34 results about "Brinzolamide" patented technology

A sterile aqueous formulation of a carbonic anhydrase inhibitor such as brinzolamide in combination with polymers like Soluplus® and a surfactant like polysorbate 80, as well as methods of preparation thereof, is disclosed. The formulation relates to the highly solubilized or an amorphous form of poorly insoluble drugs/active ingredient(s) to improve its bio-availability and manufacturability.

The invention relates to the field of medicines and in particular relates to a brinzolamide nanosuspension preparation used for eyes as well as a preparation method and application thereof, aiming to lengthen the residence time of the preparation on the eyes or improve the bioavailability of the preparation. The preparation can be used for treating the diseases, such as intraocular hypertension and glaucoma. Gels can conduce to lengthening the retention time of the medicine on the eyes and reducing the number of times of administration and the dosage of administration, so that not only is the patient compliance improved but also the side effects of the medicine can be reduced. Meanwhile, no preservative is added and single-dosage package is adopted, thus reducing the irritation of eye drops used for a long term to the eyes and greatly improving the medication safety.

The invention relates to the field of medicines and in particular relates to a brinzolamide nanoparticle preparation used for eyes as well as a preparation method and application thereof, aiming to lengthen the residence time of the preparation on the eyes or improve the bioavailability of the preparation. The preparation can be used for treating the diseases, such as intraocular hypertension and glaucoma. Gels can conduce to lengthening the retention time of the medicine on the eyes and reducing the number of times of administration and the dosage of administration, so that not only is the patient compliance improved but also the side effects of the medicine can be reduced. Meanwhile, no preservative is added and single-dosage package is adopted, thus reducing the irritation of eye drops used for a long term to the eyes and greatly improving the medication safety.

The invention belongs to the technical field of drugs, and particularly relates to a brinzolamide brimonidine eye drop and a preparation method thereof. The brinzolamide brimonidine eye drop is prepared from, by weight, 1-3% of brinzolamide, 1-5% of brimonidine, 0.3-0.8% of osmotic pressure conditioning agent, 0.1-1% of glycosaminoglycan, pH conditioning agent and balance water for injection, wherein the addition amount of the pH conditioning agent enables pH of the eye drop to be 5.5-7.5. The prepared eye drop containing the brinzolamide brimonidine and iso-osmia with tears have the advantages of not containing preservative, being capable of effectively reducing intraocular pressure and having no secondary damage to eyes caused by the preservative.

The invention belongs to the technical field of pharmaceutical chemicals, in particular relates to a method for preparing an intermediate thiophene sulfonamide of brinzolamide and is applicable to industrial production. The method comprises the following steps: dissolving thiophene benzyl sulfide in a proper solvent, adding glacial acetic acid and water, controlling the temperature to 0-15 DEG C, adding trichloroisocyanuric acid in batches in 20-40 minutes, reacting at the constant temperature until the raw materials disappear, performing vacuum concentration in a water bath at the temperature of 30-50 DEG C to remove the solvent, adding ethyl acetate petroleum ether solution with the mass concentration of ethyl acetate being 25%, stirring, filtering, evaporating the filtrate under reduced pressure, thereby obtaining thiophenesulfonyl chloride; controlling the temperature to 0-15 DEG C, diluting thiophenesulfonyl chloride by ethyl acetate, dropwise adding a dilution into ammonium hydroxide or a water solution of amine, stirring and reacting until the raw materials disappear, filtering, washing, drying the solids, and obtaining the thiophene sulfonamide. The product obtained by using the method is high in yield, simple and convenient in operation, low in cost and mild in reaction conditions and is suitable for large-scale production.

The invention relates to a preparation method of a brinzolamide intermediate I and an intermediate compound III. The preparation method is simple to operate, mild in reaction condition, high in efficiency and low in cost, and is suitable for industrial production.

The present invention relates to the field of drug delivery and, particularly, to alternative processes for preparing ophthalmic compositions of Brinzolamide or pharmaceutical acceptable salts thereof.

The invention discloses preparation methods of brinzolamide and an intermediate thereof. The preparation method of the brinzolamide intermediate represented by a compound C comprises: carrying out a condensation reaction on a compound B and an orthoester-based compound at a temperature of 70-80 DEG C in an organic solvent in the presence of tertiary amine under an anhydrous condition, wherein theorthoester-based compound is one or a plurality of materials selected from trimethyl orthoacetate, triethyl orthoacetate and trimethyl orthobenzoate. According to the present invention, the condensation reaction is performed by using the tertiary amine as the catalyst, such that the reaction time for the amino protection is substantially shortened, the consumption of the protection reagent is reduced, the reaction temperature is reduced, the yield and the purity of the product are improved, the acid consumption and the alkali consumption during the post-treatment are reduced, the residue on ignition of the product is reduced, the operation is simplified, and the method is suitable for industrial production. The formulas B and C are defined in the specification.

