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Valsartan lipid microsphere solid preparation

A technology of solid preparations and valsartan fat, which is applied in the field of pharmaceutical preparations, can solve the problems of poor stability and encapsulation efficiency of lipid microspheres, and achieve the effects of improving bioavailability, increasing dissolution rate, and simple preparation methods

Inactive Publication Date: 2011-07-27
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The inventor finally screened the combination of the three materials of tragacanth gum, sodium glycocholate and octadecylamine, and unexpectedly found that the combination of the three materials of tragacanth gum, sodium glycocholate and octadecylamine The combination solves the problem of poor stability and encapsulation efficiency of lipid microspheres, and obtains unexpected technical effects, thus providing high-quality lipid microspheres

Method used

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  • Valsartan lipid microsphere solid preparation
  • Valsartan lipid microsphere solid preparation
  • Valsartan lipid microsphere solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The preparation of embodiment 1 valsartan tablet

[0046] Prescription (1000 tablets)

[0047]

[0048] making process:

[0049] (1) Add 240g tragacanth gum, 40g sodium glycocholate and 120g octadecylamine into 4000ml purified water, then add 80g valsartan and mix evenly, heat and stir in a water bath at 80°C until it melts, and use a tissue masher to cut Cut and stir for 20 minutes at a speed of 15000r / min to obtain the first emulsion, and then circulate and emulsify it through a high-pressure homogenizer for 5 times to obtain an emulsion, and then freeze-dry to obtain lipid microspheres.

[0050] (2) Mix the prepared lipid microspheres with 260g pregelatinized starch, 100g microcrystalline cellulose, and 80g low-substituted hypromellose, then add 250ml of 2% hypromellose aqueous solution to prepare a soft material, 30 mesh Sieve the wet granules, dry at 55°C, granulate with a 20-mesh sieve, add 10g of magnesium stearate and mix uniformly, compress into tablets, w...

Embodiment 2

[0051] The preparation of embodiment 2 valsartan capsules

[0052] Prescription (1000 capsules)

[0053]

[0054] making process:

[0055] (1) Add 480g of tragacanth gum, 200g of sodium glycocholate and 320g of octadecylamine into 12000ml of purified water, then add 80g of valsartan and mix evenly, heat and stir in a water bath at 90°C until it melts, and use a tissue masher to cut Cut and stir for 10 minutes at a rotational speed of 15000r / min to obtain the primary emulsion, and then circulate and emulsify it through a high-pressure homogenizer for 4 times to obtain an emulsion, which is then spray-dried to obtain lipid microspheres.

[0056] (2) Mix the prepared lipid microspheres with 800g starch and 100g crospovidone, then add 50% ethanol solution 300ml of 5% povidone K30 to prepare soft material, 20 mesh sieve wet granules, 60°C Drying, 18-mesh sieve granulation, adding 60g of silicon dioxide and mixing evenly, filling capsules to obtain valsartan capsules.

Embodiment 3

[0057] The preparation of embodiment 3 valsartan dispersible tablets

[0058] Prescription (1000 tablets)

[0059]

[0060] making process:

[0061] (1) Add 640g tragacanth gum, 160g sodium glycocholate and 480g octadecylamine into 15000ml purified water, then add 160g valsartan and mix evenly, heat and stir in a water bath at 70°C until it melts, use a tissue masher to cut Cut and stir for 20 minutes at a speed of 12000r / min to obtain the first emulsion, and then circulate and emulsify it through a high-pressure homogenizer for 5 times to obtain an emulsion, and then freeze-dry to obtain lipid microspheres.

[0062] (2) Mix the prepared lipid microspheres with 1200g microcrystalline cellulose, 600g starch, 200g aspartame, and 100g croscarmellose sodium, and then add 500ml of 2% hypromellose aqueous solution to prepare Soft material, wet granulation with 20 mesh sieve, drying at 60°C, granulation with 18 mesh sieve, adding 40g of magnesium stearate, mixing evenly, tableti...

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Abstract

The invention provides a valsartan lipid microsphere solid preparation which is mainly prepared by firstly preparing lipid microspheres from valsartan, tragacanth, sodium glycocholate and octadecylamine and then adding other pharmaceutically acceptable excipients. The valsartan lipid microsphere solid preparation comprises the following components in parts by weight: 1 part of the valsartan, 2-15 parts of the tragacanth, 0.2-4 parts of the sodium glycocholate, 1.3-8 parts of the octadecylamine and 4-35 parts of the other excipients. In the valsartan lipid microspheres prepared in the invention, the dissolubility of the valsartan is improved to a great extent so as to benefit dissolution out of a pharmaceutical preparation and improve the bioavailability and the stability of a solid preparation. In addition, the valsartan lipid microsphere solid preparation provided by the invention has the advantages of improved product quality, reduced toxic and side effects and more remarkable curative effect.

Description

technical field [0001] The invention relates to a new preparation of valsartan, in particular to a valsartan lipid microsphere, a solid preparation and a preparation method thereof, and belongs to the field of pharmaceutical preparations. Background technique [0002] Angiotensin, the main active substance of the renin-angiotensin system, is a powerful vasoconstrictor polypeptide, and its biological functions are mainly reflected in the regulation of vascular tension, blood flow, promotion of cell growth, proliferation and inflammation . Valsartan is a non-peptide angiotensin (AT) II receptor antagonist, which can antagonize the synthesis of angiotensin II, block the combination of angiotensin II molecules and corresponding receptors, and achieve antihypertensive effects. Systemic blood pressure plays a key role in maintaining electrolyte and fluid balance. [0003] Valsartan is a highly specific angiotensin (AT) II receptor antagonist that acts selectively on the AT1 rece...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/41A61K47/36A61P9/12
Inventor 杨明贵
Owner HAINAN MEILAN SMITH KLINE PHARMA