Solubilized sertraline compositions

A composition and technology of sertraline, applied in the field of treating mental illness and other diseases, can solve the problems such as the inability to fully release the drug in the dosage form and the reduction of transmission

Inactive Publication Date: 2000-08-02
PFIZER PRODS ETAT DE CONNECTICUT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Gel formation in both mechanisms can reduce delivery by an order of magnitude or more and, in some cases, may result in i

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] excipient

[0049] According to the above tests, the preferred acids are malic acid, citric acid, erythorbic acid and adipic acid. Maleic acid, L-aspartic acid, tartaric acid and L-glutamic acid can also significantly improve the solubility of sertraline hydrochloride. Sustained release dosage forms with such acids in the drug core will be more effective than dosage forms without such acids. Example 2

Embodiment 2

120

150

120

[0054] This example discusses that the solubilizer of sertraline can also improve the dissolution rate of sertraline. The effect of candidate excipients on the dissolution rate of sertraline can be determined as follows. The solid drug, candidate solubilizing excipients, and in some cases additional excipients such as organic acids and osmotic agents (eg sugars) are added to a 1.8 ml centrifuge tube. The sample tubes were centrifuged at 14K G for 5 minutes in a microcentrifuge to compact the powder. 150 [mu]l gastric buffer was added to the compacted powder, and the sample was agitated gently, then centrifuged at 14K G for 2 minutes in a microcentrifuge. Remove the samples from the microcentrifuge and let stand until the solution is removed. Samples were removed from the solution after adding gastric buffer to the compacted powder for a total of 10 minutes and analyzed by HPLC to determine the concentration of sertraline.

[0055] ...

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PUM

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Abstract

Compositions of matter comprising sertraline and a solubilizing agent which increases the solubility of sertraline in aqueous chloride ion-containing use environments.

Description

field of invention [0001] The invention relates to a composition containing sertraline or a pharmaceutically acceptable salt thereof and a solubilizing agent, the role of the solubilizing agent is to prevent sertraline from forming a gel or maintain its solubility in an environment containing chloride ions. The invention also relates to methods of treating psychiatric and other disorders comprising administering to a mammal in need thereof, including a human patient, a solubilized composition comprising sertraline. Background of the invention [0002] Sertraline is a selective serotonin reuptake inhibitor (SSRI), which is used as an antidepressant and anorectic for the treatment of obsessive-compulsive disorder, premenstrual dysphoria, post-traumatic stress disorder, Chemical dependence, anxiety-related disorders, panic attacks and premature ejaculation. [0003] Sertraline is the most commonly used prescription for the treatment of depression, usually, the dosage is in the...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/20A61K47/02A61K31/136A61K47/10A61K47/12A61K47/14A61K47/18
CPCA61K9/2013A61K47/02A61K9/0004A61K47/12A61K9/2009A61K47/14A61K47/183A61P25/00A61K31/135
Inventor D·T·弗里森S·M·赫比格R·M·尚克J·B·韦斯特
Owner PFIZER PRODS ETAT DE CONNECTICUT
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