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Medicinal preparation

A preparation and medicine technology, applied in the field of pharmaceutical preparations, can solve the problem of no record of stability, and achieve the effect of improving stability

Pending Publication Date: 2019-10-25
KOWA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in this document, the preparation of each composition is carried out for use in pharmacological tests, and there is no description about the stability of netadil and verosudil in the composition. In addition, what kind of material is the container? , and the characteristic container has no record

Method used

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  • Medicinal preparation
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0223] Below, the present invention is further described by enumerating examples, but the present invention is not limited by them.

[0224] In addition, in the following test examples, in the measurement of netadil using HPLC, an ODS column was used as a column, 0.01 mol / L phosphate buffer and acetonitrile were used as a mobile phase, and an ultraviolet absorptiometry (wavelength : 254nm).

manufacture example 1~36

[0300] Aqueous compositions containing the ingredients and amounts (amount (g) per 100 mL of the aqueous composition) described in Tables 9 to 17 were prepared in accordance with a conventional method, and contained in Test Example 3 using a mixture containing benzotriazole The container (primary package) for eye drops made of polypropylene, which is an ultraviolet absorber, can produce the pharmaceutical preparations of Production Examples 1 to 36.

[0301] [Table 9]

[0302]

[0303] [Table 10]

[0304]

[0305] [Table 11]

[0306]

[0307] [Table 12]

[0308]

[0309] [Table 13]

[0310]

[0311] [Table 14]

[0312]

[0313] [Table 15]

[0314]

[0315] [Table 16]

[0316]

[0317] [Table 17]

[0318]

manufacture example 37~72

[0320] In Production Examples 1 to 36, except that the container was made of polyethylene instead of polypropylene, the pharmaceutical preparations of Production Examples 37 to 72 could be produced using the same container as that used in Test Example 3.

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PUM

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Abstract

The present invention establishes a technology for stably formulating an isoquinoline-6-amino derivative as an ophthalmic agent or the like. Provided is a medicinal preparation that is obtained by housing, in a package capable of blocking light having a wavelength of 320-380 nm, an aqueous composition containing a compound represented by general formula (1) (in the formula: R1 and R2 each independently represent a hydrogen atom or a C1-C4 alkyl group; R3 represents a hydrogen atom or a hydroxyl group; 'A' denotes -CH(R4)- or -CH2-CH(R4)- (here, R4 is an optionally substituted C6-C10 aryl groupor an optionally substituted 5 to 10-membered heteroaryl group); and formula (1) also includes a tautomer thereof) or a salt thereof, or a solvate thereof.

Description

technical field [0001] The present invention relates to pharmaceutical preparations and the like. Background technique [0002] So far, several isoquinoline-6-amino derivatives have been known to be useful for the prevention and treatment of eye diseases such as ocular hypertension and glaucoma. [0003] Specifically, for example, the following structural formulas are reported: [0004] [0005] The compound shown (chemical name: {4-[(2S)-3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl]phenyl}methyl 2, 4-Dimethylbenzoate ([4-[(2S)-3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl]phenyl]methyl 2,4-dimethylbenzoate), International common name: netarsudil. In addition, hereinafter, in this specification, it may be referred to as "netarsudil".) Also known as AR-13324, which has Rho kinase inhibitory activity, norepinephrine transporter inhibitory activity, etc. Pharmacological actions are useful for the prevention and treatment of eye diseases such as ocular hypertens...

Claims

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Application Information

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IPC IPC(8): A61K31/472A61J1/05A61K9/08A61K31/4725A61K47/04A61K47/10A61P27/02A61P27/06B65D1/00B65D65/20
CPCA61K9/08A61K31/472A61K31/4725A61K47/10A61P27/02A61P27/06A61K31/5575A61K31/5377A61K9/0048A61K2300/00A61J1/1468
Inventor 山北佳央
Owner KOWA CO LTD
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