Compound preparation containing fosaprepitant and palonosetron hydrochloride, and preparation method thereof

A technology of palonosetron and compound preparations, which is applied in the field of medicine, can solve the problems of reducing treatment compliance, poor patient compliance, and inconvenient use by doctors, and achieves a technology suitable for large-scale industrial production, improving compliance, and simple process Effect

Inactive Publication Date: 2012-10-31
QILU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Chemotherapy is one of the main means of treating malignant tumors. However, nausea and vomiting caused by chemotherapy drugs are becoming more and more common and serious, which has become a serious problem in clinical practice: if the control is not satisfactory, it will affect the quality of life of patients and reduce the compliance of treatment. sex
[0005] In the clinical dosing regimen to prevent nausea and vomiting associated with highly emetogenic chemotherapy, NK-1 receptor antagonists (injection of fosaprepitant dimeglumine or oral aprepitant) are recommended on the first day. 5-HT3 receptor antagonists (setron-like drugs) must be given, and the patient's compliance is poor with two injections respectively, and it is inconvenient for doctors to use
There is no report on the research and development of the compound preparation of fosaprepitant dimeglumine and palonosetron hydrochloride

Method used

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  • Compound preparation containing fosaprepitant and palonosetron hydrochloride, and preparation method thereof
  • Compound preparation containing fosaprepitant and palonosetron hydrochloride, and preparation method thereof
  • Compound preparation containing fosaprepitant and palonosetron hydrochloride, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Embodiment 1. prepare 1000 bottles, each bottle contains the sterile lyophilized compound preparation of 115mg fosaprepitant, 0.25mg palonosetron hydrochloride.

[0052] Formula: Fosaprepitant dimeglumine 188g, palonosetron hydrochloride 0.25g, polysorbate 80 57.5g, edetate disodium 14.4g, anhydrous lactose 287.5g, sodium hydroxide / hydrochloric acid, plus injection Make up to a total volume of 4000 mL with water.

[0053] Process: 1) Liquid preparation: Weigh according to the formula, mix 188g of fosaprepitant dimeglumine, 0.25g of palonosetron hydrochloride, 57.5g of polysorbate 80, 14.4g of disodium edetate, Stir and dissolve 287.5g of anhydrous lactose in an appropriate amount of sterile water for injection, add sterile water for injection to 4000mL, adjust the pH value to 6.0 with sodium hydroxide / hydrochloric acid, and then pass the liquid medicine through sterile micropores with a pore size of 0.22 microns Membrane, packed into 1000 bottles, half stoppered with h...

Embodiment 2

[0055] Embodiment 2. prepare 1000 bottles, each bottle contains the sterile lyophilized compound preparation of 120mg fosaprepitant, 0.24mg palonosetron hydrochloride.

[0056] Formula: Fosaprepitant dimeglumine 196.2g, palonosetron hydrochloride 0.24g, polysorbate-80 65g, edetate disodium 16.5g, glucose 325g, sodium hydroxide / hydrochloric acid, add water for injection to The total volume is 5000mL.

[0057] Process: 1) Liquid preparation: Weigh according to the formula, 196.2 g of fosaprepitant dimeglumine, 0.24 g of palonosetron hydrochloride, 65 g of polysorbate-80, and 16.5 g of edetate disodium , glucose 325g was stirred and dissolved in an appropriate amount of sterile water for injection, added sterile water for injection to 5000mL, adjusted the pH value to 6.5 with sodium hydroxide / hydrochloric acid, and then passed the liquid medicine through a sterile microporous filter membrane with a pore size of 0.22 microns, Pack 1,000 vials, half stoppered with halogenated buty...

Embodiment 3

[0059] Embodiment 3. prepare 1000 bottles, each bottle contains the sterile lyophilized compound preparation of 130mg fosaprepitant, 0.22mg palonosetron hydrochloride.

[0060] Recipe: Fosaprepitant Dimeglumine 212.6g, Palonosetron Hydrochloride 0.22g, Polysorbate-80 70g, Edetate Disodium 17.2g, Mannitol 332g, Sodium Hydroxide / HCl, add Water for Injection to a total volume of 5000 mL.

[0061] Process: 1) Liquid preparation: weighing according to the formula, 212.6 g of fosaprepitant dimeglumine, 0.22 g of palonosetron hydrochloride, polysorbate-8070 g, 17.2 g of disodium edetate, Stir and dissolve 332g of mannitol in an appropriate amount of sterile water for injection, add sterile water for injection to 5000mL, adjust the pH value to 7.0 with sodium hydroxide / hydrochloric acid, then pass the liquid medicine through a sterile microporous filter membrane with a pore size of 0.22 microns, Pack 1,000 vials, half stoppered with halogenated butyl rubber and put into a freeze drye...

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Abstract

The invention provides a sterile lyophilized compound preparation containing fosaprepitant and palonosetron hydrochloride, and a preparation method thereof. According to the invention, effective dosages of fosaprepitant dimeglumine and palonosetron hydrochloride are adopted as effective components, and auxiliary materials such as a solubilizer, a complexing agent, an excipient, and an acidity adjusting agent are contained in the preparation. The preparation is filtered, sterilized, sub-packaged, and lyophilized. When in use, the sterile lyophilized compound preparation provided by the invention is added into a solvent, such that injection solution with an appropriate concentration is prepared and can be used. With one time of medication, clinical demands of two treatment medicines can be satisfied, such that patient compliance is improved. The preparation method of the compound preparation is simple, and the method is suitable for industrialized productions.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a compound preparation containing fosaprepitant dimeglumine and palonosetron hydrochloride and a preparation method thereof. Background technique [0002] Chemotherapy is one of the main means of treating malignant tumors. However, nausea and vomiting caused by chemotherapy drugs are becoming more and more common and serious, which has become a serious problem in clinical practice: if the control is not satisfactory, it will affect the quality of life of patients and reduce the compliance of treatment. sex. The neurotransmitters that form the vomiting reflex in the vomiting caused by tumor chemotherapy are mainly dopamine, acetylcholine, histamine, 5-hydroxytryptamine and neurokinin. According to the above-mentioned mechanism and clinical efficacy of nausea and vomiting caused by chemotherapy drugs, the therapeutic drugs include early drugs, such as (1) dopamine rec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/675A61K31/473A61K9/19A61P1/08
Inventor 王晶翼余汪洋杨清敏黄惠峰徐先艳张明会
Owner QILU PHARMA
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