li et al., Int. J. of Pharmaceuticals, vol.237, p.p.77-85, 2002, described microemulsions for fast delivery of diazepam through the nose. Microemulsions of diazepam, such as those described in Li et al., but possessing improved properties provided by the present invention.
According to this invention provides new compositions of microemulsions containing diazepam. Diazepam is injected intranasally in the form of microemulsions, which have better properties as compared with such emulsions are known from the literature. Microemulsions are composed of approximately equal amounts of ether, fatty acid and water, and the rest is hydrophilic surface-active agent, a polar solvent and an alcohol, preferably an aliphatic alcohol in the weight ratio providing alcohol in larger quantities than the amount of any of the other two components. Nasal introduction of the proposed microemulsions provides a high concentration of diazepam in plasma is e almost as fast as intravenous. These micro-emulsions are particularly suitable for rapid and timely treatment of patients in acute and/or urgent treatment of epileptic status and other seizures caused by fever.
Detailed description of the invention
According to this invention provides a microemulsion containing diazepam, which has advantages compared to microemulsions, are known from the literature. The microemulsion diazepam, described by Li et al., characterized by the content of acellerate about 15 wt.% and comparable water content. The compositions also contain an aliphatic alcohol, namely ethanol, glycol, namely propylene glycol, and Polysorbate 80, namely polyoxyethylene (20)-servicemanual. In one of the compositions described in Li et al., the concentration of ethanol is about one quarter of the concentration of each of glycol and Polysorbate 80. Another weight ratio of the three components is the same. It is argued that the composition in which the weight ratio of the alcohol, glycol and Polysorbate 80 is 1:1:1, exceed the properties of the composition with a lower alcohol content compared with quantities of glycol and Polysorbate 80.
According to this invention provides compositions with a low content of polar solvent, such as glycol, even compared with the best composition described in Li et al. Yes is it in contrast to the compounds described by Li et al., the compositions according to the invention are characterized by the alcohol content greater than the amount of the polar solvent and the hydrophilic surfactants (e.g. Polysorbate 80) separately. These compositions have the best properties regarding at least one of several criteria, such as described by Li et al., and it is the speed of the commencement of the active substance, solubilization of diazepam, particle size and in vivo absorption. The compositions of this invention contain about equal quantities of water and fatty acid ester, preferably at least 10 wt.% each, more preferably about 10-25 wt.% each and most preferably about 15 wt.% everyone else is surface-active hydrophilic substance, a polar solvent and an alcohol, and alcohol is always present in greater numbers than the other two components. Suitable fatty acid esters include, without limitation, tillaart, atelierista, Etisalat, ethyllinoleate, proprietorial, isopropylene, isopropylmyristate and combinations thereof. Particularly preferred fatty acid ester is tillaart. Suitable hydrophilic surfactants include, without limitation, TWEEN 80 (POLYSORBAT 80), TWEEN 20, 40, 60, and combinations thereof. Suitable polar solvents is clucalc, without limitation, propylene glycol, polyethylene glycols such as PEG 300, PEG 400, PEG 600, and combinations thereof. Particularly preferred alcohols include lower alkanols, such as ethanol and isopropanol. You can use any aliphatic alcohol containing from 2 to 12 and, more preferably, from 2 to 8 carbon atoms. Particularly suitable alcohol is ethanol.
According to one preferred variant compositions according to the invention contain equal amounts of water and acellerate, preferably about 15 wt.% everyone else are Polysorbate 80, polypropylenglycol and ethanol, and the ethanol content of these three components is always greater than the content of the other two.
Compositions containing tillaart, according to the invention may include Polysorbate 80: polypropylenglycol: ethanol in a weight ratio 1,0:0,86:1,15; 1,0:0,72:1,29 and 1,0:1,0:1,5. Specific examples of the compounds shown in the Table, where the content of each component is indicated in percent by weight. These examples serve to illustrate but not limit the invention.
|Component||Composition (% weight/weight)||Composition (% weight/weight)||Composition (% weight/weight)|
These emulsions receive the usual way. First diazepam is dissolved in acellerate, which is the oil component. The emulsion obtained two-phase and have a good spatter due to a higher content of ethanol. Diazepam is dissolved in the proposed emulsions at a concentration of about 40 mg/ml Therefore, the introduction of therapeutic doses of diazepam intranasally by one or two clicks in the nostril using a suitable conventional spray containing 250-500 ál of microemulsions.
