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Ciclosporin solid dispersion and tablet preparation method thereof

A solid dispersion and solid dispersion technology, applied in the direction of cyclic peptide components, medical preparations of non-active ingredients, pill delivery, etc., can solve the problems of rare application of polypeptide drugs, achieve good recrystallization inhibition, and in vivo blood medicine The effect of high concentration and simple preparation process

Pending Publication Date: 2021-07-09
LIAOCHENG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Existing methods for preparing cyclosporine solid dispersions include solvent method, solvent-melt method, spray drying method, freeze drying method, etc., while hot melt extrusion technology is often used for solid dispersion of chemical small molecule drugs with better thermal stability. The preparation of body, the application in polypeptide drugs (such as cyclosporine) is relatively rare

Method used

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  • Ciclosporin solid dispersion and tablet preparation method thereof
  • Ciclosporin solid dispersion and tablet preparation method thereof
  • Ciclosporin solid dispersion and tablet preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0029] Experimental Example 1 prepared 50 mL of each polymer solution with a concentration of 100 μg / mL (the polymer includes HPMCAS-LF, HPMCAS-MF, PVP VA64, PVP K12), quantitative excess CsA was added to the above solution respectively, and as a blank control, each sample was measured in duplicate, and then the solubilization of each polymer to CsA was measured under different pH conditions. Determination conditions: temperature 25°C, rotation speed 150rpm / min, shaker 24h, UV method to determine the concentration of CsA.

[0030] The results are shown in Table 1, PVP K12, and PVP VA64 have strong solubilizing ability, while HPMCAS-LF and HPMCAS-MF have almost no solubilizing effect. At the same time, it can be seen that the dissolution behavior of CsA has no pH dependence.

[0031] Table 1

[0032]

experiment example 2

[0033] Experimental Example 2 Weighed an appropriate amount of CsA raw material and dissolved it in the least amount of organic solvent (3.5 mL of methanol) to form a uniform supersaturated solution to be crystallized to simulate the supersaturated drug system of CsA. Weigh 70mg of each polymer, add 700mL of medium with pH 6.8 to prepare a solution with a concentration of 100μg / mL, duplicate in parallel and make a blank control. The supersaturated drug solution was added to the above polymer solution, and the experiment was carried out at 37° C. and 50 rpm / min by using the paddle method. At different sampling time points, 4 mL samples were taken, filtered through a 0.45 μm filter membrane, and the subsequent filtrate was taken. The absorbance was measured by UV method, and the drug concentration was calculated.

[0034] Such as figure 1 As shown, in the blank control without adding polymer, the drug crystallized rapidly within 5 minutes, and was always in a low concentration ...

Embodiment 1

[0035] Example 1 Mix cyclosporine and PVP K12 uniformly at a ratio of 1:2 to prepare a physical mixture. Set the extrusion temperature at 140°C and the rotation speed at 30rpm. After the temperature rises to the set value and stabilizes, add the physical mixture at a constant speed , to obtain strip-shaped extrudates, cooled, and crushed through an 80-mesh sieve to obtain cyclosporine solid dispersion powder for in vitro dissolution experiments.

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Abstract

The invention discloses a cyclosporin solid dispersion and a tablet preparation method thereof. The solid dispersion is prepared from cyclosporin serving as an active component and a hydrophilic carrier polyvinylpyrrolidone (PVP) K12. The solid dispersion is prepared by a hot melt extrusion technology, and cyclosporin exists in the solid dispersion in an amorphous form. The hydrophilic carrier not only can greatly improve the dissolution rate of cyclosporine, but also has a very good crystallization inhibition effect, and can maintain the supersaturation state of cyclosporine, so that the bioavailability is improved, and meanwhile, adverse reactions are reduced.

Description

technical field [0001] The invention relates to a preparation method, in particular to a cyclosporine solid dispersion and a preparation method for tablets thereof. Background technique [0002] Cyclosporine is a neutral cyclic polypeptide composed of 11 lipophilic amino acids, the English name is CyclosporineA, and the chemical name is [(E)(2S,3R,4R)-3-hydroxy-4-methyl-2-( Methylamino)-6octenoyl]-L-2aminobutyryl-N-methylglycyl-N-methyl-L-leucyl-L-valyl-N-methyl-L-leucyl Aminoyl-L-alanyl-D-alanyl-N-methyl-L-leucyl-N-methyl-L-leucyl-N-methyl-L-valyl, the structural formula is as follows Shown: [0003] [0004] Cyclosporine (CsA) is a potent immunosuppressant that prolongs the survival of allografts such as skin, kidney, liver, heart, pancreas, bone marrow, small intestine, and lung in animals. CsA has been shown to suppress certain humoral and, to a greater extent, cell-mediated immune responses such as allograft rejection, delayed-type hypersensitivity, experimental a...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/32A61K9/20A61K47/38A61K38/13A61P37/06
CPCA61K9/146A61K9/2054A61K9/2027A61K9/2095A61K38/13A61P37/06
Inventor 赵燕娜蒋欣欣韩军刘敏王正平
Owner LIAOCHENG UNIV
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