37 results about "Pranoprofen" patented technology

The invention discloses a novel preparation method of pranoprofen. The novel preparation method of the pranoprofen has the advantages of being high in yield, having less impurities, and being safe andenvironmentally friendly. The novel preparation method of the pranoprofen comprises the following steps that step 1, 5H-[1]-benzopyran[2,3-b]pyridine and propionyl chloride are directly acylated; step 2, bromination is carried out; step 3, potassium tert-butoxide or sodium tert-butoxide is used for hydrolysis, and finally, rearrangement is carried out to obtain the pranoprofen.

The present invention discloses a preparation method to produce a compound with formula (I) 9-oxa-1-aza athrone, in which a compound with formula (II) reacts with a cyclization reagent under high temperature to obtain the compound with the formula (I), which is an important medium substance in preparation process of Pranoprofen.

An antibacterial eye medicine containing pranoprofen contains non-steroid antiphlogistic medicine, aminoglycoside-type antibacterial medicine, polyvinyl pyrrolidone, and pharmacologically acceptable carrier. Its preparing process is also disclosed.

A kind of eye-drops of pranoprofen with long stay time in eye and no bitter taste is prepared through dissolving pranoprofen and relative additives in water, adding the aqueous solution of sodium hyaluronate, stirring, adding water, filtering and filling it in containers.

The novel positively charged pro-drugs of aryl- and heteroarylpropionic acids in the general formula (1) 'Structure 1' and general formula (2) 'Structure 2' were designed and synthesized. The compounds of the general formula (1) 'Structure 1' and general formula (2) 'Structure 2' indicated above can be prepared from functional derivatives of naproxen, suprofen, a- methyl-(p-chlorobenzoyl)-5-methoxy-2-methylindole 3-acetic acid, flurbiprofen, carprofen, pranoprofen, benoxaprofen, alminoprofen, tiaprofenic acid, pirprofen, zaltoprofen, bermoprofen, loxoprofen, indoprofen, fenclorac, oxaprozin, fenbufen, orpanoxin, ketorolac, clidanac, and related compounds, (for example acid halides or mixed anhydrides), by reaction with suitable alcohols, thiols, or amines. The positively charged amino groups of these pro-drugs not only largely increases the solubility of the drugs, but also bonds to the negative charge on the phosphate head group of membranes and pushes the pro-drug into the cytosol. The results suggest that the pro-drugs diffuses through human skin -100-130 times faster than do their parent drugs. It takes 2-4 hours for naproxen, suprofen, a- methyl-(p-chlorobenzoyl)-5-methoxy-2-methylindole 3-acetic acid, flurbiprofen, carprofen, pranoprofen, benoxaprofen, alminoprofen, tiaprofenic acid, pirprofen, zaltoprofen, bermoprofen, loxoprofen, indoprofen, fenclorac, oxaprozin, fenbufen, orpanoxin, ketorolac, clidanac, and related compounds to reach the peak plasma level when they are taken orally, but these prodrugs only took about 40-50 minutes to reach the peak plasma level when they are taken transdermally. In plasma, more than 90% of these pro-drugs can change back to the drug in a few minutes. The prodrugs can be used medicinally in treating any NS AIAs-treatable conditions in humans or animals. The prodrugs can be administered not only orally, but also transdermally for any kind of medical treatments.

The invention discloses a purification method of pranoprofen, and relates to the field of preparation of nonsteroidal anti-inflammatory drugs. The problem that a simple, practicable and low-cost purification method of the pranoprofen does not exist in the prior art, and consequently the prepared pranoprofen cannot reach the expected quality requirements is solved. According to the technical key point, the purification method comprises the following steps that (1) beating is conducted, specifically, pranoprofen powder is added in a methanol aqueous solution, the temperature is risen to 50-60 DEG C, stirring is conducted for 3-5 hours under the temperature, and serous liquid is obtained; (2) the serous liquid is filtered; and (3) the pranoprofen obtained through filtering is mixed with the methanol aqueous solution and is dissolved, filtering, devitrification and drying are conducted while the solution is hot, and the f pranoprofen finished product is obtained. According to the purification method of the pranoprofen, operation is easy and convenient, and the prepared pranoprofen is high in purity, low in impurity content and high in yield.