From a clinical point of view intranasal introduction often provides greater duration of anticonvulsive effect. Therefore, the microemulsion according to the invention is preferred in the treatment of epileptic status and other conditions, require fast suppression of convulsions. The high content of water in these emulsions compared to the solutions described above, leads to more rare irritation of the nasal tissues. Although this invention is described for diazepam as anticonvulsant, it is obvious that the proposed emulsion can be applied to other recognized therapeutic substitutes diazepam.
This invention is not limited to the described specific examples. Indeed, in addition to described various modifications of the invention are evident from the description. Such modifications are included in the scope of this invention defined by the claims.
1. The microemulsion for transnasal administration of diazepam, comprising a carrier containing water, a fatty acid ester, a hydrophilic surfactant, a polar solvent and alcohol, and the fatty acid and water contained in the carrier in approximately equal amounts, and the alcohol contains in excess of the amount of each surfactant and a polar solvent.
2. The microemulsion according to claim 1, characterized in that the fatty acid ester is selected from the group consisting of acellerate, atelierista, aterballetto, ethyllinoleate, profiletemplate, Isopropylamine, isopropylmyristate and the x combinations.
3. The microemulsion according to claim 1, characterized in that the hydrophilic surfactant selected from the group consisting of Polysorbate 80, Tween 20, 40, 60, and combinations thereof.
4. The microemulsion according to claim 1, wherein the polar solvent is selected from the group consisting of propylene glycol, polyethylene glycol and combinations thereof.
5. The microemulsion according to claim 4, characterized in that the polyethylene glycol is selected from the group consisting of PEG 300, PEG 400, Peg 600, and combinations thereof.
6. The microemulsion according to claim 1, wherein the alcohol is selected from the group consisting of ethanol, isopropanol and combinations thereof.
7. The microemulsion according to claim 1, characterized in that the fatty acid ester and water are individually not less than 10% by weight of the carrier.
8. The microemulsion according to claim 1, characterized in that the fatty acid ester and water are separately about 10-25% by weight of the carrier.
9. The microemulsion according to claim 1, characterized in that the fatty acid ester and water are separately about 15% by weight of the carrier.
10. The microemulsion according to claim 1, characterized in that it contains about 20 wt.% the specified hydrophilic surfactant and the weight ratio of the hydrophilic surfactant: the polar solvent: alcohol is about 1.0:1.0 to:1,5.
11. The way transnasal administration of diazepam to a patient in need of it, consisting in the introduction of diazepam in the microemulsion according to any one of claims 1 to 10.
12. The microemulsion for transnasal administration of diazepam, in which the medium contains tillaart, Polysorbate 80, propylene glycol, ethanol and water, each component of acellerate and water is 15% by weight of the carrier, and the weight ratio of Polysorbate 80: propylene glycol: ethanol is such that the number of alcohol more quantities of the other two components.
13. The microemulsion according to item 12, characterized in that it contains about 23,3% wt. Polysorbate 80 and the weight ratio of Polysorbate 80: propylene glycol: ethanol is 1.0:0,86:1,15.
14. The microemulsion according to item 12, characterized in that it contains about 23,3% wt. Polysorbate 80 and the weight ratio of Polysorbate 80: propylene glycol: ethanol is 1.0:0,72:1,29.
15. The microemulsion according to item 12, characterized in that it contains about 20 wt.% Polysorbate 80 and the weight ratio of Polysorbate 80: propylene glycol: ethanol is 1.0:1.0 to:1,5.
16. The way transnasal administration of diazepam to a patient in need of it, consisting in the introduction of diazepam in the microemulsion according to any one of p-15.
