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Medicinal composition for improving stability of crystal medicines, and preparation method thereof

A technology of composition and stability, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of not being able to guarantee the stability of crystal I, and accelerate the crystal formation of agomelatine Transformation, narrow choice of accessories, etc.

Inactive Publication Date: 2015-06-24
TIANJIN TAIPU PHARMA SCI & TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] (2) Narrow selection of excipients: commonly used excipients such as microcrystalline cellulose and pregelatinized starch are not available, mainly because the above excipients can accelerate the transformation of agomelatine crystal form;
Therefore, the conventional granulation and tableting process cannot guarantee the stability of the crystal I type.

Method used

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  • Medicinal composition for improving stability of crystal medicines, and preparation method thereof
  • Medicinal composition for improving stability of crystal medicines, and preparation method thereof
  • Medicinal composition for improving stability of crystal medicines, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0152] Agomelatine (Crystal Form I 99%) 25g

[0153] water 20ml

[0154] Lactose 102g

[0155] Hydroxypropyl Cellulose 3g

[0156] Polyvinylpyrrolidone k30 3g

[0157] Croscarmellose Sodium 13g

[0158] Magnesium Stearate 1.3g

[0159] Stearic acid 2.6g

[0160] Silica 0.3g

[0161] Process: Sieve the crystalline form I agomelatine according to the above weight for later use; take hydroxypropyl cellulose and polyvinylpyrrolidone k30 and stir to dissolve in water, then add the crystalline form I agomelatine and stir evenly to obtain the protected The crystalline form I agomelatine of the agent is ready for use; then lactose, part (1 / 2) of croscarmellose sodium is added to the wet mixing granulator and mixed, and then the crystalline form I containing the protective agent is added. Agomelatine, granulated for 2 minutes, granulated by a oscillating granulator (833 μm aperture sieve); fluidized bed drying (inlet air temperature 45°C, boiling bed temperature 35°C), granulate...

Embodiment 2

[0163] Tenofovir (more than 90% crystalline form I) 300g

[0164] water 450ml

[0165] Hypromellose 15g

[0166] Polyvinylpyrrolidone k30 15g

[0167] Lactose 120g

[0168] Microcrystalline Cellulose 40g

[0169] 25g pregelatinized starch

[0170] Cross-linked polyvinylpyrrolidone 13g

[0171] Magnesium Stearate 1.3g

[0172] Process: sieve the crystalline type I tenofovir according to the above weight for later use; take hydroxypropyl methylcellulose and polyvinylpyrrolidone k30 in water and stir to dissolve, then add the crystalline type I tenofovir and stir well; obtain the protective agent containing The crystalline type I tenofovir is ready for use; then add lactose, microcrystalline cellulose, pregelatinized starch, and part (1 / 2) cross-linked polyvinylpyrrolidone into the wet mixing granulator and mix well, and then add protective Crystal type I tenofovir, granulated for 2min, granulated by a swing granulator (833μm aperture sieve); fluidized bed drying (inlet ai...

Embodiment 3

[0174] Adefovir dipivoxil (more than 85% crystal type I) 10g

[0175] water 50ml

[0176] Hypromellose 5g

[0177] Mannitol 115g

[0178] Microcrystalline Cellulose 39g

[0179] Sodium carboxymethyl starch 8g

[0180] Magnesium Stearate 3g

[0181]Process: sieve crystal I adefovir dipivoxil according to the above weight for later use; take hydroxypropyl methylcellulose and stir and dissolve it in water, add crystal I type adefovir dipivoxil and stir evenly; obtain crystal I type containing protective agent Adefovir dipivoxil is ready for use; then add mannitol, microcrystalline cellulose, and part (1 / 2) sodium carboxymethyl starch into the wet mixing granulator and mix well, then add crystal I Adefovir containing protective agent Granulate, granulate for 2 minutes, granulate through a oscillating granulator (833μm sieve); fluidized bed drying (inlet air temperature 45°C, boiling bed temperature 35°C), granulate, add the rest of the excipients in proportion and mix we...

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Abstract

The invention discloses a medicinal composition for improving the stability of crystal medicines, and a preparation method thereof. The medicinal composition is composed of a metastable crystal medicine, a protection agent and pharmaceutical adjuvant; and the protection agent is one or a mixture of more of polyvinylpyrrolidone, hydroxypropyl methyl cellulose, hydroxy propyl cellulose and polyethylene glycol. The preparation method mainly comprises the following steps: adding the protection agent into a solvent, stirring for dissolving until a clear state, adding the metastable crystal medicine, and uniformly stirring to obtain a metastable crystal medicine containing the protection agent; and adding the pharmaceutical adjuvant according to a certain proportion, uniformly mixing to prepare particles, drying, and granulating to obtain active component-containing uniform particles. The preparation method can maximally maintain the metastable crystal medicine unchanged in the preparation process, so the stability of the metastable crystal form is greatly improved, and the growth of substances related with the medicines is controlled, thereby the integral stability of the medicines is enhanced.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a pharmaceutical composition for improving the stability of crystal medicine and a preparation method thereof. Background technique [0002] When the substance is crystallized, due to the influence of various factors, the intramolecular or intermolecular bonding mode changes, so the molecules or atoms are arranged differently in the lattice space to form different molecular structures. That is to say, the same substance has two or more spatial arrangements or unit cell parameters, forming polymorphism. In terms of stability, polymorphic forms of drugs can be divided into stable, metastable and unstable forms. The stable type has low entropy value, high melting point, and the best chemical stability, but the dissolution rate and solubility are the smallest, so the bioavailability is also poor. Unstable is the opposite. The metastable type is between the stable...

Claims

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Application Information

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IPC IPC(8): A61K47/38A61K47/34A61K47/32A61K47/04A61K47/10A61K47/08A61K47/06A61K47/14A61K45/00
Inventor 周世旺代奕安适之赵健
Owner TIANJIN TAIPU PHARMA SCI & TECH DEV
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