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Oral liquid preparation

A liquid preparation and liquid technology, applied in the field of medical liquid preparations, can solve the problems of improving dissolution, undisclosed, blonanserin solubility, and dissolution have not been studied, and achieve good dissolution effect

Inactive Publication Date: 2012-05-16
SUMITOMO DAINIPPON PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Patent Document 1 discloses tablets, powders, and injections containing blonanserin as an active ingredient. However, no studies have been conducted on the stability of the formulation or the solubility and dissolution of blonanserin at various pHs. There is also no disclosure of a stable formulation that improves dissolution by solubilizing blonanserin, etc., and maintains a solution state

Method used

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Examples

Experimental program
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Effect test

Embodiment 1～4

[0059] Citric acid (anhydride) was added to purified water to prepare a 25 mM citric acid aqueous solution. Then, according to the formula of Example 1 in Table 1, blonanserin was added to the citric acid aqueous solution, and a magnetic stirrer was used to stir at room temperature until the blonanserin was dissolved to prepare a liquid preparation containing blonanserin (implementation example 1). After preparation, the pH of the liquid formulation is measured.

[0060] Similarly, according to the method of Example 1, each component was charged in the amount described in Table 1, and liquid preparations containing blonanserin were respectively prepared (Examples 2 to 4).

[0061] [Table 1]

[0062] .

Embodiment 5～10

[0064] A 25 mM citric acid aqueous solution was prepared in the same manner as in Example 1. Next, each component was added in the amount described in Table 2 to this citric acid aqueous solution, and the liquid preparation containing blonanserin was prepared by the method similar to Example 1 (Examples 5-10).

[0065] [Table 2]

[0066] .

Embodiment 11～13

[0068] Using purified water and malic acid, a 50 mM malic acid aqueous solution was prepared. Next, each component was added to the malic acid aqueous solution in the amount described in Table 3, and a liquid preparation containing blonanserin was prepared by the same method as in Example 1 (Examples 11 to 13).

[0069] [table 3]

[0070] .

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Abstract

Disclosed is an oral liquid preparation which contains 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10- hexahydrocycloocta[b] pyridine (an active ingredient) stably and can exhibit good elution behavior of the active ingredient in a wide pH range. The oral liquid preparation comprises the active ingredient and a dissolution aid for the active ingredient, and has an elution rate of 50% or more in an elution test in accordance with the Japanese pharmacopoeia 15th edition 15 minutes after the start of the test in a second elution test solution.

Description

technical field [0001] The present invention relates to a medical liquid preparation for oral administration containing 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)- 5,6,7,8,9,10-hexahydrocyclooctatetraeno[b]pyridine (hereinafter sometimes referred to as "blonanserin" or "active ingredient") as an active ingredient. Background technique [0002] Blonanserin is for dopamine D 2 receptor and serotonin 5-HT 2 A compound that has a strong receptor blocking action and exhibits few side effects such as extrapyramidal symptoms, drowsiness, hypotension, and weight gain (Patent Document 1). Blonanserin is already marketed by Dainippon Sumitomo Pharmaceutical Co., Ltd. as a therapeutic drug for schizophrenia under the trade names of "Lonasen Tablet" and "Lonasen Powder". In addition, in recent years, as dosage forms for the treatment of schizophrenia, from the viewpoint of improvement in medication compliance and increase in treatment options, not only the existing oral solid prepa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61K9/08A61K47/02A61K47/12A61K47/26A61P25/18A61P43/00
CPCA61K31/496A61K9/08A61K9/0095A61P25/18A61P43/00A61K47/12A61K47/26
Inventor 大仁田麻衣子鉾之原和博斎藤晃一
Owner SUMITOMO DAINIPPON PHARMA CO LTD
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