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Efavirenz micro-tablet as well as preparation method and application thereof

A technology of efavirenz and microtablets, which is applied in the field of medicine, can solve the problems of limited dissolution efficiency and bioavailability, and differences in blood drug concentrations, and achieve the effects of improving bioavailability, reducing differences, and reducing side effects

Active Publication Date: 2021-01-22
蓝龙药业(北京)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, in the subject population with the same daily dose, the measured plasma drug concentration in the subjects showed significant inter-individual differences
The reason for this phenomenon, on the one hand, is that there are differences in genotypes related to the metabolism of efavirenz in different subjects; on the other hand, it may be related to the limited dissolution efficiency and bioavailability caused by the low solubility of efavirenz relevant

Method used

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  • Efavirenz micro-tablet as well as preparation method and application thereof
  • Efavirenz micro-tablet as well as preparation method and application thereof
  • Efavirenz micro-tablet as well as preparation method and application thereof

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preparation example Construction

[0030] On the other hand, the embodiment of the present application provides a method for preparing the aforementioned efavirenz microtablets, which includes the following steps: predissolving the surfactant and part of the binder in water to obtain a granulation solution, adding the granulation solution to the granulation solution Add efavirenz, filler, disintegrant and remaining binder in the internal phase in sequence, stir and mix evenly to obtain a premixed material; granulate the premixed material, sieve, and dry to obtain dry granules; The dry granules and the materials in the external phase except the thickener and the lubricant are premixed, the thickener is added therein and mixed, and the lubricant is added therein and mixed, and the efavirenz microtablet is obtained after tableting.

[0031] On the other hand, the embodiment of the present application provides an application of the aforementioned efavirenz microtablets in the preparation of anti-cancer or anti-tumor...

Embodiment 1

[0034] The purpose of the present embodiment is to provide a kind of efavirenz microtablet, comprising internal phase and external phase (total 100%), internal phase used raw material (mass percentage): efavirenz 70%, microcrystalline cellulose PH101 7.25%, Hydroxypropyl cellulose 2%, Edison 10% and sodium lauryl sulfate 2%; External phase raw materials (mass percentage): granulated lactose 7.5%, magnesium stearate 1% and fumed silicon dioxide 0.25%, The mass ratio of the inner phase and the outer phase is: 91.25:8.75.

[0035] The efavirenz microtablet is mainly prepared through the following steps:

[0036] S1, granulation

[0037] S11 preparation of granulation solution: prepare purified water, sodium lauryl sulfate and part of binder (hydroxypropyl cellulose); add sodium lauryl sulfate, purified water and part of binder (hydroxypropyl cellulose) in a 250mL beaker Propyl cellulose), stirred with a magnetic stirrer until dissolved to obtain a granulation solution;

[0038...

Embodiment 2

[0050] The purpose of this embodiment is to provide an efavirenz microtablet, which includes an inner phase and an outer phase, and the inner phase is mainly prepared from the following raw materials in mass percentage: efavirenz 70%, microcrystalline cellulose PH101 6.5%, polymer Povidone k29 / 324%, crospovidone INF-10 5% and sodium lauryl sulfate 2%; the external phase is mainly prepared from the following raw materials in mass percentage: microcrystalline cellulose PH102 6.75%, cross-linked poly Vitone INF-10 5%, magnesium stearate 0.5%, fumed silicon dioxide 0.25%, the mass ratio of the inner phase and the outer phase is: 87.5:12.5.

[0051] The efavirenz microtablet is mainly prepared through the following steps:

[0052] S1, granulation

[0053] S11 prepares granulation solution: prepare purified water, sodium lauryl sulfate and part of adhesive (povidone k29 / 32); add sodium lauryl sulfate, purified water and part of adhesive ( Povidone k29 / 32), stirred with a magnetic ...

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Abstract

The invention provides an efavirenz micro-tablet as well as a preparation method and application thereof, and relates to the technical field of medicines. The efavirenz micro-tablet comprises an innerphase and an outer phase, the mass percent of the inner phase is 87-91.25%, and the mass percent of the outer phase is 8.75-13%; The inner phase comprises 70%-80% of efavirenz, 4.5%-10.25% of a filling agent, 2%-4% of an adhesive, 1.5%-10% of a disintegrating agent and 1%-4% of a surfactant; and the outer phase comprises 4.75%-10.5% of a filling agent, 0.5%-1% of a lubricating agent and 0.25%-0.5% of a thickening agent. The efavirenz micro-tablet has the advantages that the existing 600 mg / tablet large-dose efavirenz is adjusted and optimized into a 22.5-26.6 mg / tablet micro-tablet dosage form, the efavirenz micro-tablet is high in dissolution rate in unit time, the peak can be reached within 6.5-7 hours after the efavirenz micro-tablet is taken, and the bioavailability the same as or even better than that of the original efavirenz can be kept.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an efavirenz microtablet, a preparation method and an application thereof. Background technique [0002] At present, prostate cancer has become the second most common cancer in men in the world, and it is also the fifth most common cancer in men in my country. The incidence of prostate cancer in my country is far lower than that in European and American countries, but due to the low rate of early diagnosis, the mortality rate of prostate cancer patients in my country is much higher than that in developed countries. Existing treatments for prostate cancer include surgery, radiotherapy, endocrine therapy, chemotherapy, and new endocrine therapies. With the prolongation of prostate cancer treatment time, due to factors such as treatment pressure, prostate cancer cells continue to mutate, and eventually prostate cancer enters the stage of castration resistance, that is, castration-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/26A61K31/536A61P35/00
CPCA61K31/536A61K9/2054A61K9/2013A61K9/2077A61P35/00
Inventor 雅克·普什·阿兰萨尔瓦多·罗·布朱丹
Owner 蓝龙药业(北京)有限公司