Drug-loading material and composition thereof of sustained-release preparation, sustained-release preparation and preparation method therefor

A sustained-release preparation and composition technology, applied in the field of medicine, can solve the problems of poor ethanol tolerance, poor tolerance, easy damage, etc.

Active Publication Date: 2020-12-25
江苏集萃新型药物制剂技术研究所有限公司
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  • 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

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  • Drug-loading material and composition thereof of sustained-release preparation, sustained-release preparation and preparation method therefor
  • Drug-loading material and composition thereof of sustained-release preparation, sustained-release preparation and preparation method therefor
  • Drug-loading material and composition thereof of sustained-release preparation, sustained-release preparation and preparation method therefor

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...

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Abstract

The invention relates to the field of medicines and particularly relates to a drug-loading material and composition thereof of a sustained-release preparation, the sustained-release preparation and apreparation method therefor. The composition comprises a liposome group and a matrix group which are independently preserved mutually, wherein the liposome group comprises phospholipid and optional cholesterol; the matrix group comprises a matrix, wherein the matrix comprises one or more selected from fatty acid esters, aqueous gel compounds, fat-soluble sustained-release skeleton matrix compoundsand water-soluble sustained-release skeleton matrix compounds; and a weight ratio of the liposome group to the matrix group is 1: (2 to 200). The sustained-release preparation prepared from the composition can stably release drugs at a set release rate, is high in controllability, can achieve large-dose release and can be suitable for serving as an anal sustained-release suppository, thereby being friendlier to skin and safer in use. The sustained-release preparation is particularly suitable for being applied to male hormone drugs or female hormone 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

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Application Information

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Patent Type & Authority Applications(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
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