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Controlled-release preparation using live erythrocyte to load betamethasone sodium phosphate and preparation method and application thereof

A technology of sodium metasone phosphate and slow-release preparations, which is applied to medical preparations with no active ingredients, medical preparations containing active ingredients, anti-inflammatory agents, etc., can solve the problems of short half-life, large side effects, side effects, etc., and achieve a solution Side effects, obvious sustained release effect, and the effect of solving the rapid decline of blood drug concentration

Inactive Publication Date: 2019-03-12
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because this type of drug metabolizes quickly in the body, in order to maintain the curative effect, it often needs to be administered in large quantities in a short period of time, which will lead to various side effects.
Like most glucocorticoids, betamethasone sodium phosphate also has the problem of short half-life and large side effects, and the existing various dosage forms such as tablets, injections, drops, external ointments, etc. cannot solve this problem

Method used

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  • Controlled-release preparation using live erythrocyte to load betamethasone sodium phosphate and preparation method and application thereof
  • Controlled-release preparation using live erythrocyte to load betamethasone sodium phosphate and preparation method and application thereof
  • Controlled-release preparation using live erythrocyte to load betamethasone sodium phosphate and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1 Preparation of Packed Red Blood Cells

[0042] Male SD rats with a body weight of about 300 g were taken, and blood was taken from the retro-orbital venous plexus with a capillary tube with a diameter of 0.5 mm, and the blood volume was 0.2-0.3 ml each time. Centrifuge at 3800r / min at 4°C for 5min, discard the supernatant, remove the plasma and white blood cell layer, then add 1ml of pre-cooled PBS to wash 1-2 times until the supernatant is nearly colorless, and the lower layer is packed red blood cells.

Embodiment 2

[0043] The preparation of embodiment 2 drug-loaded erythrocytes

[0044] (1) Prepare a hypotonic betamethasone sodium phosphate medicinal solution with a mass fraction of 0.55% sodium chloride and a concentration of 4 mg / ml betamethasone sodium phosphate, and the solvent is water.

[0045] (2) Take 0.1ml of packed red blood cells prepared in Example 1 and add them to 1ml of hypotonic betamethasone sodium phosphate medicinal solution, mix gently, and place at 4°C for 30min to obtain live red blood cells-betamethasone sodium phosphate medicinal solution .

[0046] (3) Add 0.1ml hypertonic nutrient solution (mass fraction is 5.5% sodium chloride, 5mg / ml sodium pyruvate, 10mg / ml glucose, solvent is water) in 1ml live erythrocyte-betamethasone sodium phosphate medicinal solution, Mix gently and incubate at 37°C for 30min.

[0047] (4) Centrifuge the mixture obtained in step (3) at 4°C, 2000r / min, 5min / time, remove the supernatant and wash with pre-cooled PBS for 3 times under the...

Embodiment 3

[0048] The mensuration of embodiment 3 drug loads

[0049]Collect the supernatant of each step in Example 2, draw 0.2ml, add 1ml methanol and mix, centrifuge at 12000r / min for 30min, take the supernatant and filter it with a 0.22 μm disposable filter membrane, and inject it into a high-performance liquid chromatograph. The content of free betamethasone sodium phosphate in the supernatant was determined.

[0050] Drug loading=the total amount of betamethasone sodium phosphate added-the content of free betamethasone sodium phosphate in the supernatant.

[0051] Wherein the measuring condition of high performance liquid chromatography is:

[0052] Column: Agilent XB-C18 (5μm, 4.6×250nm); detector: AgilentTechnologics UV detector; mobile phase: methanol-0.05mol / l potassium dihydrogen phosphate (1:1); flow rate: 1ml / min; column temperature: 40°C; Detection wavelength: 254nm.

[0053] The final drug loading measurement result was 2.5 mg / ml (ml refers to the volume of packed red...

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Abstract

The invention belongs to the technical field of pharmacy, and particularly relates to a controlled-release preparation using live erythrocyte to load betamethasone sodium phosphate and a preparation method and application thereof. The controlled-release preparation comprises live erythrocyte and betamethasone sodium phosphate, wherein the betamethasone sodium phosphate is enclosed into the live erythrocyte. Compared with free medicines, the controlled-release preparation has the advantages that the obvious controlled-release function is realized, and the problem of short maintaining time of plasma concentration after injection of betamethasone sodium phosphate can be solved; after the controlled-release preparation enters a body, the medicine can be slowly released, and the medicine effectmaintains for about 5 d; by slowly releasing the betamethasone sodium phosphate, the problem of quick reduction of plasma concentration of the traditional injection of betamethasone sodium phosphateis solved, and the problem of side effect due to multiple times of administration within short time of the traditional injection of betamethasone sodium phosphate is solved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a sustained-release preparation of live red blood cells loaded with betamethasone sodium phosphate, a preparation method and application thereof. Background technique [0002] Betamethasone sodium phosphate is a typical glucocorticoid drug, widely used clinically in the treatment of various inflammatory diseases, including eczema, dermatitis, arthritis, allergic diseases, etc. Since the middle of the last century, glucocorticoids have been used in the treatment of various inflammatory diseases. It has good curative effect and quick onset, and has always been regarded as a panacea. Until the 1980s, the frequent clinical side effects such as hypertension, hyperglycemia, osteoporosis, ulcers, etc., gradually restricted the application of glucocorticoids. Scientific research has found that many side effects of glucocorticoids are caused by long-term high-dose a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K9/52A61K47/46A61K31/661A61P17/00A61P29/00A61P19/02A61P37/08
CPCA61K9/5068A61K31/661A61P17/00A61P19/02A61P29/00A61P37/08
Inventor 苏靖邱明丰袁伟恩张秀梅郭朋程徐恩格连雨玫
Owner SHANGHAI JIAO TONG UNIV