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Liposome solid preparation of losartan potassium hydrochlorothiazide pharmaceutical composition

A technology of losartan potassium hydrochlorothiazide and solid preparations, which is applied in the field of liposome solid preparations, and can solve the problems of rapid drug release process, easy peak and trough phenomena, bioavailability, and light and heat instability.

Inactive Publication Date: 2010-08-11
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The above-mentioned patents have all introduced the related losartan potassium hydrochlorothiazide pharmaceutical composition, which mainly uses the method of separately preparing hydrochlorothiazide and losartan potassium, which has certain advantages, but still has poor stability, is unstable when exposed to light and heat, releases The drug process is rapid, prone to peaks and valleys and low bioavailability

Method used

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  • Liposome solid preparation of losartan potassium hydrochlorothiazide pharmaceutical composition
  • Liposome solid preparation of losartan potassium hydrochlorothiazide pharmaceutical composition
  • Liposome solid preparation of losartan potassium hydrochlorothiazide pharmaceutical composition

Examples

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Comparison scheme
Effect test

Embodiment 1

[0073] The preparation of embodiment 1 losartan potassium hydrochlorothiazide liposome sheet

[0074] Prescription (1000 tablets):

[0075] Losartan Potassium 50g

[0076] Hydrochlorothiazide 12.5g

[0077] Hydrogenated egg yolk lecithin 60g

[0078] Cholesterol 30g

[0079] Poloxamer 188 8g

[0080] Starch 30g

[0081] Mannitol 20g

[0082] Low-substituted hydroxypropyl cellulose 10g

[0083] Hypromellose 2g

[0084] Talc powder 5g

[0085] Micronized silica gel 3g

[0086] Preparation Process

[0087] (1) 60g of hydrogenated egg yolk lecithin, 30g of cholesterol, and 8g of poloxamer 188 were dissolved in 400ml of dichloromethane and isopropanol mixed solvent with a volume ratio of 1:1, mixed evenly, and reduced on a rotary thin film evaporator. Remove the mixed solvent under pressure to obtain a phospholipid film;

[0088] (2) Add 200ml of citric acid-sodium citrate buffer solution with a pH value of 5.5, shake and stir to fully hydrate the phospholipid membrane,...

Embodiment 2

[0093] The preparation of embodiment 2 losartan potassium hydrochlorothiazide liposome sheet

[0094] Prescription (1000 tablets):

[0095] Losartan Potassium 50g

[0096] Hydrochlorothiazide 12.5g

[0097] Hydrogenated egg yolk lecithin 80g

[0098] Cholesterol 50g

[0099] Poloxamer 188 20g

[0100] Starch 65g

[0101] Sorbitol 70g

[0102] Carboxymethyl starch sodium 8g

[0103] Low-substituted hydroxypropyl cellulose 10g

[0104] Sodium Carboxymethyl Cellulose 2g

[0105] Talc powder 5g

[0106] Preparation Process

[0107] (1) 80g of hydrogenated egg yolk lecithin, 50g of cholesterol, and 20g of poloxamer 188 were dissolved in 600ml of dichloromethane and isopropanol mixed solvent with a volume ratio of 1:1, mixed evenly, and reduced on a rotary thin film evaporator. Remove the mixed solvent under pressure to obtain a phospholipid film;

[0108] (2) Add 300ml of citric acid-sodium citrate buffer solution with a pH value of 5.5, shake and stir to fully hydrate ...

Embodiment 3

[0114] The preparation of embodiment 3 losartan potassium hydrochlorothiazide liposome dispersible tablet

[0115] Prescription (1000 tablets):

[0116] Losartan Potassium 50g

[0117] Hydrochlorothiazide 12.5g

[0118] Hydrogenated egg yolk lecithin 70g

[0119] Cholesterol 40g

[0120] Poloxamer 188 14g

[0121] Starch 70g

[0122] Dextrin 40g

[0123] Crospovidone 10g

[0124] Low-substituted hydroxypropyl cellulose 10g

[0125] Hypromellose 2g

[0126] Talc powder 5g

[0127] Micronized silica gel 2g

[0128] The preparation process is the same as in Example 1, and losartan potassium hydrochlorothiazide liposome dispersible tablets are obtained.

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Abstract

The invention discloses a liposome solid preparation of a losartan potassium hydrochlorothiazide pharmaceutical composition and a preparation method thereof. In the invention, active components of losartan potassium and hydrochlorothiazide and specific combined hydrogenated yolk lecithin, cholesterol and poloxamer 188 are prepared into a liposome which is then mixed with other pharmaceutical accessories to prepare the solid preparation, thereby greatly improving the pharmaceutical stability and bioavailability and having stable and lasting effect, small side effect and obvious curative effect.

Description

technical field [0001] The invention relates to a liposome solid preparation, in particular to a liposome solid preparation of losartan potassium hydrochlorothiazide pharmaceutical composition and a preparation method thereof, and further relates to its application in the treatment of essential hypertension, which belongs to medical technology field. Background technique [0002] Hypertension is the most common disease with the highest incidence rate in the world today. The prevalence of hypertension in my country is about 12%, and there are more than 100 million hypertensive patients, and the number is increasing at a rate of 3 million per year. However, high blood pressure itself is not terrible, and diagnosis and treatment are easy. What is terrible is the various complications of high blood pressure: due to the continuous increase of arterial pressure in patients with high blood pressure, it will cause systemic arteriosclerosis, which will affect the blood supply of tis...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/549A61K9/20A61K9/48A61K9/30A61K47/34A61K47/24A61K47/28A61P9/12A61K31/4178A61K47/10
Inventor 王明
Owner HAINAN MEILAN SMITH KLINE PHARMA
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