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一种组合物、药物的技术，应用在药物组合、纳米药物、杂环化合物有效成分等方向，能够解决未能得到等问题
Inactive Publication Date: 2014-06-25
ASKAT
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Abstract
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Problems solved by technology
[0011] As a method of maintaining the basicity of the third-generation coxib-drugs, addition of basic alkaline earth metal salts such as calcium carbonate, calcium hydroxide, magnesium carbonate, magnesium silicate, and magnesium aluminate as excipients has been attempted. method, but when adding alkaline alkaline earth metal salts to compound A, no preferred results could be obtained
Method used
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Embodiment 1
[0161] [Example 1] Tablets of compound A containing trometamol as a basic amine
[0162] dosage form
[0163] The 60 mg tablet of Compound A containing tromethamine was prepared according to the dosage forms described in Table 1, Table 2 and Table 3. Tablets of other doses are prepared proportional to the dose according to the weight % of each ingredient. Tablets containing other basic amines such as triethanolamine, diethanolamine, monoethanolamine, etc. are prepared in a similar manner to the dosage form in tromethamine. In fact, tablets can be prepared by substituting other basic amines for tromethamine in Table 1, Table 2 and Table 3.
[0164] Manufacturing method 1
[0165] Each compound A that was ground through a 0.006-inch wheel sieve at 1800 rpm, tromethamine and mannitol both of which were ground through a 0.018-inch wheel sieve at 1800 rpm were weighed. Avicel PH102 was added to the PK-blender and blended for 1 minute to coat the surface. Compound A, milled tro...
Embodiment 2
[0181] [Example 2] Capsules of compound A containing trometamol as a basic amine
[0182] dosage form
[0183] 60 mg capsules of Compound A containing trometamol were prepared in the dosage form described in Table 4. Capsules of other doses are prepared in proportion to the dose according to the weight % of each ingredient. Capsules containing other basic amines such as triethanolamine, diethanolamine, monoethanolamine, etc. are prepared by a method similar to the dosage form in tromethamine. In fact, capsules were prepared by substituting other basic amines for trometamol in Table 4.
[0184] Manufacturing method
[0185] Mill Compound A, trometamol, lactose monohydrate, microcrystalline cellulose PH102, hydroxypropylmethylcellulose and cross- Sodium carboxymethyl cellulose for blending. A solution of polysorbate 80 dissolved in purified water was added to the granulator. The granular material was milled through a 0.25 inch wheel screen and dried on trays. The granular...
Embodiment 3
[0189] [Example 3] Tablets of compound A containing meglumine as a basic amine
[0190] dosage form
[0191] Tablets were prepared using meglumine instead of trometamol as described in Table 3.
[0192] Manufacturing method
[0193] Tablets were prepared by a method similar to Production Method 3 in Example 1. In fact, meglumine was used instead of trometamol as described in Table 3 to prepare 60 mg tablets of Compound A containing meglumine.
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Abstract
The present invention provides a medicinal composition capable of preventing a decrease in the blood exposure level of a third generation coxib drug, a method for preparing the composition and utilization of the same. It was discovered that, by adding a basic amine or a basic amino acid or cyclodextrin to a third generation coxib compound, a medicinal composition capable of inhibiting a decrease in the blood concentration thereof, a decrease in the area under concentration thereof and a decrease in the bioavailability thereof can be obtained. In addition, the medicinal composition according to the present invention is highly stable and useful as a medicine. That is, a technical idea that a decrease in blood concentration, a decrease in area under concentration and a decrease in bioavailability can be inhibited by adding a basic amine or a basic amino acid or cyclodextrin is thus established.
Description
technical field [0001] The present invention relates to a composition containing a compound represented by chemical formula (I) or a pharmaceutically acceptable salt thereof, a preparation method of the pharmaceutical composition and an application for treating diseases mediated by cyclooxygenase-2 . [0002] [0003] (Explanations in chemical formulas will be described later) Background technique [0004] Prostaglandins play an important role in inflammation and inhibit the production of prostaglandins especially PGG 2 、PGH 2 and PGE 2 The generation of anti-inflammatory agents has become a common goal in the development. However, commonly used non-steroidal anti-inflammatory drugs (NSAIDs) that act to reduce prostaglandin-induced pain and swelling associated with inflammatory processes also act on other prostaglandin-regulated processes not associated with inflammatory processes. Thus, the use of the most commonly used NSAIDs at higher doses produces side effects s...
Claims
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Application Information
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