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Small molecule drug sustained-release delivery system

A drug and sustained-release carrier technology, which is applied in the field of small-molecule drug sustained-release drug delivery system, can solve the problems of unsatisfactory incision drug administration, difficult-to-degrade sustained-release carrier, complicated preparation process, etc., and achieve good drug safety and tolerance Sexuality, improved sustained-release effect, good patient tolerance

Active Publication Date: 2022-01-18
NANJING DELOVA BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The sustained-release systems that have been approved or are currently under research have problems such as complex preparation process, difficult degradation of sustained-release carriers, and safety caused by burst release.
In addition, the lipid-based sustained-release systems under research or on the market all have low viscosity and cannot meet the problem of incisional drug delivery.

Method used

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  • Small molecule drug sustained-release delivery system
  • Small molecule drug sustained-release delivery system
  • Small molecule drug sustained-release delivery system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] Different types of alcohol on the viscosity of the composition

[0083] The composition is formulated according to Table 1-1, in a heated state in the SPC was dissolved BA, were added to glycerol, propylene glycol, PEG200, PEG400, PEG600, heated and stirred until a homogeneous solution was allowed to stand at room temperature to investigate different types of alcohol on the viscosity of the system Influence. Using a rotor No. 14, 50rpm rotational speed detecting viscosity of the composition, the results shown in Table 1-2.

[0084] Table 1-1 compositions containing the active ingredient

[0085]

[0086] Table 1-2 in solution viscosity of the composition and

[0087]

[0088] The inventors have surprisingly found that the addition of glycerol phospholipid solution, can significantly increase the viscosity of the composition, propylene glycol and polyethylene glycol of different molecular weight and viscosity of the composition not significantly increase.

Embodiment 2

[0090] Glycerol / organic solvent / slow release carrier ratio of viscosity of the composition

[0091] Table 2-1 and 2-2 was formulated compositions, in a heated state and the SPC was dissolved in the proportion of different types of solvents, glycerin, heated and stirred until a homogeneous solution was allowed to stand at room temperature, the study group of the compound materials the viscosity ratio Impact.

[0092] TABLE 2-1 Viscosity detection result of the composition containing different solvents

[0093]

[0094]

[0095] TABLE 2-2 Viscosity detection result of the composition containing different solvents

[0096]

Embodiment 3

[0098] Study of composition homogeneity

[0099] Different viscosities taken in Tables 2-1 and 2-2 in compositions PE tube, centrifuged at 9000rpm 15min, the solution state was observed after centrifugation. The results are shown in Table 3-1 and Table 3-2.

[0100] Table 3-1 different solvents (benzyl alcohol) composition uniformity of results

[0101]

[0102] Table 3-2 different solvents (ethanol) results uniformity of composition

[0103]

[0104] From the results, the samples were centrifuged at high speed in the state of different viscosities no delamination, was homogeneous state, indicating good physical stability.

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PUM

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Abstract

The invention relates to a pharmaceutical composition. The pharmaceutical composition comprises a pharmaceutically active ingredient, glycerol, a sustained release carrier and a pharmaceutically acceptable solvent, wherein the pharmaceutical composition is small in irritation, has good slow release performance, medication safety and tolerance, is a high-viscosity liquid at normal temperature, and is particularly beneficial to perfusion therapy.

Description

Technical field [0001] The present invention belongs to the field of pharmaceutical preparations, particularly relates to a small molecule drug release drug delivery systems. Background technique [0002] Injectable sustained-release formulation is one of the focus of the present pharmaceutical formulation, intended to provide a drug depot, it can be used for administration subcutaneous injection, intramuscular injection, intramuscular injection, local injection and the like. Wherein, in the local injection means topical administration, spinal cavities, joint cavity, wounds, and other parts of the intraocular injections, slow release after drug administration topically play a role in. [0003] Injectable sustained-release formulation has many advantages, for example: the formulation may be directly injected into the desired site of administration, slow release, reduced systemic toxicity, increased therapeutic effect; secondly, the formulation may also reduce the frequency of admi...

Claims

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Application Information

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IPC IPC(8): A61K47/10A61K47/24A61K45/00A61K9/00A61K9/08A61P23/00A61P25/00A61P29/00
CPCA61K9/0019A61K47/10A61K47/24A61K45/00A61K9/08A61K9/0014A61K9/0031A61P29/00A61P25/00A61P23/00
Inventor 李玲武曲储仙王娇王青松
Owner NANJING DELOVA BIOTECH CO LTD
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