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Citalopram pamoate and crystal form thereof, and preparation method and application thereof

A technology of pamolate and citalopram, which is applied in the field of medicine, can solve problems such as poor patient compliance, interruption of treatment, and serious side effects of patients, and achieve the effects of strong selectivity, small side effects, and high purity of crystal forms

Inactive Publication Date: 2017-11-03
GUANGZHOU HENOVCOM BIOSCI CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The treatment of depression often requires long-term medication, and escitalopram is mainly an oral dosage form in clinical practice. Gastrointestinal reactions, such as nausea, vomiting, loss of appetite, etc., may occur after long-term administration, resulting in poor patient compliance. Some patients even discontinue treatment due to severe side effects

Method used

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  • Citalopram pamoate and crystal form thereof, and preparation method and application thereof
  • Citalopram pamoate and crystal form thereof, and preparation method and application thereof
  • Citalopram pamoate and crystal form thereof, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] A citalopram pamolate, prepared by the following method:

[0068] Add 1.0 g of D-citalopram free base (3.08 mmol) and 1.14 g of pamoic acid (2.93 mol) to 50 ml of tetrahydrofuran, stir at room temperature, filter after 12 hours of reaction, and dry the solid under reduced pressure at 50°C to obtain 1.70 g of D-citalopram Citalopram pamolate is light yellow solid powder.

[0069] The above-mentioned obtained solid is subjected to XRPD powder diffraction analysis and infrared analysis, and it is confirmed that the obtained citalopram pamolate crystalline form is a crystal form I with the following characteristics:

[0070] Measured by Cu-Kα radiation, in the X-ray powder diffraction spectrum expressed by diffraction angle 2θ, at 8.93±0.2゜, 11.29±0.2゜, 13.21±0.2゜, 18.44±0.2゜, 20.63±0.2゜, 21.90±0.2 There is a diffraction peak at ゜.

[0071] Among them, the detection equipment and detection conditions of XRPD are:

[0072] Testing instrument: Empyrean X-ray diffractometer...

Embodiment 2

[0089] A citalopram pamolate, prepared by the following method:

[0090]Add 1.0g (3.08mmol) D-citalopram free base and 0.60g (1.54mmol) pamolic acid to 50ml tetrahydrofuran, the molar ratio of citalopram to pamoic acid is 2:1, that is, X=1 / 2. Stir at room temperature. After reacting for 5 hours, stop the reaction, spin the reaction solution to dryness, and dry under reduced pressure at 50° C. to obtain 1.6 g of D-citalopram hemipamoic acid salt as a light yellow solid powder.

[0091] D-citalopram hemipamolate was tested for solubility in different solvents, and the results were as follows:

[0092] Table 3 Solubility of D-citalopram hemipamolate in different solvents

[0093] solvent

[0094] It can be seen from the above results that when X is 1 / 2, that is, two molecules of D-citalopram and one part of pamoic acid form a salt, the solubility is relatively large, and the long-term release performance is not as good as that of citalopram with X being 1. molybdenum...

Embodiment 3

[0096] A citalopram pamolate, prepared by the following method:

[0097] Add 1.0g (3.08mmol) of D-citalopram free base and 1.14g (2.93mmol) of pamoic acid to 50ml of tetrahydrofuran, stir at 50°C, react for 3 hours, stop the reaction, cool to room temperature, filter, solid 50 °C and dried under reduced pressure to obtain 1.72 g of D-citalopram pamolate as a light yellow solid powder, which was verified to be a crystal form I product.

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Abstract

The invention relates to citalopram pamoate and a crystal form thereof, and a preparation method and application thereof, belonging to the technical field of medicine. The citalopram pamoate has a structure as shown in a formula I which is described in the specification. The citalopram pamoate has low solubility, can be used for intramuscular injection or subcutaneous injection when made into a suspension, forms a medicine storehouse in vivo, prolongs in-vivo drug release speed and achieves the purpose of long-acting treatment.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to citalopram pamolate, its crystal form, its preparation method and application. Background technique [0002] Depression is a syndrome with affective mental disorder as the main manifestation type and marked and persistent depression as the main feature. Patients with severe depression will appear pessimistic, hopeless, hallucinations and delusions, loss of appetite, functional decline, and accompanying symptoms. There are serious suicide attempts, or even suicidal behavior. As the pace of contemporary life continues to accelerate, people's mental pressure is gradually increasing. Depression has become a common disease in modern society, with a high incidence, and its incidence is rising rapidly. According to the statistics of the World Health Organization, depression has become the fourth largest in the world. It is estimated that by 2020, it may become the second largest disea...

Claims

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Application Information

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IPC IPC(8): C07D307/87A61K31/343A61P25/24
CPCC07B2200/13C07D307/87
Inventor 李德耀张建存邹晴安
Owner GUANGZHOU HENOVCOM BIOSCI CO LTD
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