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Lamivudine liposome solid preparation

A technology of lamivudine lipid and solid preparations, which is applied in the field of medicine, can solve the problems of liposome stability and poor encapsulation efficiency, and is beneficial to large-scale industrial production, and improves stability, dissolution rate, and utilization high effect

Inactive Publication Date: 2011-01-26
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] After a long period of serious research, the inventors found that dipalmitoylphosphatidylglycerol, sodium deoxycholate, and cholesterol were combined in a specific ratio to prepare liposomes with lamivudine in a certain ratio. Then the liposome is prepared into a solid preparation, which solves the technical problems of poor stability and encapsulation efficiency of the liposome, and obtains an unexpected preparation effect, thereby providing a liposome solid preparation of good quality

Method used

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  • Lamivudine liposome solid preparation
  • Lamivudine liposome solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] The preparation of embodiment 1 lamivudine tablet

[0054] Prescription: (1000 tablets)

[0055] Component Dosage

[0056] Lamivudine 100g

[0057] Dipalmitoylphosphatidylglycerol 310g

[0058] Sodium deoxycholate 160g

[0059] Cholesterol 100g

[0060] 260g pregelatinized starch

[0061] Mannitol 120g

[0062] Crospovidone 60g

[0063] Povidone K30 25g

[0064] Talc powder 20g

[0065] Micronized silica gel 15g

[0066] Preparation Process:

[0067] (a) 310g of dipalmitoylphosphatidylglycerol, 160g of sodium deoxycholate, and 100g of cholesterol were dissolved in 4000ml of methanol and acetonitrile in a mixed solvent with a volume ratio of 1:4, mixed evenly, and removed under reduced pressure on a rotary thin film evaporator. Solvent, obtain phospholipid film;

[0068] (b) Add 2000ml of phosphoric acid-dipotassium hydrogen phosphate buffer solution with a pH value of 5.8, adjust the pH to 5.5 with 10% phosphoric acid solution, shake and stir to completely h...

Embodiment 2

[0073] The preparation of embodiment 2 lamivudine tablets

[0074] Prescription: (1000 tablets)

[0075] Component Dosage

[0076] Lamivudine 100g

[0077] Dipalmitoylphosphatidylglycerol 880g

[0078] Sodium deoxycholate 460g

[0079] Cholesterol 240g

[0080] 320g pregelatinized starch

[0081] Dextrin 150g

[0082] Crospovidone 60g

[0083] Low-substituted hydroxypropyl cellulose 80g

[0084] Sodium Carboxymethyl Cellulose 20g

[0085] Micropowder silica gel v 70g

[0086] Preparation Process:

[0087] (a) 880g of dipalmitoylphosphatidylglycerol, 460g of sodium deoxycholate, and 240g of cholesterol were dissolved in 9000ml of methanol and acetonitrile in a mixed solvent with a volume ratio of 1:4, mixed evenly, and removed under reduced pressure on a rotary thin film evaporator. Solvent, obtain phospholipid film;

[0088] (b) Add 5000ml of phosphoric acid-dipotassium hydrogen phosphate buffer solution with a pH value of 5.8, adjust the pH to 6.6 with 10% potassi...

Embodiment 3

[0094] The preparation of embodiment 3 lamivudine dispersible tablets

[0095] Prescription: (1000 tablets)

[0096] Component Content

[0097] Lamivudine 100g

[0098] Dipalmitoylphosphatidylglycerol 1300g

[0099] Sodium deoxycholate 700g

[0100] Cholesterol 500g

[0101] 340g pregelatinized starch

[0102] Croscarmellose Sodium 150g

[0103] Low-substituted hydroxypropyl cellulose 90g

[0104] Povidone K30 100g

[0105] Micronized silica gel 50g

[0106] Talc powder 70g

[0107] Preparation Process:

[0108] (a) Dissolve 1300g of dipalmitoylphosphatidylglycerol, 700g of sodium deoxycholate, and 500g of cholesterol in 15,000ml of isopropanol and acetone in a mixed solvent with a volume ratio of 2:1, mix well, and remove under reduced pressure on a rotary thin film evaporator Mixing solvents to obtain a phospholipid film;

[0109] (b) Add 8000ml of acetic acid-sodium acetate buffer solution with a pH value of 5.6, adjust the pH to 6.0 with 10% sodium citrate solu...

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Abstract

The invention discloses a lamivudine liposome solid preparation and further discloses application thereof in treating chronic hepatitis B. The liposome solid preparation comprises lamivudine, dipalmityl phosphatidyl glycerol, sodium deoxycholate and cholesterol, can be prepared into tablets, dispersible tablets, capsules and the like, has the advantages of high entrapment rate, good stability, improved dissolving rate and the like, and shows favorable safety and drug resistance, better antiviral effects, and lower drug resistant rate and virus bouncing rate on treating the chronic hepatitis B.

Description

technical field [0001] The invention relates to a lamivudine liposome solid preparation and a preparation method thereof, further relates to its application in treating chronic hepatitis B, and belongs to the technical field of medicine. Background technique [0002] Chronic hepatitis B is one of the common chronic infectious diseases in my country, which seriously endangers people's health. The treatment of chronic hepatitis B is also a long-term process. The goal of treatment is to suppress or eliminate HBV to the greatest extent, reduce inflammation, necrosis and dry fibrosis of liver cells, delay and prevent disease progression, reduce and prevent liver decompensation and cirrhosis , HCC and its complications, thereby improving the quality of life and prolonging survival time. The treatment of chronic hepatitis B mainly includes antiviral, immune regulation, anti-inflammatory and liver protection, anti-fibrosis and symptomatic treatment, among which antiviral treatment ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/127A61K31/513A61K47/28A61P1/16A61P31/20
Inventor 杨明贵
Owner HAINAN MEILAN SMITH KLINE PHARMA
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