Skin external medicament as well as composition and preparation method thereof

A composition for external use and the technology of the composition, applied in the field of medicine, can solve the problems of unsteady release, easy deterioration, and unstable storage process of imidazole external preparations, so as to avoid fluctuations in blood drug concentration, reduce irritation, and inhibit deterioration. Effect

Pending Publication Date: 2021-12-10
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

[0003] However, due to the special properties of imidazoles, they cannot be released stably in external preparations, and most imidazoles external preparations are unstable and easily deteriorated during storage.

Method used

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  • Skin external medicament as well as composition and preparation method thereof
  • Skin external medicament as well as composition and preparation method thereof
  • Skin external medicament as well as composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] (1) Prepare the composition

[0083] (1) liposome group, including:

[0084] Phospholipids: distearoylphosphatidylcholine, 6.5 parts by weight;

[0085] Cholesterol: compound of formula (1), 0.7 parts by weight;

[0086] Cholesterol derivatives: compounds of formula (2-1), wherein X is H, Y is methyl, Z is -COOH, 2.7 parts by weight;

[0087] The first penetration enhancer: isopropyl myristate, 1 part by weight;

[0088] (2) matrix group, including:

[0089] Fatty acid ester: glycerin fatty acid ester (fatty acid part is a saturated C18 carbon chain), 50 parts by weight;

[0090] Water-based gel compound: hydroxyethyl cellulose, 20 parts by weight;

[0091] The second penetration enhancer: isopropyl myristate, 0.1 parts by weight;

[0092] (3) Drugs:

[0093] The first drug: luliconazole, 6 parts by weight;

[0094] The second drug: luliconazole, 1 part by weight.

[0095] (4) Other components, including:

[0096] Solvent: absolute ethanol;

[0097] Buffer so...

Embodiment 2

[0104] (1) Prepare the composition

[0105](1) liposome group, including:

[0106] Phospholipids: distearoylphosphatidylcholine, 6 parts by weight;

[0107] Cholesterol: compound of formula (1), 0.8 parts by weight;

[0108] Derivatives of cholesterol: compounds of formula (2-2), wherein X is ethyl, Y is H, and Z is -SO 3 H, 3.2 parts by weight;

[0109] The first penetration enhancer: isopropyl myristate, 1 part by weight;

[0110] (2) matrix group, including:

[0111] Fatty acid ester: sucrose fatty acid ester (fatty acid part is a saturated C12 carbon chain), 32 parts by weight;

[0112] Water-based gel compound: hydroxypropyl cellulose, 8 parts by weight;

[0113] The second penetration enhancer: isopropyl myristate, 0.1 parts by weight;

[0114] (3) Drugs:

[0115] The first drug: levconazole, 5 parts by weight;

[0116] Second drug: None.

[0117] (4) Other components, including:

[0118] Solvent: absolute ethanol;

[0119] Buffer solution: Phosphate buffer s...

Embodiment 3

[0122] (1) Prepare the composition

[0123] (1) liposome group, including:

[0124] Phospholipids: distearoylphosphatidylcholine, 7 parts by weight;

[0125] Cholesterol: compound of formula (1), 0.7 parts by weight;

[0126] Cholesterol derivatives: compounds of formula (2-3), wherein X is H, Y is -COOH, and Z is -SO 3 H, 2.3 parts by weight;

[0127] The first penetration enhancer: isopropyl myristate, 1 part by weight;

[0128] (2) matrix group, including:

[0129] Fatty acid ester: xylitol fatty acid ester (fatty acid part is a saturated C16 carbon chain), 54 parts by weight;

[0130] Aqueous gel compound: hypromellose, 46 parts by weight;

[0131] The second penetration enhancer: isopropyl myristate, 0.1 parts by weight;

[0132] (3) Drugs:

[0133] The first drug: Praconazole, 6 parts by weight;

[0134] The second drug: praconazole, 1 part by weight.

[0135] (4) Other components, including:

[0136] Solvent: absolute ethanol;

[0137] Buffer solution: Phosp...

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Abstract

The invention relates to the field of medicines, in particular to a composition of a skin external medicament, the skin external medicament containing the composition or prepared from the composition, and a preparation method of the skin external medicament. The external composition comprises a lipidosome group and a matrix group which are stored independently, wherein the lipidosome group comprises phospholipid and a cholesterol compound; the matrix group comprises a fatty acid ester compound and / or a water-based gel compound; and the composition optionally further comprises a drug group. According to the present invention, the drug can be stably released at the set release rate, the property is stable, and the shelf life is long; and according to the invention, some drugs (such as imidazole drugs) which are originally difficult to be used in skin external preparations can be used in the skin external preparations, and can still play a good drug effect. According to the invention, the application modes of a plurality of drugs are broadened, more choices are provided, and the pharmaceutical composition has important significance on clinical treatment.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a composition of an external medicament for skin, an external medicament for skin containing the composition or prepared from the composition, and a preparation method of the external medicament for skin. Background technique [0002] Imidazoles are synthetic antifungal agents. The antibacterial effect is similar to that of amphotericin. It can selectively inhibit fungal cytochrome P-450-dependent 14-α-demethylase, so that 14-α-methyl sterol can accumulate, and the cell membrane ergosterol cannot be synthesized, so that Changes in cell membrane permeability lead to the loss of important intracellular substances and the death of fungi. Imidazole antifungal drugs are currently the most commonly used drugs for the treatment of fungal infections in clinical practice, and are widely used in clinical practice. It can be seen from its chemical structure that substituting the imidazole part at ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/127A61K9/107A61K47/24A61K47/28A61K47/14A61K47/38A61K31/4178A61K31/4196A61P17/00A61P31/10
CPCA61K9/0014A61K9/127A61K9/107A61K47/24A61K47/28A61K47/14A61K47/38A61K31/4178A61K31/4196A61P17/00A61P31/10
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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