Application of chrysalis oil in improving small molecule drug bioavailability

A technology of silkworm chrysalis oil and small molecules, which is applied in the field of biomedicine, can solve the problems of low absorption, side effects, and slow effect, and achieve the effects of increased drug absorption concentration, wide application prospects, and strong improvement ability

Active Publication Date: 2014-01-22
TIANJIN YAOYU BIOLOGICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Puerarin preparations on the market, such as puerarin injections or puerarin-containing preparations, have great deficiencies, such as injections, because puerarin is a small molecule drug extracted from the traditional Chinese medicine Pueraria lobata, in the process of extraction, purification, etc. The purity of puerarin cannot be 100%, and the trace impurities contained in it can easily cause toxic and side effects after injection, such as allergic hemolysis and other adverse reactions. For tablets that can be marketed, due to the unique water insolubility of puerarin, its oral absorption is very slow low, so the curative effect is not good and the effect is relatively slow, these are the limitations of its clinical, and silkworm chrysalis oil as an auxiliary material, its bioavailability in oral administration has increased by nearly 5 times, and silkworm chrysalis oil has no toxic side effects, which is very good in itself. good health food

Method used

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  • Application of chrysalis oil in improving small molecule drug bioavailability
  • Application of chrysalis oil in improving small molecule drug bioavailability
  • Application of chrysalis oil in improving small molecule drug bioavailability

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1: Exploration of liquid phase conditions and selection of internal standard

[0024] Chromatographic column Venusil XBP C18 (4.6mm×250mm, 5m); the mobile phase is methanol: water (30:70) (v / v); the flow rate is 0.7ml / min, the column temperature is 30°C; the ultraviolet detection wavelength is 250nm; Amount of 20l internal standard is 4-hydroxybenzaldehyde.

Embodiment 2

[0025] Embodiment 2: Serum processing and determination

[0026] After the blood was collected, the mice were kept still at room temperature for 30 minutes, centrifuged at 3500 rpm at 4°C for 10 minutes, and 190 μl of the supernatant was taken into a 1.5ml EP tube, 10 μl of 4-hydroxybenzaldehyde internal standard solution (100 μg / ml) was added and shaken to mix, and 400 μl of acetonitrile was added. Vortex for 5 minutes, centrifuge at 12,000 rpm for 10 minutes, take the supernatant and pass it through a 0.22 μm organic membrane, and load 20 μl of the sample.

Embodiment 3

[0027] Embodiment 3: the preparation of standard stock solution and standard curve

[0028] Accurately weigh 10 mg of puerarin standard substance, put it in a 10ml volumetric flask, add methanol to dissolve and dilute to the mark, shake well, and then obtain 1mg / ml internal standard stock solution; then dilute to concentrations of 5, 10, 25, 50 , 100, and 225 μg / ml of puerarin methanol series standard solutions, respectively get 10 μl and add in 190 μl serum, add 10 μl 4-hydroxybenzaldehyde internal standard solution (100 μg / ml) and shake and mix well, and the processing method is the same as that in "Example 2 Serum Processing and Determination", HPLC detection, with the blood drug concentration C of puerarin as the abscissa, and the peak area ratio A of puerarin as the ordinate, the standard curve equation is A=0.0014C+0.076, at 83ng / ml~3750ng / ml Good linearity in the range.

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Abstract

The present invention relates to a use of chrysalis oil for improving bioavailability of a small molecule drug, and belongs to the field of biological medicine. The present invention uses mainly a silkworm as a material, finds the chrysalis oil, i.e. a chrysalis component which is effective to improve the bioavailability of the small molecule drug (puerarin), and validates and calculates the results. The results show that the bioavailability is improved by 4.7 times relative to a control, and up to 6-9 times relative to the control with regard to the 30 min timepoint. The chrysalis oil is safe and stable, has no toxic side effect and has an extremely wide application prospect.

Description

technical field [0001] The invention relates to the use of silkworm chrysalis oil in improving the bioavailability of small molecule drugs, belonging to the field of biomedicine. Background technique [0002] Before any kind of raw material drug is applied to the clinic, it must be made into a certain dosage form. In addition to the raw material drug, some auxiliary materials are required to form the dosage form, which is conducive to the stability, solubilization, solubility enhancement, and sustained release of these drugs. , Usually these auxiliary materials are collectively referred to as pharmaceutical excipients or drug excipients. The development of a pharmaceutical excipient is far more significant than the development of a new drug. In the preparation process of pharmaceutical preparations, whether the selection of pharmaceutical excipients is appropriate will directly affect the bioavailability, toxic and side effects, and adverse reactions of the drug. [0003] ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/44A61K31/352A61P9/00A61P9/10A61P9/12A61P3/06A61P25/28A61P7/02A61P39/06
CPCA61K47/44A61K31/353A61P3/06A61P7/02A61P9/00A61P9/10A61P9/12A61P25/28A61P39/06
Inventor 张耀洲张丽吴少峰陈剑清舒特俊
Owner TIANJIN YAOYU BIOLOGICAL TECH
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