Preparation method of chitosan-loaded capsaicin microspheres and application of microspheres in weight loss, fat-lowering and blood sugar-lowering

A technology of chitosan microspheres and capsaicin, which is applied in the application, food preparation, pharmaceutical formulation and other directions, can solve the problems of strong irritant effect of CAP, no technical report, etc., achieve excellent sustained release performance, improve compliance, good stability

Active Publication Date: 2011-12-28
健码制药(广东)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the research on the application of capsaicin is all direct application, but the strong irritation of CAP has affected its application. There is no technical report on the use of CTS as a wall material or auxiliary material loaded with capsaicin, and there is no use of CTS to load CAP to achieve relevant synergy. Synergy Technical Report

Method used

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  • Preparation method of chitosan-loaded capsaicin microspheres and application of microspheres in weight loss, fat-lowering and blood sugar-lowering
  • Preparation method of chitosan-loaded capsaicin microspheres and application of microspheres in weight loss, fat-lowering and blood sugar-lowering
  • Preparation method of chitosan-loaded capsaicin microspheres and application of microspheres in weight loss, fat-lowering and blood sugar-lowering

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Example 1 Preparation and detection experiment of CTS-CAP-MP

[0060] 1. Determination of the maximum absorption wavelength of CAP

[0061] In the wavelength range of 190-800nm, CAP, CTS and TPP are scanned at full wavelength, and the optimal absorption wavelength of CAP is selected to reduce the interference of excipients. attached figure 1 It is the ultraviolet full-wavelength scanning diagram of CAP, CTS and TPP, wherein curves 1, 2 and 3 represent the ultraviolet full-wavelength scanning diagram of CAP, TPP and CTS respectively. From attached figure 1 It is found that CAP has strong ultraviolet absorption at 239nm and 281nm and CTS and TPP have very little ultraviolet absorption at this wavelength. After analysis and summary, in order to avoid the influence of terminal absorption, the wavelength of ultraviolet absorption measurement of CAP is selected as 281nm.

[0062] 2. Preparation of CTS-CAP-MP by ionic cross-linking

[0063] Weigh 0.10 g of CTS and fully di...

Embodiment 2

[0089] Example 2 CTS-CAP-MP prescription optimization experiment

[0090] 1. Single factor experiment of CTS concentration

[0091] Under the conditions that the mass of fixed CAP added was 1.5 mg, the concentration of TPP was 1 mg / ml, the pH value was 4.5, and the mass ratio of CTS / TPP was 5:1, the concentrations of CTS were selected to be 0.5 mg / ml, 1.0 mg / ml, 1.5 mg / ml, 2.0mg / ml, 2.5mg / ml and 3.0mg / ml, the impact of CTS concentration on drug loading was investigated by measuring the encapsulation efficiency as the evaluation index. The experimental results of the effect of CTS concentration on the encapsulation efficiency are shown in the appendix Figure 6 shown. attached by Figure 6 It can be seen that as the concentration of CTS increases, the encapsulation efficiency of CAP in the solution will also increase accordingly. However, according to the analysis of the present invention, if the CTS concentration is too high and the viscosity is high, the wall sticking phe...

Embodiment 3

[0116] Example 3 Preparation process optimization experiment of CTS-CAP-MP microspheres

[0117] 1. Selection of inlet air temperature

[0118] In hot air volume 36m 3 / h, the injection rate is 400ml / h, the compressed air pressure is 10l / min, and the inlet temperature of the instrument is set at 140°C, 160°C, and 180°C respectively for single-factor comparative experiments. The experimental results are evaluated by the yield and particle size , investigate the experimental effect of different inlet temperatures, and select the appropriate inlet temperature range. Comprehensive investigation and analysis of the influence of air inlet temperature on the particle size and yield of CTS-CAP-MP, the experimental results are shown in Table 9. The data showed that inlet air temperature had little effect on particle size differences, but had an effect on yield. The yield difference between 160°C (59.6%) and 180°C (59.8%) is not much different, but considering factors such as higher ...

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Abstract

The invention discloses a preparation method of a chitosan-carried capsaicin microsphere as well as the microsphere and application of the microsphere to weight reduction and sugar reduction. In the invention, the chitosan-carried capsaicin microsphere is prepared from a chitosan solution and a capsaicin solution as main raw materials by combining an ion cross-linking method with a spray drying method; and the chitosan and trimeric sodium phosphate are firmly combined by using chemical bonds and are secondarily coated to entrap the capsaicin. The grain diameter of the microsphere is set to be0.8-4.5mum. According to the invention, the coating proportion of the chitosan to the capsaicin is determined, optimal conditions for a preparation process are provided and the secondary coating action on the capsaicin in the ion cross-linking and spray drying is realized. The microsphere has favorable controlled-release characteristics and can be used for realizing synergistic actions of reducing weight, blood fat and blood sugar of the chitosan and the capsaicin; with successful secondary coating, the simulation of the capsaicin is remarkably reduced; the defects that the traditional prepared medicament-carried microsphere is insufficient in yield, uses an organic solvent, poor entrapment rate and medicament-carried amount and the like are overcome; and favorable industrial application significance is realized.

Description

technical field [0001] The invention belongs to the technical field of medicine and health food, and in particular relates to a preparation method of chitosan-loaded capsaicin microspheres (CTS-CAP-MP), the microspheres and their application in weight loss, blood fat reduction and blood sugar reduction. Background technique [0002] Chitosan (Chitosan, CTS) is a natural polycation polysaccharide derivative, which exists in large quantities in the shells of marine arthropods (shrimp, crab, etc.), and also in the cell membranes of lower animal fungi, insects, and algae. Resources It is very abundant. At present, CTS is usually used as a wall material or excipient for the preparation of other drug particles. [0003] Capsaicin (Capsaicin, CAP) is a natural plant alkaloid, which is an active ingredient extracted from the ripe fruit of the Solanaceae plant pepper. It is mainly used for analgesia and antipruritic. Morphine has a long-lasting effect. [0004] At present, the rese...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/165A61K47/36A61P3/04A61P3/06A61P3/10A23L1/29A23L33/00
Inventor 苏政权陶毅高冰谭思荣
Owner 健码制药(广东)有限公司
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