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Disulfiram in-situ-forming gel eye drops as well as preparation and application thereof

A technology of disulfiram and eye drops, which is applied in the field of pharmaceutical preparations, can solve problems such as poor patient compliance, inaccurate dosage, and drugs with low bioavailability, so as to improve wettability, prolong corneal residence time, repeat good sex effect

Active Publication Date: 2018-05-01
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Ophthalmic liquid preparations often have problems such as low bioavailability and drug absorption by tissues around the eyes, while ophthalmic gels have problems such as inaccurate dosage and poor patient compliance

Method used

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  • Disulfiram in-situ-forming gel eye drops as well as preparation and application thereof
  • Disulfiram in-situ-forming gel eye drops as well as preparation and application thereof
  • Disulfiram in-situ-forming gel eye drops as well as preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1 Disulfiram solid dispersion (DSF SD ) preparation

[0042] The low solubility of DSF results in slow drug release from the formulation, and the purpose of solid dispersion formulation design is to solve this problem.

[0043] Using DSF release rate as an index to screen DSF SD The recipe and process are as follows.

[0044] Preparation of DSF by melting method SD . According to the weight ratio of disulfiram and solid dispersion matrix Poloxamer P188 is 1:5, put into a round-bottomed flask, placed in a beaker, heated at 50-80° C., heating time of 30 min, and protected from light. Remove the beaker and quickly bathe in ice water at 4°C for 30 min to fully cool the sample. Take out the light yellow solid, grind again or use a pulverizer to pulverize, pass through a 300-mesh sieve to obtain DSF SD powder.

[0045] Preparation of DSF by solvent methodSD . Take an appropriate amount of anhydrous methanol, disulfiram and solid dispersion matrix Poloxamer P18...

Embodiment 2

[0049] Embodiment 2 Disulfiram instant gel eye drops prescription screening

[0050] The aqueous solution of polymer material P407 has temperature thixotropy, which is an ideal material for preparing temperature-sensitive instant gel. The study found that with the increase of the concentration ratio of P407, the gel temperature (GT) decreased, and the GT of the P407 aqueous solution with a concentration of 20% was close to the physiological temperature of the human body, and the GT value could be controlled between 20 °C and 40 °C through prescription adjustment. . This temperature range can ensure that the sample does not undergo phase transition behavior at room temperature. The temperature in the human eye environment is about 34°C, and the gel temperature (SGT) after dilution of the gel tears should not be higher than this temperature to ensure that the human eye environment of the preparation plays a role in temperature thixotropy. For this reason, 20% P407 solution was...

Embodiment 3

[0058] Embodiment 3 The optimal prescription and preparation process of the instant gel eye drops based on the disulfiram solid dispersion prepared by the melt method:

[0059]

[0060]

[0061] crafting process:

[0062] (1) pulverize recipe quantity Disulfiram and solid dispersion matrix P188, mix well;

[0063] (2) the temperature is controlled at 60°C, the pressure is controlled at 11~21KPa, and the mixture of (1) is continuously mixed under reduced pressure for 60min;

[0064] (3) The mixture of (2) is immersed in a 4°C ice-water mixture with a container for quenching;

[0065] (4) pulverize the cooled disulfiram solid dispersion to fine powder, pass through a 300-mesh sieve, for subsequent use;

[0066] (5) Take 20 mL of 0.01% BBS (pH value is 7.4), the content of benzalkonium bromide is 0.01%, and at 4°C, under the speed of 300 rpm, slowly add 4.0 g of poloxamer P407, which is equivalent to a concentration of 20% (w / w); then slowly add the prescribed amount of ...

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Abstract

The invention belongs to the technical field of medicines, relates to disulfiram in-situ-forming gel eye drops as well as preparation and application thereof, in particular to in-situ-forming gel eyedrops which are treated based on a solid dispersion technology and prepared from disulfiram. The disulfiram in-situ-forming gel eye drops are prepared from a main drug, a solid dispersion matrix, an in-situ-forming gel matrix, a bacteriostatic agent, a pH value regulator, a gelation temperature regulator, an osmotic pressure regulator and injection water, wherein the main drug is the disulfiram; the solid dispersion matrix is one or more of HPMC, P407, P188 and PVP; the pH value regulator is borate and has the concentration of 0.001-0.05 percent; and the gel matrix is one or more of the P188 and the P407. The disulfiram in-situ-forming gel eye drops provided by the invention have the efficacy of preventing and treating cataract. According to the preparation, the solid dispersion technologyimproves the solubility and the permeability of indissolvable drugs, and an in-situ-forming gel technology prolongs the corneal retension time of the drugs. The eye drops improve the efficacy of thedisulfiram and have wide development prospect.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a disulfiram instant gel eye drop and its preparation and application. More specifically, the present invention relates to an instant gel eye drop prepared by disulfiram solid dispersion , and in the treatment and prevention of cataracts. Background technique [0002] Disulfiram (DSF), a dimer of diethyldithiocarbamate (DDC), is listed in the American, European, and Japanese Pharmacopoeia as a drug for alcohol withdrawal. Since the disulfide bond in DSF is biotransformed into DDC with pharmacological activity, and it has better stability than DDC, its research has attracted much attention in recent years. It has been documented in the literature that DSF has the potential to treat cancer, prevent and treat cataracts. effect. [0003] The lipid solubility of DSF facilitates its penetration through the corneal epithelial layer, but its water solubility is extrem...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K9/14A61K47/10A61K31/145A61P27/12
CPCA61K9/0048A61K9/06A61K9/146A61K31/145A61K47/10
Inventor 姜同英王思玲聂常璐
Owner SHENYANG PHARMA UNIVERSITY
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