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Preparation method and application of a colorectal localized drug release pharmaceutical composition and its preparation

A colorectal and composition technology, which is applied in the field of medicine, can solve the problems that it is impossible to have a significant improvement, the change of the dissolution of the sample after acid and alkali is not investigated, and the characteristics of colorectal localized release are not considered.

Active Publication Date: 2021-07-06
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the above studies have prepared artemisinin drugs into solid dispersions, they are limited to improving the solubility and dissolution rate of artemisinin and its derivatives, and achieving the effect of sustained release, without considering the colorectal localized release. characteristics, did not investigate the change of the dissolution of the sample in the process of first acid and then alkali (to pH7.6), and did not further develop into a usable dosage form
However, Ma Yin et al. prepared artemether pH-dependent colon-targeted pellets in the "Preparation of artemether colon-targeted pellets and evaluation of in vitro release rate" published in 2016, and investigated their release in vitro. The drug is prepared into pellets, and then coated with methacrylic acid and methyl methacrylate (1:2). The result of disintegration of the pellets in the colon is achieved by means of coating, but the absorption of the drug is different from that of the pellets. There is a direct relationship between the particle size of the drug, and this key parameter is not mentioned in this article
Because the nature of artemether is poor stability, the smaller the particle size, the larger the specific surface area, the poorer the stability, especially unstable under hot and humid conditions, and the preparation of pellets must go through a hot and humid process, so the particle size of artemether is impossible To the extent that improved dissolution
Therefore, although the enteric coating can disintegrate artemether pellets in the colon, the release rate is equivalent to that of ordinary artemether tablets or capsules, and it is impossible to significantly improve

Method used

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  • Preparation method and application of a colorectal localized drug release pharmaceutical composition and its preparation
  • Preparation method and application of a colorectal localized drug release pharmaceutical composition and its preparation
  • Preparation method and application of a colorectal localized drug release pharmaceutical composition and its preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Example 1, Preparation of artemether colorectal localized drug release solid dispersion tablet

[0066] Prescription composition:

[0067]

[0068] Completely dissolve hypromellose acetate succinate (HPMCAS-HF) in 300ml of 80% ethanol, completely dissolve artemether with an appropriate amount of 95% ethanol, and add the ethanol to HPMCAS-HF under the condition of mechanical stirring 500rpm / min solution, continue to stir for 30min. The mixed solution is spray-dried with a spray dryer, and the operating parameters are: set inlet temperature: 50°C, maximum pumping speed percentage: 100%, nitrogen flow rate: 30mm, feed rate: 15% (5mL / min), condensation temperature : 0 ℃, spray dry to obtain artemether colorectal localized drug release solid dispersion. Take the dispersion and add hypromellose aqueous solution to prepare wet granules, dry; mix lactose, microcrystalline cellulose, and sodium carboxymethyl starch evenly, add hypromellose aqueous solution to prepare wet gr...

Embodiment 2

[0069] Example 2, Preparation of Dihydroartemisinin Colorectal Targeted Release Solid Dispersion Tablets

[0070] Prescription composition:

[0071]

[0072] Completely dissolve hypromellose acetate succinate (HPMCAS-HF) in 350ml of 80% ethanol, completely dissolve dihydroartemisinin with an appropriate amount of 95% ethanol, and add it to HPMCAS-HF under the condition of mechanical stirring 500rpm / min In the ethanol solution, continue to stir for 30min. The mixed solution is spray-dried with a spray dryer, and the operating parameters are: set inlet temperature: 50°C, maximum pumping speed percentage: 100%, nitrogen flow rate: 30mm, feed rate: 15% (5mL / min), condensation temperature : 0°C, spraying and drying to obtain the solid dispersion of dihydroartemisinin for colorectal targeted release. Take the dispersion and add carboxymethylcellulose sodium aqueous solution to prepare wet granules, and dry; mix mannitol, microcrystalline cellulose, and carboxymethyl starch sodi...

Embodiment 3

[0073] Example 3, Preparation of Artemisinin Colorectal Targeted Release Solid Dispersion Tablets

[0074] Prescription composition:

[0075]

[0076]

[0077] Completely dissolve methacrylic acid and methyl methacrylate (1:2) in 600ml of 80% ethanol, completely dissolve artemisinin with an appropriate amount of 95% ethanol, and add methacrylic acid and methyl methacrylate under the condition of mechanical stirring at 500rpm / min. In the ethanol solution of methyl acrylate (1:2), continue to stir for 30min. The mixture was spray-dried with a spray dryer. The operating parameters are: set the inlet temperature: 50°C, the maximum pumping speed percentage: 100%, the nitrogen flow rate: 30mm, the feed rate: 15% (5mL / min), the condensation temperature: 0°C, and spray dry to obtain artemisinin Solid dispersion for colorectal localized drug release. Take the dispersion and add carboxymethylcellulose sodium aqueous solution to prepare wet granules, dry; mix sucrose, starch, de...

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Abstract

The invention belongs to the technical field of medicine, and in particular relates to a preparation method and application of a colorectal localized drug release pharmaceutical composition and its preparation. The colorectal localized drug release pharmaceutical composition comprises a colorectal localized drug release solid dispersion containing artemisinin and its derivatives and pharmaceutically acceptable auxiliary materials. The colorectal localized drug release solid dispersion containing artemisinin and its derivatives includes artemisinin and its derivatives and a carrier, wherein the mass ratio of artemisinin and its derivatives to the carrier is 1:0.5-9 , preferably 1:1~6, more preferably 1:1~3. The pharmaceutical composition of the invention can achieve colorectal localized drug release, and because the solid dispersion technology is used, the dissolution and release of the drug in the composition is improved, and the bioavailability is increased. The composition is suitable for the treatment of colorectal cancer, colorectal inflammation and malaria.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a preparation method and application of a colorectal localized drug release pharmaceutical composition and its preparation. Background technique [0002] Artemisinin and its derivatives are semi-synthesized by extracting artemisinin and further modifying its structure. [0003] Artemisinin and its derivatives have been used clinically to treat falciparum malaria and cerebral malaria. However, due to the fact that malaria mainly exists in Africa and Southeast Asia, coupled with the strong promotion of the World Health Organization, the incidence of malaria is decreasing, which brings a great crisis to the world-renowned artemisinin and its derivatives. In addition, artemisinin and Its derivatives also have clear effects on treating unknown high fever, autoimmune diseases, schistosomiasis, pneumonia, and dermatitis. Recent studies have found that artemisinin and its ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/22A61K9/52A61K9/16A61K31/366A61K31/357A61K47/38A61K47/32A61K47/04A61P1/00A61P35/00A61P33/06
CPCA61K9/1611A61K9/1635A61K9/1652A61K9/2009A61K9/2027A61K9/2054A61K9/2077A61K9/4808A61K31/357A61K31/366A61P1/00A61P33/06A61P35/00A61K2300/00Y02A50/30
Inventor 杨兆祥李文婷张国丽张锐武
Owner KPC PHARM INC
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