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Pharmaceutical composition of 3-butyl-3H-2-benzofuran-1-one and preparation method thereof

A technology of benzofuran and composition, applied in the direction of drug combination, cardiovascular system diseases, etc., can solve the problems of "unable to dry, absolute bioavailability less than 20%, not enough to support products, etc., to achieve stable product quality, Achieve large-scale industrial production and improve the effect of bioavailability

Inactive Publication Date: 2013-05-08
许骥 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its apparent oil-water partition coefficient P is greater than 100, lgP>2, and the ability of the drug to pass through the biomembrane is strong, but because it is almost insoluble in water, it becomes the limiting factor of bioavailability
The study found that the absolute bioavailability of oral dl-3-butyl-3H-2-benzofuran-1-one soft capsules was less than 20%
Operating according to the description of Examples 4-9, the soft material cannot be "dried" after the preparation, so the information disclosed in this patent is not enough to support the professional and technical personnel to prepare qualified products according to the examples provided by it.

Method used

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  • Pharmaceutical composition of 3-butyl-3H-2-benzofuran-1-one and preparation method thereof
  • Pharmaceutical composition of 3-butyl-3H-2-benzofuran-1-one and preparation method thereof
  • Pharmaceutical composition of 3-butyl-3H-2-benzofuran-1-one and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Preparation of 3-butyl-3H-2-benzofuran-1-one / polyethylene glycol 200 soft capsules

[0037] The composition of the prescription is as follows: (g)

[0038] 3-Butyl-3H-2-benzofuran-1-one 99.9

[0039] PEG200 0.1

[0040] Make 1000 soft capsules altogether.

[0041] Preparation Process:

[0042] Gelatin gum solutions are routinely prepared.

[0043] Weigh 99.9g of 3-butyl-3H-2-benzofuran-1-one, add the prescribed amount of PEG200, stir to make it evenly mixed, filter, transfer the filtrate to the liquid reservoir of the soft capsule machine, and press it into The soft capsule is dried to obtain the semi-finished product of the soft capsule. After passing the quality inspection, it is subpackaged, labeled and packaged to obtain the finished product of 3-butyl-3H-2-benzofuran-1-one soft capsule. Or filled hard capsules.

Embodiment 2

[0045] Preparation of 1-3-butyl-3H-2-benzofuran-1-one / polyethylene glycol 200 soft capsules

[0046] The composition of the prescription is as follows: (g)

[0047] L-3-butyl-3H-2-benzofuran-1-one 20

[0048] PEG 200 980

[0049] Make 1000 soft capsules altogether.

[0050] Preparation process: with embodiment 1.

Embodiment 3

[0052] Preparation of d-3-butyl-3H-2-benzofuran-1-one / polyethylene glycol 400 soft capsules

[0053] The composition of the prescription is as follows: (g)

[0054] 3-Butyl-3H-2-benzofuran-1-one 99.9

[0055] PEG4000.1

[0056] Make 1000 soft capsules altogether.

[0057] Preparation process: with embodiment 1.

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PUM

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Abstract

The invention discloses a pharmaceutical composition containing a compatible and miscible liquid medium of 3-butyl-3H-2-benzofuran-1-one, and a preparation thereof. The pharmaceutical composition of the invention disperses rapidly when contacting a water phase, can significantly improve the medicament bioavailability, and reduce individual difference; the product quality is improved significantly. The pharmaceutical composition of the invention is suitable for preparing soft capsules or liquid hard capsules, and is easy to realize large-scale industrial production.

Description

technical field [0001] The invention relates to the field of medical technology such as a drug delivery system for water-insoluble liquid medicine and improvement of medicine bioavailability. Specifically, by combining 3-butyl-3H-2-benzofuran-1-one with one of polyethylene glycol, propylene glycol, Tween, and Poloxamer or The combination of the four in any proportion forms a compatible and stable drug delivery system, improves the bioavailability of 3-butyl-3H-2-benzofuran-1-one, and meanwhile the stability of the product is obviously improved. Background technique [0002] Stroke is the third leading cause of death in Western industrialized countries after malignant tumors and cardiovascular diseases. Since the late last century, Western countries have strengthened early intervention on the main factors causing stroke, and the incidence and mortality of stroke have been reduced year by year. In China, which accounts for one-fifth of the world's population, stroke has becom...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61K47/34A61K47/10A61P9/10
Inventor 不公告发明人
Owner 许骥