20 (S)-PPD liposome emulsion complex oral administration preparation as well as preparation method and application thereof

A technology of body emulsion and complex, which is applied in the field of medicine, can solve the problems of less organic solvent content, high encapsulation rate, and low absorption and utilization, and achieve the effects of improved compatibility, high drug loading, and convenient administration

Active Publication Date: 2022-05-03
沈阳信康药物研究有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation of the present invention has high encapsulation efficiency, simple composition, high drug loading capacity, good stability, less organic solvent content, remarkable drug effect, and can effectively solve the problem of low oral absorption and availability of 20(S)-PPD in vivo

Method used

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  • 20 (S)-PPD liposome emulsion complex oral administration preparation as well as preparation method and application thereof
  • 20 (S)-PPD liposome emulsion complex oral administration preparation as well as preparation method and application thereof
  • 20 (S)-PPD liposome emulsion complex oral administration preparation as well as preparation method and application thereof

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preparation example Construction

[0065] The present invention also provides a preparation method for the preparation described in the above technical scheme, comprising the following steps:

[0066] 1) mixing surfactants, sugars, preservatives and water to obtain an aqueous phase;

[0067] 2) Mixing 20(S)-PPD, phospholipids and absolute ethanol to obtain a medicinal ingredient phase, injecting the medicinal ingredient phase into the water phase described in step 1) to obtain a mixed solution;

[0068] 3) Mix and emulsify the oil phase and the mixed solution in step 2), and filter to obtain the oral administration preparation of 20(S)-PPD liposome emulsion complex.

[0069] The preparation of the present invention is prepared by ethanol injection method.

[0070] In the invention, surfactant, sugar, antiseptic and water are mixed to obtain water phase. In the present invention, the surfactant, sugar and preservative are preferably mixed with part of the water, fully stirred and dissolved, and then the remain...

Embodiment 1

[0087] Weigh 0.05g of sodium oleate, 0.02g of sucralose, and 0.02g of potassium sorbate into 70ml of water, stir well to dissolve, then add the remaining 30ml of water to the full amount to prepare the water phase; weigh 0.2g of 20(S)-PPD and 3.0g of soybean lecithin are placed in a round-bottomed flask, and at a temperature of 60°C, add 5.0ml of reaction solvent absolute ethanol, stir to make it fully dissolve, and slowly inject the prepared aqueous phase with a syringe at a certain speed, water Melt for about 30 minutes; add 10 g of soybean oil, and shear at a high speed of 10,000 rpm for 3 minutes to form colostrum; leave the obtained colostrum to defoam, cool to room temperature, and transfer it to a high-pressure homogenizer. Under the pressure of 800bar, circulate the high-pressure homogenization for 6 times, fill it, and get it.

[0088] The prepared 20(S)-PPD liposome emulsion complex oral administration preparation has an average particle diameter of 160.4±20.0nm, a P...

Embodiment 2

[0090] Weigh 0.05g of sodium oleate, 0.02g of sucralose, and 0.02g of potassium sorbate into 70ml of water, stir well to dissolve, then add the remaining 30ml of water to the full amount to prepare the water phase; weigh 0.2g of 20(S)-PPD and 3.0g of soybean lecithin are placed in a round-bottomed flask, and at a temperature of 60°C, add 5.0ml of reaction solvent absolute ethanol, stir to make it fully dissolve, and slowly inject the prepared aqueous phase with a syringe at a certain speed, water for about 30 minutes; add 10 g of medium-chain triglycerides, and shear at a high speed of 10,000 rpm for 3 minutes to form colostrum; leave the obtained colostrum to defoam, cool to room temperature, transfer to a high-pressure homogenizer, and circulate Under the condition of cold water, circulate high-pressure homogenization with 800 bar pressure 6 times, fill, and obtain.

[0091] The prepared 20(S)-PPD liposome emulsion complex oral administration preparation has an average parti...

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Abstract

The invention relates to a 20 (S)-PPD liposome emulsion complex oral administration preparation as well as a preparation method and application thereof, and belongs to the technical field of medicines. The preparation comprises a water phase, a medicinal ingredient phase and an oil phase, the water phase comprises water, saccharides, a surfactant and a preservative; the medicinal component phase is prepared from 20 (S)-PPD, phospholipid and absolute ethyl alcohol; the oil phase comprises soybean oil and / or medium chain triglyceride. The 20 (S)-PPD liposome emulsion complex oral administration preparation disclosed by the invention is high in drug loading capacity and good in stability, and the concentration of 20 (S)-PPD in the preparation can be controlled to be 1-20mg / ml (m / v); the encapsulation efficiency measured by using an ultracentrifugation method reaches 85% or above, and RSD is less than 2%; the absolute bioavailability of oral administration is high and can reach 31%; after oral administration, damage of podocyte maintaining the integrity of a glomerular filtration barrier can be remarkably relieved, and NS and other chronic nephrotic syndromes can be treated.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a 20(S)-PPD liposome emulsion complex oral administration preparation and a preparation method and application thereof. Background technique [0002] Nephrotic syndrome (NS) is a common chronic kidney disease in the department of nephrology. Nephrotic syndrome (NS) can be caused by various etiologies, and its clinical manifestations include various degrees of edema, hypoalbuminemia and hyperproteinuria, etc. symptom. At present, NS is gradually becoming a chronic urinary system disease that endangers human health. Currently, glucocorticoids (GC) are widely used in clinics at home and abroad, or glucocorticoids plus auxiliary drugs, namely cytotoxic drugs and immunotherapy, are used for treatment. Although the therapeutic effect of glucocorticoids is obvious, there are many serious side effects. For example, a large amount of glucocorticoids in the early stage of treatment can c...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K9/127A61K47/44A61K47/14A61K47/26A61K47/10A61K47/24A61K47/12A61K31/575A61P13/12
CPCA61K9/107A61K9/1271A61K9/0053A61K47/44A61K47/14A61K47/26A61K47/10A61K47/24A61K47/12A61K31/575A61P13/12
Inventor 唐星孟宣瑾刘珂黄浩于叶玲
Owner 沈阳信康药物研究有限公司
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