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Slow-release sirolimus ophthalmic preparation

A sirolimus eye, sustained-release technology, applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, aerosol delivery, etc., can solve problems such as difficulty and difficulty in sirolimus , to achieve the effects of less toxic and side effects, increased compliance, and good intraocular penetration

Active Publication Date: 2012-09-19
GUANGDONG WHOLEWIN TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, sirolimus is insoluble in water and is easily degraded in aqueous solution, making it difficult to make a sirolimus that is convenient for clinical use

Method used

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  • Slow-release sirolimus ophthalmic preparation
  • Slow-release sirolimus ophthalmic preparation
  • Slow-release sirolimus ophthalmic preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-3

[0020] Example 1-3 Components and dosage of raw materials for preparing sustained-release sirolimus eye drops

[0021]

[0022] According to the technical scheme of the present invention, the adjuvant materials that can be selected for the preparation of sirolimus eye drops are not limited to the species listed in the above table, and there are also multiple options, such as bacteriostatic agents, any bacteriostatic agents known in pharmacy can be used , and its dosage is according to the conventional dosage in pharmacy. For example, ① 0.002% ~ 0.005% thimerosal; ② quaternary ammonium salts (including benzalkonium chloride, benzalkonium bromide), dumiphene, spirityl, etc., the effective concentration is 0.002% ~ 0.01%; ③ alcohols, commonly used 0.3 ~ 0.6% chlorobutanol; ④ Parabens, commonly used 0.03-0.06% ethylparaben; ⑤ Acids, such as 0.01-0.08% tricolic acid. The concentrations of the above substances are all volume-weight percentages, that is, every 100 milliliters co...

Embodiment 4-6

[0025] Example 4-6 Preparation of slow-release sirolimus ophthalmic gel raw material components and dosage

[0026]

[0027] According to the technical scheme of the present invention, the kinds of auxiliary materials that can be selected for preparing sirolimus ophthalmic gel are not limited to the varieties listed in the above table, and the following multiple options can also be selected:

[0028] Wherein, the kind selection and consumption of antibacterial agent are the same as embodiment 1~3.

[0029] The weight ratio of the thickener to sirolimus is 0.5-5.0: 1.0.

[0030] The preparation method is to add 80% ethanol to Bletilla striata, heat and reflux twice for 2 hours each time, combine the alcohol extracts, filter, recover ethanol under reduced pressure, and obtain a clear paste for later use.

[0031] Dissolve the full amount of sirolimus with bletilla striata clear ointment or bletilla striata polysaccharide gel first, then dissolve the thickener with water f...

Embodiment 7-9

[0032] Example 7-9 Preparation of sustained-release sirolimus ophthalmic ointment raw material components and dosage

[0033]

[0034] Preparation method: take Bletilla striata and add 80% ethanol, heat and reflux twice, each time for 2 hours, combine alcohol extracts, filter, recover ethanol under reduced pressure, and obtain clear ointment for later use.

[0035] Dissolve the full amount of sirolimus with bletilla striata clear paste or bletilla striata polysaccharide glue, add an appropriate amount of sterilized and cooled liquid paraffin, grind it into a fine paste, pass it through a 200-mesh sieve, and then gradually add sterile and filtered lanolin, yellow Vaseline mixture, mix well, that is. All preparation equipment and packaging containers used must be sterilized.

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Abstract

The invention relates to an external slow-release sirolimus ophthalmic preparation for ophthalmology, which is prepared by sirolimus as a pharmacodynamic raw material, bletilla striata as a slow release formulation, and appropriate excipients according to a ratio of sirolimus to bletilla striata of 1.0: (0.1 to 10.0). According to the external slow-release sirolimus ophthalmic preparation for the ophthalmology, the bletilla striata is used as a mucoadhesive polymer drug release system, so that the problems that solubility and stability of the sirolimus in a pure aqueous solution are poor are solved; and the convergence, hemostasis, heat clearing and diuresis promoting, detumescence and granulation promoting effects of the bletilla striata are utilized to enhance the immunosuppressive effect and the eye tissue penetration of the sirolimus.

Description

technical field [0001] The present invention relates to medical preparations, in particular to topical eye preparations for treating ophthalmic diseases. Background technique [0002] Sirolimus (SRL), namely rapamycin, is a macrolide antibiotic produced by Streptomyces hygroscopicus, which is effective against various non-T cells, such as B cells, macrophages, It plays a role in the proliferation of cells such as granulocytes and endothelial cells, as well as in cell function. Clinical trials have shown that sirolimus has a significant immunosuppressive effect on organ transplant patients. [0003] In contemporary ophthalmology, moderate to severe intraocular inflammation, especially ophthalmic autoimmune diseases such as uveitis, urgently needs effective immunosuppressants. Studies have found that FK506-binding protein (FKBP) is highly expressed in corneal and retinal tissues, suggesting the potential value of sirolimus for ocular immunosuppression. [0004] For ocular d...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K9/06A61K31/436A61K36/898A61K47/46A61P27/02A61P37/02A61P37/06
Inventor 王延东吴绮峰
Owner GUANGDONG WHOLEWIN TECH
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