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Difenidol hydrochloride tablets and preparation method thereof

A technology of diphenidol hydrochloride and magnesium stearate, applied in the field of medicine, can solve problems such as low dissolution rate, and achieve the effects of small RSD of the drug, easy promotion and production, and improved dissolution rate

Inactive Publication Date: 2019-09-20
ZHUZHOU QIANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The object of the present invention is to provide a kind of difenidol hydrochloride tablet for the low dissolution rate problem of the generic drug difenidol hydrochloride tablet prepared in the prior art in pH6.8 medium

Method used

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  • Difenidol hydrochloride tablets and preparation method thereof
  • Difenidol hydrochloride tablets and preparation method thereof
  • Difenidol hydrochloride tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Physicochemical properties of difenidol hydrochloride bulk drug: white crystalline powder; odorless; easily soluble in methanol, soluble in ethanol, slightly soluble in water or chloroform; pH value should be 5.0~7.0 ("China Pharmacopoeia 2015 Edition, Part II); melting point is 217-222°C ("Chinese Pharmacopoeia" 2015 Edition General Rule 0612, the first method), melting and decomposing simultaneously ("Chinese Pharmacopoeia" 2015 Edition Volume 2).

[0049] The Diphenidol hydrochloride bulk drug used in the following examples comes from Hunan Qianjin Xiangjiang Pharmaceutical Co., Ltd., which has impurity I(ene compounds, and its structure is shown in the following formula, 1-(4,4-diphenyl- 3-butenyl) piperidine, the chemical formula is C 21 h 25 N, the molecular weight is 291.44) shall not exceed 0.5%, and the sum of the peak areas of other impurities shall not be greater than 0.5% of the sum of the peak areas, which is equivalent to 34.59 mg of difenyl hydrochloride...

Embodiment 2

[0056] The preparation of embodiment 2 difenidol hydrochloride tablets

[0057] For every 1000 tablets of difenidol hydrochloride tablets, the specific components are: difenidol hydrochloride 25g, lactose 68g, starch 10g, pH regulator (potassium hydrogen tartrate) 16g, polyvinyl alcohol 1.6g, carboxymethyl cellulose Calcium 8g, magnesium stearate 1.3g.

[0058] The specific preparation process is as follows: pulverize difenidol hydrochloride, control the particle size of Dv90 between 10 and 50 μm, weigh the prescribed amount of difenidol hydrochloride, lactose, starch, potassium hydrogen tartrate, carboxymethyl cellulose Calcium is mixed evenly, and polyvinyl alcohol is weighed to form a slurry, and the evenly mixed material is added, after drying, the prescribed amount of magnesium stearate is added, mixed evenly, tableted according to the measured content, and coated.

Embodiment 3～8

[0059] The preparation of embodiment 3~8 difenidol hydrochloride sheet

[0060] 1. According to the preparation method of Example 2, Diphenidol Hydrochloride Tablets were prepared according to the dosage of the components in Table 2, and at the same time, the formulation without adding pH regulators and the addition of different types and dosages of pH regulators were used as comparative examples. Difenidol Hydrochloride Tablets.

[0061] Table 2 Component types and dosage ratio

[0062]

[0063] 2, measure the pH value of the prepared difenidol hydrochloride tablet

[0064] The difenidol hydrochloride tablet prepared by the embodiment in table 2 and the difenidol hydrochloride tablet prepared by the comparative example are samples to be tested, and measure the pH value of its medicine. Samples with a ratio of 1 to 11 were prepared into a solution containing difenidol hydrochloride 2 mg / mL, and the pH value was measured according to the general rule 0631 of the fourth par...

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Abstract

The invention discloses difenidol hydrochloride tablets and a preparation method thereof. The difenidol hydrochloride tablets are composed of, by weight, 15-25% of difenidol hydrochloride and 85-75% of auxiliary materials, Dv90 particle size of difenidol hydrochloride is 10-50um, and pH of the difenidol hydrochloride tablets is controlled to 3.55-5.54. By controlling pH value of the difenidol hydrochloride tablets and Dv90 particle size of difenidol hydrochloride which is an active pharmaceutical ingredient within a range of 10-50um, dissolution rate of the difenidol hydrochloride tablets prepared by the method in water and media with pH values being 1.2, 4.0 and 6.8 is enabled to be consistent with that of original drug, the dissolution rate (dissolution rate of 15min is greater than 90%) is increased, and improving of bioavailability of the difenidol hydrochloride tablets in a human body is facilitated; the difenidol hydrochloride tablets prepared by the method are small in RSD and difference and stable and reliable in quality. The difenidol hydrochloride tablets are simple and mature in formula and preparation process, can be industrially produced on a large scale and are convenient for popularization and production.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a difenidol hydrochloride tablet and a preparation method thereof. Background technique [0002] Diphenidol hydrochloride was synthesized in 1946 and listed in the United States on April 5, 1967 by GlaxoSmithKline for the treatment of dizziness and vomiting. In 1968, Nippon Shinyaku Co., Ltd. started the research and development of this product in Japan. In 1973, it was approved for the treatment of vertigo caused by ear diseases. It was launched in 1974 with a specification of 25 mg; in October 1981, it was launched in granules; in 2008, the company changed its trade name to named [0003] Due to its remarkable curative effect, difenidol hydrochloride has been approved for the production and application of registered generic drugs in China, among which Hunan Qianjin Xiangjiang Pharmaceutical is the first domestic company to generically market this product. At present, the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/26A61K47/36A61K31/4453A61P1/08
CPCA61K9/2018A61K9/2059A61K9/2095A61K31/4453A61P1/08
Inventor 陈涛宿亮李雪如王玲兰王新军袁秀菊王洪锋吴超男
Owner ZHUZHOU QIANJIN PHARMA
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