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Slowly released type sirolimus eye-drops preparation and preparation method thereof

A sirolimus ophthalmic, sustained-release technology, applied to non-active ingredient medical preparations, active ingredient-containing medical preparations, pharmaceutical formulations, etc., can solve problems such as poor solubility and stability of sirolimus , to achieve the effect of low incidence of adverse reactions, good intraocular penetration and high yield

Pending Publication Date: 2016-02-10
GUANGDONG WHOLEWIN TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Salvia miltiorrhiza and polycarbophil are used as a mucoadhesive polymer drug delivery system, which can embed water and active molecule sirolimus in it to form a stable aqueous gel-like eye drop, solving the problem of sirolimus in simple Problems of poor solubility and stability in aqueous solution

Method used

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  • Slowly released type sirolimus eye-drops preparation and preparation method thereof
  • Slowly released type sirolimus eye-drops preparation and preparation method thereof
  • Slowly released type sirolimus eye-drops preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-3

[0021] Embodiment 1-3 prepares sustained-release sirolimus eye drops raw material components and consumption

[0022]

[0023] 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 cont...

Embodiment 4-6

[0025] Example 4-6 Preparation of Sustained Release Sirolimus Ophthalmic Gel Raw Material Components and Consumption

[0026]

[0027] According to the technical scheme of the present invention, the types of auxiliary materials that can be used to prepare sirolimus ophthalmic gel are not limited to the types listed in the above table, and the following multiple choices can also be made: wherein, the type selection and dosage of the bacteriostatic agent are the same as in Example 1 ~3. The dosage ratio of the thickener to sirolimus is 0.5-5.0:1.0.

[0028] The preparation method is as follows: dissolve the whole amount of sirolimus with salvia miltiorrhiza, dissolve the thickener with water for injection, disperse and let it cool, and dissolve the pH regulator and bacteriostat with water for injection, and then add the thickener and western medicine that have been dissolved. Rolimus is obtained by adding water for injection to the required volume and aseptically dispensing....

Embodiment 7-9

[0029] Embodiment 7-9 Preparation of sustained-release sirolimus ophthalmic ointment raw material components and dosage

[0030]

[0031] Preparation method: dissolve the whole amount of sirolimus with Salvia miltiorrhiza, add an appropriate amount of sterilized and cooled liquid paraffin, grind it into a fine paste, pass through a 200-mesh sieve, and then gradually add sterile and filtered lanolin and yellow petrolatum mixture, Mix well and serve. All preparation equipment and packaging containers used must be sterilized.

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PUM

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Abstract

The invention relates to a slowly released type sirolimus eye-drops preparation and a preparation method thereof. The slowly released type sirolimus eye-drops preparation is characterized in that the slowly released type preparation is prepared by using sirolimus as a pharmacodynamic raw material, using salviae miltiorrhizae and polycarbophil as a mucosa adhesion polymer drug releasing system, and using auxiliary materials which can be received by eyes locally, and the weight ratio of the using amount of the sirolimus, the salviae miltiorrhizae and the polycarbophil is 1:0.5-5.0: 0.5-2. The related dosage forms comprise eye drops, ophthalmic gel, eye ointment or any pharmaceutic external dosage forms suitable for eyes locally. The salviae miltiorrhizae and the polycarbophil serve as the mucosa adhesion polymer drug releasing system, and the problem that the sirolimus is poor in solubility and stability when used in a pure aqueous solution is solved. Meanwhile, the salviae miltiorrhizae facilitates improvement of immunosuppressive effect and eye tissue penetrability of the sirolimus, and a pharmacology experiment shows that the eye-drops preparation can be used for treating eye immune diseases well.

Description

technical field [0001] The invention belongs to the field of medicines, and more specifically relates to a sirolimus ophthalmic preparation and a preparation method thereof. Background technique [0002] Sirolimus, also known as rapamycin, is a macrolide antibiotic immunosuppressant whose mechanism is that it can block the late reaction (proliferation) of T lymphocyte activation and inhibit cells from The G1 phase enters the S phase, blocking the combination of interleukin-2 (IL-2) and its receptor, so that Tc and Td cells cannot become sensitized T lymphocytes with immune response and exert their immune function. As a third-generation immunosuppressant, sirolimus is a new and powerful immunosuppressant with less toxicity discovered so far, and it is becoming the basic drug for long-term immunosuppressive treatment of organ transplant patients. Clinically, it can be used for the anti-rejection effect of organ transplantation and the treatment of autoimmune diseases such as ...

Claims

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Application Information

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IPC IPC(8): A61K47/46A61K47/32A61K31/436A61K36/537A61P27/02A61P37/06
Inventor 王延东王海英李晓纯吴绮峰曹琛
Owner GUANGDONG WHOLEWIN TECH
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