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Application of PLGA in preparation of SSRI antidepressant drug microspheres

An antidepressant and drug technology, which is applied in the application field of preparing SSRI antidepressant drug microspheres, can solve the problems of unstable blood drug concentration, lethal dose of blood drug concentration, patients not taking drugs according to rhythm, etc., so as to shorten the side effects. The effect of time, blood drug concentration rising rapidly, prolonging drug action time

Pending Publication Date: 2020-08-25
鸡西代悦科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] (2) There is a first-pass effect of oral drugs, which leads to differences in blood drug concentrations in the body when each patient takes the same dose of drugs orally, resulting in significant differences in drug efficacy (genetic differences in liver drug metabolism enzymes)
Puts patients at greater risk when physicians are given inaccurate information to alter drug doses
[0009] (3) The blood drug concentration is unstable, and changes in blood drug concentration beyond the normal range will cause irritation to patients, especially in the field of mental / psychotherapy
Toxic / intolerable concentrations that exceed the normal dosage of the drug will cause relapse of the disease, and even lead to suicidal tendencies, which will bring great distress to the patient and family members, especially when the patient's compliance is poor and the family members are unable to take care of them
In the previous clinical practice, doctors expressed the helplessness of recognizing the value but not enough control in the control of blood drug concentration: when receiving inaccurate and non-objective information, doctors may make decisions that are not conducive to psychological treatment plans, including blindly changing psychotherapy. This not only affects the curative effect, but also may increase the risk of side effects at the same time, and the iatrogenic compliance will also be reduced, or it may cause some patients’ resistance
[0010] (4) Difficulty in supervising drug administration, resulting in safety issues or poor treatment effects, such as:
[0011] Safety issues brought about by difficulty in medication supervision: Psychotherapy is not the same as psychotherapy, and 24-hour supervision rarely exists, and the risk of taking related drugs is much higher than conventional drugs. The worry that every psychologist / psychotherapist faces is : When the patient holds the drug by himself, he takes a large amount of drug privately in some way, causing the blood drug concentration to reach a lethal dose, or causing irreversible permanent damage to the human body, etc.
[0012] Compliance problems caused by medication supervision: patients do not take medication according to the rhythm, poor compliance, and active / passive refusal to take medication is very common. According to research, only 30% of patients will fully follow the doctor's advice to take medication
After administration, only 1%-15% exists in the systemic circulation, and the plasma protein binding rate is 80%-95%, which leads to the slow onset of the drug and takes a long time
5-HT in the central nervous system is widely involved in a variety of physiological processes in the central and peripheral nervous systems, including the gastrointestinal tract and platelets, causing appetite, cognitive and emotional functions, etc., but because the physiological processes involved in 5-HT are in When the antidepressant effect is not reached, the 5-HT receptor is inhibited, and the secretion of 5-HT is reduced, which in turn affects some other normal physiological processes

Method used

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  • Application of PLGA in preparation of SSRI antidepressant drug microspheres
  • Application of PLGA in preparation of SSRI antidepressant drug microspheres
  • Application of PLGA in preparation of SSRI antidepressant drug microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] The preparation of sertraline hydrochloride microspheres comprises the steps:

[0054] (1) PLGA (50:50, M=5000-15000, end group is carboxyl, IV=0.152) is dissolved in organic solvent and is prepared into the solution that concentration is 5wt%, according to feeding mass ratio sertraline: PLGA=1: 15. Slowly add sertraline into the above solution, pre-stir to homogenize, and sonicate at 25 kHz for 15 min as the dispersed phase; use 1% polyvinyl alcohol aqueous solution as the continuous phase;

[0055] Wherein, the organic solvent is a mixed solvent composed of dichloromethane and ethyl acetate in a volume ratio of 1:0.05.

