A nano-carrier slow-release preparation for treating cardiovascular disease and its preparation method

A nano-carrier and sustained-release preparation technology, which is applied in the field of nano-carrier sustained-release preparations for cardiovascular treatment and its preparation, can solve the problems of pentoxifylline being difficult to store, affecting the curative effect, etc., and achieves reduction of adverse reactions, stable dissolution rate, Avoid burst effects

Active Publication Date: 2022-05-31
HEBEI CHEM & PHARMA COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The problem in the existing technology is that pentoxifylline is not easy to store, and it is easy to degrade and produce impurities under high temperature or exposure to light, thereby affecting the curative effect. There are many adverse reactions caused by vasodilation and unstable blood drug concentration, such as headache Adverse reactions such as edema, fatigue, insomnia, nausea, abdominal pain, flushing, palpitations, dizziness, itching, rash, dyspnea, weakness, muscle cramps, indigestion, myocardial infarction and chest pain restrict clinical application

Method used

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  • A nano-carrier slow-release preparation for treating cardiovascular disease and its preparation method
  • A nano-carrier slow-release preparation for treating cardiovascular disease and its preparation method
  • A nano-carrier slow-release preparation for treating cardiovascular disease and its preparation method

Examples

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Effect test

preparation example 1

[0040] Preparation Example 1: Preparation of Pentoxifylline Nanocarrier Lyophilized Powder

[0041] The molecular weight of chitosan oligosaccharide is 2400Da; the weight ratio of chitosan oligosaccharide, deoxycholic acid and albumin is 1: 2.8: 3.2, and the specific preparation method is as follows:

[0042] (1) Preparation of chitosan oligosaccharide-deoxycholic acid composite microspheres

[0043] The chitosan solution with a concentration of 1 mg / mL was adjusted to pH 5.5 with sodium hydroxide solution to obtain a chitosan solution, which was used for later use;

[0044] A deoxycholic acid solution with a concentration of 1 mg / mL was adjusted to pH 5.5 with a dilute hydrochloric acid solution; a deoxycholic acid solution was obtained, which was used for later use.

[0045] The chitosan solution and the deoxycholic acid solution were uniformly mixed according to the volume ratio of 1:2.8, and stirred at 25° C. for 2 h to form a solution of chitosan-deoxycholic acid composi...

preparation example 2

[0051] Preparation Example 2: Preparation of Pentoxifylline Nanocarrier Lyophilized Powder

[0052] The molecular weight of chitosan oligosaccharide is 2300Da, and the rest are the same as in Preparation Example 1.

preparation example 3

[0053] Preparation Example 3: Preparation of Pentoxifylline Nanocarrier Lyophilized Powder

[0054] The molecular weight of chitosan oligosaccharide is 2500Da, and the rest are the same as in Preparation Example 1.

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Abstract

The invention provides a nano-carrier slow-release preparation for treating cardiovascular disease and a preparation method thereof, which is composed of pentoxifylline nano-carrier freeze-dried powder and pharmaceutical auxiliary materials. Described pentoxifylline nano-carrier lyophilized powder, the weight ratio of pentoxifylline and nano-carrier is 4~5:1; Described nano-carrier material is the composition of chitosan-deoxycholic acid-albumin, wherein The weight ratio of chitooligosaccharide, deoxycholic acid and albumin is 1:2-3:3.0-3.3; the weight ratio of the pentoxifylline and the pharmaceutical excipient is (4-7):1, the drug The excipients are composed of hydroxyethyl cellulose, micropowder silica gel and magnesium stearate, wherein the weight ratio of hydroxyethyl cellulose, micropowder silica gel and magnesium stearate is (5-6):(3-4):1. The dissolution rate of the sustained-release nanocarrier preparation for the treatment of cardiovascular provided by the present invention is stable, basically showing zero-order linear dissolution, avoiding sudden release, greatly ensuring the therapeutic effect of pentoxifylline, and significantly reducing adverse reactions; placed under accelerated conditions After 6 months, the content of degradation products is low and the quality is stable.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, relates to a nanocarrier sustained-release preparation for cardiovascular treatment and a preparation method thereof, and more particularly relates to a nanocarrier sustained-release preparation for cardiovascular treatment comprising pentoxifylline and a preparation method thereof. Background technique [0002] Pentoxifylline is a methylxanthine derivative, the chemical name is 3,7-dihydro-3,7-dimethyl-1-(5oxohexyl), the structural formula is as follows, it is extracted from cocoa beans An alkaloid obtained by re-introducing the hexanone group from the theobromine, which is white powder or granules; slightly odorous, slightly bitter; easily soluble in triazomethane, soluble in water or ethanol, slightly soluble in ether . [0003] Pentoxifylline can improve blood circulation in the brain and limbs, increase blood flow in arteries and capillaries, and reduce peripheral vascular resista...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/22A61K9/19A61K31/522A61K47/42A61K47/36A61K47/28A61P9/00A61P7/02A61P9/10A61P11/08
CPCA61K31/522A61K9/19A61K47/42A61K47/36A61K47/28A61K9/2063A61K9/2054A61K9/205A61K9/2013A61P9/00A61P7/02A61P9/10A61P11/08Y02A50/30
Inventor 赵静
Owner HEBEI CHEM & PHARMA COLLEGE
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