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Stable loteprednol etabonate and tobramycin compound composition

A technology of ecaroteprednol tobramycin and ecaroteprednol, which is applied in drug combinations, steroids, and pharmaceutical formulations, and can solve the problems of rapid growth of impurities and poor stability

Inactive Publication Date: 2017-06-30
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] After investigation, it was found that the commercially available Eccaroteprednol Suspension Eye Drops and commercially available Etran, Loteprednol / Tobramycin Suspension Eye Drops Poor stability, impurity grows rapidly

Method used

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  • Stable loteprednol etabonate and tobramycin compound composition
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  • Stable loteprednol etabonate and tobramycin compound composition

Examples

Experimental program
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Effect test

Embodiment 1

[0049] Invention Example 1 Preparation of etabacloteprednol monohydrate

[0050] Invention Example 1-1 Supercritical method for preparing etabac loteprednol monohydrate

[0051] ⑴Configure etaborteprednol solution 1: Dissolve 5g etabaclotepdnol completely in a mixed solution of 300ml acetone and 30ml water at 50°C;

[0052] (2) The etabacloteprednol solution 1 configured in step (1) is connected to the solution pump 2, and the working pressure is controlled to be 15MPa;

[0053] (3) Carbon dioxide feed: the CO in the cylinder 2 Input the supercritical fluid anti-solvent equipment system through the booster pump 8, enter the crystallization kettle 4, control the flow rate at 10ml / min, control the starting temperature at 50°C, and the pressure at 15MPa;

[0054] (4) The etaban loteprednol solution 1 configured in the above steps (1) is rapidly sprayed into the crystallization kettle 4 through the nozzle 3 in the supercritical fluid antisolvent equipment system by the solution ...

Embodiment 1-2

[0059] Invention Example 1-2 Preparation of Eccarteprednol Monohydrate

[0060] Take 5g of carteprednol and add 100ml of ethanol, 20ml of water, and 20ml of acetonitrile in a mixed solution, heat to 50°C, heat filter to remove insoluble matter, cool to 30°C (if crystals are precipitated, take the supernatant ), then add the seed crystals prepared in Example 1-1 of the invention, heat and stir for 30 minutes, a large amount of crystals are precipitated, cooled to 0-5°C, filtered, and dried. The dried crystals are analyzed by TG-DTA, and the weight loss is about 3.7%. , identified as etabacloteprednol monohydrate. The obtained crystal was subjected to X-ray powder diffraction measurement, and the measured characteristic peak positions were 2θ=9.8°, 15.0°, 15.6°, 16.6°, 17.2°, 18.1°, 19.8°, 23.0°, 24.8°, 26.3°.

Embodiment 1-3

[0061] Invention Example 1-3 Preparation of Eccarteprednol Monohydrate

[0062] Take 5g of carteprednol and add 100ml of ethanol, 20ml of water, and 30ml of acetonitrile and heat to 50°C, heat filter to remove insoluble matter, cool to 30°C (if crystals are precipitated, take the supernatant ), then add the seed crystals prepared in Example 1-1 of the invention, heat and stir for 30 minutes, a large amount of crystals are precipitated, cooled to 0-5°C, filtered, and dried. The dried crystals are analyzed by TG-DTA, and the weight loss is about 3.7%. , identified as etabacloteprednol monohydrate. The obtained crystal was subjected to X-ray powder diffraction measurement, and the measured characteristic peak positions were 2θ=9.8°, 15.0°, 15.6°, 16.6°, 17.2°, 18.1°, 19.8°, 23.0°, 24.8°, 26.3°.

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Abstract

The invention relates to a stable loteprednol etabonate and tobramycin compound composition which contains loteprednol etabonate monohydrate as an active ingredient, tobramycin , water, a suspending agent and other auxiliary materials; other auxiliary materials are selected from one or more of a pH regulator, an osmotic pressure regulator, a surfactant and a bacteriostatic agent; the loteprednol etabonate monohydrate is in a form of a crystal; and X-ray powder diffraction have characteristic peaks at diffraction angles of 2 theta equal to 9.8 degrees, 15.0 degrees, 15.6 degrees, 16.6 degrees, 17.2 degrees, 18.1 degrees, 19.8 degrees, 23.0 degrees, 24.8 degrees and 26.3 degrees.

Description

technical field [0001] The invention relates to a compound composition of glucocorticoids and antibiotics, in particular to a compound composition of etabaclotepdnol monohydrate and tobramycin. It belongs to the field of pharmaceutical technology. Background technique [0002] Loteprednol etabonate (CAS: 82034-46-6, Loteprednol etabonate), is a new type of glucocorticoid, developed and produced by American PharmaS, and designed according to the principle of "soft medicine". In 1998, Loteprednol etabonate Prednol Suspension Eye Drops was approved for marketing in the United States, and then ophthalmic ointment and ophthalmic gel were successively launched for the treatment of ocular inflammation, especially steroids for eyelids and bulbar conjunctiva, cornea and anterior part of the eye Medications for sensitive inflammatory and post-operative eye symptoms. In 2005, FDA approved Bausch&Lomb's compound etabac loteprednol / tobramycin suspension eye drops Listed, for the trea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/702A61K31/56A61K9/10A61K47/44A61P27/02C07J3/00
CPCA61K31/56A61K9/0048A61K9/10A61K31/702A61K47/44C07B2200/13C07J3/005A61K2300/00
Inventor 李静王淑丽韩昆颖金玉鑫
Owner TIANJIN JINYAO GRP
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