SUBSTANCE: invention refers to medicine, particularly to hot flush treatment in mammals, including human. Method involves (3S,5R)-3-aminomethyl-5-methyloctane acid or its pharmaceutically acceptable salt introduced in the patient organism in effective amount.
EFFECT: method provides treatment of moderate and severe vasomotor symptoms, including in post menopause in women, ensured by predominant high activity of the acid as alpha-2-delta ligand.
SUBSTANCE: invention relates to novel atropoisomers of formula , in which R and R1 each independently represents hydrogen or methyl; R2, R3 and R4 each independently represents hydrogen or trifluoromethyl, on condition that R2, R3 and R4 all do not represent hydrogen; and R5 represents bromine, chlorine; or to its non-toxic pharmaceutically acceptable salt, solvate. Invention also relates to pharmaceutical composition, as well as to method of treatment.
EFFECT: obtaining novel biologically active compounds, possessing properties which open calcium-activated potassium channels of high conductivity.
12 cl, 6 ex, 2 tbl, 7 dwg
SUBSTANCE: liquid pharmaceutical composition for peroral introduction contains pregabalin, at least, one preservative, at least, one substance masking taste, at necessity, a viscosity regulator. The composition has pH in a range from 5.5 to 7.0 and as preservative contains methyl paraben and ethyl paraben. Concentration of methyl paraben makes, at least, 2 mg/ml, and concentration of ethyl paraben - at least, 0.5 mg/ml.
EFFECT: invention provides obtaining of stable pharmaceutical composition of pregabalin with low level of chemical and microbiological impurity.
11 cl, 2 tbl, 9 ex
FIELD: medicine; pharmacology.
SUBSTANCE: pharmaceutical composition contains Topyramat as active substance and additives, including starch, lactose, microcrystalline cellulose, cross-linked polyvinylpyrrolidone and dusting agent. Preparation is produced by wet granulation technique in the form of coated tablets with 25 mg, 50 mg, 100 mg or 200 mg of Topyramat content.
EFFECT: fast decomposition, high reactant release and high durability, storage stability.
10 cl, 1 tbl, 3 ex
FIELD: medicine; pharmacology.
SUBSTANCE: composition includes effective amount of carbamazepine as active ingredient, and carbomer 71G, microcrystalline cellulose, sodium carboxymethylstarch, aerosol, and stearate salt as auxiliary ingredients. The composition is manufactured by direct pressing method, preferably in form of tablets.
EFFECT: composition stability during storage period, release profile reproducibility of active substance, satisfactory pharmacokinetic characteristics, and high strength of the tablets.
5 cl, 1 tbl, 4 ex
FIELD: medicine; pharmacology.
SUBSTANCE: presented is 8-trifluoromethylbenzo[f][1,2,3,4,5] pentatiepin-6-amine of formulas with anticonvulsant and antianxious activity, and can be used in medicine.
EFFECT: anticonvulsant and antianxious activity, lower toxicity, do not potentiate hypnotic action and manifest anticholinergic activity.
1 cl, 8 ex, 6 tbl
SUBSTANCE: invention relates to medicine, particularly to psychiatry; it can be applied in adult patient with disease duration 10 years and over, and symptomatic arterial hypertension. At arterial pressure (AP) maximum value of 160/100 mm Hg, and absence of hyperkaliemia and/or chronic renal impairment symptoms, standard anti-epileptic complex therapy is administered; if satisfactory response not obtained, additionally starting dose 2.5 mg of lisinopryl is injected, anti-epileptic drugs dosage being left unchanged. If the response is satisfactory, showing clinical remission or fits frequency reducing two times and more, anti-epileptic drugs dosage is lowered or anti-epileptic drugs monotherapy is administered.
EFFECT: eliminates chronic hypoxia of neural tissue, hypernatremia, hypokaliemia, neural tissue hyperhydration; allows anti-epileptic drugs dosage lowering.
