30 results about "Timolol maleate" patented technology

Biodegradable polymeric microparticle compositions containing one or more active agents, especially those useful for treating or preventing or one or more diseases or disorders of the eye, and methods of making and using thereof, are described. The microsphere compositions release an effective amount of the one or more active agents for a period greater than 14 days in vivo, preferably greater than 60 days in vivo, more preferably up to 73 days in vivo, more preferably greater than 90 days in vivo, even more preferably over 100 days in vivo, and most preferably greater than 107 days in vivo. In a preferred embodiment, the microparticle compositions contain one or more active agents useful for managing elevated intraocular pressure (TOP) in the eye. In one embodiment, the microspheres are formed from polylactide-co-glycolide (“PLGA”); in another embodiment, the microspheres are formed from a blend PLGA and poly lactic acid (“PLA”). Relatively hydrophilic, and preferably carboxylated, polymeric materials such as PLGA are used for a drug such as timolol maleate, which is relatively water soluble, to increase drug loading. Higher molecular weight polymers, as well as the ratio of LA (which has a longer degradation time, up to one to two years) to GA (which has a short degradation time, as short as a few days to a week), are used to provide release over a longer period of time. The combination of drug loading and release rate, as well as the minimization of initial burst release, result in prolonged release of a higher amount of drug.

The invention provides timolol maleate (TM) eye gel and a preparation method thereof. One hundred grams of the eye gel comprises the following components by weight: 0.10-0.70g of TM, 0.10-2.0g of gel matrix, 0.2-5.0g of osmotic pressure regulator and the balance of water, wherein the gel matrix is a mixture of cellulose derivatives and carbopol and the weight ratio of cellulose derivatives to carbopol is 1:0.02-1, the cellulose derivatives comprise more than one of methylcellulose, hydroxymethyl cellulose, hydroxypropyl methylcellulose (HPMC) and carboxymethyl cellulose (CMC), and the carbopol comprises one of polyacrylic acid (PAA), polyacrylate or crosslinking polyacrylic resin. Patients with glaucoma and ocular hypertension use the controlled-release TM eye preparation once a day; and the prescription of the eye preparation is free of preservatives, thus lowering stimulation to eyes and improving medication safety if the gel is used for a long term.

The invention relates to timolol maleate cubic liquid crystal nanoparticle eye drops and a preparation method thereof. The imolol maleate cubic liquid crystal nanoparticle eye drops are mainly prepared from, by weight, 0.4-1.0 part of timolol maleate, 1.0-18.0 parts of liquid crystal material, 0.2-3.0 parts of surface active agent and 100 parts of water. The liquid crystal material is glycerol monoolein. The surface active agent is poloxamer. According to the timolol maleate cubic liquid crystal nanoparticle eye drops, the cornea infiltration capacity of timolol maleate can be remarkably improved, intra-ocular pressure can be remarkably and stably reduced, the retention time of a drug in the eyes can be prolonged, no preservative is added, and the problems that in the prior art, the retention time of timolol maleate eye drops in the eyes is short and irritation is caused by long-time use can be effectively solved.

The invention belongs to the field of preparations and relates to a timolol maleate pharmaceutical composition and a preparation method thereof. The timolol maleate pharmaceutical composition contains timolol maleate, Carbopol, triethanolamine, propylene glycol, ethylparaben and water. The pharmaceutical composition has the advantages of good biocompatibility, easiness in coating, no greasiness and the like, and the use compliance of a patient is greatly improved; the timolol maleate pharmaceutical composition can directly act on a focus of infection, and the local drug concentration is increased, so that the drug effect is furthest exerted, and the untoward effect of the whole body caused due to oral medication or intravenous medication is avoided; and the pharmaceutical composition is suitable for industrial large-scale production, is used for treating hemangioma and is particularly suitable for treating superficial type infantile hemangioma.

The invention discloses a gel agent for treating glaucoma and its preparing process which comprises Timolol Maleate, macromolecular material, glycerin, Ethylparabenum, Disodium Edetate, anti-oxidant agent, and distilled water, the preparation consists of steeping the macromolecular material into water, dissolving the Ethylparabenum with hot-water, charging Ethylparabenum solution, Timolol Maleate, glycerin, anti-oxidant agent, Disodium Edetate into macromolecular solution, agitating homogeneously.

The invention discloses an immediate type ophthalmic gelatin of timolol maleate and a preparation method thereof. 100 milliliters of the immediate type ophthalmic gelatin of timolol maleate contains 1 to 1.5 grams of the timolol maleate, 0.05 to 1 gram of preservative, 1.0 to 7.5 grams of permeation pressure conditioning agent and 30 to 150 grams of gelatin substrate. Remaining components are acid-base buffer regent and water for injection. The invention enriches the dosage forms of the timolol maleate by optimizing auxiliary materials and improving technology so that lag time in eyes is greatly prolonged and a curative effect is improved without adverse stimulus reaction.

