Enteric solid preparation containing lycopene, resveratrol or melatonin and preparation method of enteric solid preparation

A technology of solid preparations and lycopene, which is applied in the field of enteric-coated solid preparations and its preparation, and can solve problems such as poor solubility improvement, loose binding, and unsaturation

Active Publication Date: 2012-05-16
SINOTHERAPEUTICS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Chinese patent application CN1981742A discloses the application of HPMCAS as a solid dispersion carrier of insoluble drugs, but the application also lists several prior art documents, showing that when HPMCAS and some insoluble drugs are made into solid dispersions, the solubility improves The effect is not good, such as T.Yamaguchi in Yakuzaigaku, 53(4), 221-228(1993), when MAT and HPMCAS or CMEC are made into solid dispersions, the effect of CMEC is better described
After oral administration of MT, MT is absorbed into the blood by passive diffusion and only binds to plasma albumin with a binding rate of about 33%, but its binding is very loose and unsaturated

Method used

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  • Enteric solid preparation containing lycopene, resveratrol or melatonin and preparation method of enteric solid preparation
  • Enteric solid preparation containing lycopene, resveratrol or melatonin and preparation method of enteric solid preparation
  • Enteric solid preparation containing lycopene, resveratrol or melatonin and preparation method of enteric solid preparation

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preparation example Construction

[0061] The preparation method of the water-soluble / enteric-coated solid dispersion of the present invention can adopt the commonly used method for preparing solid dispersion, including melting method, solvent method, solvent-melting method, grinding method, solvent-freeze drying method, solvent-spray drying method and hot-melt extrusion method, etc., for details, please refer to pages 26-29 of the first edition of "New Dosage Forms of Drugs" published by Chemical Industry Press and edited by Zhu Shengshan.

[0062] As a preferred embodiment, the present invention provides an enteric solid preparation, which contains lycopene as an active ingredient, an enteric carrier and / or a water-soluble carrier; The solid dispersion form exists in the preparation, or the water-soluble carrier and the lycopene exist in the solid preparation in the form of a water-soluble solid dispersion, and the solid preparation is coated with an enteric-coated carrier containing an enteric carrier. coati...

Embodiment 1-1

[0094] Weigh 10g each of HPMCAS AS-LF, HPMCP HP-55, Kollidone VA64, Poloxamer188, and Soluplus and dissolve them in 1000g of dichloromethane, then add 0.05g of vitamin C to the above solution and stir until completely dissolved, then add lycopene respectively (manufactured by Changsha Huirui Biotechnology Co., Ltd.) 1 g to form a homogeneous solution. Use Buchi mini spray dryer B-290 to spray dry to remove the organic solvent to obtain a solid dispersion of lycopene. During the spray drying process, the temperature of the material is controlled at 50-55°C.

Embodiment 1-2

[0096] Weigh 20g and 16g of Soluplus and dissolve them in 1000g of dichloromethane respectively, then add 0.05g of vitamin C to the above solution and stir until completely dissolved, then add 1g of lycopene (produced by Changsha Huirui Biotechnology Co., Ltd.) to form homogeneous solution. Use Buchi mini spray dryer B-290 to spray dry to remove the organic solvent to obtain a solid dispersion of lycopene. During the spray drying process, the temperature of the material is controlled at 50-55°C.

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Abstract

The invention relates to the field of medical preparations, in particular to an enteric solid preparation containing lycopene, resveratrol or melatonin and a preparation method of the enteric solid preparation. The enteric solid preparation comprises one or more of lycopene, resveratrol and melatonin as an active ingredient, water-soluble and/or enteric carrier adjuvants or other pharmaceutic adjuvants. The water-soluble carrier adjuvants can be used as water-soluble solid dispersoid carriers; and the enteric carrier adjuvants are enteric polymers and can be used as enteric solid dispersoid carriers or enteric coating film materials. The lycopene, the resveratrol and the melatonin of the enteric solid preparation have favorable dissolubility in the intestinal tract, so that the medicament, namely, the enteric solid preparation, can be rapidly dissolved and released in the intestinal tract, and thus absorption and bioavailability of the lycopene, the resveratrol and the melatonin are increased. The enteric solid preparation containing the lycopene, the resveratrol and the melatonin can be suitable for application and industrial production of oral preparations, such as tablets, particles, pellets, capsules, enteric capsules, enteric coating tablets, enteric coating pellets, enteric coating particles and the like.

Description

technical field [0001] The invention relates to an enteric-coated solid preparation containing lycopene, resveratrol and / or melatonin as active components and a preparation method thereof. Specifically, the enteric solid preparation of the present invention increases the solubility and / or Absorption, which improves the bioavailability of the active ingredients. Background technique [0002] With the development of automated synthesis, combinatorial chemistry and high-throughput screening technologies, more and more new active drugs are also insoluble drugs placed on the pipeline of pharmaceutical engineering. It is estimated that more than 40% of commercially available drugs are insoluble drugs, and insoluble drugs in pharmaceutical industry laboratories account for more than 60% of the total. For drugs with low solubility and high permeability, the rate-limiting step of absorption is the low dissolution rate of the drug. Traditional ordinary tablets are difficult to impr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4045A61K31/01A61K31/05A61K31/375A61K9/00A61K9/28A61P39/06A61P3/06A61P9/00A61P35/00A61P37/04A61P37/02A61P25/20A23L1/30A23L1/302A23L33/15
CPCA61K9/146A61K31/05
Inventor 顾茂健郑启兰
Owner SINOTHERAPEUTICS
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