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Asarone nanocrystallization method

A kind of asarone and nanotechnology, which is applied in nanotechnology, nanotechnology, nanomedicine, etc., can solve the problems of low bioavailability and difficulty in dissolution of oral preparations of asarone, and achieve simple preparation process and high bioavailability in vivo Improvement, the effect of small particle size

Active Publication Date: 2021-05-14
CHINA PHARM UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The object of the present invention is to provide a kind of asarone nanometerization method, improve the solubility and dissolution rate of asarone through nanotechnology, solve the problem of difficult dissolution and low bioavailability of asarone oral preparations

Method used

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Examples

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Effect test

Embodiment 1

[0026] The nanometerization method of asarone

[0027] Weigh 0.250g of polyethylene glycol 15-hydroxystearate and 0.250g of polyvinyl alcohol, place them in a beaker, add about 50g of water to dissolve them completely, and prepare an aqueous stabilizer solution. Weigh 0.500g of asarone crude drug, place it in a 10mL sample bottle, add 5g of polyethylene glycol 400, shake to dissolve the drug, and make an organic phase. Under the conditions of probe ultrasound (2s on, 3s off), the parameters of ultrasound are power 60W, time 5min, absorb the organic phase with a dropper and add it into the stabilizer aqueous solution at a uniform speed to obtain the nano-scale colloidal dispersion of asarone. The particle size measured by the laser particle size analyzer is 119.37nm, and the PDI is 0.261, see figure 1 .

Embodiment 2

[0029] Effects of Probe Ultrasonic Power and Time on the Size of Asarone Nanoparticles

[0030] Weigh 0.050g of polyethylene glycol 15-hydroxystearate and 0.050g of polyvinyl alcohol, place them in a beaker, add about 50g of water to dissolve them completely, and prepare an aqueous stabilizer solution. Weigh 0.050g asarone crude drug, place in a 10mL sample bottle, add 5g polyethylene glycol 400, shake to dissolve the drug, and make an organic phase.

[0031] (1) Ultrasonic power

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Abstract

The invention discloses an asarone nanocrystallization method, and belongs to the technical field of pharmaceutical preparations. According to the nanocrystallization method, an anti-solvent precipitation method is adopted, asarone is firstly dissolved in an organic solvent and then mixed with an aqueous solution of a stabilizer, so that the asarone is supersaturated and separated out to form a stable nanoscale colloidal dispersion. The solubility and dissolution rate of asarone are improved through a nanocrystallization technology, and the problems that an asarone oral preparation is difficult to dissolve out and low in bioavailability are solved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a method for nanometerization of asarone. Background technique [0002] Asarone (Asarone, ARE) is one of the main active ingredients in the rhizomes of plants such as Chinese medicine Shichangpu, also known as α-asarone and asarone, and its chemical name is 2,4,5-trimethoxy-1- Propylbenzene, formula C 12 h 16 O, relative molecular mass 208.26. Asarone is soluble in ethanol, ethyl acetate, chloroform and ether, but hardly soluble in water. A large number of studies have proved that asarone has multiple pharmacological effects such as expectorant, bronchial smooth muscle relaxation, central sedation, anticonvulsant, antibacterial and anti-inflammatory, anticancer and blood lipid lowering. [0003] Currently, the clinically available asarone dosage forms are tablets, capsules and injections, which are commonly used in the treatment of pneumonia, b...

Claims

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Application Information

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IPC IPC(8): A61K31/09A61K47/38A61K47/32A61K47/10A61K47/14A61K47/20A61P11/10A61P11/08A61P35/00A61P31/04A61P3/06A61P25/20A61P25/08B82Y5/00
CPCA61K31/09A61K47/38A61K47/32A61K47/10A61K47/14A61K47/20A61P11/10A61P11/08A61P35/00A61P31/04A61P3/06A61P25/20A61P25/08B82Y5/00
Inventor 蒋曙光尹赛楠赵新宇
Owner CHINA PHARM UNIV
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