Acedofenac-paracetamol pharmaceutical composite and liposome solid preparation thereof

A technology of acetaminophen and aceclofenac, applied in the field of medicine, can solve the problems of poor stability, low bioavailability, poor dissolution and the like, and achieve the effects of low cost, simple production process and fast onset of action

Inactive Publication Date: 2010-01-20
HAINAN YONGTIAN PHARMA INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Patent literature CN101411699A discloses tablets containing aceclofenac and acetaminophen, which are made by adding conventional fillers such as starch....

Method used

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  • Acedofenac-paracetamol pharmaceutical composite and liposome solid preparation thereof
  • Acedofenac-paracetamol pharmaceutical composite and liposome solid preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1 Preparation of liposomes of aceclofenac and acetaminophen

[0053] prescription:

[0054] Aceclofenac 100g

[0055] Acetaminophen 500g

[0056] Soy Lecithin 1200g

[0057] Cholesterol 300g

[0058] Sodium deoxycholate 200g

[0059] Poloxamer 188 500g

[0060] Preparation Process

[0061] (1) Dissolve 1200g of soybean lecithin, 300g of cholesterol, 200g of sodium deoxycholate and 500g of poloxamer 188 in 8000ml of isopropanol, mix well, and remove isopropanol under reduced pressure on a rotary film evaporator to prepare Get phospholipid membrane;

[0062] (2) Add 2000ml of phosphoric acid-sodium dihydrogen phosphate buffer solution with pH=4.2, stir to completely hydrate the phospholipid membrane, and then homogenize and emulsify with a tissue masher for 20 minutes at a speed of 12000r / min to prepare a blank liposome suspension Liquid; (100g of aceclofenac is 1 part, 2000ml of buffer solution is 2000g, 2000g / 100g=20 parts)

[0063] (3) Disperse 100g of aceclofenac and 5...

Embodiment 2

[0081] Example 2 Preparation of liposomes of aceclofenac and acetaminophen

[0082] prescription:

[0083] Aceclofenac 100g

[0084] Acetaminophen 500g

[0085] Soy Lecithin 2400g

[0086] Cholesterol 900g

[0087] Sodium deoxycholate 600g

[0088] Poloxamer 188 1200g

[0089] Preparation Process

[0090] (1) Dissolve 2400g soybean lecithin, 900g cholesterol, 600g sodium deoxycholate and 1200g poloxamer 188 in 18000ml isopropanol, mix well, and remove isopropanol under reduced pressure on a rotary film evaporator to prepare Get phospholipid membrane;

[0091] (2) Add 5000ml of citric acid-sodium citrate buffer solution with pH=5.6, stir to completely hydrate the phospholipid membrane, and then homogenize and emulsify with a tissue masher for 15min at a rotation speed of 15000r / min to prepare blank liposomes Suspension

[0092] (3) Disperse 100g of aceclofenac and 500g of acetaminophen in 5000ml of water evenly, add them to the blank liposome suspension, keep at 55℃, and then homogenize ...

Embodiment 3

[0105] Example 3 Preparation of Aceclofenac and Acetaminophen Tablets

[0106] 600g of liposomes containing aceclofenac and acetaminophen (containing aceclofenac 100g, acetaminophen (from Example 1) phenol 500g)

[0107] Microcrystalline cellulose 76g

[0108] Lactose 50g

[0109] Crospovidone 40g

[0110] Hypromellose 3g

[0111] Colloidal silica 15g

[0112] Talcum powder 20g

[0113] Preparation Process

[0114] (1) The liposomes containing 600g of aceclofenac and acetaminophen prepared in Example 1 were crushed, passed through an 80-mesh sieve, and set aside;

[0115] (2) Weigh 76 g of microcrystalline cellulose, 50 g of lactose, and 40 g of crospovidone, pass through an 80 mesh sieve, mix, and set aside;

[0116] (3) Mix the above raw and auxiliary materials uniformly, add 150ml of 2% hypromellose 50% ethanol solution to make soft material, pass through a 20-mesh sieve to granulate, dry at 60°C, and pass through an 18-mesh sieve for granulation;

[0117] (4) Compress the dried granules ...

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Abstract

The invention relates to an acedofenac-paracetamol pharmaceutical composite and a liposome solid preparation thereof and a preparation method thereof; the solid preparation comprises the liposome of acedofenac-paracetamol and the excipient which is accepted in pharmacy and the liposome comprises the following components according to the parts by weight percent: 1 part of acedofenac, 5 parts of paracetamol, 5-32 parts of soybean lecithin, 2-17 parts of cholesterol, 2.5-15 parts of sodium deoxycholate and 4-24 parts of poloxamer 188.

Description

Technical field [0001] The invention specifically relates to a solid preparation containing aceclofenac and acetaminophen pharmaceutical composition liposomes and a preparation method thereof, and belongs to the technical field of medicine. Background technique [0002] Aceclofenac was first synthesized by Prodesfarma, Spain, and was first marketed in 1992. It has been on the market for less than 10 years. It has been marketed and used in more than 20 countries including Spain, Portugal, Germany, the United Kingdom, France, Finland and Belgium. It was included in the European Pharmacopoeia and the British Pharmacopoeia in 1998, proving its safety and The effectiveness has been widely affirmed. However, clinical trials have confirmed that aceclofenac can be quickly and completely absorbed by healthy people after oral administration, and its bioavailability is almost 100%, and the peak blood concentration time is 1.25-3 hours after administration. The average plasma elimination h...

Claims

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Application Information

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IPC IPC(8): A61K31/216A61K31/167A61K9/127A61K9/20A61K47/34A61K47/28A61K47/24A61P29/00A61P19/02A61P19/04A61P19/00A61P1/02A61P15/00A61P27/16A61P11/02A61P11/04A61K47/10A61K47/32A61K47/36A61K47/38A61K47/40
Inventor 王明
Owner HAINAN YONGTIAN PHARMA INST
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