Check patentability & draft patents in minutes with Patsnap Eureka AI!

Riociguat oral fast-dissolving film and preparation method thereof

An oral instant film, riociguat technology, which is applied in pharmaceutical formulations, medical preparations without active ingredients, medical preparations containing active ingredients, etc., can solve the complex preparation process, bitter taste, low solubility of riociguat problem, to achieve the effect of high bioavailability, rapid onset of action, and improved taste

Inactive Publication Date: 2020-05-01
合肥圣迪利克医药科技有限公司
View PDF1 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Riociguat has low solubility in water and a bitter taste. CN201410635422.6 discloses a solid pharmaceutical preparation containing Riociguat, which uses a water-soluble polymer material as a drug carrier, and is prepared by heating, high-speed stirring, low-temperature cooling, and pulverization. Solid dispersion, complex preparation process

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
  • Riociguat oral fast-dissolving film and preparation method thereof
  • Riociguat oral fast-dissolving film and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033]

[0034]

[0035] (1) Take the riociguat bulk drug of the prescribed amount, and use a jet mill to pulverize until the D90 is within the range of 5-15 μm;

[0036] (2) Dissolving the polacrilin sodium and the pulverized riociguat bulk drug in an appropriate amount of solvent, and stirring for 30 minutes;

[0037] (3) Then add low-substituted hydroxypropyl cellulose, aspartame, strawberry flavor, natural carotene, triethyl citrate, chlorobutanol, use a homogenizer at a speed of 1500rpm, stir evenly, and vacuum degass ;

[0038] (4) Apply with a film coating machine, dry in a horizontal hot air circulation oven for 2 hours, and put it in the drying room to cool to room temperature;

[0039] (5) Laser cutting machine cutting, inner packaging, inspection, and outer packaging after passing the inspection.

Embodiment 2

[0041] name % by weight Rio Ciguat 2.5 Low-substituted hydroxypropyl cellulose 80 Polacrilin Potassium 15.44 Cyclamate 0.01 Tween 60 2 aspartame 0.01 Banana Spice 0.02 grape purple pigment 0.01 sodium benzoate 0.01 Ethanol solution (ethanol evaporates when dry) /

[0042] (1) Take the riociguat bulk drug of the prescribed amount, and use a jet mill to pulverize until the D90 is within the range of 5-15 μm;

[0043] (2) Dissolving the polacrilin potassium and the pulverized Riociguat bulk drug in an appropriate amount of solvent, and stirring for 30 min;

[0044] (3) Then add low-substituted hydroxypropyl cellulose, aspartame, banana flavor, grape violet, Tween 60, and sodium benzoate, use a homogenizer at a speed of 1500 rpm, stir evenly, and vacuum degas;

[0045] (4) Apply with a film coating machine, dry in a horizontal hot air circulation oven for 2 hours, and put it in the drying room to cool to ro...

Embodiment 3

[0048] name % by weight Rio Ciguat 2.5 Low-substituted hydroxypropyl cellulose 80 Polacrilin sodium 15.44 Cyclamate 0.01 triethyl citrate 2 aspartame 0.01 orange spice 0.02 Gardenia yellow pigment 0.01 sodium benzoate 0.01 Ethanol solution (ethanol evaporates when dry) /

[0049] (1) Take the riociguat bulk drug of the prescribed amount, and use a jet mill to pulverize until the D90 is within the range of 5-15 μm;

[0050] (2) Dissolving the polacrilin potassium and the pulverized Riociguat bulk drug in an appropriate amount of solvent, and stirring for 30 min;

[0051] (3) Then add low-substituted hydroxypropyl cellulose, aspartame, banana flavor, grape violet, Tween 60, and sodium benzoate, use a homogenizer at a speed of 1500 rpm, stir evenly, and vacuum degas;

[0052] (4) Apply with a film coating machine, dry in a horizontal hot air circulation oven for 2 hours, and put it in the drying room to co...

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 invention discloses a riociguat oral fast-dissolving film and a preparation method thereof, and relates to the technical field of pharmaceutical preparations. The riociguat oral fast-dissolving film comprises the following components: riociguat, a taste masking agent, a film forming material, a plasticizer, a sweetening agent, a spice, a pigment and a bacteriostatic agent. The riociguat oral fast-dissolving film is prepared through scientific combination of auxiliary materials and a main drug, namely the riociguat; the prepared riociguat oral fast-dissolving film can effectively cover thebitter taste of the riociguat, and the taste of the preparation is remarkably improved; meanwhile, the riociguat oral fast-dissolving film takes effect quickly, is high in bioavailability and is superior to a conventional riociguat tablet; and the preparation method is suitable for industrial production.

Description

Technical field: [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a riociguat oral instant film and a preparation method thereof. Background technique: [0002] Riociguat is a stimulator of soluble guanylate cyclase (sGC), an enzyme in the cardiopulmonary system and a receptor for nitric oxide (NO). When NO binds to sGC, the enzyme catalyzes the synthesis of the signaling molecule cyclic guanosine monophosphate (cGMP), which plays an important intracellular role in the regulation of vascular tone, proliferation, fibrosis and inflammation. Pulmonary hypertension is accompanied by endothelial dysfunction, impaired nitric oxide synthesis and insufficient stimulation of the NO-sGC-cGMP pathway. Riociguat has a dual mode of action. It synthesizes GC to endogenous NO by stabilizing NO-sGC binding. Riociguat also directly stimulates through a different binding site independent of NO. Riociguat stimulates the NO-sGC-cGMP pathwa...

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): A61K9/70A61K31/506A61K47/38A61P9/12A61P11/00A61P7/02
CPCA61K9/006A61K9/7007A61K31/506A61K47/38A61P7/02A61P9/12A61P11/00
Inventor 高扬张中涛何新欢
Owner 合肥圣迪利克医药科技有限公司
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More