3 cl, 4 tbl
SUBSTANCE: invention pertains to new substituted 2,3,4,5-tetrahydro-1N-pyrido[4,3-b]indoles with general formula 1.1, 1.2 or 1.3, their pharmaceutical salts and/or hydrates with antihistamine activity. In general formulae 1.1, 1.2 or 1.3 radicals assume values given below . In 1.1 compounds, R1 represents a substitute, chosen from hydrogen or unsubstituted C1-C5 alkyl; R2 represents a hydrogen atom or C1-C4 alkyl; R3 i represents one or more single or different substitutes, chosen from hydrogen, halogen, C1-C3 alkyl or CF3; n=0 or 1-3; in 1.2 compounds R1 represents a substitute of an amino group, chosen from hydrogen or optionally substituted C1-C5 alkyl; R3 represents one or more single or different substitutes, chosen from hydrogen, halogen, C1-C3 alkyl or CF3, and Ar1 represents an aryl or heterocyclyl, containing at least one carboxyl and/or alkoxycarboxyl substitute or R3 i represents a carboxyl and/or alkyloxycarboxyl substitute, and Ar1 represents optionally substituted aryl or heterocyclyl; in 1.3 compounds, R2 represents a hydrogen atom or C1-C4 alkyl; R3 i represents one or more single or different substitutes, chosen from hydrogen, halogen, C1-C3 alkyl or CF3, and Ar2 represents optionally substituted aryl or heterocyclyl; k=0 or 1-4; m=1 or 2.
EFFECT: compounds can be used for making drug formulation for treating allergies, autoimmune diseases such as pollen allergy, urticaria, bronchial asthma etc.
17 cl, 10 dwg, 2 tbl,13 ex
SUBSTANCE: invention refers to the pharmaceutical-processing industry and concerns application of a phytogenesis agent possessing anxiolytic, nootropic, anticonvulsant, anticonvulsant, cerebro-protecting activity and ability to normalise transfer processes in brain synapses. Application of water or aqueous-alcoholic or carbon-dioxide extract of a plant of forget-me-not sort (Myosotis) as an agent possessing anxiolytic, nootropic, anticonvulsant, cerebro-protecting activity and ability to normalise transfer processes in brain synapses is offered. The forget-me-not extract can be used in the liquid form and in the form of a dry extract. The agent possesses a wide spectrum of therapeutic action on the declared pharmacological administration.
EFFECT: obtaining of the agent possessing possessing anxiolytic, nootropic, anticonvulsant, cerebro-protecting activity and ability to normalize transfer processes in brain synapses.
3 cl, 9 tbl
SUBSTANCE: invention concerns single-stage method of obtaining fructopiranose sulfamate derivatives of the general formula (I) , where X is selected out of CH2 or O; R3, R4, R5 and R6, each selected independently out of hydrogen or low-grade alkyl, then X is CH2, R5 and R6 can be alkene groups linked with formation of benzene ring, then X is O, R3 and R4 and/or R5 and R6 together can be methylenedioxy group of the formula: , where R7 and R8 are equal or different and denote hydrogen, low-grade alkyl, or are an alkyl and are linked together to form cyclopentyl or cyclohexyl ring; , involving reaction of compound of the formula (II) with sulfuryldiamide at high temperature in the presence of 0 to ca. 10% of water, resulting in obtaining of respective compound of the formula (I); and method of obtaining compound of the formula (1a).
EFFECT: development of a single-stage method for obtaining fructopiranose sulfamate derivatives.
29 cl, 10 tbl, 10 ex
SUBSTANCE: it is offered: Ivermectine application for obtaining of a pharmaceutical composition for local application for treatment of pink eels, a pharmaceutical composition for the local drawing, intended for the person, containing Ivermectine both certain dissolvents and water, and also its application in dermatology.
EFFECT: invention is distinguished by Ivermectine high stability in compositions at different value pH and good acceptability for a skin.
