Unlock instant, AI-driven research and patent intelligence for your innovation.

Ophthalmic Suspension Preparations

A suspension and preparation technology, applied in the field of ophthalmic suspension preparations, can solve the problems of patient invasiveness and patient pain, and achieve the effect of avoiding side effects and reducing burden

Inactive Publication Date: 2020-12-11
SUMITOMO DAINIPPON PHARMA CO LTD
View PDF1 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, all these current treatments, i.e. injection into the eye etc., are very invasive for the patient and cause pain to the patient, so it is desired to develop new drug administration such as eye drops

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
  • Ophthalmic Suspension Preparations
  • Ophthalmic Suspension Preparations
  • Ophthalmic Suspension Preparations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0133] The present invention will be described in detail below by referring to Examples, Reference Examples, Comparative Examples, Tests, etc., but should not be limited thereto.

reference example 1

[0134] Reference Example 1: Preparation of Compound A

[0135] Compound A according to T. Negoro et al. J. Med. Chem. 1998, 41, 4118-4129 prepared by the method described in. Activated carbon (50% humidity, 0.8g) and 2-propanol (101g) were added to its crude product (10g), and the reaction solution was heated to its reflux temperature (about 84°C) and allowed to stand at the same temperature for 30 minutes. The reaction solution was filtered at the same temperature, washed with 2-propanol (13.8 g). The resulting filtrate was heated to 75°C or higher, cooled to 60°C, kept at 60°C for 1 hour, and then cooled to 0°C. The precipitated solid was collected on a filter and dried in vacuo to afford compound A as white crystals (9.3g).

[0136] XRD; 32.4.

[0137] Differential scanning calorimetry (DSC) showed an endothermic peak with an extrapolated melting onset temperature of 186.7 °C.

[0138] The measurement of the above-mentioned powder X-ray diffraction is carried out usi...

reference example 2

[0141] Reference example 2: Preparation of dispersion medium (pH5.0)

[0142]To an aqueous solution of 0.9% (w / v) sodium chloride in 0.02 mol / L aqueous disodium hydrogen phosphate (a) was added a solution of 0.9% (w / v) sodium chloride in 0.01 mol / L aqueous citric acid (b ) to adjust the pH of the solution (a) to 5.0 (addition ratio (a):(b) = about 1:1), to obtain a citrate-phosphate buffer solution with a pH of 5.0. 20 g of hydroxypropyl methylcellulose was dissolved in 380 g of pure water to prepare 400 g of a 5% aqueous solution of hydroxypropyl methylcellulose, to which 1600 g of citrate-phosphate buffer solution of pH 5.0 was added to prepare 2000 g of 1 % hydroxypropyl methylcellulose in water. Dissolve 500mg of 27-33% aqueous solution of alkyldiaminoethylglycine hydrochloride in 400g of 1% aqueous solution of hydroxypropyl methylcellulose, add 2.5g of polysorbate 80 to it, and then dissolve the mixture . The weight of the solution was made 500 g by adding 1% hydroxypr...

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

PropertyMeasurementUnit
particle sizeaaaaaaaaaa
particle sizeaaaaaaaaaa
particle sizeaaaaaaaaaa
Login to View More

Abstract

An ophthalmic suspension formulation comprising (R)-(-)-2-(4-bromo-2-fluorobenzyl)-1,2,3,4-tetrahydropyrrolo[1,2- a] pyrazine-4-spiro-3'-pyrrolidine-1,2',3,5'-tetraketone, the suspension formulation can avoid side effects caused by systemic exposure, and is effective for posterior eye diseases, etc., And has excellent stability.

Description

technical field [0001] The present invention mainly relates to compounds comprising (R)-(-)-2-(4-bromo-2-fluorobenzyl)-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine-4 - Ophthalmic suspension formulations of spiro-3'-pyrrolidine-1,2',3,5'-tetraketone, especially for diseases of the posterior ocular segment. Background technique [0002] Posterior ocular tissues such as the vitreous, retina, choroid, and sclera are important areas for visual performance. If this area is damaged, it can often result in severely reduced visual acuity or loss of vision. Typical diseases of the posterior segment include age-related macular degeneration, diabetic retinopathy, diabetic macular edema, macular edema, myopic choroidal neovascularization, retinal vein occlusion, choroidal neovascularization, uveitis, retinitis pigmentosa, Proliferative vitreoretinopathy and central serous chorioretinopathy. In particular, age-related macular degeneration or diabetic retinopathy is a major disease that cau...

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
Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/499A61K9/10A61P27/02A61P27/06
CPCA61K9/10A61K47/38A61P27/06A61P27/02A61K31/499A61K9/0048
Inventor 落合康加藤佑香佐佐木真纪松本考史
Owner SUMITOMO DAINIPPON PHARMA CO LTD