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Self-microemulsifying calcium alginate gel pellets for loading drugs and preparation method thereof

A technology of calcium alginate gel pellets and self-microemulsification, which is applied in the direction of pharmaceutical formulations, medical preparations containing no active ingredients, medical preparations containing active ingredients, etc., and can solve the problem of inability to achieve effective drug loading and solid adsorption To avoid problems such as large amount of dosage, to achieve the effect of increasing drug stability, low production cost, and convenient adjustment

Inactive Publication Date: 2014-03-26
CHONGQING MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the amount of solid adsorbent used in this method is relatively large, and the amount of self-microemulsion preparation that can actually be carried is small, and the effective drug loading cannot be achieved in many cases.

Method used

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  • Self-microemulsifying calcium alginate gel pellets for loading drugs and preparation method thereof
  • Self-microemulsifying calcium alginate gel pellets for loading drugs and preparation method thereof
  • Self-microemulsifying calcium alginate gel pellets for loading drugs and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0018] Preparation of puerarin self-microemulsifying gel pellets

[0019] The composition of the self-microemulsifying formulation is as follows:

[0020] Caprylic capric acid glyceride (ODO): 0.175g

[0021] Polyoxyethylene hydrogenated castor oil (Cremophor RH40): 0.550g

[0022] Diethylene glycol monoethyl ether (Transcutol P): 0.275g

[0023] Puerarin: 50.0mg

[0024] Mix oil phase ODO, surfactant Cremophor RH40 and co-surfactant Transcutol P, add puerarin raw material drug, stir at 37°C until the drug is completely dissolved, and obtain a clear and transparent puerarin self-microemulsification preparation; take 0.3g puerarin Add the self-microemulsifying preparation into 3.0% sodium alginate solution, mix well and add 3.2M CaCl dropwise 2 In the solution, after gelation reaction for 1 hour, filter, rinse with distilled water three times, and dry at 50°C to obtain puerarin self-microemulsified calcium alginate gel pellets.

[0025] The prepared puerarin self-microemul...

example 2

[0029] Preparation of baicalein self-microemulsifying gel pellets

[0030] The composition of the self-microemulsifying formulation is as follows:

[0031] Caprylic capric acid glyceride (ODO): 0.2500g

[0032] Polyoxyethylene hydrogenated castor oil (Cremophor RH40): 0.5357g

[0033] Diethylene glycol monoethyl ether (Transcutol P): 0.2143g

[0034] Baicalein: 30.0mg

[0035] Mix oil phase ODO, surfactant Cremophor RH40 and co-surfactant Transcutol P, add baicalein raw material drug, stir at 37°C until the drug is completely dissolved, and obtain a clear and transparent baicalein self-microemulsification preparation; take baicalein self-emulsification Add 0.3g of the preparation to 1ml of 3% sodium alginate solution and mix well; add the mixed solution dropwise to 100ml of CaCl with a concentration of 0.4M 2 In the solution, after 60 minutes of cross-linking reaction, filter and wash with distilled water, and dry at 50°C to obtain baicalein self-microemulsified calcium al...

example 3

[0039] Preparation of naftopidil self-microemulsifying gel pellets

[0040] The composition of the self-microemulsifying formulation is as follows:

[0041] Caprylic capric acid glyceride (ODO): 0.25g

[0042] Polyoxyethylene hydrogenated castor oil (Cremophor RH40): 0.50g

[0043] Diethylene glycol monoethyl ether (Transcutol P): 0.25g

[0044] Naftopidil: 20.0mg

[0045] After mixing the oil phase ODO, surfactant Cremophor RH40 and co-surfactant Transcutol P, add naftopidil crude drug, and stir at 37°C until the drug is completely dissolved to obtain a clear and transparent naftopidil self-microemulsion preparation; Add 0.3g of naftopidil self-emulsifying preparation into 1ml of 3% sodium alginate solution, and mix well; add the mixed solution dropwise to 100ml of CaCl with a concentration of 0.6M 2 In the solution, after 60 minutes of cross-linking reaction, filter and wash with distilled water, and dry at 50° C. to obtain naftopidil self-microemulsified calcium alginat...

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Abstract

The invention discloses self-microemulsifying calcium alginate gel pellets and a preparation method thereof. The preparation method comprises the following steps: uniformly mixing an oil phase, a surfactant and a co-surfactant, adding an indissolvable drug until the indissolvable drug is completely dissolved; uniformly mixing the prepared liquid drug-loading self-microemulsifying preparation and a sodium alginate solution, performing complex crosslinking between the sodium alginate and calcium ions in calcium chloride to prepare the self-microemulsifying calcium alginate gel pellets for loading drugs by an ion gelatinizing method. According to the method, sustained-release and controlled release of a medicine can be controlled by changing the concentration of sodium alginate, the concentration of calcium chloride and other conditions. By virtue of the method, a solid self-microemulsifying preparation can be prepared from the liquid self-microemulsifying preparation, so that various defects of a liquid self-microemulsifying preparation can be effectively avoided. The preparation method is simple in process, low in production cost and easy for industrial production.

Description

technical field [0001] The invention relates to drug-loaded self-microemulsified calcium alginate gel pellets and a preparation method thereof, belonging to the field of medicines. Background technique [0002] Self-microemulsifying drug delivery system (self-microemulsifying drug delivery system, SMEDDS) is an isotropic, homogeneous transparent liquid containing drugs formed by an oil phase, a surfactant, and a co-surfactant. °C) and mild stirring, it will spontaneously emulsify into a microemulsion with a particle size of less than 100nm. Traditional self-microemulsifying preparations usually exist in liquid form, which has the disadvantages of being inconvenient to carry and store, volatile, and low stability. It is usually prepared in the form of soft capsules or liquid-filled hard capsules. But in actual production and use, there are some defects in liquid self-microemulsifying preparations, 1) the cost of soft capsules or liquid-filled hard capsules is high; 2) alcoh...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/44A61K47/36A61K31/352A61K31/495A61K31/12
Inventor 张良珂江兴龙贾运涛黄源锐
Owner CHONGQING MEDICAL UNIVERSITY
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