Nano-carrier sustained release preparation for treating cardiovascular diseases and preparation method of nano-carrier sustained release preparation

A nano-carrier and sustained-release preparation technology, which is applied in the field of nano-carrier sustained-release preparations for the treatment of cardiovascular diseases and its preparation, can solve the problems of affecting the curative effect and difficult storage of pentoxifylline, and achieve the reduction of adverse reactions, stable dissolution rate, The effect of stable quality

Active Publication Date: 2022-02-18
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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  • Nano-carrier sustained release preparation for treating cardiovascular diseases and preparation method of nano-carrier sustained release preparation
  • Nano-carrier sustained release preparation for treating cardiovascular diseases and preparation method of nano-carrier sustained release preparation
  • Nano-carrier sustained release preparation for treating cardiovascular diseases and preparation method of nano-carrier sustained release preparation

Examples

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Effect test

preparation example 1

[0040] Preparation Example 1: Preparation of Pentoxifylline Nano-carrier Freeze-dried 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; the specific preparation method is as follows:

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

[0043] The chitosan solution with a concentration of 1 mg / mL is adjusted to a pH value of 5.5 with sodium hydroxide solution to obtain a chitosan solution for subsequent use;

[0044] The deoxycholic acid solution with a concentration of 1 mg / mL was adjusted to pH 5.5 with dilute hydrochloric acid solution; the deoxycholic acid solution was obtained and set aside.

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

[0046] (2)...

preparation example 2

[0051] Preparation example 2: Preparation of pentoxifylline nanocarrier lyophilized powder

[0052] Chitooligosaccharide molecular weight is 2300Da, all the other are the same as preparation example 1.

preparation example 3

[0053] Preparation example 3: Preparation of pentoxifylline nanocarrier lyophilized powder

[0054] Chitooligosaccharide molecular weight is 2500Da, all the other are the same as preparation example 1.

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Abstract

The invention provides a nano-carrier sustained release preparation for treating cardiovascular diseases and a preparation method of the nano-carrier sustained release preparation. The nano-carrier sustained release preparation consists of freeze-dried pentoxifylline nano-carrier powder and pharmaceutic adjuvants. A weight ratio of pentoxifylline to a nano-carrier in the freeze-dried pentoxifylline nano-carrier powder is (4-5): 1; the nano-carrier is made of a composition of chitosan oligosaccharide, deoxycholic acid and albumin, wherein a weight ratio of chitosan oligosaccharide to deoxycholic acid to albumin is 1: (2-3): (3.0-3.3); a weight ratio of pentoxifylline to the pharmaceutic adjuvants is (4-7): 1; and the pharmaceutic adjuvants are composed of hydroxyethyl cellulose, aerosil and magnesium stearate, wherein a weight ratio of hydroxyethyl cellulose to aerosil to magnesium stearate is (5-6): (3-4): 1. The nano-carrier sustained release preparation for treating cardiovascular diseases provided by the invention is stable in dissolution speed, basically realizes zero-order linear dissolution, avoids burst release, greatly ensures the treatment effect of pentoxifylline, and obviously reduces adverse reactions; and after being placed for 6 months under an accelerated condition, the content of a degradation product is low, and stable quality is realized.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, and relates to a sustained-release nanocarrier preparation for treating cardiovascular disease and a preparation method thereof, more particularly to a sustained-release nanocarrier preparation for treating cardiovascular disease containing 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-(5-oxohexyl), the structural formula is as follows, it is extracted from cocoa beans An alkaloid obtained by introducing theobromine into hexanone group, it is white powder or granule; slightly smelly, slightly bitter; easily soluble in triazine, soluble in water or ethanol, slightly soluble in ether . [0003] Pentoxifylline can improve blood circulation in the brain and extremities, increase blood flow in arteries and capillaries, and reduce peripheral vascular resistance, but...

Claims

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Application Information

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Patent Type & Authority Applications(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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