The invention discloses a preparation method of timolol maleate sustained release microspheres. The preparation method comprises the following steps: by adopting an oil-in-oil technology, preparing an internal phase from timolol maleate, modified montmorillonite, acrylic resin, tween and a plasticizer and preparing an external phase from vegetable oil and span; carrying out ultrasonic treatment on an obtained oil-in-oil emulsion; then, electromagnetically stirring to evaporate the internal phase to obtain the timolol maleate sustained release microspheres. The grain diameter of the timolol maleate sustained release microspheres can be controlled in a range of 10 mu m, so that the demand of eye-drops preparations is met. The medicine encapsulation rate reaches up to 80-99%, and the in vitro releasing time can be prolonged to 10-12 hours. The timolol maleate sustained release microspheres prepared by the method serving as an ocular hypotensive agent can reduce intraocular discomfort and reduce the medication frequency, so that the purpose of reducing intraocular pressure for a long time by one-time delivery is realized.

The invention provides a timolol maleate liposome gel and a preparation method thereof. The gel is prepared from timolol maleate, a penetration enhancer, a humectant, a preservative, a liposome forming agent, a gel matrix, a pH regulator and medical purified water. The prepared timolol maleate liposome gel is uniform and delicate, suitable in viscosity and easy to spread, the drug release time is prolonged through the liposome technology, the concentration of the drug at the diseased region is kept, the gel is used for treating infantile hemangioma, drug administration is convenient, meanwhile, the first-pass effect of the liver is avoided, and meanwhile the gel is convenient to use, high in safety, simple in production process and good in application prospect.

The invention discloses a method for determining impurities in timolol maleate. The method comprises the following steps: taking a timolol maleate sample homologous with a timolol maleate sample to be detected, and reacting to obtain a destroying solution containing an impurity X; the method comprises the following steps: taking a timolol maleate sample to be detected, and preparing a test solution by using a solvent; diluting the test solution as a contrast solution; respectively carrying out liquid chromatography detection on the destroyed solution, the test solution and the contrast solution so as to calculate the content of the impurity X in the to-be-detected sample. According to the method, impurities G, B, D, E, C and 5 can be directionally damaged, the interference impurity is small, the positioning of each impurity is not influenced, an impurity reference substance is not used, an ion pair reagent and a peak shape improver are removed from a chromatographic system, the loss of a chromatographic column is relatively small, the method can be simultaneously used for liquid chromatography and liquid chromatography-mass spectrometry detection, the qualitative analysis on the impurities can be conveniently carried out at the same time, and the detection accuracy is high. The economical efficiency and the universality of the method are improved.

The invention discloses a pharmaceutical composition consisting of latanoprost and timolol maleate, with weight percentages of 0.004-0.007% and 0.6-0.8% respectively. The invention also provides a compound preparation of the pharmaceutical composition, wherein the mass content of the timolol maleate is 0.6-0.8%, and the mass content of the latanoprost is 0.004-0.007%; and auxiliary materials include benzalkonium chloride or RH40 hydrogenated castor oil, sodium chloride, sodium dihydrogen phosphate, disodium hydrogen phosphate and purified water, with the pH of 5.0-6.5. The compound preparation can be used for treating glaucoma with small side effect, so that patient compliance is higher.

The invention discloses timolol maleate eye drops and a preparation process. The timolol maleate eye drops are prepared from the following raw materials in parts by weight: 10 to 12 parts of dispersion liquid C, 5 to 7 parts of timolol maleate nanoparticles, 20 to 30 parts of a water-based solvent, 4 to 6 parts of a buffering solution, 100 to 200 parts of a diluting agent and 0.01 to 0.03 part ofbenzalkonium chloride. The timolol maleate eye drops are prepared through the following steps: step 1, preparing the dispersion liquid C; step 2, adding the timolol maleate nanoparticles into the dispersion liquid C prepared by step 1 to prepare a nano mixed solution; and step 3, mixing a glucose solution with the mass percent of 8 percent and the nano mixed solution obtained by step 2, and carrying out vacuum freeze-drying for 8h to 10h; after freeze-drying is finished, adding a solid obtained by the freeze-drying into the buffering solution and the diluting agent; raising the temperature to80 DEG C, and keeping the heat for 30min; then cooling to 40 to 50 DEG C; adding the benzalkonium chloride and stirring and dissolving; filtering by a filter element; filling and sealing.