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Ebastine solid dispersion and high-dissolubility ebastine tablet prepared by the same

A technology of solid dispersion and ebastine tablets, which is applied in the field of medicine, can solve problems such as insoluble water, low bioavailability, and poor dissolution rate of tablets, and achieve improved solubility, no significant change, and stable dissolution rate Effect

Active Publication Date: 2011-10-19
JIANGSU LIANHUAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Ebastine is a strongly hydrophobic substance, which is extremely difficult to dissolve in water. If conventional preparation methods are used, the tablets made have poor dissolution rate, low bioavailability, and are difficult to absorb in the body, which affects the therapeutic effect of the drug.

Method used

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  • Ebastine solid dispersion and high-dissolubility ebastine tablet prepared by the same
  • Ebastine solid dispersion and high-dissolubility ebastine tablet prepared by the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1 (blank control)

[0028] prescription

[0029] Ebastine 5.7%

[0030] Lactose 51.4%

[0031] Starch 28.6%

[0032] Punch starch 11.4%

[0033] Low-substituted hydroxypropyl cellulose 2.9%

[0034] Magnesium Stearate 0.1%

[0035] method

[0036] Weigh the pulping starch according to the prescription, use appropriate amount of water to make 12% starch slurry, and weigh lactose, starch, and low-substituted hydroxypropyl cellulose according to the prescription ratio, crush them separately, pass through a 100-mesh sieve, mix, and add 12% Starch slurry, made into soft material, granulated with a 16-mesh sieve, dried at 55-60°C, magnesium stearate added to the dry granules, granulated with a 14-mesh sieve, mixed, compressed into tablets, packed in aluminum and aluminum.

[0037] Dissolution test results

[0038] film number

Embodiment 2

[0040] prescription

[0041] Ebastine 5.7%

[0042] Lactose 45.7%

[0043] Starch 22.9%

[0044] Punch starch 11.4%

[0045] Low-substituted hydroxypropyl cellulose 2.9%

[0046] Poloxamer F68 11.4%

[0047] Magnesium Stearate 0.1%

[0048] method

[0049]Weigh ebastine and loxamer F68 according to the prescription ratio, add medicinal ethanol, stir, heat to 60°C, fully mix, continue to stir for 1 hour, evaporate the solvent under reduced pressure at 65°C, cool to room temperature, Filtrate and dry in vacuum at 70°C to obtain solid dispersions of ebastine and poloxamer F68; weigh the pulped starch according to the prescription, and make 12% starch slurry with an appropriate amount of water; weigh lactose and starch according to the ratio of the prescription , low-substituted hydroxypropyl cellulose, solid dispersion of ebastine and poloxamer F68, respectively crushed, passed through a 100-mesh sieve, mixed, added 12% starch slurry, made into a soft material, and granula...

Embodiment 3

[0053] prescription

[0054] Ebastine 5.7%

[0055] Lactose 40.0%

[0056] Starch 17.1%

[0057] Punch starch 11.4%

[0058] Low-substituted hydroxypropyl cellulose 2.9%

[0059] Poloxamer F68 22.8%

[0060] Magnesium Stearate 0.1%

[0061] method

[0062] Weigh ebastine and loxamer F68 according to the prescription ratio, add medicinal ethanol, stir, heat to 40°C, fully mix, continue to stir for 2 hours, evaporate the solvent under reduced pressure at 45°C, cool to room temperature, Filtrate and dry under vacuum at 50°C to obtain solid dispersions of ebastine and poloxamer F68; weigh the starch for pulping according to the prescription, and make 12% starch slurry with an appropriate amount of water; weigh lactose and starch according to the ratio of the prescription , low-substituted hydroxypropyl cellulose, solid dispersion of ebastine and poloxamer F68, respectively crushed, passed through a 100-mesh sieve, mixed, added 12% starch slurry, made into a soft material, a...

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Abstract

The invention provides an ebastine solid dispersion which comprises ebastine, poloxamer F68 and / or polyvinylpyrrolidone k30. The invention also provides a preparation method of the ebastine solid dispersion, and a high-dissolubility ebastine tablet. The method of the invention adopts poloxamer F68, polyvinylpyrrolidone k30 or a mixture of the two as a carrier, and prepares the solid dispersion by the carrier and ebastine; and the solubility of ebastine in water in the ebastine tablet is significantly improved. After accelerated tests and long-term tests, the dissolubility is stable without obvious changes.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to an ebastine solid dispersion and high-dissolution ebastine tablets prepared therefrom. Background technique [0002] Allergic reaction, also known as allergic reaction, is an abnormal or pathological immune response caused by tissue damage or dysfunction after the body is stimulated by antigenic substances. Common clinical allergic diseases include acute urticaria, chronic urticaria, pruritus, eczema, dermatitis, perennial rhinitis, seasonal rhinitis, allergic asthma, and motion sickness. It is a common and frequently-occurring disease that affects people's normal work, study and life, and endangers human health. [0003] In 1937, Bovet and Staub discovered the first compound 2-isopropyl-5-methylphenoxyethyldiethylamine, which has antihistamine activity and can be used to treat allergic diseases. Since then, chlorpheniramine, non- Nageng, diphenhydramine, tripyramine, deoxyhy...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/445A61K47/34A61K47/38A61P37/08A61P11/02A61P1/08A61P17/00A61P17/04
Inventor 贺曾佑
Owner JIANGSU LIANHUAN PHARMA
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