Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Sustained-release preparation drug-loading material and its composition, sustained-release preparation and preparation method thereof

A technology for sustained-release preparations and compositions, applied in the field of medicine, can solve problems such as difficulty in achieving satisfactory blood drug concentration, small dose, and increase in blood drug concentration, avoiding fluctuations in blood drug concentration, stable drug release, and good biocompatibility. sexual effect

Active Publication Date: 2022-02-01
江苏集萃新型药物制剂技术研究所有限公司
View PDF16 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, most of the researches on the controlled-release dosage form of testosterone are transdermal patches. However, patients with testosterone deficiency are usually elderly, and the skin function is declining and easy to break
Moreover, most of the existing studies use high-concentration lower alcohols as solvents for testosterone. On the one hand, a considerable number of people are allergic to lower alcohols, which limits the use of medicaments. On the other hand, the skin’s tolerance to ethanol is relatively poor. , especially the skin of the elderly with fragile skin has poor tolerance to ethanol, and once the skin is damaged, it is easy to cause a large amount of drugs to enter the blood in a short period of time, resulting in a sudden increase in blood drug concentration, resulting in obvious toxic side effects
At present, there is still a way of nasal administration, but the dose of this way is also very small, and it is difficult to achieve a satisfactory blood concentration

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Sustained-release preparation drug-loading material and its composition, sustained-release preparation and preparation method thereof
  • Sustained-release preparation drug-loading material and its composition, sustained-release preparation and preparation method thereof
  • Sustained-release preparation drug-loading material and its composition, sustained-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] (I) Ingredients

[0076] I1-liposome group:

[0077] Phospholipids: distearoylphosphatidylcholine, 83 parts by weight;

[0078] Cholesterol: compound of formula (1), 17 parts by weight;

[0079] The first penetration enhancer: isopropyl myristate, 187 parts by weight.

[0080] I2-matrix group:

[0081] Aqueous gel compound: hypromellose, 118 parts by weight;

[0082] Fatty acid ester: monoglyceride stearate, 4137 parts by weight;

[0083] The second penetration enhancer: isopropyl myristate, 53 parts by weight.

[0084] I3-Other:

[0085] Medicine: testosterone, 120 parts by weight;

[0086] Solvent: dehydrated alcohol, 500 parts by weight;

[0087] Phosphate buffer: 22200 parts by weight.

[0088] (II) Preparation of anal sustained-release suppositories

[0089] II1-Preparation of matrix: heating and melting the prepared aqueous gel compound, fatty acid ester and second penetration enhancer in a water bath at 100°C to obtain an oil phase;

[0090] II2-Preparat...

Embodiment 2

[0094] (I) Ingredients

[0095] I1-liposome group:

[0096] Phospholipids: egg yolk lecithin, 80 parts by weight;

[0097] Cholesterol: compound of formula (1), 20 parts by weight;

[0098] The first penetration enhancer: N-methylpyrrolidone, 116 parts by weight.

[0099] I2-matrix group:

[0100] Aqueous gel compound: hydroxypropyl cellulose, 81 parts by weight;

[0101] Fatty acid ester: propylene glycol stearate, 2025 parts by weight;

[0102] The second penetration enhancer: N-methylpyrrolidone, 50 parts by weight.

[0103] I3-Other:

[0104] Medicine: dihydrotestosterone, 110 parts by weight;

[0105] Solvent: dehydrated alcohol, 500 parts by weight;

[0106] Phosphate buffer: 22200 parts by weight.

[0107] (II) Preparation of anal sustained-release suppositories

[0108] II1-Preparation of matrix: heating and melting the prepared aqueous gel compound, fatty acid ester and second penetration enhancer in a water bath at 100°C to obtain an oil phase;

[0109] II...

Embodiment 3

[0113] (I) Ingredients

[0114] I1-liposome group:

[0115] Phospholipids: soybean lecithin, 85 parts by weight;

[0116] Cholesterol: compound of formula (1), 15 parts by weight;

[0117] The first penetration enhancer: isopropyl myristate, 169 parts by weight.

[0118] I2-matrix group:

[0119] Water-based gel compound: Carbomer 940, 86 parts by weight;

[0120] Fatty acid ester: polyethylene glycol stearate, 3889 parts by weight;

[0121] The second penetration enhancer: isopropyl myristate, 56 parts by weight.

[0122] I3-Other:

[0123] Medicine: methyltestosterone, 125 parts by weight;

[0124] Solvent: dehydrated alcohol, 500 parts by weight;

[0125] Phosphate buffer: 22200 parts by weight.

[0126] (II) Preparation of anal sustained-release suppositories

[0127] II1-Preparation of matrix: heating and melting the prepared aqueous gel compound, fatty acid ester and second penetration enhancer in a water bath at 100°C to obtain an oil phase;

[0128] II2-Prep...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
particle sizeaaaaaaaaaa
pore sizeaaaaaaaaaa
particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention relates to the field of medicine, in particular to a drug-loaded material for a sustained-release preparation, a composition thereof, a sustained-release preparation and a preparation method thereof. The composition comprises a liposome group and a matrix group preserved independently of each other, the liposome group includes phospholipids and optional cholesterol; the matrix group includes a matrix, and the matrix is ​​selected from fatty acid esters, aqueous gel compounds, fat-soluble slow-release matrix One or more of the matrix compound and the water-soluble slow-release matrix matrix compound; the weight ratio of the liposome group and the matrix group is 1: (2-200). The sustained-release preparation prepared by the composition can release the drug stably at the set release rate, has strong controllability, can realize large-dose release, and can be suitable for use as an anal sustained-release suppository, so that it is more friendly to the skin and easier to use. Safety. Sustained-release formulations are particularly suitable for androgenic or estrogenic drugs.

Description

technical field [0001] The present invention relates to the field of medicine, in particular to a composition of a drug-loaded material for a sustained-release preparation, a drug-loaded material for a sustained-release preparation containing the composition or prepared from the composition, containing a drug and the drug-loaded material for a sustained-release preparation Sustained-release preparation, and preparation method of the sustained-release preparation. Background technique [0002] Existing studies have found that the dosage form used for drug administration has a significant impact on the therapeutic effect, one of the important reasons is that the dosage form will significantly affect the distribution of drug concentration in the blood, thereby affecting the treatment process. For example, after administration by conventional dosage forms, the drug's plasma concentration profile initially peaks (defined as peak plasma concentration) and then declines rapidly. T...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/02A61K9/127A61K31/565A61K31/566A61K31/568A61K47/14A61K47/24A61K47/28A61K47/32A61K47/38A61K47/44A61P5/26A61P5/30
CPCA61K9/02A61K9/127A61K31/568A61K31/565A61K31/566A61K47/24A61K47/28A61K47/32A61K47/38A61K47/44A61K47/14A61P5/26A61P5/30
Inventor 全丹毅陈东宇
Owner 江苏集萃新型药物制剂技术研究所有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com