A kind of bexarotene nano-suspension

A nano-suspension, bexarotene technology, applied in emulsion delivery, medical preparations of non-active ingredients, anti-tumor drugs, etc., can solve the problems of poor dissolution, low bioavailability and difficulty in making common preparations Injection and other problems, to achieve the effect of improving bioavailability, simple preparation process, and uniform release in vitro

Active Publication Date: 2018-06-26
LIAONING UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The dosage forms of bexarotene currently on the market include capsules and gels. Due to the extremely low water solubility of bexarotene, it is difficult to make injections
Ordinary preparations have poor dissolution rate, low bioavailability, and large inter-individual and intra-individual differences
There is no report about bexarotene nanosuspension and its preparation method

Method used

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  • A kind of bexarotene nano-suspension
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  • A kind of bexarotene nano-suspension

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1 Bexarotene nanosuspension

[0025] The prescription is composed of: 0.015g of bexarodene as the main drug, and 0.015g of polyvinylpyrrolidone as the surfactant.

[0026] The specific preparation method is as follows:

[0027] Weigh 0.015g of bexarodene, dissolve in 10ml of 0.1mol / L sodium hydroxide solution, then slowly add dropwise to 10ml of 0.1mol / L hydrochloric acid solution containing 0.015g of polyvinylpyrrolidone, and magnetically stir to obtain Milky suspension. Centrifuge the milky suspension obtained by magnetic stirring, take the precipitate, and add 20ml of distilled water to disperse. The dispersed solution was pulverized by an ultrasonic cell pulverizer at a power of 180 W for 10 minutes to obtain a bexarotene nanosuspension.

Embodiment 2

[0028] Example 2 Bexarotene nanosuspension

[0029] The prescription is composed of: 0.015g bexarotene as the main drug, and 0.0225g polyvinylpyrrolidone as the surfactant.

[0030] The specific preparation method is as follows:

[0031] Weigh 0.015g of bexarodene, dissolve it in 10ml of 0.1mol / L sodium hydroxide solution, then slowly add it dropwise to 10ml of 0.1mol / L hydrochloric acid solution containing 0.0225g of polyvinylpyrrolidone, and stir magnetically to obtain Milky suspension. Centrifuge the milky suspension obtained by magnetic stirring, take the precipitate, and add 20ml of distilled water to disperse. The dispersed solution was pulverized by an ultrasonic cell pulverizer at a power of 180 W for 10 minutes to obtain a bexarotene nanosuspension.

Embodiment 3

[0032] Example 3 Bexarotene nanosuspension

[0033] The prescription is composed of: 0.015g of bexarodene as the main drug, and 0.03g of polyvinylpyrrolidone as the surfactant.

[0034] The specific preparation method is as follows:

[0035] Weigh 0.015g of bexarodene, dissolve it in 10ml of 0.1mol / L sodium hydroxide solution, then slowly add it dropwise to 10ml of 0.1mol / L hydrochloric acid solution containing 0.03g of polyvinylpyrrolidone, and stir magnetically to obtain Milky suspension. Centrifuge the milky suspension obtained by magnetic stirring, take the precipitate, and add 20ml of distilled water to disperse. The dispersed solution was pulverized by an ultrasonic cell pulverizer at a power of 180 W for 10 minutes to obtain a bexarotene nanosuspension.

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Abstract

The invention relates to the field of pharmaceutical preparation, and particularly relates to Bexarotene nano suspension. The Bexarotene nano suspension is characterized by being prepared by Bexarotene and a surfactant. Polyvinylpyrrolidone is used as the surfactant. The weight ratio of the Bexarotene to the surfactant is preferably 1: 1 to 1: 4. By adopting the Bexarotene nano suspension, the medicinal content can be increased, the quality stability is good, the toxicity and side effect is low, and the average granularity is about 100nm to 400nm.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a bexarotene nanosuspension. Background technique [0002] Retinoic acid (Retinoic acid, RA) compounds are used to treat a variety of skin diseases, such as photoaging skin diseases, keratotic skin diseases, etc.; but among all the therapeutic effects of retinoic acid compounds, the most studied is for Prevention and treatment of some malignant tumors, including breast cancer, lung cancer, cervical cancer, skin cancer, etc., it can regulate the differentiation of many tumor cells, inhibit the growth of tumor cells and induce the programmed death of tumor cells. [0003] Bexarotene (structural formula shown in I) is the first retinoic acid X receptor drug approved by the US FDA for the treatment of cutaneous T-cell lymphoma (CTCL), with high biological activity and relatively side effects less. Recent studies have found that bexarotene exhibits high biological activity...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K31/192A61K47/32A61P35/00
Inventor 陈立江刘宇杨佳王永杰陈国良李丽
Owner LIAONING UNIVERSITY
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