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Antidepressant composition containing citalopram and cyclodextrin

A technology of composition and cyclodextrin, which is applied in the field of clathrate oral pharmaceutical composition, can solve the problems of increased production cost, increased impurities, and high requirements for equipment and operators

Inactive Publication Date: 2006-10-04
KUNMING JIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the taste of this kind of compound is extremely bitter, and the method of directly adding a flavoring and odorant cannot cover up its bitter taste. For this kind of extremely bitter drug, the commonly used taste masking method is to form a complex or powder coating of the drug and ion exchange resin. Law
The inventor found in the experiment that after the ion-exchange of this class of medicines with ion-exchange resins, its impurities increased significantly, and this was because the stability of citalopram was greatly reduced when it existed in the form of free base; and another method powder coating method Higher requirements for equipment and operators increase production costs

Method used

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  • Antidepressant composition containing citalopram and cyclodextrin

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1: Bitterness test

[0034] Add β-cyclodextrin to the 2 mg / ml citalopram hydrobromide solution, so that the molar ratio of β-cyclodextrin to citalopram hydrobromide is 0, 0.5, 1.0, 2.0, 3.0, and carry out the solution for 7 people. Bitterness test, the results are as follows:

[0035] Molar ratio (βCD / citalopram hydrobromide) 0 0.5 1.0 2.0 3.0

[0036] Very weak bitterness 0 0 3 7 7

[0037] Stronger bitterness 0 2 4 0 0

[0038] Strong bitterness 7 5 0 0 0

[0039] When β-cyclodextrin is added to the citalopram hydrobromide solution, the bitterness of the solution decreases with the increase of the amount of cyclodextrin, and when the molar ratio of cyclodextrin to citalopram reaches 2:1, the bitterness decreases very significant.

Embodiment 2

[0040] Embodiment 2: solubility test

[0041] In the presence of cyclodextrin, the water solubility of hydrophobic molecules increases, the dissolution rate and the dissolved amount of active substances both increase, so the change in water solubility is a common method to prove the formation of inclusion complexes.

[0042] Prepare three kinds of solutions A, B, C, wherein A is adding 2g citalopram hydrobromide in 50ml water; B is adding 5.6g β-cyclodextrin in 50ml water; C is adding 2g citalopram hydrobromide in 50ml water Phalopram and 5.6 g β-cyclodextrin. Stir the three solutions at the same time until they reach an equilibrium state. It can be observed that the substances in A and B cannot be completely dissolved, while the solution in C is clear. This phenomenon indicates that clathrates are formed, and the solubility of the active substance and cyclodextrin is increased.

Embodiment 3

[0043] Embodiment 3: inclusion rate test

[0044] Select three factors and three levels, and determine the best inclusion process through the following orthogonal experiments (considering the actual production situation, with the inclusion rate as the inspection target), the active substances used in this test are citalopram hydrobromide, cyclodextrin For β-cyclodextrin:

[0045] Inclusion rate = drug content in the inclusion compound / dosage × 100%

[0046] Inclusion compound three-factor three-level table

[0047]

[0048] A: Molecular ratio of drug to cyclodextrin

[0049] B: stirring temperature

[0050] C: Stirring time

[0051] Test No.

[0052] It can be seen from the R value that the influence of each factor on the inclusion rate is B>A>C, and the optimal inclusion process is: A 1 B 2 C 2 , that is, the molecular ratio is 1:2, the inclusion temperature (stirring temperature) is 50° C., and the inclusion time (stirring time) is 60 minutes. Under these...

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Abstract

The invention relates to an oral medicinal composition comprising Citalopram, its optical isomer or inclusion compound formed by their medicinal salts with cyclodextrin. The composition can be made into various dosage types including chewable tablets, dispersible tablets, orally disintegrating tablets or granules.

Description

technical field [0001] The present invention relates to an antidepressant oral pharmaceutical composition, in particular to an oral pharmaceutical composition comprising an inclusion compound formed by citalopram, its optical isomers or their pharmaceutically acceptable salts and cyclodextrin. Background technique [0002] Antidepressants are a class of drugs that mainly treat depression, moodiness, pessimism, and negativity. After medication, they can uplift the mood, enhance thinking ability, and improve energy. [0003] Citalopram is an antidepressant that acts on the central nervous system. Its antidepressant effect is through inhibiting the reuptake of 5-hydroxytryptaminergic neurons in the central nervous system. The concentration of 5-hydroxytryptamine neurotransmitter increases, thereby enhancing the activity of 5-hydroxytryptaminergic system to achieve antidepressant effect. Citalopram has a positive antidepressant effect, and does not affect cognition and psychomo...

Claims

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Application Information

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IPC IPC(8): A61K31/343A61K47/40A61P25/24
Inventor 尤广智冯朴纯
Owner KUNMING JIDA PHARMA
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