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Neogambogic acid osmotic pump type sustained-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. Realize the problems of industrialized production, low drug release efficiency, etc., to achieve stable and effective blood drug concentration, prolong the blood drug concentration time, and reduce the number of times of drug administration.

Active Publication Date: 2014-09-17
汪电雷
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, it is not only difficult to prepare insoluble drugs into single-chamber primary osmotic pump-type 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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  • Neogambogic acid osmotic pump type sustained-release preparation and preparation method thereof
  • Neogambogic acid osmotic pump type sustained-release preparation and preparation method thereof
  • Neogambogic acid osmotic pump type sustained-release preparation and preparation method thereof

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preparation example Construction

[0059] Experiment 1 Preparation of new gambogic acid osmotic pump

[0060] Preparation process and influencing factors of new gambogic acid osmotic pump tablets

[0061] 1.1 Preparation process

[0062] 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.

[0063] 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.

[0064] Tablet compression and coating: install the upper and lower punches, adjust the t...

Embodiment 1

[0202] Tablet core prescription (based on 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 about 196mg, and the weight of the film is about 4mg)

[0203]

[0204] Prescription of semipermeable film coating solution:

[0205] Cellulose acetate 15mg

[0206] Diethyl phthalate 10mg

[0207] PEG4000 30mg

[0208] Preparation process: pass the above-mentioned new gambogic 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 a soft material, and pass through a 24-mesh sieve to granulate , dried at 40°C, passed through a 24-mesh sieve for granulation, added the prescribed amount of magnesium stearate, mixed evenly, compressed into tablets, and the pressure was controlled at 60N to obtain tablet cores. Dissolve the above...

Embodiment 2

[0210] Tablet core prescription (based on 200mg 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 about 194mg, and the weight of the film is about 6mg)

[0211]

[0212] Prescription of semipermeable film coating solution:

[0213] Acrylic resin 10mg

[0214] Propylene Glycol 25mg

[0215] PEG1500 75mg

[0216]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 24 sieves for granulation, dry at 35 ° C, pass 24 Mesh sieve for granulation, add the prescribed amount of hydrogenated vegetable oil, mix evenly, compress into tablets, and control the pressure at 80N to obtain tablet cores. Dissolve acrylic resin, propylene glycol, and PEG1500 in 500 mL of acetone, and stir to make a unif...

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Abstract

The invention provides a neogambogic acid osmotic pump type sustained-release preparation and a preparation method thereof. The sustained-release preparation comprises a neogambogic acid osmotic pump type sustained-release tablet, which is a monolithic osmotic pump type sustained-release table, wherein the neogambogic acid osmotic pump type sustained-release tablet comprises a tablet core and a sustained-release semipermeable coating film, and the weight of the sustained-release semipermeable coating film is 2-5 percent that of the tablet core; the tablet core comprises the following components in percentage by weight: 2-10 percent of neogambogic acid, 25-35 percent of osmotic active substances, 10-25 percent of co-solvent, 10-25 percent of a suspending agent and the balance of filler and / or lubricate; the semipermeable film coating liquid of the sustained-release semipermeable coating film is prepared from the following components according to the weight and volume ratio: 2-5 percent (mg / ml) of a coating material, 0.5-5 percent (mg / ml) of plasticizer and 3-15 percent (mg / ml) of pore-foaming agent. The neogambogic acid osmotic pump type sustained-release preparation has the characteristic of zero-grade drug release, is high in drug release efficiency and simple in preparation 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 Applications(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