Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Medicine

A technology of medicine and compounds, applied in the field of pharmaceutical preparations, to achieve the effect of improving stability

Pending Publication Date: 2019-10-15
KOWA CO LTD
View PDF7 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in this document, the preparation of each composition is completed for use in a pharmacological test, and there is no description about the stability of netadil or verosudil in the composition. In addition, the container What kind of material and characteristics, there is no record

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Medicine
  • Medicine
  • Medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0136] Next, the present invention will be further described with reference to examples, but the present invention is not limited to these at all.

[0137] In addition, in the following test example, for the measurement of Netadil by HPLC, an ODS column was used as the column, 0.01 mol / L phosphate buffer and acetonitrile were used as mobile phases, and an ultraviolet absorbance photometer (wavelength: 254nm) was used. As a detector.

manufacture example 1~36

[0162] An aqueous composition containing the ingredients and amounts (amount (g) per 100 mL of the aqueous composition) described in Table 4 to Table 12 was prepared according to the usual method, and stored in polyethylene terephthalate eye drops The drug container can manufacture the pharmaceutical preparations of Manufacturing Examples 1 to 36.

[0163] [Table 4]

[0164]

[0165] [table 5]

[0166]

[0167] [Table 6]

[0168]

[0169] [Table 7]

[0170]

[0171] [Table 8]

[0172]

[0173] [Table 9]

[0174]

[0175] [Table 10]

[0176]

[0177] [Table 11]

[0178]

[0179] [Table 12]

[0180]

manufacture example 37~72

[0182] In Production Examples 1 to 36, a container for eye drops made of high-density polyethylene was used instead of a container for eye drops made of polyethylene terephthalate, and the pharmaceutical preparations of Production Examples 37 to 72 could be produced.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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 polyester-based resin container or polyolefin-based resin container, 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 are known to be useful in the prevention or treatment of ocular diseases such as ocular hypertension or glaucoma. [0003] Specifically, for example, the following structural formula is reported: [0004] [0005] The compound shown (chemical name: {4-[(2S)-3-amino-1-(isoquinoline-6-ylamino)-1-oxopropane-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. Hereinafter, in this specification, sometimes labeled as "netadil".), which is also known as AR-13324, has Rho kinase inhibitory effect, norepinephrine transporter inhibitory effect, etc. The pharmacological action is useful in the prevention or treatment of ocular diseases such as ocular hypertension and glaucoma (for example, Pate...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K31/472A61J1/05A61K9/08A61K31/4725A61K47/04A61K47/10A61P27/02A61P27/06B65D1/00B65D65/20
CPCA61K9/08A61K31/472A61K31/4725A61K47/10A61P27/02A61P27/06A61K9/0048A61J1/1468
Inventor 山北佳央
Owner KOWA CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products