A pranoprofen in-situ gelling eye drop is disclosed. The pranoprofen in-situ gelling eye drop comprises the components by mass percent: 0.1% of pranoprofen, 1%-40% of thickening agent, 0.03%-1.0% of pH adjusting agent, 0.01%-0.03% of bacteria inhibitor, 0.005%-0.2% of antioxidant, 0.01%-0.05% of chelating agent, and 0.1%-4.0% of solubilizing agent. The pranoprofen in-situ gelling eye drop disclosed by the invention has the characteristics that a material (e.g., poloxamer 407 and sodium alginate) with good biocompatibility and having the feature of temperature sensitivity, pH sensitivity or ion sensitivity is used as a matrix, the eye drop is administered in vitro under a solution state, phase change occurs immediately at the administered site in vivo in accordance with different environments inside and outside human body, so as to form in-situ gel; and the eye drop is convenient to use, high in bioavailability and long in residence time and results in good compliance of patients. The invention further discloses a preparation method of the pranoprofen in-situ gelling eye drop.

Disclosed are non-steroidal analgesic and analgesic anti-inflammatory agents containing carboxyl including sodium, calcium, zinc, magnesium, N-n-octylgucamine, Arginine, Lycine or Trometamol salts of Loxoprofen, Ketoprofen, Pranoprofen, Tiaprofenic acid, Butibufen, Omolofen, epoxy indene acid, Lobuprofen, Clofenamic acid, Clonixin, Fenoprofen, Benorilate, Flurbiprofen, Alminoprofen, Bucloxic acid, Sulindac, Zidometacin, Acemetacin, Ketorolac, Risedronic acid, Sulindac, Lonaprofen, aspirin, Florfenicol, tiaprofenic acid, overall evaluation shows that trometamol salts are the best choice in terms of physicochemical properties, solvability, stability, local irritation, blood vessel irritation, and bioavailability for oral administration.

The present invention provides an ophthalmic solution containing pranoprofen or a pharmacologically acceptable salt thereof, and a vasoconstrictor, which is effective for ameliorating congestion in outer ocular areas, particularly conjunctiva and pericorneal area.

The invention discloses eye drops containing pranoprofen and a preparation method of the eye drops, and relates to the technical field of eye drops. The eye drops is prepared from the following raw materials in parts by weight of 0.1-0.5 part of pranoprofen, 0.1-0.7 part of sodium hyaluronate, 0.2-0.6 part of sulfobutyl ether-beta-cyclodextrin, 0.2-0.4 part of a stabilizer, 0.1-0.3 part of a pH regulator, 0.3-1.0 part of a bacteriostatic agent, 0.3-0.8 part of an osmotic pressure regulator and 85-96 parts of water for injection. According to the eye drops prepared by the invention, the sulfobutyl ether-beta-cyclodextrin and the sodium hyaluronate are added, and the sodium hyaluronate can obviously relieve clinical symptoms such as pain, itching, burning sensation, foreign body sensation ofxerophthalmia and the like, so that hyperemia caused by diseases such as blepharitis, conjunctivitis and the like can be well relieved, the effect is remarkable, and the eye drops have a wide marketprospect; and the eye drops are good in stability and free of preservatives, the dosage of anti-inflammatory drugs is reduced, and meanwhile, the anti-inflammatory effect is enhanced, and irritation to eyes is reduced.

The invention discloses a formulation composition and a preparation method of a pranoprofen-containing suspension. The formulation composition of the pranoprofen-containing suspension comprises the following components: pranoprofen, polyvinyl alcohol, sodium microcrystalline cellulose-carboxymethyl cellulose and water, wherein polyvinyl alcohol accounts for 0.5%-2.5% by mass of the formulation composition of pranoprofen-containing suspension; sodium microcrystalline cellulose-carboxymethyl cellulose accounts for 0.5%-1% by mass of the formulation composition of pranoprofen-containing suspension. According to the invention, polyvinyl alcohol and sodium microcrystalline cellulose-carboxymethyl cellulose are conventionally mixed to achieve excellent suspension effect, while the formulation composition significantly improves the stability of products during storage.

