Ribavirin lipid microsphere effervescent granules

A technology of effervescent granules and virin lipid, applied in the field of medicine, can solve problems such as large first-pass effect, toxic and side effects, and achieve the effects of reducing drug toxicity, high bioavailability, and rapid onset of drug effect.

Inactive Publication Date: 2010-05-12
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Because ribavirin has good water solubility, the first-pass effect after oral administration is large, and it is easy to produce toxic and side effects, so it is necessary to improve the existing technology

Method used

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  • Ribavirin lipid microsphere effervescent granules
  • Ribavirin lipid microsphere effervescent granules
  • Ribavirin lipid microsphere effervescent granules

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] Example 1 Preparation of ribavirin lipid microspheres

[0074] Prescription: Ribavirin 50g

[0075] Egg yolk lecithin 125g

[0076] Cholesterol 40g

[0077] Sodium Deoxycholate 25g

[0078] Preparation Process

[0079] (1) Dissolve 125g egg yolk lecithin, 40g cholesterol, 25g sodium deoxycholate in 1000ml methanol and n-butanol mixed solvent with a volume ratio of 2:1, mix well, remove the mixed solvent under reduced pressure on a rotary thin film evaporator , to obtain a phospholipid membrane;

[0080] (2) Add 800 ml of sodium dihydrogen phosphate-disodium hydrogen phosphate buffer solution with a pH value of 4.8, shake, stir for 20 min, and rotate at 500 r / min to completely hydrate the phospholipid membrane, and then use a tissue masher to homogenize and emulsify for 10 min at a rotating speed of 500 rpm. 13000r / min, and then filtered with a 0.45μm microporous membrane to obtain a blank lipid microsphere suspension;

[0081] (3) Dissolve 50 g of ribavirin in ...

Embodiment 2

[0089] Example 2 Preparation of ribavirin lipid microspheres

[0090] Prescription: Ribavirin 150g

[0091] Egg yolk lecithin 750g

[0092] Cholesterol 570g

[0093] Sodium Deoxycholate 675g

[0094] Preparation Process

[0095] (1) Dissolve 750g egg yolk lecithin, 570g cholesterol, 675g sodium deoxycholate in 15000ml methanol and n-butanol mixed solvent with a volume ratio of 2:1, mix well, remove the mixed solvent under reduced pressure on a rotary thin film evaporator , to obtain a phospholipid membrane;

[0096] (2) Add 10000ml of citric acid-sodium citrate buffer solution with pH value of 6.8, shake, stir for 40min, rotating speed 200r / min, make the phospholipid membrane completely hydrated, then use a tissue masher to homogenize and emulsify for 20min, rotating speed 12000 / min, and then filtered with a 0.45 μm microporous membrane to obtain a blank lipid microsphere suspension;

[0097] (3) Dissolve 150 g of ribavirin in 1200 ml of water, filter with a 0.45 μm ...

Embodiment 3

[0105] Example 3 Preparation of Ribavirin Effervescent Granules

[0106] Prescription (1000 packs)

[0107] Ribavirin Lipid Microspheres (as Ribavirin) 50g

[0108] Tartaric acid 140g

[0109] Sodium Bicarbonate 200g

[0110] Cane sugar 450g

[0111] Mannitol 150g

[0112] Orange Flavor 5g

[0113] Povidone K30 7.5g

[0114] PEG6000 10g

[0115] Preparation Process

[0116] (1) pulverize the lipid microspheres containing 50g of ribavirin, pass through an 80-mesh sieve, for subsequent use;

[0117] (2) 140g tartaric acid, 200g sodium bicarbonate, 150g mannitol, 450g sucrose are pulverized respectively, pass through 80 mesh sieves, mix, for subsequent use;

[0118] (3) Prepare 5% Povidone K 30 80% ethanol solution 150ml, add 5g orange essence, mix well, set aside;

[0119] (4) Mix 140g tartaric acid with lipid microspheres containing 25g ribavirin, 75g mannitol, and 225g sucrose, add binder system soft material, sieve and granulate, and dry; 200g sodium bicarbonate ...

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PUM

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Abstract

The invention relates to ribavirin lipid microspheres of a targeting drug delivery system and a method for preparing the same, in particular to ribavirin lipid microsphere effervescent granules and a method for preparing the same. The method comprises the steps of: adopting film dispersion technology to obtain the ribavirin lipid microspheres by combining a certain amount of yolk lecithin, cholesterol and deoxysodium cholate with an active component, namely ribavirin, and then mixing the ribavirin lipid microspheres with certain excipient to obtain the effervescent granules. The effervescent granules have the advantages of quick response, high bioavailability, and less toxic and side effects, so that the satisfactory technical effect is achieved.

Description

technical field [0001] The invention relates to a ribavirin lipid microsphere and a preparation method thereof, in particular to a ribavirin lipid microsphere effervescent granule and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Ribavirin, chemical name: 1-β-D-ribofuranosyl-1H-1,2,4-triazole-3-carboxamide, molecular formula: C 8 h 12 N 4 o 5 , molecular weight: 244.21, structural formula: [0003] [0004] Ribavirin is a broad-spectrum antiviral drug. Its mechanism of action is mainly to inhibit inosine dehydrogenase and block the conversion of inosine-phosphate to xanthine-phosphate, thereby inhibiting nucleic acid synthesis and preventing virus replication. Ribavirin is absorbed quickly, and the plasma concentration reaches its peak within 60 to 90 minutes. After entering the body and being phosphorylated, an active metabolite-ribavirin monophosphate is formed, which can be concentrated in red blood cell...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/7056A61K47/28A61K47/24A61P31/12A61P31/22
Inventor 王明
Owner HAINAN LINGKANG PHARMA CO LTD
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