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Sustained-release drug delivery system

A drug and pharmacy technology, applied in the direction of drug delivery, pharmaceutical formulation, aerosol delivery, etc., can solve the problems of pain and irritation at the injection site, oil gel preparations that have not been seen, preparation application restrictions, etc., to achieve good biophase Compatibility, good drug safety and tolerability, and ease of administration

Active Publication Date: 2021-06-25
NANJING DELOVA BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the oil gel also has the following problems. First, the oil gel is a semi-solid preparation with high viscosity and difficult injection, which is not conducive to clinical administration. Secondly, most of the gel factors may have safety problems and have not been used for injection. Oleogel formulation
[0008] Moreover, the currently used formulations containing non-aqueous solvents are also prone to pain and irritation at the injection site, which limits the application of such formulations

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0102] The dissolving situation investigation of embodiment 1 different types of saturated phospholipids in castor oil and each organic solvent

[0103]Take 1g of castor oil and organic solvent respectively in an EP tube, add 0.1g of saturated phospholipid (about 100mg / g, 10% w / w), ultrasonicate at 50°C, and observe the dissolution. The results are shown in Table 1-1.

[0104] Table 1-1 Dissolution investigation

[0105]

[0106] Among them, EtOH represents absolute ethanol; BB represents benzyl benzoate; BA represents benzyl alcohol; NMP represents N-methylpyrrolidone; DMSO represents dimethyl sulfoxide.

[0107] According to the dissolution investigation, saturated phospholipids (HSPC, DPPC, DMPC, DSPC) have good solubility in alcohol solvents (ethanol, benzyl alcohol, propylene glycol, etc.), while phosphatidylglycerol (DPPG), phosphatidylethanolamine (DPPE) , Phosphatidic acid (DPPA) can not be dissolved in the above solvents.

Embodiment 2

[0108] Embodiment 2 composition ratio research

[0109] (1) Morphological test of the composition at room temperature

[0110] Compositions were prepared according to each ingredient and ingredient ratio shown in Table 2-1 below. Mix the solvent phospholipid, oil and solvent, stir while heating until a transparent and uniform solution is formed, cool to room temperature, and examine the physical form. At the same time, the room temperature morphology of the unsaturated phospholipid composition was used as a comparative study.

[0111] Table 2-1 The room temperature form of the composition under different proportions

[0112]

[0113] In this example, the preparation form of the composition containing 0.5-30% (w / w) saturated phospholipids (HSPC, DPPC, DSPC and DMPC) and 0-50% (w / w) solvent at room temperature is investigated, and the results are shown in Table 2 As shown in -1, the room temperature form of the composition of the present invention is related to the amount ...

Embodiment 3

[0122] (1) Effects of different types of phospholipids on the phase transition of the composition

[0123] According to Table 3-1, pharmaceutical compositions containing saturated phospholipids (composition 16), phospholipid-free (pure castor oil group) and unsaturated phospholipids were prepared respectively. Dissolve meloxicam in N-methylpyrrolidone to prepare a concentrated solution of 50 mg / g, add ropivacaine, soybean lecithin or dipalmitoyl phosphatidylcholine to liquid oil, solvent and meloxime at 50°C In the Kang solution, stir while heating until a transparent and uniform solution is formed, and cool to room temperature. Slowly inject the composition into water with a syringe, and observe the morphological changes of different compositions in water. see results Picture 1-1 .

[0124] Table 3-1 Different Compositions

[0125]

[0126] Above-mentioned experiment has investigated the morphological change in water containing saturated phospholipid (composition 16), ...

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Abstract

The invention relates to a pharmaceutical composition, which comprises liquid oil, at least one compound as shown in the following formula I and at least one pharmaceutical active component. The pharmaceutical composition can be used for a sustained release preparation system, so that the medicine is in a semi-solid or solution form at normal temperature, the semi-solid preparation can be directly used as a medicine storage bank at the administration part, the liquid preparation is subjected to phase change to form the medicine storage bank after the administration part is in contact with body fluid, and meanwhile, the medication safety and tolerance are improved.

Description

technical field [0001] The invention belongs to the field of sustained-release pharmaceutical preparations, and in particular relates to a sustained-release drug delivery system composition and a preparation method thereof. Background technique [0002] Injectable sustained-release preparations are one of the current research hotspots of pharmaceutical preparations, which aim to provide a drug reservoir, which can be used for subcutaneous injection, intramuscular injection, intramuscular injection, local injection and other administration methods. Among them, local injection refers to local administration, such as injection in the spinal cavity, joint cavity, wound, eye, etc., and the drug can exert its effect locally after the drug is slowly released. [0003] Injectable sustained-release preparations have many advantages, for example: the preparation can be directly injected into the desired administration site for slow drug release, reducing systemic toxicity and increasi...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K45/00A61K47/14A61K47/24A61K47/28A61K47/44
CPCA61K9/06A61K45/00A61K47/24A61K47/44A61K47/14A61K47/28A61K9/00A61K9/08
Inventor 王青松武曲邹丽敏
Owner NANJING DELOVA BIOTECH CO LTD
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