12 results about "Sulindac" patented technology

The application discloses a method for industrial production of sulindac. The method comprises the following steps: condensation reaction of compound 1 (5-fluoro-2-1-(4-methylthio benzyl) indene) and glyoxylic acid under catalysis of an organic base (benzyl trimethyl ammonium hydroxide) to generate compound 2, isomerization reaction of the compound 2 under hydrobromic acid-acetic acid solution to generate compound 3, which greatly improves reaction conversion rate and yield, reduces three waste problems, and finally obtains compound 4 (sulindac crude product) through oxidation of the obtained compound 3 by hydrogen peroxide, and high-purity sulindac is obtained through recrystallization of the crude product by isopropyl alcohol. The raw materials and reagents used in the preparation process of the sulindac are relatively cheap and low in cost, the whole preparation process is mild in reaction condition, simple and safe in operation, and convenient for industrial production.

The present invention features methods of treating pain, e.g., pain associated with central sensitization, using modified NSAIDs, e.g., using sulindac phosphate.

This invention discloses a method for preparing sulindac. The method involves first performing an Arbuzov reaction and a Wittig-Horner reaction sequentially to obtain 6-fluoro-3-(p-methylthiobenzyl)-2-methyl-1H-indene. 6-fluoro-3-(p-methylthiobenzyl)-2-methyl-1H-indene undergoes a condensation dehydration reaction with glyoxylic acid, followed by double bond rearrangement under acidic conditions to obtain (Z)-5-fluoro-2-methyl-1-(p-methylthiobenzyl)-1H-indene-3-acetic acid. Finally, it undergoes a single oxidation reaction with an oxidant to obtain sulindac. The raw materials and excipients used in this invention are readily available, and the entire reaction route is short, the reaction conditions are mild, the operation is safe and simple, the yield is high, the purity is high, the production cost is low, and the emissions of waste are minimal, conforming to green industrial production standards. The total yield of the obtained sulindac product is over 75%, which is conducive to industrial production.

A new use of 2-[(3Z)-6-fluoro-2-methyl-3-[(4-methylsulfinylphenyl)methylidene]inden-1-yl] acetic acid (sulindac) of the formula 1 for making the pharmaceutical preparations for the treatment of difficult healing different types of wounds in patients with diabetes.The medical use of 2-[(3Z)-6-fluoro-2-methyl-3-[(4-methylsulfinylphenyl)methylidene]inden-1-yl] acetic acid (sulindac) of the formula 1 shown in the FIG. 1 for the preparation of pharmaceutical formulations for the treatment of difficult healing different types of wounds in patients with diabetes is disclosed.

The invention discloses a method for separating sulindac and impurities thereof. The method comprises the step of determining impurities of sulindac in a test sample by using a high performance liquid chromatograph. The separation and detection method disclosed by the invention is good in separation degree, simple to operate, short in peak appearance time and short in detection time, and also has good method reproducibility and stability.

The invention discloses a selenium-containing sulindac derivative and an electrochemical synthesis method thereof.According to the method, an electrochemical oxidation technology is adopted, clean and mass-free electrons serve as an oxidizing agent, and carboxylic acid with low oxidation potential of sulindac serves as a source of free radicals to start a reaction, so that the selenium-containing sulindac derivative is obtained. The bifunctional activation of sulindac which is a traditional non-steroidal anti-inflammatory drug (NSAIDs) and a diselenide compound is realized, and the multi-functional selenium-containing sulindac derivative with anti-inflammatory activity is constructed in one step. The synthesis method provided by the invention has remarkable green chemical characteristics, avoids the use of an expensive transition metal catalyst, an excessive oxidant and strong alkali, solves the problems of substrate pre-functionalization and multi-step reaction in traditional synthesis, and provides a synthesis approach with mild conditions and controllable reaction process. The compound also has good anti-inflammatory activity, and the product obtained after modification greatly improves the anti-inflammatory activity of the original drug.

