Bilastine-containing pharmaceutical composition and preparation method thereof

A bilastine and composition technology, applied in the field of pharmaceutical preparations, can solve the problems of sensitization, toxicity and the like, and achieve the effect of simple operation

Inactive Publication Date: 2013-10-23
BEIJING VENTUREPHARM BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although solubilizers have a strong solubilizing effect, such solubilizers and their metabolites are likely to cause biological changes in the body, and long-term use may cause side effects including toxicity, teratogenicity, carcinogenicity, sensitization, Safety issues such as hemolysis

Method used

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  • Bilastine-containing pharmaceutical composition and preparation method thereof
  • Bilastine-containing pharmaceutical composition and preparation method thereof
  • Bilastine-containing pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Bilastine 5% microcrystalline cellulose 64% Sodium carboxymethyl starch 26.7% Colloidal silica 3% Magnesium stearate 1% total 100%

[0022] Preparation Process:

[0023] The active ingredient bilastine in the prescription is micronized, and the particle size is controlled at 5-50 μm. Mix the prescribed amount of bilastine with microcrystalline cellulose, sodium carboxymethyl starch, colloidal silicon dioxide, and magnesium stearate in a mixer. On a tablet press, compress the tablets.

Embodiment 2

[0025] Bilastine 13.3% lactose 57.2% microcrystalline cellulose 20% Crospovidone 8% Povidone K30 0.5% Magnesium stearate 1% total 100%

[0026] Co-micronize the active ingredient Bilastine and part of lactose in the prescription, and control the particle size of 90% of the volume or more particles to be in the range of 5-50 μm, so the excipients are passed through a 100-mesh sieve, and the micronized product and The remaining lactose, microcrystalline cellulose, and cross-linked povidone are mixed evenly by the method of equal addition, and an appropriate amount of PVP K30 is added to make a soft material, which is extruded through a 18-mesh sieve to granulate, and the wet granules are dried at a constant temperature at 50°C After 2 hours, the dry granules were sieved with a 24-mesh sieve, added with additional magnesium stearate, mixed evenly, and compressed into tablets.

[0027]

Embodiment 3

[0029] Bilastine 20% Mannitol 50.5% microcrystalline cellulose 20% Crospovidone 8% Povidone K30 0.5% Magnesium stearate 1% total 100%

[0030] Co-micronize the active ingredient Bilastine and part of mannitol in the prescription, and control the particle size of 90% of the volume or more particles to be in the range of 5-50 μm, so the excipients are passed through a 100-mesh sieve, and the micronized product Mix with the remaining lactose, microcrystalline cellulose, and crospovidone evenly in equal amounts, add an appropriate amount of PVP K30, make a soft material, squeeze and sieve through a 18-mesh sieve to granulate, and place the wet granules at a constant temperature of 50°C Dry for 2 hours, sieve the dry granules through a 24-mesh sieve, add additional magnesium stearate, mix well, and compress into tablets.

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Abstract

The invention belongs to the technical field of medicines, and relates to a bilastine pharmaceutical composition with good dissolution effect. The pharmaceutical composition comprises bilastine, a water-soluble excipient, a disintegrating agent, a lubricating agent and the like, wherein the bilastine is micronized, the grain size of 90% of the bilastine is controlled to 5 to 50 microns and is specifically preferable to 10 to 20 microns. A medicine prepared by the preparation method shows good dissolution effect, and therefore, the bioavailability of the medicine can be effectively improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a pharmaceutical preparation whose active ingredient is bilastine. Bilastine is used as an active ingredient in an oral solid dosage form for the treatment of allergic rhinoconjunctivitis (seasonal and perennial) and urticaria. The invention additionally relates to a process for the preparation of this formulation. Background technique [0002] Bilastine 4-[2-[4-(2-ethoxyethyl)-1H-benzimidazol-2-yl]-1-piperidinyl]ethyl]-α,α-dimethyl Phenylacetic acid is the second generation of histamine H developed by Spanish FAES pharmaceutical company 1 Receptor antagonist for the treatment of diseases of allergic rhinoconjunctivitis (seasonal and perennial) and urticaria. Studies in healthy subjects and patients with rhinitis have shown that this product is safe, without the sedative effect and cardiotoxicity of commonly used antihistamines. The description of bilast...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/454A61K47/26A61K47/10A61K47/36A61P11/02A61P37/08A61P17/00
Inventor 付珊珊孟旻郭夏宋雪梅
Owner BEIJING VENTUREPHARM BIOTECH
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