Mizolastine sustained release pellet and preparation method thereof

A technology for mizolastine and sustained-release pellets, applied in the field of mizolastine sustained-release pellets and preparation thereof, can solve the problems of inability to eliminate the cause of the disease by drugs, burying serious hidden dangers in human health, and large toxic and side effects, so as to improve biological Availability, stable therapeutic effect, effect with less side effects

Inactive Publication Date: 2016-06-15
HARBIN SHENGJI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] There are many medicines for treating urticaria on the market, but most medicines cannot eliminate the cause, but only ach

Method used

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  • Mizolastine sustained release pellet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] A kind of mizolastine sustained-release pellets, comprising drug-containing pellets and a coating layer, the coating layer wraps the drug-containing pellets, and the drug-containing pellets include: 10mg mizolastine, 70mg blank core, 120-220mg filler, 25-125mg lubricant, 5-35mg binder, the coating layer includes: 35-175mg Eudragit NE30D, 5-52mg talcum powder.

[0038] The optimal mass ratio of raw materials in the drug-containing pellets is: 10 mg mizolastine, 70 mg blank pellet core, 200 mg filler, 50 mg lubricant, and 10 mg binder.

[0039] The optimal mass ratio of raw materials in the coating layer is: 95mg Eudragit NE30D, 21mg talcum powder.

[0040] The filler is microcrystalline cellulose.

[0041] Described lubricant is talcum powder.

[0042] The binder is hypromellose.

[0043] The coating layer also includes traces of sodium lauryl sulfate or polyethylene glycol.

Embodiment 2

[0045] A preparation method of mizolastine sustained-release pellets, comprising the following steps:

[0046] Step 1: Prepare materials: according to the above mass ratio, use a pulverizer to pulverize mizolastine, and pass through a 100-mesh sieve;

[0047] Step 2: Mixing: Weigh mizolastine and microcrystalline cellulose according to the above mass ratio and mix them in a three-dimensional mixer for 30 minutes to make a fine powder of the drug, which is taken out for later use;

[0048] Step 3: Preparation of adhesive: Weigh an appropriate amount of hypromellose according to the above mass ratio, add an appropriate amount of hot water to prepare an adhesive with a concentration of 2%, and set aside;

[0049] Step 4: Pill making: put the mixed drug fine powder into the feeding tank of the centrifugal pellet machine, put the adhesive into the liquid supply tank, put the blank pellet core into the pot, turn on the machine, adjust the parameters, and start spraying When the bal...

Embodiment 3

[0055] pharmacological effect

[0056] Mizolastine has unique dual effects of antihistamine and anti-inflammatory mediator of allergic reaction. Both in vivo and in vitro pharmacological tests have shown that mizolastine is a potent and highly selective histamine H1 receptor antagonist. In experiments using animal models of allergic reactions, mizolastine can also inhibit the release of histamine from activated mast cells (0.3 mg / kg, orally) and inhibit the chemotaxis of inflammatory cells such as neutrophils (3 mg / kg). kg, orally). At the same time, mizolastine also inhibits the release of intercellular adhesion molecule-1 during allergic reactions. Pharmacological tests have shown that mizolastine has anti-inflammatory activity, which may be related to its ability to inhibit 5-lipoxygenase.

[0057] Studies of histamine-induced wheals and erythema in humans have shown that after administration of 10 mg of this product, its antihistamine effect is rapid, potent (80% of sym...

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Abstract

The invention discloses a mizolastine sustained release pellet, which consists of a drug-containing pellet body and a coating layer, wherein the drug-containing pellet body is covered by the coating layer; the drug-containing pellet body consists of 10mg of mizolastine, 70mg of a blank pellet core, 120-220mg of a filling agent, 25-125mg of a lubricating agent and 5-35mg of a binding agent; the coating layer consists of 35-175mg of Eudragit NE30D and 5-52mg of talcum powder; and a preparation method comprises the following steps: 1, preparing materials; 2, mixing; 3, preparing the binding agent; 4, preparing the pellet; 5, preparing a coating agent; 6, coating; 7, filling; and 8, aluminum-molding and obtaining a finished product. The mizolastine sustained release pellet disclosed by the invention is mainly used for treating skin allergy symptoms such as urticaria and the like, seasonal allergic rhinitis (pollinosis) and perennial allergic rhinitis; the sustained release pellet, which makes use of two advanced technologies, namely a novel sustained release preparation and a novel pellet preparation, is stable in therapeutic effect and relatively high in bioavailability, and the sustained release pellet has the advantages of being good in drug stability, convenient in packaging, transportation and storage and the like; and the preparation is simple and easy to implement and is applicable to industrial production.

Description

technical field [0001] The invention belongs to the field of chemical drug sustained-release preparations, and in particular relates to a mizolastine sustained-release pellet and a preparation method thereof. Background technique [0002] Skin allergy is a very common form of allergy, with 20% of people having skin allergies. Skin allergies are also known as "sensitive" skin. From a medical point of view, skin allergy mainly refers to when the skin is subjected to various stimuli such as adverse reactions of cosmetics, chemical agents, pollen, certain foods, polluted air, etc., resulting in redness, swelling, itching, peeling and allergic dermatitis. and other abnormal phenomena. [0003] Urticaria (urticaria), commonly known as wheal, is a localized edema reaction due to the expansion and increased permeability of small blood vessels in the skin and mucous membrane. , without leaving any traces after healing. [0004] Divided into acute and chronic according to the cour...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K9/16A61K31/506A61K47/32A61P37/08A61P17/00A61P11/02
Inventor 马玉国
Owner HARBIN SHENGJI PHARMA
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