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A kind of rivaroxaban self-emulsifying preparation and preparation method thereof

A rivaroxaban, self-emulsification technology, applied in the field of medicine, can solve the problems of rivaroxaban's low solubility and bioavailability, limited release, bioavailability in vivo, slow dissolution, etc.

Active Publication Date: 2021-04-23
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Rivaroxaban belongs to Class II (low solubility and hypertonicity) in the classification of Biopharmaceutics Classification System (BCS). The low solubility of the drug leads to slow or incomplete dissolution in vitro, which greatly limits its in vitro efficacy. release and in vivo bioavailability
[0006] In summary, due to its low solubility and bioavailability, rivaroxaban greatly limits its application in the field of medicine.

Method used

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  • A kind of rivaroxaban self-emulsifying preparation and preparation method thereof
  • A kind of rivaroxaban self-emulsifying preparation and preparation method thereof
  • A kind of rivaroxaban self-emulsifying preparation and preparation method thereof

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Effect test

Embodiment 1

[0045] Embodiment 1: Rivaroxaban self-emulsifying preparation

[0046] formula:

[0047]

[0048] Preparation:

[0049] Weigh the above prescription amount of oleic acid, polyoxyethylene castor oil and glycerin, mix, and magnetically stir for 10 minutes to form a uniform liquid, then add the prescription amount of rivaroxaban, continue stirring for 30 minutes, and obtain rivaroxaban after fully dissolving Self-emulsifying formulation.

Embodiment 2

[0050] Embodiment 2: Rivaroxaban self-emulsifying preparation

[0051] formula:

[0052]

[0053] Preparation:

[0054] Weigh the above prescription amount of oleic acid, polyoxyethylene castor oil and glycerin, mix, and magnetically stir for 10 minutes to form a uniform liquid, then add the prescription amount of rivaroxaban, continue stirring for 30 minutes, and obtain rivaroxaban after fully dissolving Self-emulsifying formulation.

Embodiment 3

[0055] Embodiment 3: Rivaroxaban self-emulsifying preparation

[0056] formula:

[0057]

[0058] Preparation:

[0059] Weigh the oleic acid, poloxamer 188 and glycerin of the above prescription, mix them, and stir them magnetically for 15 minutes to form a homogeneous liquid, then add the prescribed quantity of rivaroxaban, continue stirring for 30 minutes, and obtain rivaroxaban after fully dissolving Self-emulsifying formulation.

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Abstract

The invention belongs to the field of medicine, in particular to a rivaroxaban self-emulsifying preparation and a preparation method thereof. The rivaroxaban self-emulsifying preparation provided by the present invention comprises 1-13% rivaroxaban, 5-50% oil phase, 20-70% emulsifier, 0-50% co- emulsifier. The varoxaban self-emulsifying preparation of the invention has a particle size distribution of less than 1 μm, can spontaneously emulsify in vivo to form tiny emulsion droplets with a particle size in the range of 20-1000 nm, and improves the solubility and bioavailability of rivaroxaban. The rivaroxaban self-emulsifying preparation can be mixed with suitable solid excipients to achieve solidification, and the obtained rivaroxaban self-emulsifying dispersible tablet improves the low permeability problem of rivaroxaban and dissolves more rapidly. The preparation method of the rivaroxaban self-emulsifying preparation of the present invention has the advantages of simple process and low cost.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to a rivaroxaban self-emulsifying preparation and a preparation method thereof. Background technique [0002] Rivaroxaban is a drug for the prevention and treatment of venous thrombosis. It is also the world's first oral direct factor Xa inhibitor. It was developed by Bayer / Johnson & Johnson. It is mainly used clinically to prevent patients after hip and knee replacement surgery. The formation of deep vein thrombosis (DVT) and pulmonary embolism (PE) can also be used to prevent stroke and non-central nervous system embolism in patients with non-valvular atrial fibrillation, and reduce the risk of recurrence of coronary syndrome. At present, rivaroxaban has been registered and approved in Canada, the European Union, South America, China, Australia and other countries and regions, and its trade name is Xarelto. [0003] Molecular formula of rivaroxaban: C 19 h 18 C l N 3 o 5 S, the chemi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/5377A61K47/44A61K47/12A61K47/10A61K47/26A61K47/14A61K9/20A61P7/02A61P9/14A61P9/10A61P11/00
CPCA61K9/107A61K9/2054A61K9/2095A61K31/5377A61K47/14A61K47/44A61K9/20A61P7/02A61P9/10A61P9/14A61P11/00
Inventor 颜携国张伟明陶安进袁建成
Owner HYBIO PHARMA
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