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Ornidazole ester microsphere solid preparation

A technology of solid preparation and ornidazole ester, applied in the field of medicine, can solve the problems of loss of drug efficacy, poor solubility of ornidazole, and reduced bioavailability, and achieve the effects of reducing drug side effects, improving solubility and high dissolution rate

Inactive Publication Date: 2010-06-02
HAINAN YONGTIAN PHARMA INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the above effervescent tablet patent disintegrates quickly, ornidazole has poor solubility and cannot be absorbed quickly after disintegration, resulting in loss of drug efficacy and reduced bioavailability

Method used

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  • Ornidazole ester microsphere solid preparation
  • Ornidazole ester microsphere solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Example 1 Preparation of Ornidazole Lipid Microspheres

[0070] Prescription: Ornidazole 100g

[0071] Hydrogenated egg yolk lecithin 330g

[0072] Cholesterol 140g

[0073] Poloxamer 188 180g

[0074] Sodium Glycocholate 220g

[0075] Preparation Process

[0076] (1) 100g ornidazole, 330g hydrogenated egg yolk lecithin, 140g cholesterol, 180g poloxamer 188, 220g sodium glycocholate are dissolved in 4000ml volume ratio of acetone and isopropanol mixed solvent of 1:3, Mix evenly, and remove the mixed solvent under reduced pressure on a rotary thin film evaporator to obtain a phospholipid film;

[0077] (2) Add 2500ml of acetic acid-sodium acetate buffer solution with a pH value of 4.5, shake, stir for 20min, and rotate at a speed of 600r / min to completely hydrate the phospholipid film, then homogeneously emulsify with a tissue masher for 10min at a speed of 15000r / min, and then Filter with a 0.45 μm microporous membrane to prepare a suspe...

Embodiment 2

[0086] Example 2 Preparation of Ornidazole Lipid Microspheres

[0087] Prescription: Ornidazole 100g

[0088] Hydrogenated egg yolk lecithin 850g

[0089] Cholesterol 530g

[0090] Poloxamer 188 400g

[0091] Sodium Glycocholate 350g

[0092] Preparation Process

[0093] (1) 100g ornidazole, 850g hydrogenated egg yolk lecithin, 530g cholesterol, 400g poloxamer 188, 350g sodium glycocholate are dissolved in 15000ml volume ratio of acetone and isopropanol mixed solvent of 1:3, Mix evenly, and remove the mixed solvent under reduced pressure on a rotary thin film evaporator to obtain a phospholipid film;

[0094] (2) Add 11,000ml of citric acid-sodium citrate buffer solution with a pH value of 6.5, shake, stir for 30min, and rotate at a speed of 200r / min to completely hydrate the phospholipid film, then use a tissue masher to homogeneously emulsify for 20min, and rotate at a speed of 200r / min. 13000 / min, and then filtered through a 0.45 μm micropo...

Embodiment 3

[0103] Example 3 Preparation of Ornidazole Tablets

[0104] Prescription (100 tablets)

[0105] Ornidazole lipid microspheres (calculated as ornidazole) 25g

[0106] Starch 5g

[0107] Microcrystalline Cellulose 4.5g

[0108] Sodium starch glycolate 1.5g

[0109] Povidone K30 2g

[0110] Magnesium stearate 0.5g

[0111] Preparation Process

[0112] (1) Pulverize the lipid microspheres containing 25g ornidazole, cross 80 mesh sieves, and set aside;

[0113] (2) 5g starch, 4.5g microcrystalline cellulose, and 1.5g carboxymethyl starch sodium are passed through an 80-mesh sieve, mixed, and set aside;

[0114] (3) Prepare 5% Povidone K 30 100ml of 80% ethanol solution, set aside;

[0115] (4) Mix the above raw and auxiliary materials evenly, add 5% povidone K 30 40ml of 80% ethanol solution to make soft material, granulate through 20 mesh sieve, and dry at 60°C;

[0116] (5) Add 0.5 g of magnesium stearate to the dried granules and mix evenly, sieve the granules wit...

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Abstract

The invention discloses an ornidazole ester microsphere solid preparation. Specifically, ornidazole ester microspheres are prepared by adopting film dispersion technology through the combination of hydrogenated yolk lecithin, cholesterol, poloxamer 188, sodium glycyl-cholate and ornidazole serving as active component with certain contents, and then the ornidazole ester microspheres are mixed with certain accessories to obtain the solid preparation such as tablets and capsules. The solid preparation has the surprising technical effects of high dissolution degree, high bioavailability, small toxic and side effect and the like.

Description

technical field [0001] The invention relates to ornidazole lipid microspheres, in particular to a solid preparation of ornidazole lipid microspheres, which belongs to the technical field of medicine. Background technique [0002] Ornidazole, chemical name: 1-(3-chloro-2-hydroxypropyl)-2-methyl-5-nitroimidazole, molecular formula: C 7 h 10 ClN 3 o 3 , molecular weight: 219.63, structural formula: [0003] [0004] Ornidazole is the third generation of nitroimidazole derivatives. The exact mechanism of its antimicrobial effect is not yet clear. It may be through the reduction of the nitro group in its molecule to an amino group in an oxygen-free environment or through the formation of free radicals. form, interact with cellular components, and result in the death of microorganisms. The plasma elimination half-life of ornidazole is 14 hours, and the plasma protein binding rate is less than 15%. Widely distributed in human tissues and body fluids, including cerebrospina...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/48A61K31/4164A61K47/34A61P31/00A61K47/28
Inventor 陶小刚
Owner HAINAN YONGTIAN PHARMA INST
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