[0056] (2) Add the dispersed phase to the continuous phase at a speed of 0.05ml / s, the continuous phase: dispersed phase (v / v)=(1:0.9)-(1:1.1), adjust the pH to 6.5, 32°C Next, the volume of the agitator: stirring area = 0.4, the closed reaction system was homogenized for 1 hour, and the homogenization speed was 1000 r / min.

[0057] (3) Open the tra...

Embodiment 2

[0065] For the sertraline hydrochloride microspheres prepared in Example 1, according to the requirements of the latest version of "Chinese Pharmacopoeia", the following inspections are made:

[0066] (1) Wash the microspheres several times with ethanol and deionized water, destroy them with solvents such as acetonitrile, deionized water and ethanol, and extract sertraline hydrochloride in the solution. The extracted sertraline hydrochloride was dissolved and diluted with ethanol to make a solution with a concentration of about 0.2 mg / ml. According to the ultraviolet-visible spectrophotometry (general rule 0401), there should be obvious absorption at the wavelengths of 266nm, 274nm and 282nm.

[0067] According to the ultraviolet spectrophotometer, the ultraviolet absorption spectrum of the microsphere product before and after dissolution is as follows: Figure 4 As shown, there are maximum absorption peaks at 266nm, 274nm and 282nm (±0.2nm), and the peak positions are consist...

Embodiment 3

[0071] 1. the mensuration of the drug loading of the sertraline hydrochloride microspheres prepared by embodiment 1 and the encapsulation efficiency:

[0072] (1) Standard curve

[0073] Take 20 mg of sertraline hydrochloride crude drug in a 100ml volumetric flask, use a diluent to set the volume to the mark, and obtain a 0.2 mg / ml solution as a reference substance stock solution; dilute the reference substance stock solution with a diluent to prepare a mass concentration A series of standard solutions of 5, 10, 20, 50, 100, 200 μg / ml. The diluent used is a mixed solution of ethanol and acetonitrile, ethanol:acetonitrile (v / v)=50:50. Use a UV spectrophotometer to detect the absorbance value of each level of sample at 274 nm. The results are shown in Table 1.

[0074] Table 1

[0075] Concentrationμg / ml Absorbance 0 0.001 5 0.021 10 0.036 20 0.075 50 0.185 100 0.362 200 0.718

[0076] Use the obtained absorbance value as t...

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Abstract

The invention discloses application of PLGA in preparation of SSRI antidepressant drug microspheres and belongs to the field of pharmaceutical preparations. The invention also discloses the SSRI antidepressant drug microspheres prepared by combining PLGA and an SSRI antidepressant drug, the particle size of the microspheres is 18-22 [mu]m, and the invention also discloses a preparation method of the microspheres. The combination of the SSRI antidepressant drug and the pharmaceutical adjuvant PLGA can make the blood drug level reach an antidepressant effect in a human body in a relatively shorttime, reduce adverse reactions in the blood drug level rising process, release the antidepressant drug steadily, and completely improve patient compliance and medication safety. The SSRI drug and PLGA complement each other in terms of medication safety in the human body. The SSRI antidepressant drug microspheres are administered by injection, thereby avoiding the problem of individual differencein the blood drug level caused by the liver metabolism process in an oral absorption process.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to the application of PLGA in the preparation of SSRI antidepressant drug microspheres. Background technique [0002] With the increasing pressure of modern life, people's psychological problems are becoming more and more common. More and more people in the society have realized the importance of mental health. Whether it is in psychotherapy or psychological counseling, the demand at home and abroad is becoming more and more extensive. , strong, and its field is increasingly popular and recognized by society. Many people are subjectively willing to improve their mental health with the help of professionals, thereby improving their quality of life, which has opened up a positive concept change. The number of psychotherapy practitioners and popularizers has exploded, and the professional level is getting higher and higher. It is expected that after decades of development, p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K9/52A61K31/137A61P25/24
CPCA61K9/5031A61K9/5089A61K9/0019A61K31/137A61P25/24
Inventor 华鹏王昀许恒劲
Owner 鸡西代悦科技有限公司
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