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Preparation method of ivermectin preparation and ivermectin preparation

A technology of ivermectin and preparations, applied in the field of antiparasitic drugs, can solve the problems of low dissolution rate of ivermectin, poor uniformity, affecting drug effectiveness and safety, etc., to improve effectiveness and safety , reduce the effect of increasing and reducing the contact angle

Inactive Publication Date: 2018-05-29
FOSHAN NANHAI EASTERN ALONG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The dissolution rate of ivermectin in the ivermectin preparation prepared by the traditional process is low, and the uniformity is poor, which seriously affects the effectiveness and safety of the drug

Method used

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  • Preparation method of ivermectin preparation and ivermectin preparation
  • Preparation method of ivermectin preparation and ivermectin preparation
  • Preparation method of ivermectin preparation and ivermectin preparation

Examples

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preparation example Construction

[0048] A preparation method of ivermectin preparation, comprising the following steps:

[0049] 1) Weighing and sieving: Weigh the main ingredient of ivermectin and auxiliary materials such as disintegrants, fillers, lubricants and adhesives according to the above parts by weight, and weigh the disintegrants and fillers respectively And the lubricant is crushed, the particle size of the disintegrating agent, the filler and the lubricant is controlled to be 140 μm-160 μm, and the weighed ivermectin is ground to control the ivermectin The particle size of the element is 120μm-130μm.

[0050] Optionally, the auxiliary material also includes a flavoring agent and a preservative, and the flavoring agent and the preservative are weighed according to the above parts by weight, and the flavoring agent and the preservative are pulverized to control their particle size to 140 μm-160 μm.

[0051] Specifically, grind the ivermectin with a mortar, and pass the ground ivermectin through a ...

Embodiment 1

[0074] 1) Weigh each raw material in the following parts by weight: 0.32 parts of ivermectin, 7 parts of crospovidone, 83 parts of anhydrous sugar, 1 part of magnesium stearate and 2 parts of hypromellose. Grind the weighed ivermectin with a mortar, and pass the ivermectin through a 120 mesh sieve. The crospovidone, anhydrous sugar, magnesium stearate and hypromellose were pulverized respectively, passed through a 100-mesh sieve, and set aside.

[0075] 2) Premix the ground ivermectin, partially sieved starch, and sieved crospovidone to obtain an intermediate; then mix the intermediate with the remaining sieved starch Mix evenly by equal increment method to prepare the mixture.

[0076] 3) Add the hypromellose sieved in step 1) into purified water to prepare a hypromellose aqueous solution with a concentration of 3% (w / v).

[0077] 4) Mix the mixture prepared in step 2) and the hypromellose aqueous solution with a concentration of 3% (w / v) prepared in step 3) in a preparatio...

Embodiment 2

[0081] The raw materials were weighed in the following parts by weight: 0.1 part of ivermectin, 3 parts of crospovidone, 91 parts of anhydrous sugar, 1 part of magnesium stearate and 1 part of hypromellose.

[0082] The preparation method of this ivermectin preparation 2 is the same as that of Example 1.

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Abstract

The invention relates to a preparation method of an ivermectin preparation and the ivermectin preparation. The preparation method of the ivermectin preparation comprises the following steps: (1) weighed ivermectin is ground, and the grain size of the ivermectin is controlled at 120 mu m to 130 mu m; (2) the ground ivermectin, part of screened filler and a screened disintegrating agent are first premixed, so that an intermediate is prepared; and the intermediate and the rest of the screened filler are uniformly mixed, so that a mixture is obtained; (3) a binder solution, the concentration of which is 0.1 percent (w / v) to 10 percent (w / v), is prepared; (4) the mixture and the binder solution are uniformly mixed, so that a soft material is obtained; (5) the soft material is granulated, driedand finished, so that granules are produced; (6) a screened lubricant and the granules are uniformly mixed, and tabletting is carried out, so that the ivermectin preparation is obtained. The ivermectin preparation prepared by the preparation method has high dissolubility and good uniformity.

Description

technical field [0001] The invention relates to the technical field of antiparasitic drugs, in particular to a preparation method of an ivermectin preparation and the ivermectin preparation. Background technique [0002] Ivermectin (IVM) is a new type of broad-spectrum, high-efficiency, and low-toxicity antibiotic antiparasitic drug, which has a good killing effect on both internal and external parasites, especially for nematodes and arthropods. . [0003] Ivermectin (IVM) is the first avermectin (AVM) drug derivative obtained by Wilkinson catalyzing the double bond between C22 and C23 of AVMB1 by Merck Company in the United States, and after hydrogenation of a homogeneous system. things. The insecticidal activity of ivermectin (IVM) and avermectin (AVM) is basically the same, but IVM has stronger penetration and safety to mammalian body tissues. [0004] Ivermectin can increase the release of the inhibitory transmitter γ-aminobutyric acid (GABA) in nematodes and arthropo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61K47/36A61K47/32A61K47/38A61K47/20A61K47/26A61K47/10A61P33/00
CPCA61K31/7048A61K47/10A61K47/20A61K47/26A61K47/32A61K47/36A61K47/38
Inventor 陶映娴黄海青林孝崇周淑贞焦伟丽
Owner FOSHAN NANHAI EASTERN ALONG PHARMA CO LTD
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