24 cl, 10 ex
SUBSTANCE: in novel tocopherol-modified therapeutic drug compounds of formula 1 T-L-D, T is tocopherol, L is succinate, and D is camptotecin or its derivative, where all three fragments are bound covalently. Invention also relates to emulsions based on said compounds, formulations of micelles, including said compounds, methods of treating cell proliferative disease using said compounds and formulations, as well as to said compounds application for production of medication for treatment of cell proliferative disease.
EFFECT: increase of composition and treatment method efficiency.
18 cl, 17 dwg, 4 tbl, 19 ex
SUBSTANCE: agent for superficial mycoses treatment contains antimycotic Ketoconazole; emulsion carrier including emulsifiers, castor oil, water; end additives stabiliser and preserving agent. Agent is aerosol liniment additionally containing antioxidant Dibunolum or butylhydroxytoluene. As emulsifier agent contains emulsifiers of the first and second type that are distilled monoglycerides, emulsion wax, Tvin 80; as stabiliser it contains oxymethylpropylcellulose (OMPC), and preserving agent is mixture of Nipaginum and Nipazole.
EFFECT: provided lasting contact medicinal substance with affected region and its environmental protection; lowered risk of mycosis transfer from infected person to other people and higher sedimentation stability of agent.
3 tbl, 4 ex
SUBSTANCE: claimed invention relates to medicine and describes fatty emulsion, containing propofol in concentration from 0.4 to 5 wt/vol %, oil component in concentration from 2 to 5 wt/vol %, and emulsifying agent in concentration from 0.4 to 5 wt/vol % per total amount of fatty emulsion and local anesthetic, mixed with it before application, local anesthetic being mixed with fatty emulsion before application, and fatty emulsion additionally includes stabiliser, selected from the following (a), (b), (c) or (d): (a) at least one phospholipid, selected form group, consisting of phosphatidylglycerine, phosphatide acid, phosphatidylinosite and phosphatidylserine, where fatty acid, complexly eterificated in glycerine fragment, is C10-22 linear or branched, saturated or non-saturated fatty acid; (b) at least one derivative of phospholipid, selected from phosphatidylethanolamines, modified by polyalkylenglycol, where fatty acid, complexly eterificated in glycerine fragment, is C10-22 linear or branched, saturated or non-saturated fatty acid; or (c) at least one fatty acid, selected from group, consisting of C10-22 linear or branched, saturated or non-saturated fatty acids; or (d) mixture of at least two, selected from said above groups(a), (b) and (c),where stabiliser (a), (b) or (c)is present in concentration from 0.01 to 1 wt/vol %, from 0.01 to 1wt/vol %, from 0.05 to 5 wt/vol %, correspondingly, per total; amount of fatty emulsion and local anesthetic, mixed with it before application.
EFFECT: ensuring high stability of profol-containing fatty emulsion, with which in advance or before application local anesthetic can be mixed.
34 cl, 16 tbl, 89 ex
FIELD: medicine; stomatology.
SUBSTANCE: invention can be used for treatment of maxillofacial inflammatory diseases. For this purpose after suppurative focus is surgically opened and drained, intratissular subcutaneous or submucous introduction of Perftoran follows. Thus Perftoran is injected from four injection points equally-interspaced by perimeter, in amount 0.3-0.5 ml and more per one point, depending on wound area. Course of treatment is 4-6 days.
EFFECT: improved efficiency of anti-inflammatory therapy due to uniform distributed Perftoran emulsion directly within inflammation centre.
FIELD: medicine; stomatology.
SUBSTANCE: general and local pharmacotherapy is carried out. Additionally one day after surgery perphtoran dosed to 0.1 ml/kg body weight is singly injected in submucosa of operational interjacent fold.
EFFECT: enables to improve treatment efficiency.
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to drugs and concerns a pharmaceutical composition for oral administration and consisting of a mixture that comprises the following components: (i) one or more liquid NO-releasing nonsteroid anti-inflammatory drugs; (ii) one or more nonionogenic surfactants wherein the ratio of NO-releasing a nonsteroid anti-inflammatory agent to a nonionogenic surfactant is from 1:0.3 to 1:3, and (iii) indicated mixture is absorbed on a solid inert carrier to provide preparing a powder in the ration mixture to a solid carrier from 1:2 to 2;1. Proposed composition allows improving the oral bioavailability of liquid drugs.
