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Oral administration solid preparation containing component for reducing blood fat

A technology of solid preparations and encapsulation agents, applied in pill delivery, metabolic diseases, capsule delivery, etc., which can solve problems such as stability changes, unreachable improvements, and poor stability

Inactive Publication Date: 2008-08-20
姚俊华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The stability of the three samples is very good under the premise of effective packaging at room temperature, but once they enter the human body, the stability has undergone unexpected drastic changes. This experimental reality makes us more aware that the pravastatin sodium according to The preparation methods taught by the prior art solve the problems of poor stability and poor drug efficacy in clinical use, not only can not achieve the purpose of improvement, but even the minimum maintenance of the original toxic and side effects cannot be achieved.
We can also get the following information from it: simply relying on the addition of alkaline pharmaceutical excipients in the preparation, whether it is a diluent, a lubricant or a surfactant, only simply improves the stability of the preparation in vitro, and cannot Fundamentally change the many problems after the disintegration of the drug in the body. Although the literature suggests that we can solve it by means of preparations, so far, no one or literature has reported how to solve it.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] The formulation of pravastatin oral formulation:

[0083] Pravastatin Sodium 5mg

[0084] Anhydrous Sodium Citrate 15mg

[0085] Glyceryl monostearate 5mg

[0086] Starch 30

[0087] Mannitol 75mg

[0088] Microcrystalline Cellulose 175mg

[0089] Sodium carboxymethyl starch 50mg

[0090] Croscarmellose Sodium 40mg

[0091] Magnesium Stearate 4mg

[0092] 5% povidone aqueous solution appropriate amount

[0093] Prepare 1 capsule

[0094] Preparation

[0095] Mix pravastatin sodium and anhydrous sodium citrate evenly, pass through a 100-mesh sieve, and set aside.

[0096] Mix glycerol monostearate with a small amount of water evenly, heat until completely melted; mix starch with a small amount of water evenly, heat until completely gelatinized; mix the two evenly, let cool to between 40°C, add the above Raw and auxiliary materials, after stirring evenly, let cool to 25°C, passed through a 40-mesh sieve, granulated and dried.

[0097] Mix the dried granules w...

Embodiment 2

[0099] The formulation of pravastatin oral formulation:

[0100] Pravastatin Sodium 5mg

[0101] Calcium Sodium Oxalate Tetraacetate 25mg

[0102] Sucrose Fatty Acid Glycerides 15mg

[0103] Starch 35

[0104] Microcrystalline Cellulose 250mg

[0105] Calcium hydrogen phosphate 90mg

[0106] Low-substituted hydroxypropyl cellulose 25mg

[0107] Sodium carboxymethyl starch 50mg

[0108] Talc powder 5mg

[0109] 1% aqueous solution of hydroxypropyl methylcellulose appropriate amount

[0110] Prepares 1 tablet

[0111] Preparation

[0112] Mix pravastatin sodium and calcium sodium oxalate tetraacetate evenly, pass through an 80-mesh sieve, mix and sieve repeatedly until completely mixed and uniform, and set aside.

[0113] After mixing the sucrose fatty acid glyceride with a small amount of water, heat until completely melted; after mixing the starch with a small amount of water, heat until it is completely gelatinized; after mixing the two evenly, let it cool to betw...

Embodiment 3

[0116] The formulation of pravastatin oral formulation:

[0117] Pravastatin Sodium 10mg

[0118] Sodium Hydroxide 1mg

[0119] Starch 15mg

[0120] Macrogol 1000 5mg

[0121] Microcrystalline Cellulose 70mg

[0122] Mannitol 30mg

[0123] Crospovidone 10mg

[0124] Sodium carboxymethyl starch 27mg

[0125] Talc 2mg

[0126] Appropriate amount of water

[0127] Prepares 1 tablet

[0128] Preparation

[0129] Mix pravastatin sodium and sodium hydroxide evenly, pass through a 100-mesh sieve, mix and sieve repeatedly until completely mixed and uniform, and set aside.

[0130] After mixing polyethylene glycol 1000 with a small amount of water, heat until completely melted; after mixing starch with a small amount of water, heat until it is completely gelatinized; Excipients, after stirring evenly, let cool to 25°C, pass through a 40-mesh sieve, granulate and then dry.

[0131] Mix the dried granules with microcrystalline cellulose, mannitol, and sodium carboxymethyl s...

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PUM

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Abstract

The invention relates to an oral drug preparation containing pravastatin, in particular to an oral solid formulation with reinforced effect of pravastatin, which comprises effective amount of pravastatin and pharmaceutical adjuvant, wherein the pharmaceutical adjuvant comprises an enwrap agent; the weight proportion of the pravastatin and the wrapping agent ranges from 1: 0.2 to 1: 10. The oral drug has the advantages of quick effects, reinforced active components and easy administration without uncomfortable feeling.

Description

technical field [0001] The invention relates to an oral solid preparation made of a drug containing a blood lipid-lowering component, which can significantly enhance the formulation stability and clinical blood-lipid-lowering effect of the component. Background technique [0002] Pravastatin sodium is an HMG-CoA reductase inhibitor, a hydrophilic statin hypolipidemic drug. After being absorbed in the body, it is hydrolyzed into a β-hydroxy acid structure, thereby inhibiting the activity of 3-methyl-3-hydroxyglutaryl coenzyme A (HMG-CoA) reductase, and reducing the synthesis of cholesterol in the body. Pravastatin (Pravastatin, Pravachol) was developed by Japan's Sankyo Company and was first launched in Japan in 1989 under the trade name "Mevalotin". As a national basic medical insurance drug and a national essential drug, it is currently widely used clinically. Due to the definite clinical curative effect of pravastatin on blood lipid regulation, although pravastatin is cur...

Claims

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Application Information

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IPC IPC(8): A61K31/222A61K9/20A61K9/48A61P3/06
Inventor 姚俊华
Owner 姚俊华
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