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Silodosin film-coated tablet and preparation method thereof

A technology of silodosin tablets and silodosin, which is applied to the oral solid dosage form medicine for the treatment of benign prostatic hyperplasia, the field of silodosin, and can solve the problem of lack of physiological activity, substandard dissolution, tablet sticking and punching, etc. question

Inactive Publication Date: 2018-10-23
KUNMING JIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the present invention aims to find a brand-new prescription, all of which use commonly used inert auxiliary materials, which do not possess physiological activity and can be taken for a long time. At the same time, the commonly used preparation technology can be used to realize the industrial production of silodosin oral tablets, thereby Solve the problem of tablet sticking and punching, the dissolution rate is not up to standard, etc.

Method used

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  • Silodosin film-coated tablet and preparation method thereof
  • Silodosin film-coated tablet and preparation method thereof
  • Silodosin film-coated tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Excipient Compatibility Test

[0029] Mix 5 parts of mannitol, starch, pregelatinized starch, low-substituted hydroxypropyl cellulose with 1 part of silodosin, and then mix with 1 part of magnesium stearate. Store under storage conditions 1 and 2 respectively, observe the color change directly with the naked eye, and detect the degradation products by HPLC.

[0030] Storage conditions

[0031] Condition 1: 40°C, 75% relative humidity, 4 weeks

[0032] Condition 2: 40°C, 60% relative humidity, 4 weeks

[0033] Analytical method

[0034] Take an appropriate amount of mixed powder, add an appropriate amount of methanol, sonicate for 5 minutes to dissolve silodosin, cool, and dilute with [methanol-sodium chloride solution (1→200) (7:3)] to make about 0.2 mg silodosin solution, shake well, filter, and take the subsequent filtrate as the test solution.

[0035] Chromatographic conditions

[0036] Wavelength: 225nm

[0037] Column temperature: 40°C

[0038] Column: Age...

Embodiment 2

[0049] With pregelatinized starch, starch, and mannitol as fillers, low-substituted hydroxypropyl cellulose as disintegrant, and starch slurry as binder, silodosin tablets were prepared by wet granulation technology, and the prescription of the present invention was investigated. Electrostatic properties, compressibility, dissolution effects of silodosin.

[0050] Table 3 Prescription of Silodosin Tablets (grams)

[0051] formula

[0052] Preparation Process:

[0053] Grinding the raw material of silodosin until the particle size of D90 is 20-70 μm, weighing silodosin, pregelatinized starch and part of low-substituted hydroxypropyl cellulose respectively according to the weight ratio, mixing and wet granulating; The granulated product is dried and sized, added with additional excipients and magnesium stearate, mixed evenly, and compressed into tablets.

[0054] The content and content uniformity are used as the electrostatic detection index.

[0055] The hardness ...

Embodiment 3

[0070] Influence of adding amount of magnesium stearate on dissolution rate of silodosin

[0071] Add 1%, 1.5%, and 2% magnesium stearate to fixed proportions of silodosin, mannitol, starch, pregelatinized starch, and low-substituted hydroxypropyl cellulose compositions, measure the dissolution rate, and investigate Effect of magnesium stearate addition on the dissolution rate of silodosin. Dissolution was determined according to the same method as described in Example 2.

[0072] Table 5 Formulation composition (grams)

[0073] formula

[0074] The preparation process is the same as in Example 2.

[0075] Table 6 Effect of different magnesium stearates on dissolution rate test results

[0076] formula

[0077] The results showed that the amount of magnesium stearate had almost no effect on the dissolution rate when pregelatinized starch was added to the prescription, which further explained that the addition of pregelatinized starch allowed the prescrip...

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Abstract

The invention provides a completely-new silodosin tablet composition and a preparation method thereof, wherein the particle size D90 of the silodosin raw material is 20-70 [mu]m, and the auxiliary material comprises pregelatinized starch. According to the present invention, the formula uses the commonly used inert auxiliary material, the commonly used preparation process is used, and the raw material does not need micro-powder, such that the dissolution of the tablet can be effectively improved, the commercial production can be achieved, and the use amount of the added lubricant is not sensitive; and by using the specific prescription, the lubricant content in the silodosin tablet can be significantly increased so as to avoid the sticking problem easily generated in the actual production.

Description

technical field [0001] The invention relates to an oral solid preparation. Specifically, the present invention relates to an oral solid dosage form medicine for treating benign prostatic hyperplasia (BPH), which uses an indoline derivative as an active ingredient, and the derivative is silodosin. Background technique [0002] Silodosin can block the sympathetic nervous system mediated by the α1A-adrenergic receptor subtype distributed in the prostate, urethra, and bladder triangle in the lower urinary tract tissue, relieve the tension of smooth muscle in the lower urinary tract tissue, and inhibit the increase of urethral pressure. Thereby improving urination disorder caused by benign prostatic hyperplasia. It has a high affinity for the α1A-adrenoceptor subtype and can also inhibit the contraction of human prostate smooth muscle induced by norepinephrine. Potent antagonistic effect on norepinephrine-induced contraction in lower urinary tract tissues. The increase in the ...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K31/4045A61K47/36A61P13/08
CPCA61K9/2059A61K31/4045
Inventor 申磊李英张晓杜铎王博张云
Owner KUNMING JIDA PHARMA
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