EFFECT: improved and valuable pharmaceutical properties of compositions and drugs.
10 cl, 4 tbl, 1 dwg, 8 ex
FIELD: chemical-pharmaceutical industry and technology, pharmacy.
SUBSTANCE: invention relates to a composition in form of microemulsion concentrate designated for oral using, for example, in gelatin capsule. Proposed pharmaceutical composition provides high bioavailability of preparation. Pharmaceutical composition in form of microemulsion concentrate comprises ciclosporin and accessory components: (a) propanediol monocaprylate as a solvent; (b) monocaprylate glyceryl; (c) polyethylene glycol 40, hydrogenated castor oil and linoleic acid glycerides polyethylene glycol as surfactants; (d) 1,2-propylene glycol as a hydrophilic component; (e) alpha-tocoferol acetate as an antioxidant wherein in dilution microemulsion concentrate forms microemulsion to be easily dosed with particles size 15-20 nm.
EFFECT: improved and valuable properties of pharmaceutical composition.
1 tbl, 5 ex
SUBSTANCE: the present innovation deals with the systems of vaginal delivery of medicinal preparations at practically neutral pH value that include: emulsion at practically neutral pH value that contain globules, being of two phases: internal water-soluble phase and external water-insoluble phase or a film that contain a therapeutically active preparation or preparations, moreover, acid buffered phase contains a therapeutically active preparation or preparations independently or in combination with additional buffer substance; moreover, acid buffered phase could be isotonic, hypertonic or hypotonic. New systems provide the chance to deliver therapeutically active preparation due to modified method intravaginally for prolonged period of time, up until 168 h. The systems mentioned could take the form of multi-phase liquid or semi-solid substance to be easily introduced into vaginal cavity at no active leakage from there.
EFFECT: higher efficiency.
57 cl, 2 ex, 2 tbl
FIELD: medicine, pharmaceutical technology, hormones.
SUBSTANCE: invention describes a method for preparing isotonic oily emulsions containing estradiol and progesterone in the ratio from 2:1 to 200:1 and wherein the emulsion comprises 0.005-0.5 wt.-% of estradiol and 0.05-5 wt.-% of progesterone, and this emulsion is designated for intravenous administration. Method for preparing such emulsions involves the following steps: (A) dissolving at least one hormone, i. e. estradiol or progesterone in oily phase, and (B) emulsifying oily phase in aqueous phase in the presence of an emulsifying agent. Emulsions prepared by this method under condition of minimal supply of oil and volume (liquid) result to the higher concentrations of hormones in premature baby blood.
EFFECT: improved and valuable pharmaceutical properties of emulsion.
6 cl, 2 tbl, 1 dwg, 2 ex
SUBSTANCE: device includes core containing at least one pharmaceutically active agent. Core is made from elastomeric composition selected from the group consisting of poly(dimethylsiloxane), siloxane-based elastomer including 3,3,3-trifluoropropyl groups attached to Si atom of siloxane units, siloxane-based elastomer, which includes poly(alkyleneoxide) groups, and their mixtures. The said core is encased by membrane. Membrane is made from the same elastomeric composition as core. Pharmaceutically active agent is selected from the group, which includes anti-allergic agents, anti-infection agents, anti-asthmatic agents, anti-inflammatory agents, anti-virus agents, anti-bacterial agents, anti-histamine means, anti-fungal agents, anesthetics, opioids, vasorelaxants, muscarinic agents, sympathomimetics, corticosteroids and their mixtures. Delivering device, according to invention, for nasal or otological application ensures preliminary set, constant rates of release of one or more pharmaceutically active agents.
EFFECT: device is safe and does not cause discomfort to patients.
8 cl, 6 dwg, 1 tbl, 5 ex