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Method for preparing helicid liposome

A technology of neurasthenia fruit and liposomes, which is applied in the field of preparation of neurasthenia fruit liposomes, can solve the problems of poor cell similarity, histocompatibility, low bioavailability, and poor water solubility, etc. Bioavailability, avoiding toxic and side effects, increasing the effect of absorption in the body

Inactive Publication Date: 2011-12-07
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 out 0.04 g of commercially available Shenshoucarin (purity greater than 99%), and dissolve it in 80 g of a phosphate buffer solution with pH=7.4 to obtain the phosphate buffer solution of Shenshoucarin. The preparation of pH=7.4 phosphate buffer solution is to first weigh 31.2g of commercially available analytically pure NaH 2 PO 4 ·2H 2 O, then distilled water to make the volume to 1L, stir to obtain a molar concentration of 0.2mol / LNaH 2 PO 4 . Weigh 71.6g of commercially available analytically pure Na 2 HPO 4 ·12H 2 O, distilled water to make the volume to 1L, stir to obtain Na with a molar concentration of 0.2mol / L 2 HPO 4 Solution, and then weigh out 19.0mL of 0.2mol / L NaH prepared above 2 PO 4 And 81.0mL 0.2mol / L Na of the above configuration 2 HPO 4 , The two are mixed.

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

Embodiment 2

[0016] Weigh 0.25g of Shenshouguosu and dissolve it in 75g of phosphate buffer solution with pH=8. Weigh out 0.09 g of cholesterol, 0.03 g of egg yolk lecithin, and 0.03 g of soybean lecithin, dissolve them in 9 g of absolute ethanol, and distill off the ethanol on a rotary evaporator to prepare a lipid dry film. Dissolve the lipid dry film with 27g of ether, then add 9g of pre-prepared phosphate buffer solution of Shenshouguo, ultrasonic for 30min, 20℃ rotary evaporation to remove the ether, and finally in a 30℃ water bath, continue to rotate and incubate for 2h to obtain Shenshouguo Vegetarian liposomes.

[0017] The preparation of the phosphate buffer solution with pH=8 is: Weigh 5.3 mL of 0.2mol / L NaH prepared in Example 1 2 PO 4 Solution and 94.7mL of 0.2mol / L Na 2 HPO 4 Solution, mix the two.

Embodiment 3

[0019] Weigh 0.05g of Shenshouguosu and dissolve it in 80g of pH=6 phosphate buffer solution. Weigh out 0.04 g of cholesterol, 0.08 g of egg yolk lecithin, and 0.01 g of soybean lecithin, dissolve them in 12 g of absolute ethanol, and distill off the ethanol on a rotary evaporator to prepare a lipid dry film. Dissolve the lipid dry film with 35g ether, and then add 50g pre-prepared phosphate buffer solution of Shenshouguo, ultrasonic for 45min, 10℃ rotary evaporation to remove the ether, and finally in a 25℃ water bath, continue to rotate and incubate for 2h to obtain Shenshouguo Vegetarian liposomes.

[0020] The preparation of the phosphate buffer solution with pH=6 is: weigh 87.7 mL of 0.2mol / L NaH obtained in the configuration of Example 1 2 PO 4 Solution and 12.3mL of 0.2mol / L Na 2 HPO 4 Solution, mix the two.

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PUM

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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 helicidliposome 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 Shenshouguosu liposome. It belongs to the field of medical technology. Background technique [0002] Shenshouguosu, also known as tofu fruit glycosides, and its chemical name is p-formaldehyde benzene-O-β-D-alopyranoside. It is an effective ingredient extracted from the plant dark green mountain longan. It has hypnotic sedative, anticonvulsant, Analgesic, anti-inflammatory and anti-depressant effects. At present, there are soft capsules, tablets, etc. related to the preparation of Shenshou fruit, such as "tofu fruit glycoside soft capsule and its preparation method" (Chinese invention patent application number: 03117667.4, publication number: CN1535690). "Fruit quick-release tablet and its preparation method" (Chinese invention patent application number: 03140524.X, publication number: CN1454600) and "a tofu fruit glycoside orally disintegrating tablet" (Chinese invention patent application number: CN200410...

Claims

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Application Information

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Patent Type & Authority Patents(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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