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New gambogic acid osmotic pump type controlled release preparation and preparation method thereof

A new technology of gambogic acid and controlled-release preparations, which is applied in pharmaceutical formulations, medical preparations containing active ingredients, drug delivery, etc., can solve the problem that it is difficult to prepare single-chamber primary osmotic pump type controlled-release preparations for poorly soluble drugs, and it is impossible to achieve Industrialized production, industrialized production problems, etc., to achieve stable and effective blood drug concentration, prolong blood drug concentration time, and reduce the number of times of medication

Active Publication Date: 2017-09-26
汪电雷
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is not only difficult to prepare poorly soluble drugs into single-chamber primary osmotic pump controlled release preparations, but also its industrial production has become a major problem in this field
In recent years, although there are few reports in the literature on the preparation of some insoluble drugs into single-chamber primary osmotic pump-type controlled-release tablets, such single-chamber primary osmotic pump-type controlled-release tablets still have problems such as low drug release efficiency, incomplete release, and inability to release drugs. Defects such as realizing industrialized production
So far, there is no literature report on the preparation of insoluble drug neogambogic acid into a single-chamber primary osmotic pump type controlled release preparation.

Method used

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  • New gambogic acid osmotic pump type controlled release preparation and preparation method thereof
  • New gambogic acid osmotic pump type controlled release preparation and preparation method thereof
  • New gambogic acid osmotic pump type controlled release preparation and preparation method thereof

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preparation example Construction

[0055] Experiment 1 Preparation of new gambogic acid osmotic pump

[0056] Preparation process and influencing factors of new gambogic acid osmotic pump tablets

[0057] 1.1 Preparation process

[0058] Tablet core: pass new gambogic acid, PEO-N10, lactose, sodium chloride, L-arginine through 80-mesh sieve, weigh according to the prescription amount, mix by equal addition method, add 95% ethanol solution to make soft material, Granulate with a 20-mesh sieve, dry at 40°C for 6 hours, add an appropriate amount of magnesium stearate and mix well.

[0059] Preparation of coating solution: Weigh the prescribed amount of cellulose acetate and dissolve it in acetone to prepare a certain concentration of cellulose acetate acetone solution, add a certain amount of dibutyl phthalate DBP and PEG4000, and place on a magnetic stirrer Stir without heating until the solution is completely dissolved.

[0060] Tablet compression and coating: install the upper and lower punches, adjust the t...

Embodiment 1

[0199] Tablet core prescription (based on about 200mg per tablet, based on the weight of the controlled-release semipermeable coating film accounting for 2% of the weight of the tablet core, the weight of the tablet core is 196mg, and the weight of the film is 4mg):

[0200] Neogambogic acid 3.92mg; Sodium chloride 49mg; PEO-N10 19.6mg; L-arginine 29mg; Sodium lauryl sulfate 20mg; Lactose 30.48mg; Microcrystalline cellulose 24mg; Magnesium stearate 20mg;

[0201] Prescription of semipermeable film coating solution: 15 mg of cellulose acetate; 10 mg of diethyl phthalate; 30 mg of PEG4000.

[0202] Preparation process: pass the above-mentioned neogambogic acid and auxiliary materials (other auxiliary materials except magnesium stearate) according to the prescription amount through a 100-mesh sieve, mix well, use 95% ethanol solution to make soft materials, and pass through a 24-mesh sieve to granulate , dried at 40°C, passed through a 24-mesh sieve for granulation, added the pre...

Embodiment 2

[0204] Tablet core prescription (based on about 200 mg per tablet, based on the weight of the controlled-release semipermeable coating film accounting for 3% of the weight of the tablet core, the weight of the tablet core is 194 mg, and the weight of the film is 6 mg):

[0205] Neogambogic acid 19.4mg; Polyoxyethylene 67.9mg; PEO-N10 48.5mg; Sodium bicarbonate 20mg; Sodium lauryl sulfate 28.5mg; Lactose 10.1mg; Compressible starch 14mg; Hydrogenated vegetable oil 5mg;

[0206] Prescription of semipermeable film coating solution: acrylic resin 10mg; propylene glycol 25mg; PEG1500 75mg.

[0207] Preparation process: pass new gambogic acid and auxiliary materials (other auxiliary materials except hydrogenated vegetable oil) through a 100-mesh sieve, mix well, use 95% ethanol solution to make soft materials, pass through a 24-mesh sieve to granulate, dry at 35 ° C, and pass through Sieve with a 24-mesh sieve, add the prescribed amount of hydrogenated vegetable oil, mix evenly, pre...

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Abstract

The invention discloses a new gambogic acid osmotic pump type controlled release preparation, the controlled release preparation comprises a new gambogic acid osmotic pump type controlled release tablet, which is a single-chamber primary osmotic pump type controlled release tablet; the new gambogic acid osmotic pump type Type controlled-release tablet comprises tablet core and controlled-release semi-permeable coating film, and the weight of described controlled-release semi-permeable coating film is 2%-5% of tablet core weight; Tablet core comprises the following components by weight percentage: Xinteng Xanthic acid 2-10%; osmotic pressure active substance 25-35%; co-solvent 10-25%; suspending agent 10-25%; filler and / or lubricant balance; the controlled release semi-permeable coating film The semipermeable film coating solution comprises the following components by weight to volume: coating material 2-5% (weight to volume ratio, mg / ml); plasticizer 0.5 to 5% (weight to volume ratio, mg / ml ); porogen 3-15% (weight to volume ratio, mg / ml); it not only has zero-order drug release characteristics, but also has higher drug release efficiency. The invention also provides a preparation method of the above-mentioned controlled-release preparation, which has a simple process and is suitable for industrial production.

Description

technical field [0001] The invention relates to a new gambogic acid osmotic pump type controlled release preparation and a preparation method thereof. Background technique [0002] Gambogenic acid (GNA) is a compound with high anti-tumor activity isolated from the traditional Chinese medicine Gamboge. It is a weakly acidic insoluble substance with a broad anti-cancer spectrum and low toxicity. Non-small cell lung cancer cell A549, human nasopharyngeal carcinoma cell CNE-1, HePG2 cell and S180 cell line all have obvious inhibitory effect on the proliferation. However, due to the poor water solubility of neogambogic acid, low solubility, high blood vessel irritation, and short biological half-life in vivo, its clinical promotion and application are limited. [0003] Osmotic pump-type controlled-release preparations use osmotic pressure as the driving force for drug release and are characterized by zero-order release kinetics. A high osmotic pressure is formed inside, so that...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/36A61K9/32A61K31/352A61P35/00
Inventor 汪电雷蔡莉黄鹏黄和平陈金佩王效山
Owner 汪电雷