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External preparation of Levocetirizine hydrochloric acid

A technology of levocetirizine hydrochloride and ointment, which is applied in the field of pharmaceutical preparations, can solve the problems of unfavorable tissue distribution of levocetirizine hydrochloride, unsatisfactory administration methods, and less blood flow distribution, etc., and achieve good local anti-inflammatory effects. Allergic and anti-inflammatory effects, increased free drug concentration, good transdermal absorption effect

Active Publication Date: 2010-02-17
LUNAN PHARMA GROUP CORPORATION
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] 3. Levocetirizine hydrochloride has rapid absorption in vivo, limited distribution and low metabolic rate;
However, the blood flow distribution of skin tissue is relatively small, which makes the tissue distribution of levocetirizine hydrochloride very unfavorable for its treatment of skin allergic diseases and dermatitis, and is applied to skin diseases through oral administration in large doses , it will inevitably bring some unexpected serious systemic adverse reactions, which is a very unsatisfactory way of administration

Method used

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  • External preparation of Levocetirizine hydrochloric acid
  • External preparation of Levocetirizine hydrochloric acid
  • External preparation of Levocetirizine hydrochloric acid

Examples

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preparation example Construction

[0024] 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.

[0025] Operation method: Inject the serum of sensitized rats (containing rich IgE antibody) intradermally into the abdominal wall or back of normal rats, forming a mound at each point. IgE binds to the Fc receptors of local skin mast cells, making them passively sensitized. When the antigen is attacked, the local mast cells are caused to release allergic mediators, thereby increasing the permeability of the local blood vessels. Evans blue is injected, which can seep out of the pichu and form a coeruleus. According to the range or depth of coeruleus, the...

Embodiment 1

[0057] Levocetirizine Hydrochloride Liniment

[0058] Levocetirizine Hydrochloride 20g

[0059] Ethanol 35ml

[0060] Propylene glycol 100ml

[0061] Add phosphate buffered saline (PBS) to 1000ml

[0062] Preparation Process:

[0063] Dissolve levocetirizine hydrochloride in an appropriate amount of phosphate buffered saline (PBS), add the prescribed amount of ethanol and propylene glycol, and then add phosphate buffered saline (PBS) to 1000ml.

Embodiment 2

[0065] Levocetirizine Hydrochloride Liniment

[0066] Levocetirizine Hydrochloride 10g

[0067] Ethanol 200ml

[0068] Propylene glycol 300ml

[0069] Add distilled water to 1000ml

[0070] Preparation Process:

[0071] Dissolve levocetirizine hydrochloride in an appropriate amount of distilled water first, add the prescribed amount of ethanol and propylene glycol, and then add distilled water to 1000ml.

[0072] The liniment prepared in embodiment 1 and embodiment 2 is packed in a specific container (sprayer or atomizer), and can be used as a spray.

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Abstract

An exterior-applied levocetirizine hydrochloride for preventing and treating the anaphylaxia and inflammation without untoward effect is disclosed.

Description

Technical field [0001] The invention belongs to the technology of pharmaceutical preparations. Background technique [0002] With the change of climate and environment, various harmful gases, dust and other pollution sources emerge in large numbers, which become 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, allergic rhinitis, urticaria, skin redness, itching, redness Asthma caused by spots and allergens is very common. Therefore, it is very important to develop drugs for the treatment of allergic diseases. [0003] At present, the second-generation antihistamine drugs are mainly used in the clinical treatment of allergic diseases, among which cetirizine has the strongest drug activity, has better anti-inflammatory and anti-allergic effects, and has the highest bioavailabil...

Claims

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Application Information

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