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Granisetron hydrochloride microemulsion-based gel and preparation method thereof

A technology of granisetron hydrochloride and granisetron micro, which is applied in the field of medicine, can solve the problems such as the dose affecting the administration, the effect of the actual application of the medicine, and the like, and achieve the effect of good transdermal absorption.

Inactive Publication Date: 2011-01-05
CHONGQING MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Microemulsions can significantly increase the transdermal amount of drugs and are excellent carriers of drugs, but the low viscosity of microemulsions affects their application in external transdermal drug delivery preparations. When microemulsions are used alone, it is difficult to make drugs Residing on the skin surface for a long time will affect the dosage of the drug, which will affect the actual application of the drug

Method used

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  • Granisetron hydrochloride microemulsion-based gel and preparation method thereof
  • Granisetron hydrochloride microemulsion-based gel and preparation method thereof
  • Granisetron hydrochloride microemulsion-based gel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Embodiment 1.GH microemulsion gel, its prescription is composed as follows:

[0044] Microemulsion: GH 2.0g Blank Gel: Carbomer-940 0.6g

[0045] Isopropyl myristate 1.6g Triethanolamine 1.5g

[0046] Polyoxyethylene hydrogenated castor oil 7.5g Glycerin 2.5g

[0047] Tween-80 5.0g Propylene Glycol 10.0g

[0048] Propylene Glycol 2.5g Water to 50.0g

[0049] Add water to 50.0g

[0050] Azone 2.0g

[0051] Triethanolamine to adjust the pH to 7.2

[0052] Preparation:

[0053] (1) Preparation of microemulsion: put polyoxyethylene hydrogenated castor oil, Tween-80 and propylene glycol in a flat-bottomed Erlenmeyer flask according to the prescription ratio, stir under a constant temperature magnetic stirrer at 25°C, and then add isomyristic acid Propyl ester was stirred until the system was fully uniform to obtain solution I; another GH was dissolved in water to obtain solution II. Slowly drop II into I under stirring to obtain a clear ...

Embodiment 2

[0056] Embodiment 2.GH microemulsion gel, its prescription is composed as follows:

[0057] Microemulsion: GH 2.5g Blank Gel: Carbomer-940 0.5g

[0058] Isopropyl myristate 2.4g Triethanolamine 1.2g

[0059] Lecithin 2.0g Glycerin 2.5g

[0060] Tween-80 8.0g Propylene Glycol 10.0g

[0061] Ethanol 2.5g water to 50.0g

[0062] Add water to 50.0g

[0063] Azone 1.0g

[0064] Triethanolamine to adjust pH to 6.8

[0065] Preparation:

[0066] (1) Preparation of microemulsion: Place lecithin, Tween-80 and ethanol in a flat-bottomed Erlenmeyer flask with a stopper according to the prescription ratio, stir under a constant temperature magnetic stirrer at 25°C, and then stir with isopropyl myristate until The system is sufficiently uniform to obtain solution I; another GH is dissolved in water to obtain solution II. Slowly drop II into I under stirring to obtain a clear and transparent microemulsion.

[0067] (2) Preparation of blank gel: Spr...

Embodiment 3

[0069] Embodiment 3.GH microemulsion gel preparation, prescription is composed as follows:

[0070] Microemulsion: GH 2.5g Blank Gel: Carbomer-940 0.6g

[0071] Isopropyl Palmitate 2.0g Triethanolamine 1.2g

[0072] Lecithin 2.2g Glycerin 2.5g

[0073] Tween-80 8.8g Propylene Glycol 10.0g

[0074] Propylene Glycol 3.0g Water to 50.0g

[0075] Add water to 50.0g

[0076] Azone 2.0g

[0077] Triethanolamine to adjust pH to 7.5

[0078] Preparation:

[0079] (1) Preparation of microemulsion: put polyoxyethylene hydrogenated castor oil, Tween-80 and propylene glycol in a flat-bottomed Erlenmeyer flask according to the prescription ratio, stir under a constant temperature magnetic stirrer at 25°C, and then add isomyristic acid Propyl ester was stirred until the system was fully uniform to obtain solution I; another GH was dissolved in water to obtain solution II. Slowly drop II into I under stirring to obtain a clear and transparent microemulsi...

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Abstract

The invention discloses a granisetron hydrochloride microemulsion-based gel and a preparation method thereof. The preparation contains microemulsion and blank gel, wherein the microemulsion consists of granisetron hydrochloride or free alkali thereof, oil phase, emulsifier, co-emulsifier and water phase; and the blank gel consists of gel matrix, neutralizer, humectant and water. The preparation method of the preparation uses the conventional pharmaceutical equipment and comprises the following steps: evenly mixing microemulsion and blank gel in a certain ratio, adding a certain amount of penetration enhancer, and adjusting the pH value to obtain the granisetron hydrochloride microemulsion-based gel. The preparation has simple preparation technology, high production efficiency, low cost, stable quality and easy industrial production. The product of the invention has good effect of transdermal absorption, hardly has any stimulation on the skin and can satisfy the clinical medication requirements basically, thus the product is a novel preparation with good compliance and high therapeutic index.

Description

technical field [0001] The invention relates to granisetron hydrochloride microemulsion gel and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Cancer is one of the important factors that threaten human health and life. As the first choice of cancer treatment, radiotherapy and chemotherapy have been accepted by more and more patients, but radiotherapy and chemotherapy are often accompanied by some side effects, especially gastrointestinal reactions,75 More than 100% of patients with radiotherapy and chemotherapy will experience nausea and vomiting in varying degrees. Severe vomiting will lead to water and electrolyte imbalance, nutritional deficiency, weaken the body's own resistance, and directly affect the curative effect of radiotherapy and chemotherapy and the patient's quality of life. [0003] Clinically, phenothiazines, dopamine antagonists, and antihistamines can control nausea and vomiting, but these drugs h...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K9/00A61K31/439A61K47/44A61K47/42A61K47/36A61K47/34A61K47/32A61P1/08A61K47/10A61K47/26
Inventor 余瑜张雪梅
Owner CHONGQING MEDICAL UNIVERSITY
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