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Bexarotene nano suspension

A technology of nanosuspension and bexarotene, which is applied in the directions of emulsion delivery, medical preparations of inactive ingredients, organic active ingredients, etc., can solve the problems of poor dissolution, low bioavailability and difficult preparation of common preparations injection and other problems, to achieve the effect of improving bioavailability, simple preparation process and uniform in vitro release

Active Publication Date: 2015-09-23
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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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1 Bexarotene Nanosuspension

[0025] The composition of the prescription is as follows: 0.015 g of bexarotene is used as the main drug, and 0.015 g of polyvinylpyrrolidone is used as the surfactant.

[0026] The specific preparation method is as follows:

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

Embodiment 2

[0028] Example 2 Bexarotene Nanosuspension

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

[0030] The specific preparation method is as follows:

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

Embodiment 3

[0032] Example 3 Bexarotene Nanosuspension

[0033] The prescription consists of: 0.015 g of bexarotene as the main drug, and 0.03 g of polyvinylpyrrolidone as the surfactant.

[0034] The specific preparation method is as follows:

[0035] Weigh 0.015g of bexarotene, dissolve it in 10ml of 0.1mol / L sodium hydroxide solution, then slowly dropwise add it to 10ml of 0.1mol / L hydrochloric acid solution containing 0.03g of polyvinylpyrrolidone, and stir magnetically to obtain Milky suspension. The milky suspension obtained by magnetic stirring was centrifuged, the precipitate was collected, and 20 ml of distilled water was added for dispersion. The dispersed solution was pulverized by an ultrasonic cell pulverizer for 10 min under the condition of a power of 180 W 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 (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 tumor cell growth and induce tumor cell programmed death. [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). It has high biological activity and relatively few side effects. less. Recent studies have found that bexarotene exhibits high biological activity in the treatment of lun...

Claims

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Application Information

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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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