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Ziprasidone artificial antigen and preparation method thereof

A technology of ziprasidone and artificial antigen, which is applied in the field of ziprasidone artificial antigen and its preparation, can solve the problems of being expensive and requiring professional and technical personnel to operate, and achieve saving time and labor costs, low price, and reducing non-specific Effects of opposite-sex unions

Inactive Publication Date: 2020-03-27
HANGZHOU BIOTEST BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Methods for determining serum or plasma concentration levels of drugs such as ziprasidone involve the use of high performance liquid chromatography (HPLC) with UV or mass detection, gas chromatography-mass spectrometry (GC-MS) detection, and immunoassay, etc. Among them, high performance liquid chromatography (HPLC), gas chromatography-mass spectrometry (GC-MS), etc. require large-scale analytical instruments. These analytical methods are expensive and require professional and technical personnel to operate. Disadvantages such as performing in professional laboratories

Method used

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  • Ziprasidone artificial antigen and preparation method thereof
  • Ziprasidone artificial antigen and preparation method thereof
  • Ziprasidone artificial antigen and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] (1) Preparation of ziprasidone hapten

[0039] Weigh 100mg (0.24mmol) ziprasidone, add it to a 50ml single-necked round-bottomed flask, then add 5ml pyridine, 50mg (0.44mmol) glutaric anhydride, add a stirrer, stir and react at room temperature for 20 hours; , the solvent was evaporated to dryness under reduced pressure, purified by thin layer chromatography, TLC: the chromatographic solution was ethyl acetate, and the product ratio shift value Rf=0.2~0.3; the hapten (2) 75mg was obtained, and the specific synthetic route was as follows figure 1 shown.

[0040] (2) Preparation of ziprasidone artificial antigen

[0041] a. Weigh 50mg (0.09mmol) ziprasidone hapten in a 50ml round bottom flask, add 3ml N,N-dimethylformamide (DMF), then add 64mg (0.57mmol) N-hydroxysuccinyl Amine (NHS) and 114mg (0.55mmol) N,N-dicyclohexylcarbodiimide (DCC), stirred at room temperature overnight, centrifuged after the reaction, and the supernatant was taken as solution A.

[0042] b. Wei...

Embodiment 2

[0055] (1) Preparation of ziprasidone hapten

[0056] Weigh 100mg (0.24mmol) ziprasidone, add it to a 50ml single-necked round bottom flask, then add 5ml pyridine, 0.24mmol glutaric anhydride, add a stirrer, stir and react at room temperature for 22 hours; after the reaction, depressurize Evaporate the solvent to dryness, purify by thin-layer chromatography, TLC: the chromatographic solution is ethyl acetate, the product ratio shift value Rf=0.2~0.3; obtain hapten (2) 85 mg, the specific synthetic route is as follows figure 1 shown.

[0057] (2) Preparation of ziprasidone artificial antigen

[0058] a. Weigh 0.15mmol of hapten in a 50ml round bottom flask, add 4ml of N,N-dimethylformamide (DMF), then add 0.15mmol of N-hydroxysuccinimide (NHS) and 0.15mmol of N,N-di Cyclohexylcarbodiimide (DCC), stirred overnight at room temperature, centrifuged after the reaction, and the supernatant was taken as liquid A.

[0059] b. Weigh 14.5 g of disodium hydrogen phosphate dodecahydrat...

Embodiment 3

[0065] (1) Preparation of ziprasidone hapten

[0066] Weigh 0.20mmol ziprasidone, add it to a 50ml single-necked round bottom flask, then add 5ml pyridine, 0.80mmol glutaric anhydride, add a stirrer, stir and react at room temperature for 10 hours; after the reaction, evaporate the solvent under reduced pressure , purified by thin-layer chromatography, TLC: the chromatographic solution is ethyl acetate, and the product ratio shift value Rf=0.2~0.3; the hapten (2) is obtained, and the specific synthetic route is as follows figure 1 shown.

[0067] (2) Preparation of ziprasidone artificial antigen

[0068] a. Weigh 0.10mmol of hapten in a 50ml round bottom flask, add 3ml of N,N-dimethylformamide (DMF), then add 0.28mmol of N-hydroxysuccinimide (NHS) and 0.48mmol of N,N-dimethylformamide Cyclohexylcarbodiimide (DCC), stirred overnight at room temperature, centrifuged after the reaction, and the supernatant was taken as liquid A.

[0069] b. Weigh 14.5 g of disodium hydrogen ph...

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Abstract

The invention discloses a ziprasidone artificial antigen and a preparation method thereof. A ziprasidone hapten is prepared by directly introducing a glutaric anhydride connecting arm to a secondary amino group of ziprasidone. The introduced connecting arm does not have other characteristic structures, so that non-specific binding caused by a connecting arm can be effectively reduced, and the prepared artificial antigen has better specificity. The hapten reacts with N-hydroxysuccinimide and N, N-cyclohexylcarbodiimide to obtain active ester, and the active ester and carrier protein are subjected to a coupling reaction to obtain the ziprasidone artificial antigen. The ziprasidone artificial antigen is simple in preparation process and low in production cost, and the prepared ziprasidone artificial antigen can be used for animal immunization to obtain a corresponding antibody. The prepared ziprasidone artificial antigen and antibody can be used for detecting whether a sample contains ziprasidone and derivative drugs thereof by using an immunodetection method.

Description

technical field [0001] The invention specifically relates to a ziprasidone artificial antigen and a preparation method thereof. Background technique [0002] Ziprasidone is an atypical antipsychotic with the structural formula: [0003] [0004] In vitro studies have shown that ziprasidone has high affinity for dopamine D2, D3, 5-hydroxytryptamine 5HT2A, 5HT2C, 5HT1A, 5HT1D, a-adrenergic receptors, and moderate affinity for histamine H1 receptors, including No affinity was seen for other receptors / binding sites tested, including M cholinergic receptors. Ziprasidone has an antagonistic effect on dopamine D2, 5-HT2A, and 5-HT1D, and an agonistic effect on 5-HT1A receptors. Ziprasidone inhibits synaptic reuptake of 5-HT and norepinephrine. [0005] Therapeutic drug monitoring (therapeutic drμg monitoring, referred to as TDM) refers to the regular collection of blood (sometimes urine, saliva and other fluids) of patients during the clinical drug treatment process, while ob...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/12C07K14/765C07K1/107C07K16/44
CPCC07D417/12C07K14/765C07K16/44C07K2317/33
Inventor 王百龙苏祥煌
Owner HANGZHOU BIOTEST BIOTECH CO LTD
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