Naproxen hydrate crystal, preparation method thereof and medicinal composition containing naproxen hydrate crystal and sumatriptan

A technology of hydrate and naproxen, which is applied in the field of medicine, can solve the problems affecting drug dissolution effect and bioavailability, low solubility, and clinical use restrictions, etc.

Inactive Publication Date: 2013-11-20
HAINAN JINRUI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] But, because naproxen is almost insoluble in water, the solubility is also very low under the pH condition of gastric acid environment, and this has influenced the stripping effect and bioavailability of medicine greatly, and long-term taking is bigger to gastrointestinal irritation, clinical use heavily restricted

Method used

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  • Naproxen hydrate crystal, preparation method thereof and medicinal composition containing naproxen hydrate crystal and sumatriptan
  • Naproxen hydrate crystal, preparation method thereof and medicinal composition containing naproxen hydrate crystal and sumatriptan
  • Naproxen hydrate crystal, preparation method thereof and medicinal composition containing naproxen hydrate crystal and sumatriptan

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] [Example 1] Preparation of Naproxen Hydrate Crystal

[0076] (1) Cool the mixed solution of solvent ethanol 30ml and acetone 25ml to 6°C, put in 10g of naproxen and dissolve to obtain solution 1;

[0077] (2) Add 48ml of deionized water dropwise to solution 1 under an ultrasonic field with a power of 0.5kw until crystallization occurs; the temperature of solution 1 is controlled at 6°C during the dropping process;

[0078] (3) Turn off the ultrasonic field after the dropwise addition, maintain the above temperature and stir for 1.5h, then stand at 6°C to grow crystals for 3.5 hours, and filter; the filter cake is washed with 10ml of purified water and 15ml of ethyl acetate, and vacuum-dried to obtain Naproxen Hydrate crystals.

[0079] The X-ray powder diffraction spectrogram (see figure 1 ) at 2θ of 7.3°, 12.5°, 13.0°, 13.5°, 17.0°, 17.9°, 18.8°, 22.1°, 23.4°, 24.2°, 25.0° and 27.4°.

[0080] Adopt U.S. Perkin-Elmer company PE Pyris Diamond TG thermal analyzer, thermo...

preparation Embodiment 1

[0085] [Preparation Example 1] Preparation of Naproxen / Sumatriptan Tablets

[0086] The prescription is as follows:

[0087]

[0088]

[0089] Preparation:

[0090] 1) Preparation of naproxen sumatriptan wrapper

[0091] i) the sumatriptan of said consumption is pulverized through 80 mesh sieves, for subsequent use;

[0092] ii) Weigh the naproxen hydrate crystal of Example 1 according to the stated amount, and mix it with the above-mentioned pulverized and sieved sumatriptan to obtain a mixture of naproxen and sumatriptan;

[0093] iii) Heat and melt the gelatin in the stated amount, add the above-mentioned mixture of naproxen and sumatriptan, stir evenly, and after cooling, pulverize and pass through an 80-mesh sieve to obtain the naproxen-sumatriptan coating.

[0094] 2) Preparation of Naproxen / Sumatriptan Tablets

[0095] i) The pharmaceutical excipients compressible starch, microcrystalline cellulose, low-substituted hydroxypropyl cellulose, cross-linked polyvin...

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Abstract

The invention relates to a naproxen hydrate crystal, a preparation method thereof and a medicinal composition containing the naproxen hydrate crystal and sumatriptan. The naproxen hydrate crystal has the molecular formula as follows: C14H14O3.1.5H2O. The medicinal composition comprises the following components in parts by weight: 125-750 parts of naproxen, 25-100 parts of sumatriptan, 130-200 parts of gelatine, 10-45 parts of compressible starch, 10-35 parts of microcrystalline cellulose, 10-30 parts of low-substituted hydroxy propyl cellulose, 10-30 parts of cross-linked polyvinylpyrrolidone, 10-20 parts of sodium carboxymethylcellulose, 20-40 parts of maltodextrin, 5-20 parts of lecithin, 5-20 parts of magnesium stearate and 10-20 parts of sodium bicarbonate. According to the crystal provided by the invention, the dissolubility of naproxen is obviously improved, the medicinal composition of the naproxen hydrate crystal is prepared by using a direct tabletting method and has better disintegration time and dissolution rate, and the bioavailability of the naproxen is obviously improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a naproxen hydrate crystal, a preparation method thereof and a pharmaceutical composition containing the crystal and sumatriptan. Background technique [0002] Migraine is a headache caused by periodic attacks of neuro-vascular dysfunction. It is a common clinical and frequently-occurring disease characterized by diffuse or unilateral attacks, severe pain, and recurrent attacks. It often has a family history. This disease belongs to the category of diseases such as headache in traditional Chinese medicine. Migraine is divided into migraine without aura (ordinary) and migraine with aura (classic). Migraine attacks are generally limited to one side of the head, can last for several hours or even days, have the characteristics of recurrent attacks, and are often accompanied by symptoms such as nausea, vomiting, photophobia, and dizziness. With the rapid development of...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C59/64C07C51/43A61K31/4045A61K31/192A61K9/20A61P25/06A61P29/00
Inventor 马鹰军王小树
Owner HAINAN JINRUI PHARMA CO LTD
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