Granisetron sustained-release microspheres and preparation method thereof

A technology of sustained-release microspheres and hydrophobic segments, which is used in pharmaceutical formulations, medical formulations with inactive ingredients, and medical formulations containing active ingredients, etc., can solve the problems of poor patient compliance and short formulation release time, and achieve The effect of slow release of drug load, reduced drug loss and high encapsulation efficiency

Active Publication Date: 2019-05-07
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] In order to solve the above-mentioned technical problems, the object of the present invention is to provide a granisetron sustained-release microsphere and its preparation method. The preparation method is simple and fast, without sudden release phenomenon, and can effectively solve the problems of short release time of the preparation and poor patient compliance.

Method used

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  • Granisetron sustained-release microspheres and preparation method thereof
  • Granisetron sustained-release microspheres and preparation method thereof
  • Granisetron sustained-release microspheres and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Weigh 5 mg of granisetron and 250 mg of PLGA (molar ratio of lactide to glycolide = 75:25, Mw = 1.2w g / mol), dissolve in 5 mL of dichloromethane, and mix the drug-containing PLGA with stirring The solution was added to 100 mL of the water phase containing 1% (w / v) stabilizer PVA to form an O / W emulsion, and the stirring was continued at room temperature for 6 h to volatilize the dichloromethane, wherein the stirring rate was 300-500 rpm. Stand still, and after the suspended matter sinks to the bottom, remove the supernatant, wash with water three times, collect microspheres by centrifugation, and freeze-dry.

Embodiment 2

[0038] Weigh 5 mg of granisetron and 250 mg of PLGA (molar ratio of lactide to glycolide = 75:25, Mw = 1.2w g / mol), dissolve in 5 mL of dichloromethane, and mix the drug-containing PLGA with stirring The solution was added to 200 mL of water phase containing 1% (w / v) stabilizer PVA to form an O / W emulsion. Stirring was continued at room temperature for 6 h to volatilize dichloromethane, wherein the stirring rate was 300-500 rpm. Stand still, and after the suspended matter sinks to the bottom, remove the supernatant, wash with water three times, collect microspheres by centrifugation, and freeze-dry.

Embodiment 3

[0040] Weigh 5 mg of granisetron and 250 mg of PLGA (molar ratio of lactide to glycolide = 75:25, Mw = 1.2w g / mol), dissolve in 5 mL of dichloromethane, and mix the drug-containing PLGA with stirring The solution was added to 50 mL of water phase containing 1% (w / v) stabilizer PVA to form an O / W emulsion. Stirring was continued at room temperature for 6 h to volatilize dichloromethane, wherein the stirring rate was 300-500 rpm. Stand still, and after the suspended matter sinks to the bottom, remove the supernatant, wash with water three times, collect microspheres by centrifugation, and freeze-dry.

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Abstract

The invention relates to a preparation method of granisetron sustained-release microspheres. The method comprises the following steps: dissolving granisetron and a degradable polymer containing a hydrophobic chain segment in an organic solvent to obtain a drug-containing polymer solution; adding the drug-containing polymer solution to an aqueous phase with stirring to form O/W emulsion, and removing the organic solvent from the emulsion, wherein the aqueous phase contains a stabilizer, and the ratio of the stabilizer to the aqueous phase is 0.1-5% (w/v); and adding the obtained dispersion system into water for solidification under the condition of stirring to obtain the granisetron sustained-release microspheres. The granisetron sustained-release microspheres disclosed by the invention aresuitable in particle size, round in shape, high in encapsulation rate, good in drug loading rate, free from sudden release phenomenon, and capable of effectively solving the problems of short releasetime of a preparation and poor compliance of a patient.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to granisetron sustained-release microspheres and a preparation method thereof. Background technique [0002] Chemotherapy is currently one of the effective means of treating cancer, but it is also accompanied by many toxic and side effects, such as digestive system reactions, bone marrow suppression, and hair loss. Among them, chemotherapy-related nausea and vomiting (CINV) is the most common adverse reaction of patients during chemotherapy. Severe CINV can reduce patients' chemotherapy compliance. In addition, CINV can produce a series of related complications, such as electrolyte disturbance, dehydration and so on. Patients suffer from decreased immunity, malnutrition, mental stress and anxiety, a sharp drop in quality of life, and poor efficacy of chemotherapy. Prevention and mitigation of CINV is one of the important means to ensure the smooth progress of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/439A61K47/34A61P1/08
Inventor 曹青日陈利清阿特夫·穆罕默德·卡塞姆·哎哈迈德
Owner SUZHOU UNIV
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