Albendazole ivermectin enteric-coated sustained-release pellet and preparation method thereof

A technology of albendazole ivermectin and sustained-release pellets, which is applied in the field of albendazole ivermectin enteric-coated sustained-release pellets and its preparation, can solve the problem of high toxicity and time-consuming albendazole , cost and other issues, to achieve the effect of good intestinal disintegration and dissolution, safety and high efficiency, and reduced dosage

Pending Publication Date: 2021-08-31
WUHAN XINLIANDA BIOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The effect of the drug on the parasites in the pig body is acceptable under the conventional dose, but the effect on the parasites on the surface of the body is not good. High toxicity, poisoning of fattening pigs, miscarriage and stillbirth of sows, dead sperm of boars and other toxic side effects often occur
Therefore, many farms also use injection or pouring ivermectin preparations to drive and kill ectoparasites while feeding albendazole ivermectin powder, which is time-consuming, costly and stressful.

Method used

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  • Albendazole ivermectin enteric-coated sustained-release pellet and preparation method thereof
  • Albendazole ivermectin enteric-coated sustained-release pellet and preparation method thereof
  • Albendazole ivermectin enteric-coated sustained-release pellet and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1 Preparation of enteric-coated pellets of the present invention

[0034] Take the raw and auxiliary materials according to the following weight ratio:

[0035] The amount of raw and auxiliary materials per 100g ball core:

[0036] Albendazole 50.0g

[0037] Ivermectin 1.0g

[0038] Hypromellose 49.0g

[0039] Per 100g enteric-coated layer, the amount of excipients:

[0040] Eudragit L30D-55 Water Dispersion 42.0g

[0041] Diethyl phthalate 1.1g

[0042] Talc powder 1.9g

[0043] Purified water 55.0g;

[0044] The ratio of the core to the coating layer of the enteric-coated pellets by weight is 8:2.

[0045] The preparation method is as follows

[0046] a. Preparation of ball core: fully mix albendazole and ivermectin, add a 1.6% v / v hydroxypropyl methylcellulose aqueous solution to make a soft material, and make the soft material at a speed of 50r / min Extruded under the same conditions to make strips, and then cut and spheronized by a spheronizer w...

Embodiment 2

[0048] Embodiment 2 Preparation of enteric-coated pellets of the present invention

[0049] Take the raw and auxiliary materials according to the following weight ratio:

[0050] The amount of raw and auxiliary materials per 100g ball core:

[0051] Albendazole 70.0g

[0052] Ivermectin 1.4g

[0053] Hypromellose 28.6g

[0054] Per 100g enteric-coated layer, the amount of excipients:

[0055] Eudragit L30D-55 Water Dispersion 42.0g

[0056] Diethyl phthalate 1.1g

[0057] Talc powder 1.9g

[0058] Purified water 55.0g;

[0059] The ratio of the core to the coating layer of the enteric-coated pellets by weight is 8:2.

[0060] The preparation method is as follows

[0061] a. Preparation of ball core: fully mix albendazole and ivermectin, add a 1.6% v / v hydroxypropyl methylcellulose aqueous solution to make a soft material, and make the soft material at a speed of 50r / min Extruded under the same conditions to make strips, and then cut and spheronized by a spheronizer w...

Embodiment 3

[0063] Embodiment 3 Preparation of enteric-coated pellets of the present invention

[0064] Take the raw and auxiliary materials according to the following weight ratio:

[0065] The amount of raw and auxiliary materials per 100g ball core:

[0066] Albendazole 55.0g

[0067] Ivermectin 1.1g

[0068] Hypromellose 43.9g

[0069] Per 100g enteric-coated layer, the amount of excipients:

[0070] Eudragit L30D-55 Water Dispersion 42.0g

[0071] Diethyl phthalate 1.1g

[0072] Talc powder 1.9g

[0073] Purified water 55.0g;

[0074] The ratio of the core to the coating layer of the enteric-coated pellets by weight is 8:2.

[0075] The preparation method is as follows

[0076] a. Preparation of ball core: fully mix albendazole and ivermectin, add a 1.6% v / v hydroxypropyl methylcellulose aqueous solution to make a soft material, and make the soft material at a speed of 50r / min Extruded under the same conditions to make strips, and then cut and spheronized by a spheronizer w...

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Abstract

The invention discloses an albendazole ivermectin enteric-coated sustained-release pellet. The albendazole ivermectin enteric-coated sustained-release pellet is prepared by taking classical anthelmintic drug combination albendazole ivermectin powder (10% albendazole and 0.2% ivermectin) as an active ingredient and adding proper auxiliary materials, and comprises a pellet core layer and an enteric-coated layer, wherein the weight percentage of the pellet core layer and the enteric-coated layer is as follows: 70-85% of pellet core and 15-30% of enteric-coated layer. The invention further discloses a preparation method and application of the enteric-coated sustained-release pellet. The enteric-coated sustained-release pellet disclosed by the invention is used for expelling and killing in-vivo and in-vitro parasites such as pig nematodes, trematodes, tapeworms, mites and lice. The albendazole and the ivermectin both have certain toxicity, the bioavailability of the common albendazole ivermectin powder orally taken by pigs is only 40-50%, and toxic and side effects are often caused if an effective dose is expected in clinical use; the enteric-coated sustained-release pellet disclosed by the invention can release a large amount of drugs only in an intestinal environment with a pH value of 6.8 or above, thus reducing the damages of an acidic stomach environment to the drugs; amd the drugs are stably and slowly released in the intestinal tract, the maintenance time of an effective blood concentration is prolonged, the bioavailability is 80% or above, the clinical dosage can be reduced by 30% or above, the safety is greatly improved, and the application prospect is wide.

Description

technical field [0001] The invention relates to albendazole ivermectin enteric-coated sustained-release pellets and a preparation method thereof, belonging to the field of veterinary drugs. Background technique [0002] Parasitic diseases are one of the three major diseases, infectious diseases, medical diseases, and parasitic diseases that often occur in pig production. , soft ticks, fleas, lice and mosquitoes. The parasite competes with the pig body for nutrients, destroys the functions of various physiological systems, and infects individuals with weak constitution, stunted growth and susceptibility to various other diseases. According to statistics, incomplete deworming will reduce the net profit of breeding by no less than 10%, which is extremely harmful. [0003] Albendazole ivermectin powder is a classic combination of anthelmintic drugs. Albendazole has a broad-spectrum repellent endoparasite activity, and has a strong repellent effect on nematodes, tapeworms and t...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K47/32A61K31/7048A61K31/4184A61P33/10A61P33/14
CPCA61K9/5026A61K31/4184A61K31/7048A61P33/10A61P33/14A61K2300/00
Inventor 童庆平陈培源高艳梅
Owner WUHAN XINLIANDA BIOLOGY
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