Externally applied formulation of cetirizine hydrochloride

A technology of cetirizine and external preparations, which is applied in the field of pharmaceutical preparations and can solve problems such as arrhythmia and toxic reactions

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

Studies have also shown that the dose of terfenadine that can significantly improve asthma symptoms has the risk of causing arrhythmia, so some people think that it is not suitable to use terfenadine to prevent and treat allergic asthma, and it is easy to interact with multiple drugs to produce toxic reactions

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0039] Preparation of antiserum Take 8 healthy rats weighing 90-100g, and intramuscularly inject them 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.

[0040] 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 o...

Embodiment 1

[0098] Cetirizine liposome liniment

[0099] Cetirizine 8g

[0100] Lecithin 70g

[0101] Cholesterol 30g

[0102] Octadecylamine 2g

[0103] Vitamin E 5g

[0104] Phosphate buffer saline (PBS) 1000ml

[0105] Preparation Process:

[0106] Dissolve the fat-soluble film material lecithin, cholesterol, octadecylamine and vitamin E in the prescription amount in an appropriate amount of organic solvents such as chloroform or ether, subject to the minimum amount that can be completely dissolved, and then add the prescription amount Phosphate buffered saline (PBS) of cetirizine, the ratio of PBS solution to organic solvent is between 1:3 and 1:6, and a probe-type ultrasonic instrument is used to sonicate briefly for 2 to 5 minutes until a stable W / O is formed. Emulsion, remove the organic solvent under reduced pressure, and after reaching the colloidal state, add PBS buffer solution and continue to evaporate under reduced pressur...

Embodiment 2

[0108] Cetirizine liposome liniment

[0109] Cetirizine 5g

[0110] Lecithin 50g

[0111] Cholesterol 40g

[0112] Ceramide 25g

[0113] Vitamin E 10g

[0114] Phosphate buffer saline (PBS) 1000ml

[0115] The preparation process is the same as in Example 1.

[0116] implementation benefit 3

[0117] Cetirizine liposome liniment

[0118] Cetirizine 12g

[0119] Lecithin 60g

[0120] Cholesterol 20g

[0121] Octadecylamine 8g

[0122] Vitamin E 10g

[0123] Menthol 3g

[0124] Phosphate buffer saline (PBS) 1000ml

[0125] The preparation process is the same as in Example 1.

[0126] 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

Pharmacological test shows that the externally-used preparation of Cetirizine has ideal allergy resistant and anti-inflammatory action to the rat passive cutaneous anaphylaxis (Rat PCA) model and dimethylbenzene caused mouse otitis model, and also prevents the adverse effect to the central system caused by whole body administration. It is also found in the test, that the externally used preparation of Cetirizine also has very fine inhibitory action to dinitrofluorobenzene caused mouse porphyria hypersensitivity (PTH), the novel pharmacological action of the Cetirizine shows that the Cetirizine 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] Cetirizine, as a powerful anti-allergy drug, has the following advantages: [0004] 1. Strong antihistamine effect Some studies have found that cetirizine has a fast...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K9/12A61K31/495A61P17/00A61P37/08
Inventor 赵志全
Owner LUNAN PHARMA GROUP CORPORATION
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