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Nasal-delivery temperature-sensitive in-situ gel sustained-release preparation comprising ketorolac tromethamine

A technology of ketorolac tromethamine and in-situ gel, which is applied in the directions of non-central analgesics, antipyretics, anti-inflammatory agents, etc., can solve the problems of inconvenient use, insufficient absorption, and frequent administration of patients. , to achieve the effect of less irritation, convenient administration and outstanding sustained release effect

Inactive Publication Date: 2017-01-11
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The ketorolac tromethamine has been used clinically in nearly 20 countries as a novel non-steroidal anti-inflammatory drug, and it plays an increasingly important role in postoperative analgesia; Alcohol is strong, non-addictive, and non-narcotic. Its single-dose efficacy is stronger than that of morphine, pethidine, etc., and its duration of action is longer. Its analgesic effect is stronger than that of aspirin, indomethacin, and Zepson. It is stronger than indomethacin, Cai Pusheng and phenylbutazone; since 1990, it has been approved for marketing in dozens of countries such as the United States and Europe, and is recorded in the United States Pharmacopoeia; it was approved for registration in my country in 1993, and the dosage forms currently on the market are tablets injections, eye drops, nasal drops, etc.; the injection route of said ketorolac tromethamine mainly includes intramuscular injection and intravenous injection, and intramuscular injection of 30mg ketorolac is effective in alleviating postoperative pain, etc. Effective in intramuscular injection of 6-12mg morphine (Rachel Bacona 2012), ketorolac tromethamine can also be administered nasally, and the U.S. FDA has approved ketorolac tromethamine nasal spray (U.S. Syntex company’s ) is used for short-term analgesia, and the analgesic effect produced is equivalent to that of intravenous and intramuscular injections, but the loss in the nasal cavity is fast, the retention is short, the absorption is insufficient, and the administration is frequent, which brings inconvenience to patients.
[0010] In summary, so far there has been no report on the temperature-sensitive bioadhesive in situ gel containing ketorolac tromethamine for nasal administration based on the combination of poloxamer and carrageenan and its preparation method

Method used

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  • Nasal-delivery temperature-sensitive in-situ gel sustained-release preparation comprising ketorolac tromethamine
  • Nasal-delivery temperature-sensitive in-situ gel sustained-release preparation comprising ketorolac tromethamine
  • Nasal-delivery temperature-sensitive in-situ gel sustained-release preparation comprising ketorolac tromethamine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1 Preparation of Blank Gel I

[0042] Weigh an appropriate amount of κ-carrageenan and dissolve it in pure water at 70-80°C, stir to fully dissolve it, and cool to room temperature to obtain a carrageenan stock solution (0.25%, w / w). Add 1 part of Poloxamer 407 to 4 parts (by weight) of 0.25% carrageenan stock solution, leave it to stand at 4 ℃ and stir evenly after the solid components are dissolved to obtain a uniform mixture, which is blank gel I; The gelling temperature is about 22-23°C, and the weight percentage of each component is shown in Table 1:

[0043] Table 1

[0044] Reagent

[0045] .

Embodiment 2

[0046] Example 2 Preparation of Blank Gel II

[0047] The experimental procedure is the same as in the above-mentioned Example 1, but adding an appropriate amount of methyl p-hydroxybenzoate while adding Poloxamer407 to the carrageenan stock solution, the resulting gel is blank gel II; the gelation temperature of this embodiment About 22~23°C, wherein the weight percentage of each component is shown in Table 2:

[0048] Table 2

[0049] Reagent

[0050] .

Embodiment 3

[0051] Example 3 Ketorolac tromethamine bioadhesive thermosensitive in situ gel I

[0052] Experimental procedure is identical with above-mentioned Example 1; In gained blank gel I, add ketorolac trometamol (Ket) in right amount and stir evenly, make its final medicine content be 150 mg ACV / g gel; The The gelling temperature of embodiment is about 34 ℃, and wherein each component weight percent is as shown in table 3:

[0053] table 3

[0054]

[0055] .

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PUM

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Abstract

The invention belongs to the field of medicine preparations and relates to a nasal-delivery temperature-sensitive in-situ gel sustained-release preparation comprising ketorolac tromethamine and a preparation method thereof. The preparation is composed of poloxamer, carrageenan and ketorolac tromethamine in effective dose. The preparation integrates reverse-phase gelatinization property of the poloxamer and the property that the carrageenan can significantly improve erosion of the temperature-sensitive gel, and improves retention effect of the poloxamer gel in nasal cavity and improves absorption of the ketorolac tromethamine. The preparation is improved in bioavailability of the ketorolac tromethamine through nasal delivery and improves patient compliance.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a temperature-sensitive in-situ gel sustained-release preparation for nasal administration containing ketorolac tromethamine and a preparation method thereof. Background technique [0002] The prior art discloses that a nasal drug delivery system (NDDS) refers to a preparation that is used in the nasal cavity and absorbed through the nasal mucosa to exert a therapeutic effect. Studies have shown that nasal administration can not only be used as a local treatment of the nasal cavity, but also can play a role in the treatment and prevention of systemic diseases. According to reports, nasal administration has a long history. As early as in the "Compendium of Materia Medica", it has been recorded that using croton oil paper to twist the nose and burning smoke to smoke the nose can treat apoplexy, phlegm, qi, poisoning and other diseases. Diseases also have a history of decad...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K31/407A61K47/36A61K47/10A61P29/00
Inventor 刘瑜黄志刚李晨曦魏刚陆伟跃
Owner FUDAN UNIV
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