The invention relates to the technical field of medicine, and particularly discloses sulindac external gel emplastrum and application thereof.The sulindac and a functional matrix with hydrophilic amino functional groups are subjected to molecular self-assembly, the functional matrix and carboxyl of the sulindac are subjected to non-covalent interaction through hydrogen bonds, ionic bonds and the like, and the sulindac external gel emplastrum is obtained. The stable micromolecular hydrogel with the three-dimensional network structure is spontaneously formed. The hydrogel can be prepared into an external gel emplastrum through simple compounding, the three-dimensional network structure endows the gel emplastrum with appropriate viscosity and skin adhesiveness, and the gel emplastrum can be tightly attached to the skin after being smeared on painful parts (such as joints and muscles) and is not prone to falling off due to movement. The preparation process has the advantages of simplicity and convenience in operation, economy and high efficiency, complex equipment is not needed in the micromolecule self-assembly process, the gel emplastrum can be compounded only through simple mixing, industrial production is facilitated, and the preparation method has high clinical conversion value and application potential.

The invention provides sulindac as a GPR119 agonist and application of sulindac in preparation of a product for improving IFPD, and belongs to the technical field of new application of drugs. The invention particularly provides application of sulindac as a non-steroidal anti-inflammatory drug in preparation of a GPR119 agonist product and application of sulindac in preparation of a product for improving fat deposition in pancreas. A sulindac intervention experiment shows that the expression of the sulindac on GPR119 / CaM / AKT / Foxo1 pathway protein of a C57BL / 6J mouse tends to a normal level, which indicates that the sulindac has the potential as a GPR119 agonist and also has the effect of improving IPFD.

The present application relates to the technical field of pharmaceutical preparation, and discloses a sulindac tablet composition and a preparation method thereof; the sulindac tablet composition comprises sulindac, a filler, a binder, a disintegrant and a lubricant, the binder is povidone K30, the disintegrant is corn starch, and the preparation method comprises the following steps: (1) uniformly mixing the prescription amount of sulindac, the disintegrant and the filler; (2) preparing the binder into a binder solution and performing wet granulation; (3) performing whole granulation; and (4) performing total mixing and tablet pressing. The sulindac tablet composition has simple process and stable quality, and compared with the original research, the dissolution stability under high-temperature and high-humidity conditions is better than that of the original research.

The application discloses a selenium-containing sulindac acid derivative and an electrochemical synthesis method thereof. The method adopts an electrochemical oxidation technology, uses clean and massless electrons as an oxidant, starts a reaction through a carboxylic acid with a low oxidation potential of sulindac acid as a free radical source, realizes the dual functional group activation of sulindac acid, a traditional non-steroidal anti-inflammatory drug (NSAIDs), and a diselenide compound, and constructs a selenium-containing sulindac acid derivative with anti-inflammatory activity and multi-functional groups in one step. The synthesis method has the characteristics of green chemistry, avoids the use of expensive transition metal catalysts, excessive oxidants and strong alkalis, solves the problems of pre-functionalization of a substrate and multi-step reactions in traditional synthesis, and provides a synthesis path with mild conditions and controllable reaction process. The compound has good anti-inflammatory activity, and the anti-inflammatory activity of the original drug is greatly improved after modification.

The application discloses stable sulindac tablets and a preparation method thereof, which contain the following components in parts by weight: 53-65 parts of sulindac, 17.4-35.4 parts of microcrystalline cellulose, 10.7-17.2 parts of corn starch and 1-3.8 parts of stearic acid. The sulindac tablets provided by the application reduce the viscosity of particles, increase the flowability of particles, have small tablet weight difference after tabletting, reduce the RSD value of dissolution, reduce the quality difference of tablets, improve uniformity, have similar dissolution to a reference preparation, and improve the stability of products.

The present invention discloses the use of sulindac acid trifluoromethyl selenide in the preparation of anti-enteroviral drugs, belonging to the field of biomedicine technology. The present invention first discovered that sulindac acid trifluoromethyl selenide can significantly inhibit the viral titer of enterovirus 71 and coxsackievirus A16, and can also significantly inhibit the viral replication of enterovirus 71 and coxsackievirus A16, as well as significantly inhibit the expression of 3D protein of enterovirus 71 and the expression of VP1 protein of coxsackievirus A16, and the above inhibition is dose-dependent. Therefore, the sulindac acid trifluoromethyl selenide has good anti-enteroviral activity, providing new ideas and solutions for the development of anti-enteroviral drugs and clinical treatment.