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Injectable temperature-sensitive gel preparation for treating acute pancreatitis

A technology of acute pancreatitis and temperature-sensitive gel, which is applied in the field of medicine and can solve the problems of low blood drug concentration in target organs, low effective concentration in target organs, and large side effects

Inactive Publication Date: 2016-02-24
GENERAL HOSPITAL OF PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The onset of acute pancreatitis is extremely rapid. Although intravenous administration can deliver the drug to the local pancreas through the blood circulation, the onset time of this method of administration is relatively slow. Most of the drugs are distributed in the blood and act on the whole body. The drug concentration is low, resulting in large side effects and low effective concentration in target organs

Method used

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  • Injectable temperature-sensitive gel preparation for treating acute pancreatitis
  • Injectable temperature-sensitive gel preparation for treating acute pancreatitis
  • Injectable temperature-sensitive gel preparation for treating acute pancreatitis

Examples

Experimental program
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Effect test

Embodiment 2

[0046] In certain embodiments of the invention, the formulation comprises about 30% (w / w) of a 21:6 poloxamer 407 / poloxamer 188 copolymer, 0.01% (w / w) of statin. There is Example 2, it is recommended to keep

[0047] The formulations of the present invention may be administered by any route suitable to those skilled in the art. Preferably, the formulation is an injectable formulation, such as a parenteral or subcutaneous administration formulation; more preferably, it is a topical injection formulation on the surface of the pancreas, inside the pancreas.

[0048] In some embodiments, the injectable temperature-sensitive gel formulation of the present invention exists in the form of a gel liquid containing a pharmaceutically active ingredient (containing a drug); or in the form of a lyophilized gel containing a drug; in other embodiments , the formulation of the present invention exists in separate forms of blank (no active pharmaceutical ingredient) gel solution or lyophiliz...

Embodiment 1

[0081]Dissolve the poloxamer 407 / poloxamer 188 copolymers with mass ratios of 16:0, 19:3, 19:5, 21:6, and 21:7 in water, and use the inversion method [YANG.Yetal.Anovelmixedmicellegelwiththermo -sensitive property for the local delivery of docetaxel [J] Journal of Controlled Release 135 (2009) 175-182] to measure the gelation temperature, and the measured gelation temperature is between 30 and 37°C. (See figure 1 )

[0082] Example 2

[0083] Gabexate mesylate is made into an aqueous solution (1), and an appropriate amount of mannitol is added to the solution (1), the pH is adjusted with dilute hydrochloric acid, rehydrated after freeze-drying, dissolved in Poloxamer 407 / Poloxamer 188 and copolymerized 1 mg / ml gabexate mesylate thermosensitive gel (poloxamer 407 / poloxamer 188 mass ratio 21:6) was prepared.

[0084] What is the content of Gabexate mesylate in the gel system? How are the other ingredients added and how are they mixed? How to freeze dry?

Embodiment 3

[0086] The in vitro release test adopts the dynamic dialysis method. Weigh 1 g of the thermosensitive gel prepared in Example 2, place it in a pre-weighed test tube, and preheat it at 37° C. for 10 min to make the solution gel completely. Add 10mL of 37°C pH7.4 phosphate buffer as release medium, at 37°C, rotate at 40r min -1 Oscillate under certain conditions, take out all the release medium at 0, 2h, 4h, 6h, 8h, 12h, and 24h respectively, immediately add an equal amount of blank release medium at the same temperature, and continue to oscillate. After taking out the release medium, weigh the bottle, and the difference between two adjacent weights is the amount of gel erosion at adjacent time points. Calculate the cumulative dissolution amount and draw the time-cumulative dissolution curve. The eluate taken out at each time point was filtered through a 0.45 μm microporous membrane, and the subsequent filtrate was taken as the test solution, and the content of the eluate take...

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Abstract

Critical conditions of acute pancreatitis have high mortality. Trypsinization Theory is one of important pathogeneses of acute pancreatitis. Pancreatin inhibitor drugs, such as gabexate mesylate, ulinastatin and aprotinin, are selectively clinically applied against the mechanism. The routine administration mode of the drugs is intravenous injection, and has certain disadvantages. The invention provides an injectable temperature-sensitive gel preparation for treating acute pancreatitis. The dosage form of the above gel comprises a poloxamer polymer, a polylactide-co-glycolide / polyethylene glycol block copolymer, a polycaprolactam / polyethylene glycol block copolymer, a chitosan / beta-sodium glycerophosphate system, a chitosan / polyvinyl alcohol system or a chitosan-sodium bicarbonate system, or an arbitrary combination thereof. The gel has a reverse gelling characteristic, is a liquid at a low temperature, and converts to a semisolid state at a human body temperature. The invention also provides a preparation method of the injectable temperature-sensitive gel preparation for treating acute pancreatitis.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a temperature-sensitive gel preparation for local injection or other parenteral administration for treating acute pancreatitis. Background technique [0002] Acute pancreatitis is one of the acute abdominal diseases with a high incidence in clinical practice, which is characterized by rapid onset and many complications. The currently recognized pathogenesis of pancreatitis is mainly the "pancreatin self-digestion theory": due to some reasons, trypsinogen is activated, which induces other enzymes to react, causing pancreas and surrounding tissue lesions, and symptoms such as inflammation, hemorrhage, and necrosis. . If the disease is not controlled in time, it may cause multiple organ damage and cause more serious consequences, which is called "intra-abdominal burn". At present, the clinically used drugs for the treatment of pancreatitis are mainly somatostatin and its analogs and...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K47/34A61K47/36A61K45/00A61K38/17A61K38/57A61K31/235A61P1/18
Inventor 罗渝昆唐杰吕发勤梅兴国宋青汪珊高菡静
Owner GENERAL HOSPITAL OF PLA
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