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Pharmaceutical composition, sustained release preparation and preparation method thereof

A technology for sustained-release preparations and compositions, applied in the field of sustained-release preparations based on liquid crystal drug delivery systems and their preparation, and in the field of peptide pharmaceutical compositions, can solve the problems that the repeatability and uncontrollability of the production process cannot be guaranteed.

Active Publication Date: 2021-09-10
LIVZON PHARM GRP INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since the complex starts with a high-concentration (5-25 mg / mL) peptide solution, and the metal salt (such as sodium salt) Precipitation of peptides or proteins may occur in the presence of this complex, which is therefore formed in an undefined and uncontrolled manner, and the reproducibility of its production process cannot be guaranteed

Method used

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  • Pharmaceutical composition, sustained release preparation and preparation method thereof
  • Pharmaceutical composition, sustained release preparation and preparation method thereof
  • Pharmaceutical composition, sustained release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Example 1: Preparation of a pharmaceutical composition, which contains a complex (preferably covalently conjugated) of a pharmaceutically acceptable salt of a peptide drug active substance and one or more lipophilic or amphiphilic carrier macromolecular salts ( (hereinafter referred to as "Compound")

[0057] 1.1 Taking Octreotide Acetate (OCT), Leuprolide Acetate (LB), Cetrorelix Acetate (RK) and Liraglutide (LT, its acetate) as examples respectively, the preparation containing them respectively with The pharmaceutical composition of the complex formed by sodium dodecyl sulfate (SDS), palmitic acid (PA) or carboxymethylcellulose (CMC):

[0058] 1.1.1 Preparation of a pharmaceutical composition containing complex 1 (octreotide modified by sodium lauryl sulfate, SDS-OCT)

[0059] Prepare 100 mL of 0.1% sodium lauryl sulfate aqueous solution. Prepare 100 mL of 0.2% octreotide acetate aqueous solution. After fully mixing 100 mL of octreotide acetate solution with 100 mL...

Embodiment 2

[0122] Example 2: Preparation of depot compositions for liquid crystal drug delivery systems

[0123] In this Example 2, the depot composition based on the liquid crystal drug delivery system according to the present invention was exemplarily prepared, and octreotide hydrochloride was used as a model peptide drug, showing the amount of organic solvent in the depot composition, different The types of organic solvents and the effects of different liquid crystal forming agents on the sustained release performance of liquid crystal drug delivery systems.

[0124] 2.1 The impact of the amount of organic solvent DMSO and different organic solvent types (DMSO or EtOH) on the sustained release performance of the liquid crystal drug delivery system in the storage composition:

[0125] 2.1.1 Prepare a peptide sustained-release preparation containing octreotide hydrochloride and SPC / SMO (Span 80) / DMSO depot composition, and its preparation method is as follows:

[0126] According to the...

Embodiment 3

[0163] Example 3: Preparation of peptide sustained-release preparations for injection according to the present invention (hereinafter referred to as "sustained-release preparations")

[0164] 3.1 Taking the pharmaceutical composition obtained according to the preparation method described in Example 1 as an example, combined with liquid crystal drug delivery system depot composition (SPC / SMO / DMSO, SPC / GMO / DMSO, or SPC / GDO / EtOH, Wherein, SMO is Span 80), an exemplary preparation of the peptide sustained-release preparation according to the present invention:

[0165] 3.1.1 Preparation of sustained-release formulation Control group A: containing octreotide acetate (OCT) and SPC / SMO / DMSO depot composition, its preparation method is as follows:

[0166] Add 37.5wt% SPC, 37.5wt% SMO, and 20wt% DMSO to the vial in sequence, and then incubate in a 60°C biochemical incubator to a uniform solution, then add 5% OCT, and mechanically stir with an anchor paddle to make it fully Mix to obt...

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Abstract

The invention relates to a pharmaceutical composition. The pharmaceutical composition provided by the invention at least comprises a compound formed by pharmaceutical salts of peptide pharmaceutical active substances and one or more lipophilic or amphiphilic carrier macromolecular salts; and the composition comprises pure salts formed by the peptide pharmaceutical active substances and counterion carrier macromolecules, and counterions of the peptide pharmaceutical active substance in the pharmaceutical salts, and does not comprise counterions of the counterion carrier macromolecules in the carrier macromolecule salts. A preparation method of the pharmaceutical composition comprises the following steps that deionization treatment is performed on the lipophilic or amphiphilic carrier macromolecular salts, but no deionization treatment is performed on the pharmaceutical salts of the peptide pharmaceutical active substances. The peptide sustained release preparation at least comprises 1) the pharmaceutical composition, and 2) a depot composition based on a liquid crystal drug delivery system. The peptide sustained release preparation has the advantages of small initial burst release and long sustained release time, has improved industrial production adaptability, and further has remarkably improved cumulative release rate.

Description

technical field [0001] The present invention relates to a pharmaceutical composition, a sustained-release preparation and a preparation method thereof, in particular to a peptide (such as peptide, polypeptide, peptidomimetic, etc.) pharmaceutical composition and a related sustained-release preparation based on a liquid crystal drug delivery system and its preparation method. Background technique [0002] With the development of the fields of bioengineering and genetic engineering, a large number of peptide drugs (such as peptides, polypeptides, peptidomimetics, etc.) are continuously introduced into the clinic. In order to ensure rapid onset, strong efficacy, high bioavailability, and reliable pharmacokinetic and pharmacodynamic behavior of peptide drugs in vivo, these peptide drug preparations are mainly administered by parenteral administration (such as injection). However, since the plasma half-life of peptide drugs is usually short, regular repeated injections are requi...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K9/19A61K38/08A61K38/09A61K47/10A61K47/20A61K47/24A61K47/26A61K47/38
CPCA61K9/0019A61K9/0002A61K9/10A61K9/19A61K47/24A61K47/10A61K47/26A61K47/20A61K47/38A61K38/08A61K38/09
Inventor 杨博渊陈斌王燕清徐朋赵泽婷闫艳段盼盼林丽珍
Owner LIVZON PHARM GRP INC
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