Telmisartan medicinal composition, telmisartan medicinal composition tablets and preparation method for telmisartan medicinal composition tablets

A technology of telmisartan and medicine, which is applied in the field of pharmaceutical preparations and its preparation, can solve the problems affecting the quality of telmisartan sodium salt, telmisartan is difficult to dissolve in water, and low bioavailability, and achieve water solubility Good, less side effects, kidney protection effect

Active Publication Date: 2012-07-04
CHONGQING CONQUER PHARML
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, telmisartan is insoluble in water, the dissolution rate is slow, and the bioavailability is low
At present, the main technical solution to solve telmisartan is to prepare telmisartan into an alkaline salt and add a disintegrant to the preparation to accelerate disintegration, but the existing telmisartan salt-forming technology has severe reaction conditions, mainly Telmisartan is directly reacted with NaOH solution, and side reactions are prone to affect the quality of telmisartan sodium salt. There is no ideal solution at present

Method used

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  • Telmisartan medicinal composition, telmisartan medicinal composition tablets and preparation method for telmisartan medicinal composition tablets
  • Telmisartan medicinal composition, telmisartan medicinal composition tablets and preparation method for telmisartan medicinal composition tablets
  • Telmisartan medicinal composition, telmisartan medicinal composition tablets and preparation method for telmisartan medicinal composition tablets

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Embodiment 1 The preparation method of telmisartan sodium salt

[0018] Utilizing the acidic nature of the carboxyl group in the telmisartan structure, it is refined by alkali-dissolving and acid-precipitating methods. Dissolve telmisartan in ammonia water first, then add activated carbon to decolorize, filter, add hydrochloric acid dropwise to the filtrate to adjust pH, and crystallize to obtain telmisartan fine product. Adopting this refining process route does not use organic solvents chloroform and DMF, and eliminates the distillation operation, the operation is simple and economical, and there is no organic solvent residue.

[0019] Under the condition of lower than 15°C, weigh 0.02 mol of fine telmisartan about 10.3 g, and dissolve the pure telmisartan with 1-5 mol / L ammonia water to obtain telmisartan ammonium salt solution;

[0020] Weigh NaOH 0.022mol, about 0.88g, dissolve NaOH with 40-60% ethanol to obtain NaOH ethanol solution, drop NaOH ethanol solution ...

Embodiment 2

[0022] The investigation of the oil-water partition coefficient of embodiment 2 telmisartan sodium salt

[0023] Accurately weigh 2.5 mg of telmisartan, approximately 0.00000486 moL, dissolve it in n-octanol, and dilute to 10 mL to obtain a 250 μg / mL telmisartan n-octanol solution. Precisely pipette an appropriate amount of the above solution and dilute it with n-octanol to obtain 100 mu g / mL telmisartan n-octanol solution.

[0024] Accurately take by weighing 2.7 mg of telmisartan sodium salt prepared in Example 1, wherein the content of telmisartan sodium salt is about 0.00000486moL, and the operation is as preparing telmisartan n-octanol solution to obtain telmisartan sodium salt n-octanol octanol solution.

[0025] According to the appendix of Chinese Pharmacopoeia 2010 edition, prepare phosphate buffer solution. After measurement, the pH of the solution is 7.29; prepare 0.1mol / L hydrochloric acid solution according to the appendix of Chinese Pharmacopoeia 2010 editio...

Embodiment 3

[0033] Embodiment 3 The preparation method of telmisartan sodium salt tablet

[0034] The telmisartan sodium salt particles were mixed and ground for more than 60 minutes by adding lactose in increments, then mixed with microcrystalline cellulose and sorbitol and ground again for more than 20 minutes, and the grinding temperature was lower than 30°C to obtain a telmisartan lactose mixture;

[0035]Add polacrilin potassium and anhydrous calcium phosphate to the telmisartan sodium salt mixture, put it into a wet granulator and mix for more than 3 minutes, take Tween-80 and dissolve it in 95% ethanol according to the ratio of 2-4ml per kilogram of preparation weight , and then mixed with 0.5% povidone K30 aqueous solution at a ratio of 1:20 as a binder and added to the wet granulator mixture for granulation.

[0036] The granules in the above-mentioned addition are mixed and added with magnesium stearate, the hardness of the tablet machine is controlled within the 4-5 kgf metho...

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Abstract

The invention provides a telmisartan medicinal composition, telmisartan medicinal composition tablets and a preparation method for the telmisartan medicinal composition tablets. The composition consists of the following components: telmisartan sodium salt, sorbitol, polacrilin potassium, anhydrous calcium phosphate, lactose, microcrystalline cellulose and magnesium stearate. The invention provides a preparation method for the telmisartan sodium salt, reaction conditions are mild, few side reactions are performed, and the generated sodium salt has higher water solubility; meanwhile, the sorbitol in the medicine has a diuresis effect, and has a synergistic antihypertensive effect with telmisartan in human bodies, so that the therapeutic effect of the product is strengthened; and after the telmisartan is taken, the urinary albumin excretion rate (UAER) of patients with early diabetic nephropathy is remarkably reduced, so the telmisartan has a kidney protection effect.

Description

technical field [0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to a telmisartan medicine combination, a tablet and a preparation method thereof. technical background [0002] Telmisartan is a non-peptide angiotensin II receptor converting enzyme antagonist. The affinity with AT1 receptor is more than 3000 times that of AT2 receptor. It can selectively block the binding of angiotensin II to AT1 receptors in many tissues (such as vascular smooth muscle and adrenal gland), thus blocking the vasoconstriction and aldosterone secretion of angiotensin II. It is used for mild and moderate essential hypertension. However, telmisartan is insoluble in water, has a slow dissolution rate and low bioavailability. At present, the main technical solution to solve telmisartan is to prepare telmisartan into an alkaline salt and add a disintegrant to the preparation to accelerate disintegration, but the existing telmisartan salt-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4184A61K31/047A61K9/20A61P9/12A61P13/12C07D235/18
Inventor 梅勇罗磊何远东马贵勇姜艳红
Owner CHONGQING CONQUER PHARML
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