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Itopride hydrochloride micro-tablet and preparation method thereof

A technology of itopride hydrochloride and micro-tablets, which can be used in pharmaceutical formulas, medical preparations containing active ingredients, pill delivery, etc., can solve problems such as low Cmax and Tmax delay, and achieve the effect of improving postprandial bioavailability

Active Publication Date: 2019-01-04
珠海润都制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If the absorption site of the drug is in the stomach, then in the postprandial bioequivalence test, the tablet is easy to disintegrate and absorb in the stomach, while the capsule is easy to miss the absorption site of the stomach, resulting in delayed Tmax and lower Cmax. relatively low

Method used

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  • Itopride hydrochloride micro-tablet and preparation method thereof
  • Itopride hydrochloride micro-tablet and preparation method thereof
  • Itopride hydrochloride micro-tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Example 1 Preparation of Itopride Hydrochloride Microtablets (Specification: 0.05g)

[0065] As shown in Table 2, according to the type of material designed by the prescription, the bulk drug and auxiliary materials are vibrated through a 60-mesh sieve. The auxiliary materials include fillers, internally added disintegrants, surfactants, binders, externally added disintegrants, lubricants, and the raw materials, fillers, internally added disintegrants and The surfactant is placed in a fluidized bed one-step granulation coating machine, the fan is turned on, and mixed for 5 minutes. Weigh the binder according to the design amount of prescription 1-5, and prepare hypromellose binder solution or povidone K29 binder solution with 75% ethanol. Spray the adhesive evenly on the boiling material in the form of top spray. Set the material temperature to 50°C, dry the itopride hydrochloride granules in a fluidized dryer until the water content is not higher than 2%, and collect...

Embodiment 2

[0067] Example 2 Preparation of Itopride Hydrochloride Capsules (Specification: 0.05g)

[0068] Get the stomach-soluble film coating material, dissolve it in purified water, and prepare a solution with a solid content of about 6%. The itopride hydrochloride microchips prepared by Example 1 prescription 1 ~ 5 were collected, and prepared by 3% weight gain. weighing. Put the compressed microtablets in a non-porous coating pan for coating, control the air inlet temperature at 60-70 degrees, the material temperature at 40-50 degrees, the weight gain at 1-3%, and the moisture at 2 Within %. The coated chips prepared above were filled in No. 4 ordinary gelatin capsule shells to prepare samples A, B, C, D, and E.

Embodiment 3

[0072] Example 3 Comparison of the in vitro dissolution curves of itopride hydrochloride capsules (A, B, C, D, E) prepared by the present invention, existing products and the original research product (R)

[0073] Take itopride hydrochloride capsules (A, B, C, D, E) prepared in Example 2, 12 capsules or tablets each of the existing product and the original research product (R), and detect its hydrochloric acid at pH 1.0 according to the following method Solution, acetate buffered saline solution at pH 4.0, phosphate buffered saline at pH 6.8 and in vitro dissolution profiles in water. See Table 3 for prescriptions.

[0074]

[0075] The measurement results are shown in Tables 4, 5, 6, and 7.

[0076] Table 4 - The average cumulative dissolution test results of itopride hydrochloride capsules (A, B, C, D, E) and original research product R in hydrochloric acid solution at pH 1.0 (n=12)

[0077]

[0078] Table 5 - The average cumulative dissolution test results of itopri...

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Abstract

The invention discloses an itopride hydrochloride micro-tablet, a preparation method thereof and application thereof in consistency evaluation of generic drugs. According to the itopride hydrochloridemicro-tablet, the preparation method thereof and the application thereof in the consistency evaluation of the generic drugs, itopride hydrochloride and various ingredients are mixed, pelletized and dried, and then evenly mixed with an extra disintegrant and a lubricant, and the mixture is pressed into the micro-tablet of which the diameter is no more than 3MM. A capsule can be filled with the micro-tablet, multiple dissolution curves of a prepared itopride hydrochloride capsule in vitro are consistent with an original product (product name: itopride hydrochloride tablet; trade name: Weilisu;specification: 0.05g; certificate holding merchant: ABBOTT LABORATORIES (M) SDN. BHD), in the process of accelerated test and long-term test stability investigation, related substances have no significant change, and the micro-tablet has a bioequivalence trend with the original product after the meal.

Description

technical field [0001] The invention relates to an itopride hydrochloride microtablet, a preparation method thereof, and an application in the field of consistency evaluation of generic drugs. Background technique [0002] Itopride Hydrochloride was first successfully researched by Hokuriku Pharmaceutical Company of Japan, and it was approved for marketing in Japan in 1995. Its trade names are Ganaton and Elthon (the Chinese name of domestically imported tablets is "Weilisu"). Itopride hydrochloride is a dopamine D2 receptor antagonist and acetylcholinesterase inhibitor, used for various symptoms caused by functional dyspepsia, such as: epigastric discomfort, postprandial fullness, early satiety, loss of appetite, nausea, vomiting etc. In August 2002, Hokuriku Pharmaceutical Company was acquired by Abbott. [0003] Itopride Capsules is a new type of gastrointestinal prokinetic drug. Its dual mechanism of action is to antagonize dopamine D2 receptors on the one hand, stimul...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/48A61K31/166A61P1/14A61P1/08
CPCA61K9/2059A61K9/2095A61K9/4808A61K9/4866A61K31/166A61P1/08A61P1/14
Inventor 谢斌徐维莫泽艺陈新民
Owner 珠海润都制药股份有限公司
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