Externally used loratadine formulation

A technology of loratadine and external preparations, which is applied in the field of pharmaceutical preparations and can solve problems such as not being ideal

Inactive Publication Date: 2005-07-06
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no ideal medicine for many intractable skin allergic diseases and skin inflammations

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0028] Preparation of antiserum Take 8 healthy rats weighing 90-100g and inject them intramuscularly with Na 2 SO 4 Ovalbumin (10mg / kg) recrystallized 3-5 times, and intraperitoneal injection of pertussis triple vaccine 2×10 10 / only. 10-14 days after the sensitization, the animals were sacrificed to collect blood, and the serum was separated by low-speed centrifugation, and stored in a -40°C refrigerator for later use.

[0029] Passive skin sensitization and antigen challenge Another 90 healthy rats with a body weight of 150-200g were randomly divided into normal control group, model group, high-dose liposome liniment group, low-dose liposome liniment group, Common liniment high-dose group, common liniment low-dose group, ointment high-dose group, ointment low-dose group and gavage control group. The hair on the back of the rat was cut off under anesthesia, and the diluted antiserum (1:6) was intradermally injected into the back of the rat for sensitization, and a total of...

Embodiment 1

[0089] Loratadine liposome liniment

[0090] Loratadine 10g

[0091] Lecithin 75g

[0092] Cholesterol 35g

[0093] Octadecylamine 2g

[0094] Vitamin E 5g

[0095] Tris buffer 1000ml

[0096] Preparation Process:

[0097] Dissolve the fat-soluble film material lecithin, cholesterol, octadecylamine, vitamin E and drug loratadine in the prescription in an appropriate amount of chloroform-ethanol mixed organic solvent (chloroform: ethanol volume ratio is 3: 1) , put on a rotary evaporator to evaporate the organic solvent, the lecithin cholesterol lipid forms a thin film on the wall of the round bottom flask, and the residual trace organic solvent is removed with nitrogen flow. The flask was connected to a vacuum pump and left overnight. Add 1000ml, hydrate the lipid film on a vortex shaker, sonicate for 10 minutes, place it at 45°C for 1 hour, and store it at a low temperature of 4°C.

Embodiment 2

[0099] Loratadine liposome liniment

[0100] Loratadine 4g

[0101] Lecithin 50g

[0102] Cholesterol 40g

[0103] Ceramide 20g

[0104] Vitamin E 15g

[0105] Tris buffer 1000ml

[0106] The preparation process is the same as in Example 1.

[0107] implementation benefit 3

[0108] Loratadine liposome liniment

[0109] Loratadine 12g

[0110] Lecithin 65g

[0111] Cholesterol 20g

[0112] Octadecylamine 5g

[0113] Vitamin E 10g

[0114] Menthol 3g

[0115] Tris buffer 1000ml

[0116] The preparation process is the same as in Example 1.

[0117] The liposome prepared by the above prescription and method has good stability, and the encapsulation efficiency measured by Sephadex (G-50) filtration method is all above 30%.

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PUM

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Abstract

The pharmacological experiment shows that, the externally used preparation of Loratadine has very good allergy resisting and anti-inflammatory action to the rat passive cutaneous anaphylaxis (Rat PCA) model and dimethylbenzene caused mouse otitis model, in the experiment, it is found by chance that, the externally used preparation of Loratadine also has very fine inhibitory action to dinitrofluorobenzene caused mouse porphyria hypersensitivity (PTH), the novel pharmacological action mechanism of the Loratadine shows that the Loratadine external preparation has good therapeutic action to skin inflammations which mainly include porphyria hypersensitivity.

Description

Technical field [0001] The invention belongs to the technology of pharmaceutical preparations. Background technique [0002] In recent years, due to climate and environmental changes, various harmful gases, dust and other pollution sources have emerged in large numbers, making them allergens that cause people to have various allergic reactions. Seasonal changes, field work, pollen allergies, inhalation of harmful gases and dust particles, etc., have caused more and more people to suffer from various types of allergic diseases, such as allergic rhinitis, urticaria, skin redness, itching, rashes, etc. Red spots and asthma caused by allergens are very common. Therefore, it is very important to pay attention to environmental changes, strengthen self-care, and develop drugs for the treatment of allergies. [0003] Loratadine was developed by Schering Plow Company and first listed in Belgium in 1988. It is an orally effective third-generation antihistamine that selectively inhib...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K9/12A61K9/127A61K31/445A61P17/00A61P37/08
Inventor 赵志全
Owner LUNAN PHARMA GROUP CORPORATION
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