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Loratadine paster of penetrating skin

A technology of transdermal patch and loratadine, which is applied in the field of penetration-enhancing technology and medicine, can solve the problem that the penetration performance of loratadine cannot fully meet the treatment requirements, and achieve flexible and individualized drug administration , good in vivo transdermal rate and stable blood drug concentration

Inactive Publication Date: 2005-03-30
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Loratadine is a fat-soluble compound, insoluble in water, with a molecular weight of 382.89. The measurement of physical and chemical constants and the prediction of permeability coefficient show that the permeability of loratadine itself cannot fully meet the treatment requirements.

Method used

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  • Loratadine paster of penetrating skin
  • Loratadine paster of penetrating skin
  • Loratadine paster of penetrating skin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1 Selection of basic prescription

[0044]According to the use of polyacrylate polymer material Eudragit E100 as the skeleton and adhesive, succinic acid as the crosslinking agent, dibutyl sebacate as the plasticizer, and ethanol as the solvent.

[0045] The fixed dosage of EUDRAGIT E 100 in the prescription of the present invention is 1.8 g, and the calculation of the dosage of dibutyl sebacate and succinic acid is based on EUDRAGIT E 100, and the percentages of the two in EUDRAGIT E 100 are calculated. The amount of cross-linking agent and plasticizer is selected according to the product description of succinic acid, dibutyl sebacate, polymer material Eudragit E100, the effective range of succinic acid is 2~18%, and the effective range of dibutyl sebacate is effective The range is 20~70%.

[0046] The prescription was optimized according to the orthogonal experiment design. From this, determine the level of each factor, see Table 1.

[0047] Table 1 Orthogonal tes...

Embodiment 2

[0076] Example 2: Basic prescription study of loratadine transdermal patch

[0077] Composition of prescription: prescription 1

[0078] Loratadine 36mg

[0079] Eudragit E 100: 1800mg

[0080] Succinic acid: 120mg

[0081] Dibutyl sebacate: 0.85ml

[0082] Ethanol: 3ml

[0083] Weigh Eudragit E 100, succinic acid, and dibutyl sebacate according to the prescription ratio, add ethanol, and let it stand for 24 hours to fully swell Eudragit E 100. Add loratadine according to the prescription ratio and let it stand for several hours; It is made of medicine-containing glue, ultrasonically degassed, and coated on anti-sticking paper with a thickness of 0.1mm, plus a backing layer, and dried.

[0084] Cut the patch into a small round piece with a diameter of 1.9cm, place it on a transdermal diffusion tester, perform a transdermal absorption test, measure the cumulative transdermal amount Q (μg) at different times, and measure the penetration a...

Embodiment 3

[0087] Example 3: Study on the penetration promoting effect of oleic acid on loratadine

[0088] Composition of prescription: prescription 2 prescription 3 prescription 4 prescription 5

[0089] Loratadine 36mg 36mg 36mg 36mg

[0090] EudragitE100: 1.8g 1.8g 1.8g 1.8g

[0091] Succinic acid: 120mg 120mg 120mg 120mg

[0092] Dibutyl sebacate: 0.85ml 0.85ml 0.85ml 0.85ml

[0093] Oleic acid: 5%(0.15ml) 10%(0.3ml) 15%(0.6ml) 20%(0.9ml)

[0094] Ethanol: 3ml 3ml 3ml 3ml

[0095] Weigh Eudragit E 100, succinic acid, and dibutyl sebacate according to the prescription ratio, add ethanol, and let stand for 24 hours to make Eudragit E 100 fully swell, add loratadine according to the prescription ratio accurately, and add different proportions of oil. Acid, let it stand for several hours; fully stir and mix to form a drug-containing glue, ultrasonically degas, and coat it on a release paper with a thickness of 0.1mm, add a backing layer, and dry it.

[0096] Cut the patch into small round p...

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Abstract

A transdermal disk of loratadine for treating allergic disease is prepared from loratadine, adhesive aggregate, cross-linking agent, plasticizer, solvent and smosis promoter through proportionally mixing.

Description

Technical field [0001] The invention relates to a transdermal patch of loratadine, a preparation method thereof, and application thereof in the preparation of a medicine for treating allergic diseases. The present invention further includes penetration enhancement technology. Adding penetration enhancers such as oleic acid, menthol, azone, or phospholipids to the prescription can significantly increase the penetration rate of loratadine. Background of the invention [0002] Allergic disease is a common disease and frequently-occurring disease. It is estimated that about 10-25% of the world's population suffer from allergic rhinitis. Antihistamines can prevent the combination of histamine with blood vessels and peripheral nerve cells, relieve inflammation, relieve symptoms such as rhinitis, sneezing, and runny nose. It is currently the most effective class of drugs for allergic diseases such as allergic rhinitis . [0003] Loratadine is a tricyclic antihistamine developed by Scher...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/4545A61M37/00A61P37/08
Inventor 刘玉玲王春霞
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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