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

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...

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, exceeding the optimal therapeutic dose, it is easy to cause adverse reactions; when the blood drug concentration is at the trough, it is difficult to maintain the effective therapeutic concentration, and it will induce drug resistance of cancer cells

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