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Ophthalmic composition containing povidone iodine and cyclodextrin included glucocorticoid

A technology of glucocorticoids and povidone-iodine, which is applied in the direction of medical preparations containing active ingredients, drug combinations, and non-active ingredients of high-molecular compounds, and can solve the problem that the stability cannot reach the technical effect and irritating ocular surface tissue , low stability of the composition, etc., to achieve the effects of interaction inhibition, avoiding side effects, and improving stability

Active Publication Date: 2011-03-23
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Chinese patent application CN200780008873.5 discloses an ophthalmic composition containing povidone-iodine and glucocorticoids, but when the 0.3% concentration of PI solution is compatible with dexamethasone, the obtained composition Its stability is low, but preferably 0.5~2%, particularly preferably adopted 1% povidone-iodine solution and dexamethasone to carry out compatibility
In Chinese patent application CN200780008873.5, it is claimed that a stable composition can be obtained when a 1% concentration of povidone iodine is combined with dexamethasone, and the stability of the composition is higher than that of a lower concentration of povidone iodine and dexamethasone. Dexamethasone compatible composition, and in the composition, the hydroxyl group in the dexamethasone molecule unexpectedly does not react with free iodine, but the application does not disclose what technical means to avoid the dexamethasone molecule from reacting with free iodine The technical means of iodine reaction, through our experiments, found that the stability of the pharmaceutical composition prepared according to the preferred embodiment in this application does not reach the technical effect claimed in its instructions, and in addition, due to the higher content of povidone iodine used in it , also has a considerable potential for irritation or ocular surface tissue damage with continued treatment

Method used

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  • Ophthalmic composition containing povidone iodine and cyclodextrin included glucocorticoid
  • Ophthalmic composition containing povidone iodine and cyclodextrin included glucocorticoid
  • Ophthalmic composition containing povidone iodine and cyclodextrin included glucocorticoid

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Embodiment 1

[0029] The preparation of embodiment 1 hydrocortisone cyclodextrin inclusion aqueous solution

[0030] Dissolve 10g of 3-hydroxypropyl β-cyclodextrin in 75ml of 95% ethanol at room temperature, add 1g of hydrocortisone acetate, stir to dissolve, stir for another 30 minutes, filter through a microporous membrane (220nm), add 40ml of injection Stir with water for 5 minutes, concentrate under reduced pressure, and distill off ethanol to obtain an aqueous solution of hydrocortisone acetate / 3-hydroxypropyl β-cyclodextrin inclusion complex, which is set aside.

Embodiment 2

[0031] The preparation of embodiment 2 dexamethasone cyclodextrin inclusion aqueous solution

[0032] Dissolve 4g of 2-hydroxypropyl-β-cyclodextrin in 20ml of acetone at 40±2°C, add 1g of dexamethasone, stir to dissolve, stir for another 30 minutes, filter through a microporous membrane (220nm), add 6mL of Water for injection, stirred for 5 minutes, concentrated under reduced pressure, added in two times during the concentration process, each time adding 8ml of water for injection, to remove acetone, to obtain dexamethasone / 2-hydroxypropyl-β-cyclodextrin inclusion aqueous solution, set aside .

Embodiment 3

[0033] Embodiment 3 Preparation of Ruimei Songlong cyclodextrin inclusion aqueous solution

[0034] Dissolve 14g of 2-hydroxypropyl-β-cyclodextrin in 20ml of absolute ethanol at room temperature, add 1g of Remisolone, stir to dissolve, stir for another 30 minutes, filter through a microporous membrane (220nm), and stir for 5 minutes , concentrated under reduced pressure, during the concentration process, 3.5ml water for injection was added three times, and the ethanol was distilled off to obtain an aqueous solution of remisolone / -hydroxyethyl-β-cyclodextrin inclusion complex, which was set aside.

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Abstract

The invention discloses an ophthalmic composition containing povidone iodine and cyclodextrin included glucocorticoid. The composition consists of the povidone iodine and the glucocorticoid which serve as active ingredients and one or more auxiliary materials suitable for eye administration. The composition is characterized in that: the glucocorticoid is included by beta-cyclodextrin and derivatives thereof, and the povidone iodine content of the ophthalmic medicinal composition is 0.01 to 1 percent.

Description

Technical field: [0001] The invention relates to an ophthalmic pharmaceutical composition with povidone iodine and glucocorticoid as active ingredients. Background technique: [0002] Povidone-iodine (PVP-I, referred to as PI) is a compound of polyvinylpyrrolidone (PVP) and iodine, also known as iodophor, containing 9 to 12% of available iodine. Viruses, bacteria, fungi and mold spores all have a strong killing effect. It has little irritation to skin, low toxicity and long-lasting effect. Safe and easy to use. It is basically non-irritating to tissues, and is used for disinfection of skin and mucous membranes, such as cleaning before surgery, disinfection of surgical sites and wounds. Its bactericidal principle is mainly to play a bactericidal effect by releasing free iodine hydrate. Povidone is hydrophilic and is the carrier for transporting iodine to the cell membrane. Combining, denaturing, and simultaneously oxidizing the active groups of bacterial protoplasmic prot...

Claims

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Application Information

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IPC IPC(8): A61K31/79A61K31/56A61K47/40A61P27/02A61K31/573A61K31/57
Inventor 孙亮陈松赵琳
Owner TIANJIN JINYAO GRP
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