Erlotinib sustained-release preparation for treating non-small cell lung cancer

A slow-release preparation, the technology of erlotinib hydrochloride, is applied in the directions of medical preparations without active ingredients, medical preparations containing active ingredients, and pill delivery, which can solve the problem of difficulty in maintaining effective therapeutic concentrations and large fluctuations in blood drug concentrations. , adverse reactions, etc.

Active Publication Date: 2020-09-04
苏州特瑞药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The marketed formulation of erlotinib is an immediate release formulation, and the plasma concentration fluctuates greatly during each administration, resulting in a "peak-valley" phenomenon
When the blood drug concentration is at the peak, ex...

Method used

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  • Erlotinib sustained-release preparation for treating non-small cell lung cancer
  • Erlotinib sustained-release preparation for treating non-small cell lung cancer
  • Erlotinib sustained-release preparation for treating non-small cell lung cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Prescription (makes 1000 tablets):

[0045] Erlotinib Hydrochloride 150mg

[0046] Lactose 75 mg

[0047] Microcrystalline Cellulose 75mg

[0048] Sodium Lauryl Sulfate 3.75mg

[0049] Hypromellose 81.25mg

[0050] Magnesium stearate (internal addition) 1.87mg

[0051] Magnesium stearate (extra) 3.75mg

[0052] Opadry 9.38mg

[0053] Appropriate amount of purified water

[0054] Preparation:

[0055] Erlotinib hydrochloride, lactose, microcrystalline cellulose, hypromellose, and magnesium stearate of the prescribed amount were pulverized respectively and passed through an 80-mesh sieve, mixed evenly, and prepared with an aqueous solution of sodium lauryl sulfate of the prescribed amount. Made of soft material with binder, granulated, dried in a fluidized bed at 60°C, added with prescribed amount of magnesium stearate, mixed evenly, compressed into tablets, coated, ready to be obtained.

Embodiment 2

[0057] Erlotinib Hydrochloride 150mg

[0058] Lactose 75mg

[0059] Microcrystalline Cellulose 75mg

[0060] Sodium Lauryl Sulfate 3.75mg

[0061] Sodium Alginate 81.25mg

[0062] Magnesium stearate (internal addition) 1.87mg

[0063] Magnesium stearate (extra) 3.75mg

[0064] Opadry 9.38mg

[0065] Appropriate amount of purified water

[0066] Preparation:

[0067] The prescribed amount of erlotinib hydrochloride, lactose, microcrystalline cellulose, sodium alginate, and magnesium stearate were respectively crushed and passed through an 80-mesh sieve, mixed evenly, and the aqueous solution of the prescribed amount of sodium lauryl sulfate was used as a binder Preparation of soft material, granulation, drying at 60°C, adding the prescribed amount of magnesium stearate, mixing evenly, pressing into tablets, coating, to obtain.

Embodiment 3

[0069] Erlotinib Hydrochloride 150mg

[0070] Lactose 75mg

[0071] Microcrystalline Cellulose 75mg

[0072] Sodium Lauryl Sulfate 3.75mg

[0073] Polyvinylpyrrolidone 81.25mg

[0074] Magnesium stearate (internal addition) 1.87mg

[0075] Magnesium stearate (extra) 3.75mg

[0076] Opadry 9.38mg

[0077] Appropriate amount of purified water

[0078] Preparation:

[0079] Grind the prescribed amount of erlotinib hydrochloride, lactose, microcrystalline cellulose, polyvinylpyrrolidone, and magnesium stearate respectively and pass through an 80-mesh sieve, mix well, and use an aqueous solution of prescribed amount of sodium lauryl sulfate as a binder Preparation of soft material, granulation, drying at 60°C, adding the prescribed amount of magnesium stearate, mixing evenly, pressing into tablets, coating, to obtain.

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Abstract

The invention relates to an erlotinib (Erlotinib Hydrochloride) sustained-release preparation for treating the non-small cell lung cancer. The erlotinib sustained-release preparation is prepared fromthe following raw and auxiliary materials in percentage: 30% to 50% of erlotinib, 10% to 40% of sustained-release material, 30% to 50% of filler, 1% to 10% of solubilizer and 1% to 4% of lubricant. The invention further provides a preparation method of the sustained-release tablets. The preparation method comprises the steps of: firstly, placing the erlotinib, the sustained-release material and the filler into a high-efficiency wet granulator to uniformly mix; then adding the solubilizer into purified water to prepare solution; adding a proper volume of solution into a pot to carry out wet granulation; after particles are dried, adding a proper volume of lubricant; and after uniformly mixing, carrying out tabletting to form the tablets. Compared to a common drug, the erlotinib sustained-release preparation has the advantages of reducing the "peak valley" effect of in-vivo release of the drug, reducing a probability that cancer cells generate drug resistance, reducing adverse reactionson a patient, which are generated due to excessively high blood concentration of the drug, enabling the blood concentration to be continuously and stably kept to optimal treatment concentration, improving bioavailability of the drug, reinforcing the curative effect and improving administration safety.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to erlotinib. Background technique [0002] The invention belongs to pharmaceutical preparations, and mainly relates to an oral slow-release preparation for treating non-small cell lung cancer and a preparation method thereof. [0003] Lung cancer is one of the malignant tumors with the fastest-growing morbidity and mortality and the greatest threat to human health and life. Among them, non-small cell lung cancer accounts for about 80% of all lung cancers. Traditional treatment options include surgery, chemotherapy, and targeted drug therapy . Surgical therapy will cause trauma to the patient's body, and cannot remove all cancer cells, and it is easy to relapse after surgery. Chemotherapy drugs have poor selectivity and poor targeting effect, which often kill other cells except cancer cells, damage the body's own immune system, and even cause the risk of gene mutation an...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K47/38A61K47/36A61K47/26A61K47/20A61K31/517A61P35/00
CPCA61K9/2866A61K9/2054A61K9/205A61K9/2018A61K9/2013A61K31/517A61P35/00Y02A50/30
Inventor 王浩尹冉
Owner 苏州特瑞药业股份有限公司
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