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Porous composite medicine-loaded composition for improving oral absorption for probucol, and preparation method of porous composite medicine-loaded composition

A technology of probucol and composition, applied in the field of medicine, can solve the problems of low oral bioavailability, large individual differences, and low bioavailability, and achieve improved oral bioavailability, thermodynamic stability, and high bioavailability Effect

Active Publication Date: 2013-09-18
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Probucol is a water-insoluble drug, which has a small dissolution rate in the gastrointestinal tract and is difficult to absorb, resulting in low oral bioavailability and large individual differences, which limit its clinical application
At present, dosage forms such as probucol tablets and capsules have been listed on the market, but because of their poor water solubility and low bioavailability, the present invention has greatly improved this aspect.
[0005] According to literature reports, after mesoporous silica adsorbs drugs, but the toxic and side effects are relatively large, which is harmful to the human body to a certain extent.

Method used

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  • Porous composite medicine-loaded composition for improving oral absorption for probucol, and preparation method of porous composite medicine-loaded composition
  • Porous composite medicine-loaded composition for improving oral absorption for probucol, and preparation method of porous composite medicine-loaded composition
  • Porous composite medicine-loaded composition for improving oral absorption for probucol, and preparation method of porous composite medicine-loaded composition

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Experimental program
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Effect test

preparation example Construction

[0045] Preparation of probucol suspension: the original drug probucol was added to 0.5% hydroxypropyl cellulose aqueous solution and vortexed for 3 minutes to form.

[0046] Preparation of porous calcium carbonate: porous calcium carbonate can be quickly mixed with the same volume of CaCl at room temperature 2 (Contains sodium dodecyl sulfate (SDS)) and Na 2 CO 3 Aqueous solution to prepare. First, under vigorous stirring, add the same volume of 0.2mol / L CaCl 2 The solution and 0.1moL / L SDS solution are mixed quickly, keep stirring and add 0.2mol / L Na equal to the volume of the mixed solution 2 CO 3 Solution. The precipitate was collected by centrifugation, washed three times with deionized water and absolute ethanol, and dried in an oven at 60°C. The sample was calcined at 350°C for 3 hours to remove the residual surfactant SDS in the sample. After calcination, porous calcium carbonate was obtained. CaCO prepared 3 , The hollow microspheres with a nanostructured porous shell, th...

Embodiment 1

[0052] (1) Test materials:

[0053] Probucol technical (Hebei Wuyi Cihang Pharmaceutical Co., Ltd., batch number 20100904), PVPP (American International Specialty Products Company, batch number: 03700178591), isopropyl myristate (Fluka company, batch number: 121617121106124), Cremophor RH40 (Germany BASF, batch number: 04770897V0), ethanol (Sinopharm Chemical Reagent Co., Ltd.).

[0054]

[0055] (2) Test method:

[0056] According to the steps of method two: accurately weigh 1.50 g of isopropyl myristate, Cremophor RH403.85 g, and 2.95 g of ethanol, mix well, weigh 1.00 g of probucol and dissolve in the above solution to obtain a clear solution. Separately weigh 17.50 g of PVPP and stir and mix with the clear solution to obtain a probucol porous composite drug-loading composition.

[0057] (3) Test results:

[0058] Measured by the Malvern nano zs90 (UK) particle size analyzer, the Z average particle size is 22.67nm, and the PDI is 0.239. Compared with probucol bulk drug, the solubi...

Embodiment 2

[0060] (1) Test materials:

[0061] Probucol technical (Hebei Wuyi Cihang Pharmaceutical Co., Ltd., batch number 20100904), diatomaceous earth (Sinopharm Group Chemical Reagent Co., Ltd., batch number 09050204), soybean oil (Tieling Beiya Pharmaceutical Oil Co., Ltd., batch number 09050204), spit Wen 80 (Sinopharm Group Chemical Reagent Co., Ltd., batch number F20100517), Propylene Glycol (Sinopharm Group Chemical Reagent Co., Ltd.).

[0062]

[0063]

[0064] (2) Test method:

[0065] According to the steps of method two: accurately weigh 0.50 g of soybean oil, 6.90 g of Tween, and 4.50 g of propylene glycol, mix well, weigh 1.00 g of probucol and dissolve in the above solution to obtain a clear solution. Separately weigh 19.50 g of diatomaceous earth and grind and mix with a clear solution to obtain a probucol porous composite drug-carrying composition.

[0066] (3) Test results:

[0067] Measured by the Malvern nano zs90 (UK) particle size analyzer, the Z average particle size is 1...

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Abstract

The invention provides a porous composite medicine-loaded composition for improving oral absorption for probucol. The porous composite probucol medicine-loaded composition is stable in thermodynamics, capable of improving the stability of medicaments, stable in gastrointestinal tract environment and free of toxic and side effects, uniform in system dispersion, the solubility of the porous composite medicine-loaded composition in water can be improved by 3-12 times, and the bioavailability of the porous composite medicine-loaded composition can be improved by 2-45 times.

Description

Technical field [0001] The invention relates to the technical field of medicine, in particular to a porous composite drug-carrying composition for improving oral absorption of probucol and a preparation method thereof. Background technique [0002] Probucol is the first hypolipidemic drug marketed in the United States in 1977. Because it lowers high-density lipoprotein cholesterol (HDL) while lowering cholesterol, its market share is low. However, after many years of clinical research, it was found that although Probucol reduced HDL, it did not aggravate atherosclerosis. On the contrary, Probucol showed strong anti-atherosclerotic activity. In addition, probucol also has the effects of anti-oxidation, anti-aging, and treatment of restenosis after angioplasty. [0003] The pharmacological action of Probucol is to reduce blood cholesterol and low-density lipoprotein by reducing cholesterol synthesis, promoting cholesterol decomposition, and changing the nature and function of high-...

Claims

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Application Information

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IPC IPC(8): A61K31/10A61K47/02A61K47/32A61K47/34A61K47/36A61K47/38A61K47/14A61K47/44A61P3/06A61P9/10A61P39/06
Inventor 李亚平黄健顾王文张志文
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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