Indapamide solid dispersion and preparation method thereof

A technology of solid dispersion and indapamide, which can be applied to medical preparations without active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., and can solve the problems of organic solvent residues in indapamide solid dispersions. , to achieve the effects of easy control of operating conditions, improved dissolution performance, and overcoming the problem of organic solvent residues

Active Publication Date: 2022-03-18
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the indapamide solid dispersion prepared by the existing conventional solid dispersion technology has the problem of organic solvent residue, and how to further improve the dissolution performance and bioavailability is also the content that needs to be studied

Method used

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  • Indapamide solid dispersion and preparation method thereof
  • Indapamide solid dispersion and preparation method thereof
  • Indapamide solid dispersion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1: Single factor investigation of the influence of each factor on the recovery rate and drug loading of indapamide solid dispersion or the cumulative dissolution rate within 60min

[0043] Single factor experiment: the effect of solvent type on the recovery rate of indapamide solid dispersion

[0044] Investigate ethanol, acetone, dichloromethane, acetone:dichloromethane=3:2, acetone:dichloromethane=1:1, acetone:dichloromethane=2:3 solvent respectively, to indapamide solid dispersion Effect of recovery and drug loading. Other parameters are that the ratio of drug to carrier is 1:2, the crystallization pressure is 13MPa, the crystallization temperature is 43°C, the solution volume flow rate is 1.0mL / min, the solution mass concentration is 5mg / mL, CO 2 The flow rate is (3.0±0.2) L / min. Since PVP-K30 is poorly soluble in acetone, acetone is firstly excluded as a solvent, and most samples of indapamide in ethanol are formless viscous liquids. When using dichlorom...

Embodiment 2

[0055] Embodiment 2: Orthogonal optimization optimal test factor parameter

[0056] Orthogonal experimental design and results

[0057] With recovery rate as index, design orthogonal experiment to investigate crystallization pressure (A), crystallization temperature (B), solution volume flow rate (C), solution mass solubility (D), table 1 is factor level design table, and table 2 is positive Submit the experimental design and results.

[0058] Table 1 Factor level table

[0059]

[0060] Table 2 Orthogonal design and results

[0061]

[0062] Table 3 ANOVA results

[0063]

[0064]

[0065] f 0.05 (2, 2) = 19.00

[0066] The direct weighting method in the comprehensive scoring method is used for single-index integration. Under the same experimental conditions, the weight sum of the two indicators is 1. The recovery rate is the main indicator, with a weight of 0.6 and a weight of drug loading of 0.4. According to the formula, comprehensive score = recovery rate...

Embodiment 3

[0069] Example 3: Preparation of Indapamide Solid Dispersion Using Optimal Process Conditions

[0070] Application of supercritical fluid enhanced solution dispersion technology to prepare indapamide solid dispersion comprises the following steps:

[0071](1) Preparation of indapamide solution: take the indapamide bulk drug and the PVP-K30 carrier and dissolve them in an organic solvent according to the ratio of the drug to the carrier as 1: 3 to obtain the indapamide-carrier solution, the solution mass The concentration is 3 mg / mL; wherein, the organic solvent is acetone:dichloromethane=1:1.

[0072] (2) CO 2 Pass into the crystallization kettle at 3.0±0.2L / min, adjust the temperature in the crystallization kettle to 50°C, and the pressure to 19MPa;

[0073] (3) Continue to feed CO 2 , maintain the constant temperature and pressure in the crystallization tank, while the indapamide solution prepared in step (1) is sprayed into the crystallization tank from the top of the cr...

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PUM

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Abstract

The invention discloses an indapamide solid dispersion and a preparation method thereof, the indapamide solid dispersion is prepared by dissolving indapamide and a carrier in an organic solvent to obtain an indapamide-carrier mixed solution, and then subjecting the indapamide-carrier mixed solution to a supercritical fluid anti-solvent technology. According to the supercritical fluid anti-solvent technology provided by the invention, the indapamide solid dispersion with obviously improved dissolution performance can be prepared, so that the bioavailability of the indapamide solid dispersion is improved, the patent medicine performance of the indapamide solid dispersion is improved, the ubiquitous problem of organic solvent residue in the traditional technology can be overcome, the operation conditions are easy to control, the components are not easy to inactivate, and the method is suitable for industrial production. And the process is green and efficient, and high safety is achieved.

Description

technical field [0001] The invention relates to a medicine solid dispersion and a preparation method thereof, in particular to an indapamide solid dispersion and a preparation method thereof. Background technique [0002] Indapamide is white or off-white powder, odorless and tasteless. Almost insoluble in water or dilute hydrochloric acid, soluble in ethanol or ethyl acetate, easily soluble in acetone, glacial acetic acid, slightly soluble in chloroform or ether. It is an oral long-acting diuretic and antihypertensive drug with calcium ion antagonism. Because of its effective antihypertensive effect, high clinical safety and few side effects, it has become one of the widely used antihypertensive drugs in clinical practice. When the drug enters the body, it can selectively concentrate in vascular smooth muscle, inhibit the inward flow of calcium ions in cells, directly expand vascular smooth muscle, reduce blood vessel, contraction and blood vessel response to booster substa...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/404A61K47/32A61P9/12
CPCA61K9/146A61K31/404A61P9/12Y02P20/54
Inventor 王志祥贺双吕长龄史潇月王想想王凯叶明哲
Owner CHINA PHARM UNIV
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