Coatings for controlled release of highly water soluble drugs

A technology for water-soluble drugs and drugs, applied in drug delivery, antibacterial drugs, pharmaceutical formulations, etc., can solve problems such as abrasions, ruptures, and difficulties in designing stable trapping or enveloping coatings

Inactive Publication Date: 2018-11-30
INNOVATIVE SURFACE TECHNOLOGIES LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, small imperfections in the coating, including cracks, abrasions and cuts or even water absorption through the topcoat, can lead to rapid burst release of hydrophilic drugs
Therefore, it is difficult to design a coating that stably traps or encapsulates water-soluble drugs and allows controlled release of water-soluble drugs over a period of days or weeks

Method used

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  • Coatings for controlled release of highly water soluble drugs
  • Coatings for controlled release of highly water soluble drugs
  • Coatings for controlled release of highly water soluble drugs

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0108] Example 1. General Coating Procedure

[0109] A. Primer layer:

[0110] Silicone catheters (0.5 mm outer diameter) were dip-coated with a 30 mg / ml Photo-POMAS solution in isopropanol. Initially, clean the silicone rubber by rubbing it with isopropyl alcohol six times with a lint-free cloth. Then, the catheter was inserted into the coating solution at a rate of 2 cm / sec, left in the solution for 30 seconds, and withdrawn from the coating solution at 0.5 cm / sec. The primer coat was air dried at room temperature for 10 minutes and then UV irradiated with 254 nm light (40 mW / cm2) for one minute.

[0111] B. Silver nitrate layer:

[0112] An aqueous solution of silver nitrate was prepared by dissolving 20 grams of silver nitrate (USP grade, 99.8-100.2%, Sigma Aldrich, St. Louis, MO) in 10 ml of distilled water. This silver nitrate solution was sprayed onto the primer coat with a low volume, low pressure EFD 7856-46SS spray head (Nordson EFD, East Providence, RI) with a V...

example 2

[0115] Example 2. Slow Elution of Silver Nitrate

[0116] An eluting solution was prepared by adding 20 ml of ionic strength modifier (sodium nitrate solution, Orion 940011, ThermoFisher Scientific, Waltham, MA) to 1 liter of distilled water, followed by 0.03 g of sodium bicarbonate. A catheter coated with 89.9 mg of total silver nitrate as described in Example 1 was placed in 150 ml of this elution solution in a capped 500 ml Erlenmeyer flask at 37°C with rotary shaking at 50 rpm. The elution solution was changed daily and the silver content of each elution change was measured using a silver ion selective electrode (Orion IonPlus silver / sulfide electrode, ThermoFisher Scientific, Waltham, MA) and an instrument (Orion Star 214 pH / ISE meter, ThermoFisher Scientific, Waltham, MA). Table 1 shows the resulting silver content in mg / L silver ion.

[0117] Table 1.

[0118]

example 3

[0119] Example 3. Silver nitrate loading

[0120] Primer-coated pieces coated as in Example 1 were weighed in triplicate and then coated with silver nitrate as described in Example 1 with varying nozzle stroke capacities. After drying overnight, catheters were reweighed in triplicate. Table 2 contains weights showing different application of silver nitrate depending on nozzle width. A second coat of silver nitrate can be applied, repeating the conditions in Example 1B. The weight after drying overnight at room temperature is also shown in Table 2.

[0121] Table 2.

[0122]

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PUM

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Abstract

The present invention relates to multilayer coatings comprising a hydrophobic encapsulating layer and allowing controlled release of water soluble drugs. The encapsulating layer encloses the water-soluble or hydrophilic drug with a flexible layer and is in good intimate contact with the water-soluble drug layer. Therefore, the encapsulation layer is compatible with water-soluble drugs and can control drug release. Advantageously, large cuts or cracks in the coating do not result in leakage or bursting of the water-soluble drug; instead, the encapsulation continues to provide modified release of the drug. The invention also includes methods of making the coatings, methods of using the coatings, and articles comprising the coatings.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit under 35 U.S.C. §119(e) of U.S. Patent Application No. 61 / 815910, filed April 25, 2013, and entitled "RELEASE COATINGS FOR HIGHLY WATER SOLUBLE DRUGS," Attorney Docket No. 470.00060160, Its entire contents are hereby incorporated. technical field [0003] The inventive concept generally relates to the release of highly water soluble drugs from multilayer coatings. The invention also relates to methods of making and using these multilayer drug release coatings. Background technique [0004] In general, the field of drug delivery can be described as encompassing methods, formulations, techniques and systems for delivering pharmaceutical compounds in vivo to achieve one or more desired therapeutic effects. Drug delivery techniques may involve systemic administration and / or site-specific delivery of one or more drugs in vivo. Systemic and site-specific approaches typically take into a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00
CPCA61L27/34A61L27/54A61L31/10A61L31/16A61L2300/602A61L2300/608A61L29/06A61L29/085A61L29/16A61L2420/02A61L2420/08A61P31/04C08L83/04A61L29/106A61L2300/104A61L2300/206
Inventor 克莉丝汀·塔顿劳里·拉维帕特里克·伽尔
Owner INNOVATIVE SURFACE TECHNOLOGIES LLC
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