Pioglitazone hydrochloride solid dispersoid and medicinal compound thereof as well as preparation methods and applications thereof

A technology of pioglitazone hydrochloride and solid dispersion, applied in the field of biomedicine, can solve the problems of low dissolution rate, low bioavailability, incomplete dissolution and the like, and achieve the effects of rapid dissolution, increased solubility and wettability, and improved dissolution rate

Inactive Publication Date: 2012-03-28
CHENGDU HENGRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Pioglitazone hydrochloride is almost insoluble in water and is a poorly soluble drug. At present, pioglitazone hydrochlori...

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Pioglitazone hydrochloride solid dispersion, which comprises pioglitazone hydrochloride and PEG6000;

[0033] The content of each component is: pioglitazone hydrochloride 8.25g

[0034] PEG6000 57.75g;

[0035] The particle size of the pioglitazone hydrochloride is less than 75 μm.

[0036] The preparation method of pioglitazone hydrochloride solid dispersion, it may further comprise the steps:

[0037] A1. Heat the amount of PEG6000 formulated to 60°C to make it liquid;

[0038] A2, under the condition of constantly stirring the above-mentioned solution, add pioglitazone hydrochloride of formula quantity, stir and disperse for 20 minutes;

[0039] A3. The mixture is quickly poured onto a metal panel with fast heat conduction to form a thin layer of solid, immediately placed in an environment with a temperature below -20°C, quenched for 50 minutes, taken out and crushed through a 100-mesh sieve (pharmacopoeia No. 6 sieve), that is Obtain pioglitazone hydrochloride s...

Embodiment 2

[0054] Pioglitazone hydrochloride solid dispersion, which comprises pioglitazone hydrochloride and PEG6000;

[0055] The content of each component is: pioglitazone hydrochloride 9g

[0056] PEG6000 81g;

[0057] The particle size of the pioglitazone hydrochloride is less than 75 μm.

[0058] The preparation method of pioglitazone hydrochloride solid dispersion, it may further comprise the steps:

[0059] A1. Heat the amount of PEG6000 formulated to 70°C to make it liquid;

[0060] A2, under the condition of constantly stirring the above-mentioned solution, add pioglitazone hydrochloride of formula quantity, stir and disperse for 30 minutes;

[0061] A3. The mixture is quickly poured onto a metal panel with fast heat conduction to form a thin layer of solid, immediately placed in an environment with a temperature below -20°C, quenched for 60 minutes, taken out and crushed through a 100-mesh sieve (pharmacopoeia No. 6 sieve), that is Obtain pioglitazone hydrochloride solid d...

Embodiment 3

[0076] Pioglitazone hydrochloride solid dispersion, which comprises pioglitazone hydrochloride and PEG6000;

[0077] The content of each component is: pioglitazone hydrochloride 33g

[0078] PEG6000 49.5g;

[0079] The particle size of the pioglitazone hydrochloride is less than 75 μm.

[0080] The preparation method of pioglitazone hydrochloride solid dispersion, it may further comprise the steps:

[0081] A1. Heat the PEG6000 in the formula to 80°C to make it liquid;

[0082] A2, under the condition of constantly stirring the above-mentioned solution, add pioglitazone hydrochloride of formula quantity, stir and disperse for 40 minutes;

[0083] A3. The mixture is quickly poured onto a metal panel with fast heat conduction to form a thin layer of solid, immediately placed in an environment with a temperature below -20°C, quenched for 70 minutes, taken out and crushed through a 100-mesh sieve (pharmacopoeia No. 6 sieve), that is Obtain pioglitazone hydrochloride solid disp...

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Abstract

The invention discloses a pioglitazone hydrochloride solid dispersoid and a medicinal compounds thereof as well as preparation methods and applications thereof. The pioglitazone hydrochloride solid dispersoid contains pioglitazone hydrochloride and PEG6000, with the weight ratio of 1:1. 5-9. The preparation method of the pioglitazone hydrochloride solid dispersoid comprises the following steps: A1. heating the PEG6000 to 60-80 DEG C, so as to enable the PEG6000 to be in a liquid state; A2. under the condition of constantly stirring the solution, adding the pioglitazone hydrochloride with proportional amount, stirring and dispersing for 20-40 minutes; and A3. quickly pouring a mixture on a metal panel with fast heat conduction to form a thin solid layer, immediately placing the thin solid layer in an environment with temperature below -20 DEG C, quenching for 50-70 minutes, taking out, smashing and screening with a 100-mesh sieve. The invention has the beneficial effects that the solid dispersoid can greatly improve the dissolution rate of the pioglitazone hydrochloride in a dissolution medium, so as to increase bioavailability. A solid dispersing agent can be further made into the medicinal compounds in forms of tablets and capsules.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a solid dispersion of pioglitazone hydrochloride and a pharmaceutical composition thereof, as well as their preparation method and application. Background technique [0002] Pioglitazone is an insulin sensitizer that can reduce insulin resistance in peripheral tissues and liver, increase insulin-dependent glucose processing, and reduce glycogen output; it can reduce insulin resistance due to hyperglycemia, hyperinsulinemia, and high triacylglycerol; improve It inhibits the action of circulating insulin (i.e., reduces insulin resistance), so it cannot lower blood sugar in the absence of endogenous insulin. [0003] Pioglitazone hydrochloride is almost insoluble in water and belongs to insoluble drug. At present, pioglitazone hydrochloride is mainly administered in the form of oral tablets, which has low dissolution rate, incomplete dissolution and low bioavailability. For dru...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/4439A61K47/34A61K47/38A61P3/10
Inventor 朱德其李进顺
Owner CHENGDU HENGRUI PHARMA
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