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Medicinal composite tablet of pioglitazone medicine

A technology of pioglitazone hydrochloride tablets and pioglitazone hydrochloride, which is applied in the direction of drug combination, pill delivery, and pharmaceutical formulations, can solve the problems of low bioavailability of pioglitazone hydrochloride, poor water solubility of pioglitazone hydrochloride, and prolonged drug effect period, and achieve effective Conducive to the body's absorption, improve the curative effect and reduce the effect of metabolism

Active Publication Date: 2012-09-12
CHONGQING CONQUER PHARML
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In order to solve the above problems, the present invention aims at the problem of poor water solubility of pioglitazone hydrochloride, and provides a self-emulsifying tablet, which is solved from three aspects of increasing the residence time of the drug in the human body, improving the solubility of the drug, and increasing the total surface area of ​​the drug. The problem of low bioavailability of pioglitazone hydrochloride makes the drug effect cycle longer; the self-emulsifier can increase the absorption of the drug by the liver at the same time, has a certain targeting effect, and reduces the damage of the drug to the kidney; it is more conducive to the drug to play a role

Method used

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  • Medicinal composite tablet of pioglitazone medicine
  • Medicinal composite tablet of pioglitazone medicine
  • Medicinal composite tablet of pioglitazone medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] The research of embodiment 1 pioglitazone hydrochloride tablet release behavior

[0019] Pioglitazone hydrochloride (PGH) is a thiazolidinone hypoglycemic agent that acts on peroxisome proliferator-activated receptor-(PPAR-) and increases the sensitivity of insulin receptors. It is mainly used for the treatment of type 2 diabetes. Its efficacy is correlated with the dosage, and it has the characteristic of once-a-day administration. PGH not only has less adverse reactions, but also does not cause hypoglycemia. Using Tween-80 and phosphatidylcholine as emulsifiers, using hydroxypropyl methylcellulose (HPMC) and carbopol resin (carbopol) as skeleton materials, the self-emulsifying hydrophilic Gel extended-release tablet to enhance bioavailability.

[0020] Precisely weigh the quantitative pioglitazone hydrochloride raw material and add it to the quantitative buffer saline solution, in a 37°C water bath, with electric stirring at a speed of 50r / min, and observe the appea...

Embodiment 2

[0048] The preparation of embodiment 2 pioglitazone hydrochloride tablet

[0049] The mass ratio of pioglitazone hydrochloride, oil phase, emulsifier and emulsifier is 1:2-25:1-10:0.2-5.

[0050] According to the research conclusion described in Example 1, prepare pioglitazone hydrochloride tablet, take by weighing pioglitazone hydrochloride 15g, castor oil 30g, phosphatidylcholine 10g, soil temperature-80 5g, ethanol 3g, be prepared into self-emulsifying drug release part; Take HPMC 2.72g, carbopol 10.88g. Mix the drug and auxiliary materials evenly, use absolute ethanol to make soft material, granulate with a 24-mesh stainless steel sieve, dry at 45°C, and make 8.5mm shallow concave punched tablets with a hardness of 7±0.5kg. Obtain pioglitazone hydrochloride tablet drug group I.

[0051] Using the same method as above, weigh 15 g of pioglitazone hydrochloride, 45 g of castor oil, 30 g of phosphatidylcholine, 30 g of Tween-80, 15 g of ethanol, 8.1 g of HPMC, and 24.3 g of ...

Embodiment 3

[0053] Example 3 Study on the Tissue Distribution of Pioglitazone Hydrochloride Self-emulsifying Drug Release Part in Liver and Kidney

[0054] 1. Test material

[0055] Pioglitazone hydrochloride self-emulsification drug release part (drug group I prepared according to the method of Example 2 of the present invention, was diluted with physiological saline according to the required concentration during the test, and each bottle of 100ml contained 2.5g of pioglitazone hydrochloride), oral gavage of pioglitazone hydrochloride solution (Use 5% ethanol solution to prepare pioglitazone hydrochloride into a 6mg / ml solution). SD rats (male, mass 200±20g).

[0056] 2. Instrument and chromatographic conditions

[0057] Waters2695 HPLC, Waters2996 UV detector; Symmetry shield C18 column (4.6mm×250mm, 5μm); mobile phase acetonitrile: water (35:65); flow rate 0.5ml / min, column temperature 30°C, UV detection The wavelength is 269nm, and the injection volume is 20μl.

[0058] 3. Methods...

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Abstract

The invention discloses a medicinal composite tablet of a pioglitazone medicine. The medicinal composite tablet comprises a self-emulsifying medicine release part and a water-soluble carrier part, wherein the self-emulsifying medicine release part comprises pioglitazone, an oil phase, an emulsifier and a promotion emulsifier in the mass ratio of 1:(2-25):(1-10): (1-5). The self-emulsifying tablet can increase the total area of dissolution of the pioglitazone medicine. Compared with the traditional preparation, the medicine is relatively long in retention time in a human body and more facilitates the absorption of the human body. The self-emulsifying preparation provided by the invention can reduce the drug metabolism from kidneys, and the relapse of bladder cancer is reduced to a certain extent. In addition, phosphatidylcholine in the preparation also has the activity of repairing diabetic complications, such as liver impairment, caused by diseases, such as diabetic hypertension and primary hypertension, so that the treatment effect of the preparation is improved.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, more specifically to a pioglitazone hydrochloride composition tablet. technical background [0002] Diabetes mellitus is a syndrome characterized by persistent hyperglycemia as the basic biochemical feature. The relative or absolute deficiency of insulin and different degrees of insulin resistance caused by various reasons lead to the disorder of carbohydrate, fat and protein metabolism, and the clinical manifestation is diabetes. As the course of the disease prolongs, extensive microvascular and macrovascular lesions may appear, leading to blindness, renal failure, extremity gangrene, myocardial infarction, and cerebrovascular lesions, which seriously threaten the lives of patients. Among them, type 2 diabetes accounts for 90% to 95%, and the pathogenesis of type 2 diabetes is based on insulin resistance and β-cell dysfunction. Studies have found that the so-called "type 2 diabetes" is formed th...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4439A61K47/24A61K31/685A61P3/10
Inventor 梅勇罗磊何远东马贵勇姜艳红杨莉陈丽李小林
Owner CHONGQING CONQUER PHARML
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