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Nano compound eye-drop containing piptide-like medicine and preparing method

A nano-composite and eye drop technology, applied in the directions of medical preparations, drug combinations, drug delivery, etc. containing active ingredients, can solve the problems such as the inability to fully exert the drug effect in the eye, and achieve the improvement of bioavailability and preparation. Simple process and low cost effect

Inactive Publication Date: 2006-08-09
南京凯瑞尔纳米生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Aiming at the practical problem that a class of effective ophthalmic peptide drugs cannot fully exert their drug effects in the eye due to drug delivery, a nanoparticle composed of calcium phosphate and β-carotene as a carrier is provided, which contains therapeutic ingredients. Eye drop compound of peptide medicine and preparation method thereof

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Embodiment 1, preparation of nanoparticles encapsulating β-carotene active substance

[0033] preparation before preparation

[0034] Salt solution: Prepare 0.01-1.0 molar calcium chloride with deionized water.

[0035] Phosphoric acid solution: prepare 0.01-1.0 molar phosphoric acid solution with deionized water.

[0036] The active substance solution of the traditional Chinese medicine: the active substance solution of the traditional Chinese medicine β-carotene is prepared according to the ratio of every 100ml of normal saline + 450μg.

[0037] The pH value is 6.8-7.0, and the 0.01 mole phosphate buffer solution can be purchased externally.

[0038] Major equipment:

[0039] Rotary shaking constant temperature incubator (760 / 760R US).

[0040] making process:

[0041] a) After mixing 0.01~1.0 mole of calcium chloride solution and 0.01~1.0 mole of phosphoric acid solution by 1:1, stir at room temperature for 48 hours, and centrifuge at 4°C at ambient temperature fo...

Embodiment 2

[0043] The preparation of embodiment 2 compound eye drops

[0044] Vancomycin 250mg, calcium phosphate nanoparticles encapsulated with β-carotene 500mg, distilled water 100ml.

[0045] Major equipment:

[0046] Rotary shaking constant temperature incubator (760 / 760R US).

[0047] Cryogenic centrifuge (BECKMAN USA).

[0048] making process

[0049] The mass ratio of vancomycin to calcium phosphate nanoparticles encapsulated with β-carotene is 1:2, take 250 mg of vancomycin, and the calcium phosphate nanoparticles encapsulated with β-carotene obtained in step b in Example 1 Suspend 500 mg of particles in distilled water, add vancomycin to distilled water in which calcium phosphate nanoparticles encapsulated with β-carotene have been suspended, and continue to shake on a shaker at 4°C overnight to obtain encapsulated Chinese medicine β-carotene The active substance of vancomycin and the calcium phosphate nano-particles of vancomycin are prepared into a composite eye drop, and...

Embodiment 3

[0052] Embodiment 3 in vitro antibacterial experiment comparison

[0053] Experimental Materials:

[0054] 1. Medicine: norvancomycin complex solution produced according to the method of embodiment 1,2; norvancomycin.

[0055] 2. Bacteria: Staphylococcus aureus (strain number: 26112) 18-24 hour culture; Bacteria are adjusted to 10 with normal saline 6 / ml.

[0056] 3. Broth agar medium

[0057] experiment procedure:

[0058] The norvancomycin complex solution and norvancomycin were made into 1.2mg / ml and 1mg / ml with physiological saline respectively, and doubled to 0.6mg / ml and 0.5mg / ml; 0.3mg / ml and 0.25mg / ml; 0.15mg / ml and 0.125mg / ml; 0.075mg / ml and 0.063mg / ml; 0.0375mg / ml and 0.032mg / ml, a total of 6 concentrations. Add the above-mentioned two kinds of drugs with different concentrations into the plate respectively, and add the broth agar medium at a ratio of 1:10, and shake well while it is hot. Two plates were made for each concentration, and physiological saline wa...

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Abstract

The invention relates to nm compounding eye drip that contains peptide drug and the manufacture method. It adopts beta-carotene covering calcium phosphate nm particle as carrier to transmit peptide drug. The eye drip includes calcium phosphate nm particle, beta-carotene, peptide drug, distilled water, suitable osmoregulation agent, antiseptic and the pH value is between 6.5 and 7.5. The method includes: making calcium phosphate nm particle, covering beta-carotene over calcium phosphate nm particle, compounding eye drip with peptide drug. The advantages of the invention are that it changes the administrating method of the peptide drug; reducing the risk and side-effect; improving drug chroma in aqueous humor, etc.

Description

technical field [0001] The invention relates to an eye drop containing peptide drugs and a preparation method thereof, in particular to a peptide drug which uses β-carotene encapsulated calcium phosphate nanoparticles as a carrier to deliver peptide drugs and can penetrate the biological barrier of the eye. Drug-like nanocomposite eye drops and a preparation method thereof. Background technique [0002] With the development of biotechnology, more and more attention has been paid to peptide drugs, especially the development of recombinant DNA technology has enabled the large-scale production of such drugs. However, the practical application of peptide drugs is limited. This is because peptides are easily degraded by various proteases and have a short half-life. Frequent intravenous administration is usually used. At the same time, the ability of peptide drugs to pass through biological barriers is weak. This is attributed to its weak diffusion and low partition coefficient. ...

Claims

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Application Information

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IPC IPC(8): A61K38/00A61K9/08A61K47/44A61P27/02
Inventor 王淼河清冯振卿
Owner 南京凯瑞尔纳米生物技术有限公司
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