Sodium cholate coated liposoluble medicament metacortandracin intercalation hydrotalcite and preparation method thereof

A fat-soluble drug, prednisone technology, applied in the field of adrenal cortex hormone drugs, to achieve the effect of effective storage

Inactive Publication Date: 2009-02-18
BEIJING UNIV OF CHEM TECH
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] The object of the present invention is to provide a kind of fat-soluble drug prednisone intercalation hydrotalcite system and preparation method thereof, obtain a kind of hydrotalcite adrenal cortex hormone drug that drug effect is relatively stable in storage and taking process, to solve At present, prednisone has strong side effects during use

Method used

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  • Sodium cholate coated liposoluble medicament metacortandracin intercalation hydrotalcite and preparation method thereof
  • Sodium cholate coated liposoluble medicament metacortandracin intercalation hydrotalcite and preparation method thereof

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Embodiment Construction

[0019] Step A: Weigh 1.72g of cholic acid and dissolve it in 150ml to remove CO 2 in deionized water, fully stirred to obtain solution I; weigh 0.03g prednisone and dissolve it in 20ml chloroform to obtain solution II; add solution II to solution I, N 2 Protect, volatilize chloroform 4-5 hour, be that chloroform volatilizes completely when seeing that solution becomes transparent, obtain the aqueous solution of required sodium cholate micelles inclusion prednisone.

[0020] Step B: take by weighing 1.80g Mg(NO 3 ) 2 ·6H 2 O and 1.32g Al(NO 3 ) 3 9H 2 O dissolved in 25ml to remove CO 2 , deionized water to prepare a mixed salt solution, and another 0.84g NaOH was dissolved in 25ml to remove CO 2 , deionized water to obtain an alkali solution; the solution obtained in step A is placed in a four-necked flask, and the double-drop co-precipitation method is used in a water bath at 70 ° C under N 2 Add the salt solution and alkali solution dropwise to the solution obtained i...

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Abstract

The invention provides a sodium cholate entrapped fat soluble medicine prednisone insertion-layer hydrotalcite and a method for preparing the same, which belongs to the technical field of the adrenalocortical hormone medicine. The chemical formula of the sodium cholate entrapped fat soluble medicine prednisone insertion-layer hydrotalcite is as follows: (M<2+>)1-x(M<3+>)x(OH<->)2(C21H26O5)a(C24H39O5<->)x.mH2O; the fat soluble medicine prednisone is entrapped to form micelle by utilizing a surface active agent of sodium cholate, and one-step synthesized into the hydrotalcite product with the mutual insertion-layer of the prednisone and the sodium cholate by the coprecipitation method so as to form the supermolecule layering material in which the weight of the fat soluble medicine molecules is 4 percent of the total weight of the hydrotalcite. The preparation method comprises the following steps: firstly, aqueous solution with the sodium cholate micelle entrapped the prednisone is prepared, and the hydrotalcite layering material with the sodium cholate micelle entrapped the prednisone is synthesized by the double-drip coprecipitation method. The hydrotalcite and the method for preparing the same have the advantages that by utilizing the restricted space action and the interaction between the main body and the object, the fat soluble medicine prednisone is inserted in layers of the hydrotalcite by the insertion-layer, thereby realizing the effective storage of the fat soluble medicine in the hydrotalcite and simultaneously achieving the slow-release performance of the chiral medicines in the hydrotalcite.

Description

technical field [0001] The invention belongs to the technical field of adrenocortical hormone drugs, and in particular provides a fat-soluble drug prednisone intercalated hydrotalcite and a preparation method thereof. Since prednisone is a fat-soluble drug, it cannot directly enter the interlayer of hydrotalcite, so a surfactant, sodium cholate, is used to co-intercalate between the interlayers of hydrotalcite to achieve the purpose of sustained release. technical background [0002] Prednisone (Prednisone) is an adrenocorticosteroid drug, and its acetate is commonly used, which is a white or almost white crystalline powder. Prednisone must reduce the 11-position keto group to 11-hydroxyl in the liver, and convert it into prednisolone to show pharmacological activity. It has anti-inflammatory and anti-allergic effects, can inhibit the proliferation of connective tissue, reduce the permeability of capillary walls and cell membranes, reduce inflammatory exudation, and inhibit...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K47/02A61K31/573A61P29/00A61P37/08
CPCA61K31/575A61K9/107A61K31/573A61P29/00A61P37/08A61K2300/00
Inventor 卫敏李复苏陆军段雪
Owner BEIJING UNIV OF CHEM TECH
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