The invention belongs to the technical field of medicine, and discloses pranoprofen eye drops containing sulfobutyl ether-beta-cyclodextrin. The pranoprofen eye drops comprise active component pranoprofen, the solubilizer sulfobutyl ether-beta-cyclodextrin, a stabilizer, a pH conditioning agent, a bacteriostatic agent and an osmotic pressure conditioning agent. The stabilizer is one or the mixture of a high-molecular polymer polyethylene glycol, polyving akohol, povidone, polyvinylpyrrolidone, sodium hyaluronate, poloxamer and hydroxypropyl methylcellulose. According to the preparation method, SBE-beta-CD is dissolved into water for injection to be heated at the temperature of 60 DEG C, the pranoprofen is added so as to be dissolved completely, the other auxiliary materials are added in sequence, stirring is performed until thorough dissolving, then, the mixture is cooled to the room temperature, the pH value is conditioned, water for injection is replenished, and the mixture is filtered through a 0.22-micrometer micropore filter membrane to obtain the pranoprofen eye drops. According to the pranoprofen eye drops containing the sulfobutyl ether-beta-cyclodextrin, using irritation to the eyes is lowered, and the stability is remarkably improved.

The invention discloses an eye drop capable of assisting the treatment of conjunctivitis, and belongs to the field of pharmaceutical chemicals. The eye drop contains the following components in partsby weight: 100-120 parts of water, 50-60 parts of an isothiocyanate, 40-55 parts of pranoprofen, 30-40 parts of sodium nitrate, 20-30 parts of citric acid, 20-28 parts of sodium citrate, 20-26 parts of potassium nitrate, 20-25 parts of disodium hydrogen phosphate, 20-25 parts of sodium sulfate, 20-23 parts of sodium hyaluronate, 18-21 parts of ethyl acetate, 15-19 parts of soy phospholipid, 13-16parts of curcumin, 10-13 parts of a polyphenol flavonoid, 6-10 parts of povidone, 6-8 parts of mannitol, 3-6 parts of glucose, and 1-3 parts of a preservative. The eye drop solves the problem a traditional eye drops can only have a moisturizing effect on eyes and cannot assist in the treatment or relief of the conjunctivitis.

The present invention relates to an ophthalmic composition comprising pranoprofen and olopatadine and/or naphazoline. The invention also relates to a preparation method of the ophthalmic composition, which comprises the following steps: mixing the pranoprofen, the olopatadine and/or the naphazoline, the osmotic pressure regulator, the pH regulator, the metal ion chelating agent, the thickening agent, the preservative and the water for injection to obtain the ophthalmic composition. The invention also relates to an application of the ophthalmic composition in preparation of a medicine for treating ocular inflammation, and the ocular inflammation comprises external eye and/or anterior segment inflammation caused by gram-positive bacterium and/or gram-negative bacterium infection. When the ophthalmic composition provided by the invention is used as eye drops, the treatment effect on eye inflammation of a patient can be improved, and adverse effects of eye stimulation, conjunctival congestion, edema and the like after medication can be avoided, so that the medication compliance of the patient is improved, and the recovery time of the patient is shortened.

The invention discloses a novel pranoprofen eye drop and a preparation method thereof. The preparation method of the eye drop disclosed by the invention comprises the steps of: dissolving pranoprofen and relevant accessories in water; adding a swelling carbomer aqueous solution to the liquid medicine and then uniformly stirring; adding a sufficient amount of water; and finally, filtering and dispensing to obtain the eye drop. According to the novel pranoprofen eye drop and the preparation method thereof, the defects of the current pranoprofen eye drop are overcome; the residence time of the medicine on ocular surface is prolonged by the physical thickening and moisturizing lubrication effects of carbomer; and furthermore, the medicine seldom flows into mouth and nasal cavity so as to reduce medicine loss and avoid bitterness from the pranoprofen eye drop, and therefore, compliance of patients is increased and clinical curative effect is ensured.

The invention discloses a high performance liquid chromatography method for separating and detecting related substances in pranoprofen eye drops, which adopts a chromatographic column with octadecylsilane chemically bonded silica as a filler and acetate buffer solution-acetonitrile as a mobile phase for gradient elution, and can quickly and effectively separate the related substances in the pranoprofen eye drops. Comprise process impurities, illumination degradation impurities, oxidative degradation impurities and the like. Compared with the conventional high performance liquid chromatography, the method has the advantages that the analysis time is obviously shortened, the specificity is high, the sensitivity is high, the durability is good, and the operation is simple and convenient.

The present invention provides an aqueous solution containing pranoprofen or a pharmacologically acceptable salt thereof, and a sulfa drug, and a method for making pranoprofen or a pharmacologically acceptable salt thereof stable to light in an aqueous solution, which includes adding a sulfa drug to the aqueous solution containing pranoprofen or a pharmacologically acceptable salt thereof.