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Method for preparing helicid liposome

A saccharin and liposome technology, which is applied in the field of preparation of saccharin liposomes, can solve the problems of poor water solubility, low bioavailability, poor cell similarity and histocompatibility, etc. Absorption, avoiding toxic and side effects, and improving drug bioavailability

Inactive Publication Date: 2010-09-15
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the relatively poor water-solubility of neurasthenia, most of these neurasthenia preparations have disadvantages such as low bioavailability, poor cell similarity, and poor histocompatibility.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Weigh 0.04 g of commercially available neurasthenia (purity greater than 99%), and dissolve it in 80 g of phosphate buffer solution with pH=7.4 to obtain a phosphate buffer solution of neurasthenia. The preparation of the phosphate buffer solution of pH=7.4 is to take commercially available 31.2g analytical pure NaH 2 PO 4 2H 2 O, then dilute to 1L with distilled water, stir to obtain a molar concentration of 0.2mol / LNaH 2 PO 4 . Take by weighing 71.6g commercially available analytical pure Na again 2 HPO 4 12H 2 O, dilute to 1L with distilled water and stir to obtain Na with a molar concentration of 0.2mol / L 2 HPO 4 solution, then, weigh 19.0mL of the above-mentioned configured 0.2mol / L NaH 2 PO 4 and 81.0mL of 0.2mol / L Na in the above configuration 2 HPO 4 , a mixture of both.

[0014] Weigh 0.02g of analytically pure cholesterol, 0.02g of biologically pure egg yolk lecithin, and 0.005g of soybean lecithin produced by TCI (Shanghai) Chemical Industry Deve...

Embodiment 2

[0016] Weigh 0.25 g of Shenshen Fruit and dissolve it in 75 g of pH=8 phosphate buffer solution. Weigh 0.09g of cholesterol, 0.03g of egg yolk lecithin, and 0.03g of soybean lecithin, dissolve them in 9g of absolute ethanol, and distill off the ethanol on a rotary evaporator to obtain a lipid dry film. Dissolve the dry film of lipid with 27g of ether, then add 9g of pre-prepared phosphate buffer solution of Shenshen fruit, sonicate for 30 minutes, remove the ether by rotary evaporation at 20°C, and finally continue to rotate and incubate in a water bath at 30°C for 2 hours to obtain Shenshen fruit liposomes.

[0017] The preparation of the phosphate buffer solution of pH=8 is: take the 0.2mol / LNaH of 5.3mL that the embodiment 1 configuration obtains 2 PO 4 solution and 94.7mL of 0.2mol / L Na 2 HPO 4 solution, mix the two.

Embodiment 3

[0019] Weigh 0.05 g of Shenshen Fruit and dissolve it in 80 g of pH=6 phosphate buffer solution. Weigh 0.04g of cholesterol, 0.08g of egg yolk lecithin, and 0.01g of soybean lecithin, dissolve them in 12g of absolute ethanol, and distill off the ethanol on a rotary evaporator to obtain a lipid dry film. Dissolve the dry film of lipid with 35g of ether, then add 50g of pre-prepared phosphate buffer solution of Shenshen fruit, sonicate for 45 minutes, remove the ether by rotary evaporation at 10°C, and finally continue to rotate and incubate in a water bath at 25°C for 2 hours to obtain Shenshen fruit liposomes.

[0020] The preparation of the phosphate buffer solution of pH=6 is: take the 0.2mol / LNaH of 87.7mL that the embodiment 1 configuration obtains 2 PO 4 solution and 12.3mL of 0.2mol / L Na 2 HPO 4 solution, mix the two.

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Abstract

The invention relates to a method for preparing helicid liposome, which comprises the following steps of: weighing and uniformly mixing the helicid and buffer solution of phosphoric acid with a pH value of 6 to 8 in the mass ratio of 1:300-20,000 to obtain the buffer solution of phosphoric acid of the helicid; weighing and uniformly mixing cholesterol, yolk lecithin, soybean lecithin and ethanol in the mass ratio of 1: 0.2-2.5: 0.1-1: 100-800, and distilling the mixture on a rotary evaporator for removing the ethanol to obtain a lipid dry membrane; dissolving the lipid dry membrane in ether, and then adding the buffer solution of phosphoric acid of the helicid, wherein the mass ratio of the ether to the cholesterol is 300-3,000:1; the mass ratio of the buffer solution of phosphoric acid of the helicid to the cholesterol is 100-1,500:1; performing ultrasound processing on the mixture for 5 to 60 minutes, and rotationally evaporating the mixture at the temperature of between 10 and 20 DEG C for removing the ether; and finally, rotationally incubating the mixture in a water bath at the temperature of between 20 and 50 DEG C for 1 to 2 hours to obtain the helicid liposome. The helicid liposome has the advantages of high targeting performance, slow releasing performance, low toxicity and biocompatibility, and contribution to medicament absorption and improvement on bioavailability of medicament.

Description

technical field [0001] The invention relates to a preparation method of neurasthenia liposome. It belongs to the field of medical technology. Background technique [0002] Shenshouguo element, also known as tofu glucoside, chemically named p-formaldehyde benzene-O-β-D-alopyranoside, is an active ingredient extracted from the plant dark green longan, which has hypnotic and sedative, anticonvulsant, Analgesic, anti-inflammatory and antidepressant effects. At present, there are soft capsules, tablets, etc. in the reports about the Shenshen fruit preparation, such as "Tofu fruit glycoside soft capsule and its preparation method" (Chinese invention patent application number: 03117667.4, publication number: CN1535690), "A kind of Shenshen fruit Fruit element quick-release tablet and its preparation method" (Chinese invention patent application number: 03140524.X, publication number: CN1454600) and "a kind of tofu fruit glycoside orally disintegrating tablet" (Chinese invention p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7034A61P25/08A61P25/20A61P25/24A61P29/00
Inventor 甘礼华樊荣陈柳华刘明贤陈龙武
Owner TONGJI UNIV
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