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Preparation method for antitumor compound capsaicin enteric microcapsule

A capsaicin and anti-tumor technology, which is applied in the direction of anti-tumor drugs, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of incomplete drug absorption, low bioavailability, and large skin irritation and other problems, to achieve the effect of improving bioavailability, smooth surface, and reducing the number of administrations

Inactive Publication Date: 2015-05-13
GOAL TRY MEDICAL TECH HUNAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, because capsaicin has a high hepatic first-pass effect, the half-life is too short, and the bioavailability is low, currently capsaicin is mostly used in topical dosage forms, such as creams, liniments, patches, ointments and cataplasms Wait
However, the above-mentioned external preparations all have disadvantages such as slow onset of action, incomplete drug absorption, great skin irritation, and poor patient compliance, which seriously limit its clinical application.

Method used

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  • Preparation method for antitumor compound capsaicin enteric microcapsule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] 1. Accurately weigh 10g polyacrylic acid resin II, add it to 10mL concentrated ammonia solution as the capsule material solution, and weigh 0.25g poloxamer 188 to dissolve in the capsule material solution, adjust the pH to 8.0 with ammonia water after the dissolution is complete, as the aqueous phase.

[0018] 2. Precisely weigh 1.35g of capsaicin, 0.15g of soybean isoflavone and 0.5g of cod liver oil, and disperse them evenly by ultrasonication for 30min at room temperature as the oil phase.

[0019] 3. With stirring at 50°C and 6000rpm, slowly drop the oil phase into the water phase. After the drop is complete, continue to stir and emulsify for 15 minutes to obtain the primary emulsion.

[0020] 4. Add 25mL of 0.2g / mL Na2SO4 aqueous solution to the emulsion, coagulate under magnetic stirring at 200rpm for 6h, adjust the pH to 4.5 with 10% acetic acid solution, and stir for 0.5h to obtain a homogeneous emulsion.

[0021] 5. Suction filtration, rinse the filter cake wi...

Embodiment 2

[0023] 1. Prepare 200ml of 0.15g / mL polyacrylic acid resin II ammonia solution as the capsule material solution. At the same time, weigh 0.5g of poloxamer 188 and dissolve it in the capsule material solution. After the dissolution is complete, adjust the pH to 8.0 with ammonia water as the water phase.

[0024] 2. Precisely weigh 4.5g of capsaicin, 0.5g of soybean isoflavone and 1.5g of cod liver oil, and disperse them evenly by ultrasonication for 30min at room temperature as the oil phase.

[0025] 3. With stirring at 50°C and 6000rpm, slowly drop the oil phase into the water phase. After the drop is complete, continue to stir and emulsify for 24 minutes to obtain the primary emulsion.

[0026] 4. Add 50mL0.2g / mLNa2SO4 aqueous solution to the emulsion, coagulate under magnetic stirring at 300rpm for 5.5h, adjust the pH to 4.5 with 10% acetic acid solution, and stir for 1h to obtain a homogeneous emulsion.

[0027] 5. Suction filtration, rinse the filter cake with distilled w...

Embodiment 3

[0029] 1. Prepare 300ml of 0.02g / mL polyacrylic acid resin II ammonia solution as the capsule material solution. At the same time, weigh 0.75g of Poloxamer 188 and dissolve it in the capsule material solution. After the dissolution is complete, adjust the pH to 8.0 with ammonia water as the water phase.

[0030] 2. Precisely weigh 8.1g of capsaicin, 0.9g of soybean isoflavone and 3.5g of cod liver oil. At room temperature, ultrasonically disperse it for 30 minutes to make it evenly dispersed as the oil phase;

[0031] 3. With stirring at 50°C and 6000rpm, slowly drop the oil phase into the water phase. After the drop is complete, continue to stir and emulsify for 30 minutes to obtain the primary emulsion.

[0032] 4. Add 75mL of 0.2g / ml Na2SO4 aqueous solution to the emulsion, coagulate under magnetic stirring at 350rpm for 5h, adjust the pH to 4.5 with 10% acetic acid solution, and stir for 1h to obtain a homogeneous emulsion.

[0033] 5. Suction filtration, rinse the filter ...

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Abstract

Relating to the technical field of pharmaceutical preparations, the invention discloses a preparation method for an antitumor compound capsaicin enteric microcapsule. The compound capsaicin enteric microcapsule prepared by a single coacervation-spray drying method has smooth surface, good fluidity, uniform particle size distribution, a particle size of 23-68 micrometers, an average particle size of 42-50 micrometers, a drug loading capacity of 10-12%, and an entrapment rate of 80-87%. The enteric microcapsule provided by the invention can reduce the irritation of capsaicin, enhance drug bioavailability, control targeted release of capsaicin and soy isoflavone in small intestine and colon, and has significant sustained-release and controlled release effects, can increase drug efficacy and improve patient compliance.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a preparation method of anti-tumor compound capsaicin enteric-coated microcapsules. Background technique [0002] At present, the treatment of advanced cancer and chronic intractable pain has always been a difficult problem in the medical field. Oral opioids are generally used for analgesia, but long-term use of such drugs can cause adverse effects, such as excessive sedation, respiratory depression, constipation and addiction etc.; sympathetic nerve resection but the long-term effect is not satisfactory. [0003] Capsaicin (Capsaicin, CAP) is capsicum capsicum L. The main active ingredient is a natural vanillyl amide alkaloid, its chemical name is: N-[(4-hydroxy-3-methoxy-phenyl)-methyl]-8-methyl-( trans)-6-nonenamide. Capsaicin has a variety of complex physiological and pharmacological activities, including anti-inflammatory and analgesic, anti-tumor, car...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61K31/352A61K9/52A61K47/32A61P35/00A61K31/165
Inventor 彭湘林莫兵周波潘登峰
Owner GOAL TRY MEDICAL TECH HUNAN
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