The present invention relates to a process for preparing sterile ophthalmic suspension of carbonic anhydrase inhibitor. More particularly, the present invention relates to a process for preparing sterile ophthalmic suspension of brinzolamide.

Disclosed herein are safe pharmacologically acceptable and ophthalmologically suitable compositions and methods of their use in treating ophthalmic diseases or related conditions. Disclosed are compositions comprising effective amounts of carbonic anhydrase inhibitor(s) and alpha-2-adrenergic agonist(s) and an effective amount of a penetration enhancement component comprising one or more penetration enhancer compound(s)/molecule(s), e.g., benzalkonium chloride, which detectably or significantly increases the penetration of API(s) of the composition. In aspects, the invention provides compositions comprising a brinzolamide compound in an amount of about 0.1 wt. %-10 wt. % of the composition, a brimonidine compound, e.g., brimonidine tartrate, in an amount of about 0.01 wt. %-0.5 wt. % of the composition, one or more borate-polyol complexes in an amount of about 0.5 wt. %-6 wt. % of the composition, and a penetration enhancement component comprising benzalkonium chloride, in, for example, an amount of about 0.005-0.02 wt. % of the composition.

The invention provides compound nano eye drops and a preparation method thereof, and belongs to the technical field of eye drops. The compound nano eye drops provided by the invention simultaneously contain two medicines, namely the plinzolamide and the brimonidine tartrate, and the adhesive, the stabilizer and the osmotic pressure regulator are used in a matched manner, so that the complexity and the medication frequency of combined medication can be reduced; the particle size of solid particles in the eye drops is nanoscale, the specific surface area of the medicine is large, the residence time of the medicine in front of the cornea can improve the irritation effect of the large-particle medicine on eyes, and the compliance of a patient is improved. The adhesive increases the specific surface area of the brinzolamide medicine, increases the residence time of the hydrophobic medicine in front of cornea, reduces the loss of the medicine in eyes, reduces systemic side effects caused by loss through nasolacrimal ducts, improves the bioavailability, prolongs the medication cycle of the eye drops through slow release, and improves the antibacterial and anti-inflammatory effects; no preservative is contained, so that secondary injury to eyes of a patient is avoided.

Disclosed herein are safe pharmacologically acceptable and ophthalmologically suitable compositions and methods of their use in treating ophthalmic diseases or related conditions. Disclosed are compositions comprising effective amounts of carbonic anhydrase inhibitor(s) and alpha-2-adrenergic agonist(s) and an effective amount of a penetration enhancement component comprising one or more penetration enhancer compound(s)/molecule(s), e.g., benzalkonium chloride, which detectably or significantly increases the penetration of API(s) of the composition. In aspects, the invention provides compositions comprising a brinzolamide compound in an amount of about 0.1 wt. %-10 wt. % of the composition, a brimonidine compound, e.g., brimonidine tartrate, in an amount of about 0.01 wt. %-0.5 wt. % of the composition, one or more borate-polyol complexes in an amount of about 0.5 wt. %-6 wt. % of the composition, and a penetration enhancement component comprising benzalkonium chloride, in, for example, an amount of about 0.005-0.02 wt. % of the composition.

The invention relates to combination therapies useful in the treatment and/or prevention of cancer.

Disclosed herein are pharmacologically acceptable and ophthalmologically suitable compositions and methods of their use in treating ophthalmic diseases or related conditions. In aspects, the invention provides compositions comprising effective amounts of carbonic anhydrase inhibitor(s) and alpha-2-adrenergic agonist(s). In facets, compositions comprise a penetration enhancer component comprising one or more penetration enhancer compound(s)/molecule(s). In aspects, the invention provides compositions comprising effective amounts of brimonidine compound(s) and brinzolamide compound(s) capable of being administered once or twice daily for the treatment of elevated intraocular pressure, but which provide similar efficacy to a similar or substantially identical reference product requiring administration three times per day. In facets, the invention provides compositions capable of being administered at a frequency resulting in providing a lower total dose of both brinzolamide and brimonidine compound(s) to a recipient, but nonetheless are as or more effective in IOP control as such similar or substantially identical reference products.