Nifedipine solid dispersion and preparation method thereof

A technology of dipine solid and nifedipine, which is applied in the directions of non-active ingredient medical preparations, active ingredients-containing medical preparations, pharmaceutical formulas, etc., can solve the problems of low oral bioavailability, decreased solubility, slow drug release, etc. , to achieve the effect of improving bioavailability, bioavailability, and dissolution

Inactive Publication Date: 2019-05-10
GUANGDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This patent meets technical requirements through the synergistic effect of solid dispersion and disintegrant, and uses solid dispersion technology to improve drug solubility and drug absorption effect, but there are still the following defects: 1) A large amount of polyethylene glycol and mannitol are used in the preparation process and other pharmaceutical excipients, its drug loading is on the low side; 2) Since nifedipine has light instability, it must be considered to avoid light in the wet granulation preparation process; 3) Nifedipine after pre-crushing and powdering Dipine still exists in the adjuvant with tiny crystalline state, can gather during tabletting and placing process, causes solubility to decline (A Jiye, Liu Yun, Feng Lin, the influence of solid preparation process on drug crystal form, Chinese Journal of Pharmaceutical Industry, 2000 Year 11 issue), the preparation 30min in 37 ℃ 1% sodium dodecylsulfonate solution dissolution rate is 34.2% ~ 97.87%, but nifedipine is almost insoluble in water, its poor solubility and dissolution rate in water are Main reasons for its low oral bioavailability
This patent has the following defects: 1) To obtain a molecularly dispersed solid dispersion requires the use of a large amount of carrier material, resulting in a low drug loading; 2) This patent does not characterize the state of nif

Method used

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  • Nifedipine solid dispersion and preparation method thereof
  • Nifedipine solid dispersion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0042] The preparation of embodiment 1 nifedipine solid dispersion

[0043] 1, the preparation method of nifedipine solid dispersion, comprises the following steps:

[0044] S1. Weigh 300g of nifedipine and 700g of povidone PVP-VA64700g after passing through a 100-mesh sieve in the dark, and dry at 60°C for 6h;

[0045] S2. Mechanically mixing nifedipine and povidone PVP-VA64 in a closed container for 15 minutes to obtain a physical mixture;

[0046] S3. On the differential-speed asymmetric twin-screw extruder with the preset temperature of each section from the first to the sixth zone of the barrel at 150°C, 160°C, 165°C, 175°C, 175°C, and 165°C, single and double The head screw speed is 120 / 60r / min for extrusion, the extrudate is cooled and pulverized, and passed through an 80-mesh sieve to obtain the nifedipine solid dispersion.

[0047] 2. Results

[0048] figure 1 and figure 2 Infrared spectrum and XRD spectrum of nifedipine (NEP), carrier povidone (PVP-VA64), physi...

Example Embodiment

[0051] Embodiment 2 prepares nifedipine solid dispersion in different proportions

[0052] 1. Preparation method

[0053] Take by weighing respectively the nifedipine and PVP-VA64 of corresponding quality according to the ratio of table 1, then with reference to the preparation method of embodiment 1, nifedipine and PVP-VA64 are carried out mechanical mixing 15min in airtight container, obtain physical mixture; The pre-set temperature of each section from the first to the sixth zone of the barrel is 150°C, 160°C, 165°C, 175°C, 175°C, 165°C on the differential speed asymmetrical twin-screw extruder. Extrude at 120 / 60r / min, cool and pulverize the extrudate, and pass through an 80-mesh sieve to obtain nifedipine solid dispersions prepared with raw materials in different proportions.

[0054] The mass fraction of table 1 nifedipine and PVP-VA64

[0055] name

[0056] 2. Results

[0057] image 3 It is the dissolution curve of different proportions of nifedipine solid...

Example Embodiment

[0058] Embodiment 3 prepares nifedipine solid dispersion with common twin-screw extruder

[0059] 1, except that the differential speed asymmetric twin-screw extruder is replaced by a common twin-screw extruder, with reference to the method of embodiment 1, the preparation of nifedipine solid dispersion comprises the following steps:

[0060] S1. Weigh 300g of nifedipine and 700g of povidone PVP-VA64700g after passing through a 100-mesh sieve in the dark, and dry at 60°C for 6h;

[0061] S2. Mechanically mixing nifedipine and povidone PVP-VA64 in a closed container for 15 minutes to obtain a physical mixture;

[0062] S3. On an ordinary twin-screw extruder with preset temperatures of 150°C, 160°C, 165°C, 175°C, 175°C, and 165°C in each section of the barrel from zone 1 to zone 6, the screw speed is 120r / min extrusion, the extrudate was cooled and pulverized, and passed through an 80-mesh sieve to obtain a solid dispersion of nifedipine (SD-common).

[0063] 2. Results

[0...

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Abstract

The invention discloses a nifedipine solid dispersion and a preparation method thereof. The nifedipine solid dispersion comprises nifedipine and at least one carrier, and the mass fraction of the nifedipine is 10%-50%; the method comprises the steps that after the nifedipine and the carriers are respectively smashed, sieved and mixed proportionally, the mixture is extruded out through a differential asymmetric double-screw extruder, and the nifedipine solid dispersion is prepared. By optimizing the formula design and the preparation technology of extrusion of a hot melted body, the nifedipineis combined with povidone through chemical bonds, after being converted into an amorphous state from an original crystalline state, a large amount of nifedipine can be dissolved in water, the dissolution rate is greatly increased, and the bioavailability of the nifedipine is greatly improved; in addition, the solid dispersion is stable in performance, it is avoided that the solid dispersion goes bad due to long-time placement, and the nifedipine solid dispersion and the preparation method thereof have the technical advantages that the hot melting extrusion technology is simple in preparation,and the consumed time is shorter, and are beneficial for achieving industrialization.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations. More specifically, it relates to a nifedipine solid dispersion and a preparation method thereof. Background technique [0002] Cardiovascular and cerebrovascular diseases are collectively referred to as cardiovascular and cerebrovascular diseases, and generally refer to ischemic or hemorrhagic diseases of the heart, brain and systemic tissues caused by hyperlipidemia, blood viscosity, atherosclerosis, and high blood pressure. Cardiovascular and cerebrovascular diseases are a serious threat to human beings with high morbidity and mortality. Even if the most advanced and perfect treatment methods are applied, more than 50% of cerebrovascular accident survivors cannot fully take care of themselves. The number of patients with cardiovascular and cerebrovascular diseases is large, ranking first among various causes of death. [0003] Nifedipine is a 1,4-dihydropyridine calcium io...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/32A61K47/10A61K47/38A61K31/4422A61P9/12A61P9/10
Inventor 杨传忠徐百平张兴华陈琴喻慧文何亮
Owner GUANGDONG UNIV OF TECH
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