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Preparation method of insoluble drug nanosuspension

A technology of insoluble drugs and nano-suspensions, which is applied in the direction of pharmaceutical formulas, medical preparations containing active ingredients, etc., can solve the problems of complex preparation process and low drug concentration, and achieve the The effect of simple process, good reproducibility and high safety

Active Publication Date: 2017-10-24
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The technical problem to be solved by the present invention is to provide a method for preparing an insoluble drug nanosuspension in order to overcome the problems that the drug concentration in the existing insoluble drug nanosuspension is not high and the preparation process is complicated.

Method used

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  • Preparation method of insoluble drug nanosuspension
  • Preparation method of insoluble drug nanosuspension
  • Preparation method of insoluble drug nanosuspension

Examples

Experimental program
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Effect test

Embodiment 1

[0035] The preparation of embodiment 1 paliperidone palmitate nanosuspension:

[0036] (1) Disperse 2.4g of Tween-20 and 1.5g of PEG4000 in 100mL of water for injection to obtain a dispersion medium containing a stabilizer.

[0037] (2) Disperse 23.4 g of paliperidone palmitate in the dispersion medium containing a stabilizer in step (1) to obtain an initial suspension with a drug concentration of 234 mg / mL.

[0038] (3) The primary suspension obtained in step (2) was sheared at a high speed of 22000 rpm for 20 minutes in an ice-water bath to obtain a thick suspension of paliperidone palmitate.

[0039] (4) The suspension obtained in step (3) was subjected to micro-jet high-pressure homogenization, the homogenization pressure was 30,000 psi, and the number of cycles was 20 times to obtain the final product paliperidone palmitate nanosuspension.

[0040] Using a Malvern Mastersizer 3000 laser particle size analyzer to determine paliperidone palmitate API powder D 50 14.8μm (p...

Embodiment 2

[0041] The preparation of embodiment 2 paliperidone palmitate nanosuspension:

[0042] (1) Disperse 2 g of lecithin and 8 g of polyvinylpyrrolidone-K30 (PVP-K30) in 100 mL of water for injection to obtain a dispersion medium containing a stabilizer.

[0043] (2) Disperse 25 g of paliperidone palmitate in the dispersion medium containing a stabilizer in step (1) to obtain an initial suspension with a drug concentration of 250 mg / mL.

[0044] (3) The primary suspension obtained in step (2) was sheared at a high speed of 22000 rpm for 20 minutes in an ice-water bath to obtain a thick suspension of paliperidone palmitate.

[0045] (4) The coarse suspension obtained in step (3) was subjected to high-pressure micro-jet homogenization, the homogenization pressure was 22000 psi, and the number of cycles was 30 times to obtain the final product paliperidone palmitate nanosuspension.

[0046] Using Malvern Mastersizer 3000 laser particle size analyzer to determine the drug particle siz...

Embodiment 3

[0047] The preparation of embodiment 3 curcumin dicaprate nanosuspensions:

[0048] (1) Disperse 3 g of Tween-80 and 0.75 g of sodium dodecylsulfonate in 100 mL of water for injection to obtain a dispersion medium containing a stabilizer.

[0049] (2) Disperse 30 g of curcumin dicaprate in the dispersion medium containing a stabilizer in step (1) to obtain an initial suspension with a drug concentration of 300 mg / mL.

[0050] (3) The primary suspension obtained in step (2) was sheared at 22000 rpm for 30 minutes in an ice-water bath to obtain D 50 Curcumin dicaprate thick suspension of 20μm.

[0051] (4) The coarse suspension obtained in step (3) was subjected to micro-jet high-pressure homogenization, the homogenization pressure was 35000 psi, and the number of cycles was 15 times to obtain the final product curcumin dicaprate nanosuspension.

[0052] Use Malvern Mastersizer 3000 laser particle size analyzer to determine the drug particle size D in curcumin dicaprate nanosu...

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Abstract

The invention discloses a preparation method of insoluble drug nanosuspension. The preparation method comprises the following steps: firstly, dispersing an insoluble drug into an aqueous solution containing a stabilizer to obtain an initial suspension, wherein the mass ratio of the insoluble drug to the stabilizer is 2.5-1 to 8-1; secondly, carrying out high-speed shearing on the initial suspension obtained in the first step to obtain coarse suspension; thirdly, carrying out micro-jet high-pressure homogenizing on the coarse suspension obtained in the second step to obtain the insoluble drug nanosuspension, wherein the drug concentration of the insoluble drug nanosuspension is 150 to 300mg / mL. The preparation method disclosed by the invention has the advantages of no use of an organic solvent, simple preparation technology, good repeatability and good safety; in addition, the drug concentration of the prepared insoluble drug nanosuspension can reach 150 to 300mg / mL, the particle size of the drug is small and the distribution of the drug is uniform.

Description

technical field [0001] The invention relates to a preparation method of insoluble drug nano suspension. Background technique [0002] Prodrugs refer to a class of compounds that have little or no activity in vivo, but release pharmacologically active ingredients through enzymatic or non-enzymatic action in vivo to exert their medicinal effects. For example, paliperidone palmitate is an atypical antipsychotic drug mainly used for the treatment of schizophrenia and bipolar mania. . Therefore, it can be prepared as a storage preparation, which can be slowly hydrolyzed to produce paliperidone after entering the body to exert its medicinal effect, and can maintain a stable blood concentration and reduce toxic and side effects. [0003] Drug nanosuspension is a stable colloidal dispersion system composed only of drugs and a small amount of stabilizers, usually with a particle size of 10 to 1000 nm. This dosage form solves the problem of poor absorption of insoluble drugs in vivo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K47/10A61K47/32A61K47/24A61K47/26A61K31/337A61K31/519A61K31/496A61K31/7052A61K31/436A61K31/5377A61K31/585A61K31/573A61K31/7048A61K31/56A61K31/23A61K31/525
CPCA61K9/10A61K31/23A61K31/337A61K31/436A61K31/496A61K31/519A61K31/525A61K31/5377A61K31/56A61K31/573A61K31/585A61K31/7048A61K31/7052A61K47/24A61K47/26A61K47/32A61K47/34
Inventor 何军杨亚妮顾艳王冠茹吕鹏鞠晓莉张薇薇卞玮倪美萍李晓燕孙国昊
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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