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Eltrombopag oral suspension and preparation method thereof

A suspension and solution technology, applied in the fields of blood diseases, liquid delivery, pharmaceutical formulations, etc., can solve the problems that oral solid preparations are unfavorable for children and the elderly to swallow, the production cost of liquid capsules is high, and the economic burden of patients is increased. Physical and chemical stability, good physical and chemical compatibility, and good quality indicators

Inactive Publication Date: 2019-06-18
WUHAN WUYAO SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Eltrombopag ethanolamine is a reddish-brown powder, and the solvent is wine red after being slightly dissolved. The main drug in the solution will gradually transfer to the capsule shell, resulting in discoloration of the capsule shell and migration of components, which seriously affects the appearance and reduces patient compliance.
Moreover, the production cost of liquid capsules is much higher than that of solid preparations
This product is a drug for long-term use, and the cost of raw materials is high, coupled with high manufacturing costs, it will inevitably increase the economic burden on patients
[0008] In summary, liquid capsules are expensive, patients have poor compliance, oral solid preparations are not conducive to swallowing by children and the elderly, and it is not easy to divide doses, and dry suspensions cannot use non-deionized water and other existing technologies. Insufficient, it is necessary to develop a preparation that is convenient to take, easy to divide doses and accurate in dose

Method used

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  • Eltrombopag oral suspension and preparation method thereof
  • Eltrombopag oral suspension and preparation method thereof
  • Eltrombopag oral suspension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] (1) Preparation prescription (1000mL in total):

[0050]

[0051]

[0052] (2) Preparation process:

[0053] 1) Disperse sodium carboxymethyl cellulose in 800mL of water medium, heat to 80-100°C under agitation to swell and clarify, and cool to room temperature to obtain solution I.

[0054] 2) Add Eltrombopag ethanolamine (Eltrombopag particle size D90 is 20-50 μm) to solution I. Homogenization speed 3000-6000rpm, disperse for 5-10min, mix and flocculate to obtain suspension II;

[0055] 3) adding citric acid and sodium citrate to the suspension II to adjust the pH value to 6.0-6.8 to obtain the suspension III;

[0056] 4) Add preservative sodium benzoate, sweetener mannitol and flavoring agent sweet orange powder essence to suspension III, stir for 10 minutes under the condition of 30 Hz, add water to 1000 mL after dissolving, and obtain Eltrombopag oral suspension liquid.

Embodiment 2

[0058] (1) Preparation prescription (1000ml made in total):

[0059]

[0060] (2) Preparation process:

[0061] 1) Disperse sodium carboxymethyl cellulose in 800mL of water medium, heat to 80-100°C under agitation to swell and clarify, and cool to room temperature to obtain solution I.

[0062] 2) Add Eltrombopag ethanolamine (Eltrombopag particle size D90 is 10-40 μm) to solution I, disperse for 5-10 min at a homogenizing speed of 3000-6000 rpm, mix well, and flocculate to obtain suspension II;

[0063] 3) adding citric acid and sodium citrate to the suspension II to adjust the pH value to 6.0-6.8 to obtain the suspension III;

[0064] 4) Add preservative sodium benzoate, sweetener mannitol and flavoring agent sweet orange powder essence to suspension III, stir at 30 Hz for 10 min, add water to 1000 mL after dissolving, and obtain Eltrombopag oral suspension.

Embodiment 3

[0066] (1) Preparation prescription (1000mL in total):

[0067]

[0068] (2) Preparation process:

[0069] 1) Disperse sodium carboxymethyl cellulose in 800mL of water medium, heat to 80-100°C under agitation to swell and clarify, and cool to room temperature to obtain solution I.

[0070] 2) Add Eltrombopag ethanolamine (Eltrombopag particle size D90 is 50-90 μm) to solution I, disperse at a homogenizing speed of 3000-6000 rpm for 5-10 minutes, mix and flocculate to obtain suspension II;

[0071] 3) adding citric acid and sodium citrate to the suspension II to adjust the pH value to 6.0-6.8 to obtain the suspension III;

[0072] 4) Add preservative sodium benzoate, sweetener mannitol and flavoring agent sweet orange powder essence to suspension III, stir at 30 Hz for 10 min, add water to 1000 mL after dissolving, and obtain Eltrombopag oral suspension.

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Abstract

The invention discloses an eltrombopag oral suspension. The eltrombopag oral suspension is prepared from the following components: 0.15%-0.64% of eltrombopag ethanolamine, 0.5%-8.0% of carboxymethyl cellulose, 0.1%-0.5% of a PH combination regulator, 60.0%-80.0% of an aqueous medium, 0.2%-0.3% of a preservative, 18.0%-32.0% of a sweetening agent and 0.1%-0.2% of a corrigent. The eltrombopag oral suspension overcomes the defects of low solubility, difficulty in dissolution, multiple specifications and complex production process of eltrombopag, and a new dosage form selection is provided; and apreparation method of the eltrombopag oral suspension is simple and feasible and has reproducibility, and the eltrombopag oral suspension with the quality meeting the requirements can be consistentlyproduced.

Description

technical field [0001] The application belongs to the field of pharmaceutical preparations, and more specifically, the application relates to an Eltrombopag oral suspension and a preparation method thereof. Background technique [0002] Eltrombopag is a small-molecule thrombopoietin receptor (TPO-R) agonist with high oral bioavailability, and its mechanism of action is similar to, but not identical to, endogenous thrombopoietin (TPO). It can induce the proliferation and differentiation of bone marrow progenitor cells into megakaryocytes. In healthy people and patients with thrombocytopenia, daily administration of Eltrombopag can increase platelet count, and the higher the dose, the greater the increase. Therefore, Eltrombopag can treat some conditions of decreased platelet production. [0003] Eltrombopag tablets were jointly developed by Ligand Pharmaceuticals of the United States and GlaxoSmithKline (GSK) of the United Kingdom, and were approved for marketing by the FDA...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/4152A61K47/38A61P7/04
Inventor 赵寅李自毅杨波冯小路郭婷婷
Owner WUHAN WUYAO SCI & TECH
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