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Telmisartan liposome solid preparation

A technology of telmisartan and solid preparations, which is applied in the field of pharmaceutical preparations, can solve problems such as uncontrollable drug release speed and drug release process, unsatisfactory long-term stability of samples, and hidden dangers in clinical use, so as to retain drug efficacy and improve Bioavailability, the effect of reducing toxic and side effects

Inactive Publication Date: 2012-06-27
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The above patents all involve the solid preparation of telmisartan, which is mainly prepared by screening some specific excipients, which has certain advantages, but the long-term stability of the sample is not ideal, which is not conducive to long-term storage; drug release speed and drug release process Uncontrollable, thus bringing hidden dangers to clinical use

Method used

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  • Telmisartan liposome solid preparation
  • Telmisartan liposome solid preparation
  • Telmisartan liposome solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The preparation of embodiment 1 telmisartan liposome sheet

[0046] Prescription (1000 tablets)

[0047]

[0048] Preparation Process

[0049] (1) 40g telmisartan, 88g dipalmitoylphosphatidylcholine, 12g octadecylamine, 32g sodium taurocholate and 48g poloxamer 188 were dissolved in 2000ml volume ratio of 1:3 ethanol and isopropyl In a mixed solvent of ether, a lipid solution is obtained;

[0050] (2) Place the above-mentioned lipid solution in a pear-shaped bottle, and remove the mixed solvent by rotary evaporation in a constant temperature water bath at 50° C. to form a uniform lipid film;

[0051] (3) Prepare 1000 ml of citric acid-sodium citrate buffer solution with a pH value of 5.5, add it to a pear-shaped bottle and shake gently, so that the lipid film is eluted and dispersed in a hydration medium for dissolution, to obtain a liposome suspension;

[0052] (4) After the above-mentioned suspension is poured into a high-speed mixer and stirred evenly, filter w...

Embodiment 2

[0056] The preparation of embodiment 2 Telmisartan liposome sheet

[0057] Prescription (1000 tablets)

[0058]

[0059] Preparation Process

[0060] (1) 80g telmisartan, 320g dipalmitoylphosphatidylcholine, 160g octadecylamine, 400g sodium taurocholate and 240g poloxamer 188 were dissolved in 6000ml volume ratio of 1:3 ethanol and isopropyl In a mixed solvent of ether, a lipid solution is obtained;

[0061] (2) Place the above-mentioned lipid solution in a pear-shaped bottle, and remove the mixed solvent by rotary evaporation in a constant temperature water bath at 40° C. to form a uniform lipid film;

[0062] (3) Prepare 3000ml of potassium dihydrogen phosphate-dipotassium hydrogen phosphate buffer solution with a pH value of 5.5, add it to a pear-shaped bottle and shake gently, so that the lipid film is eluted and dispersed in a hydration medium for dissolution, to obtain a liposome suspension ;

[0063] (4) After the above-mentioned suspension is poured into a high-...

Embodiment 3

[0067] The preparation of embodiment 3 telmisartan liposome capsules

[0068] Prescription (1000 capsules)

[0069]

[0070] Preparation Process

[0071] (1) 40g telmisartan, 120g dipalmitoylphosphatidylcholine, 48g octadecylamine, 120g sodium taurocholate and 84g poloxamer 188 were dissolved in 2000ml volume ratio of 1:3 ethanol and isopropyl In a mixed solvent of ether, a lipid solution is obtained;

[0072] (2) Place the above-mentioned lipid solution in a pear-shaped bottle, and remove the mixed solvent by rotary evaporation in a constant temperature water bath at 45° C. to form a uniform lipid film;

[0073] (3) Prepare 1000 ml of acetic acid-sodium acetate buffer solution with a pH value of 5.5, add it to a pear-shaped bottle and shake gently, so that the lipid film is eluted and dispersed in a hydration medium for dissolving to obtain a liposome suspension;

[0074] (4) After the above-mentioned suspension is poured into a high-speed mixer and stirred evenly, filt...

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Abstract

The invention discloses a telmisartan liposome solid preparation, which is prepared by the following steps: preparing the telmisartan, dipalmitoyl phosphatidyl choline, octadecylamine, Glycocholatesodium, poloxamer 188 into liposome, then adding conventional excipient that is used for preparing the solid preparation in pharmacy, and mixing to obtain the telmisartan liposome solid preparation. Theinvention improves the quality of a preparation product, and reduces toxic side effect.

Description

technical field [0001] The invention relates to a new dosage form of angiotensin II receptor antagonist telmisartan, in particular to a telmisartan liposome solid preparation and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Telmisartan, an angiotensin II receptor antagonist developed for the treatment of hypertension and other medical conditions, as disclosed in EP502314A patent. The chemical name is 4,-[methyl]-[1,1,-biphenyl]-2-carboxylic acid, the molecular formula is C33H30N4O2, the molecular weight is 514.63, and the structural formula is: [0003] [0004] Telmisartan is a specific angiotensin II receptor (AT type I) antagonist that binds to the angiotensin II receptor and the AT I receptor subtype (the known site of action of angiotensin II). Binds with high affinity and is durable without any partial agonist effects. Since telmisartan increases angiotensin II levels, possible receptor overstim...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K9/20A61K9/48A61K31/4184A61K47/34A61P9/12A61K47/10
Inventor 杨明贵
Owner HAINAN MEILAN SMITH KLINE PHARMA
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