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Methylnaltrexone bromide solid composition and preparation method thereof

A technology of solid composition and methylnaltrexone bromide, which is applied in the direction of drug combinations, pharmaceutical formulas, medical preparations of non-active ingredients, etc., can solve problems such as instability, patient pain, and expensive products on the market

Inactive Publication Date: 2016-05-18
江苏国丹生物制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the administration of injections brings pain to patients, and subcutaneous injections often cause irritation to the skin, which affects the patient's compliance with medication
At the same time, methylnaltrexone bromide is unstable in itself, and it is prone to degradation during preparation and storage, which affects product quality and creates potential drug safety hazards.
[0006] On the other hand, in pain treatment, opioid analgesics account for about 70% of analgesic drugs, and when patients receive opioid treatment, most of them will suffer from constipation. It has huge market potential, but the current production cost of injections is relatively high, resulting in relatively expensive products on the market, which brings financial burden to many patients
[0007] Therefore, current methylnaltrexone pharmaceutical preparations still need to be improved

Method used

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  • Methylnaltrexone bromide solid composition and preparation method thereof
  • Methylnaltrexone bromide solid composition and preparation method thereof
  • Methylnaltrexone bromide solid composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Embodiment 1 prepares methylnaltrexone bromide sheet

[0053]

[0054] Adhesive is formulated into the concentration of 6%, and prescription quantity tartaric acid is dissolved in binder solution, and prescription quantity methylnaltrexone bromide is dissolved in above-mentioned solution; All the other auxiliary materials pass through 80 mesh sieves, mannitol and cross-linked carboxymethyl cellulose Mix plain sodium evenly; add the binder to the above-mentioned mixed powder to make soft material, pass through a 24-mesh sieve to granulate; dry until the water content is 1.34%, mix the above-mentioned granules with magnesium stearate evenly, and then press the tablet machine, No. 6 Punch, pressure 54N.

Embodiment 2

[0055] Embodiment 2 prepares methylnaltrexone bromide sheet

[0056]

[0057] Adhesive is prepared into the concentration of 8%, the prescription quantity of citric acid is dissolved in the binder solution, and the prescription quantity of methylnaltrexone is dissolved in the above solution; the rest of the auxiliary materials are passed through 80 mesh sieves, precrosslinked starch and crosslinked Mix povidone evenly; add the binder to the above-mentioned mixed powder to make soft material, pass through a 24-mesh sieve to granulate; dry until the water content is 2.05%, mix the above-mentioned granules with sodium lauryl sulfate evenly, and press the tablet machine , No. 6.5 punch, pressure 50N.

Embodiment 3

[0058] Embodiment 3 prepares methylnaltrexone bromide sheet

[0059]

[0060] The adhesive is prepared into a concentration of 5%, the prescription amount of L-aspartic acid is dissolved in the adhesive solution, and the prescription amount of bromidenaltrexone is dissolved in the above solution; the remaining auxiliary materials are passed through a 60-mesh sieve, lactose and hydroxyl Mix propylmethyl cellulose evenly; add the binder to the above-mentioned mixed powder to make a soft material, pass through a 20-mesh sieve to granulate; dry until the water content is 2.17%, mix the above-mentioned granules with talcum powder evenly, and then press the tablet machine, No. 5.5 Punch, pressure 62N.

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Abstract

The invention relates to a methylnaltrexone bromide solid composition and a preparation method thereof. The solid composition comprises ingredients of methylnaltrexone bromide and an acidic stabilizing agent at a weight ratio being (10:1) to (1:10). The methylnaltrexone bromide solid composition has the advantages that the formula process is advanced; the product quality is stable; the problems of stability and the content uniformity of the methylnaltrexone bromide in the preparation process can be perfectly solved; and the problem of stability of a methylnaltrexone bromide preparation in the storage process can also be perfectly solved. The methylnaltrexone bromide solid composition invented by the research group has the beneficial effects that the solid preparation and the methylnaltrexone bromide injection on the market have the identical curative effect; the administration mode is changed into oral administration; the medicine administration compliance of a patient is improved; the production cost is reduced; the selling price of a product is reduced; and the economical burden of the patient is reduced. Therefore economic, safe, effective and convenient therapeutic medicine is provided for the patient with constipation due to opioid medicine, and good social benefits and economic benefits can be obtained.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular, the invention relates to a solid composition of methylnaltrexone bromide and a preparation method thereof. Background technique [0002] The chemical name of methylnaltrexone bromide (Methylnaltrexone Bromide, trade name Relistor) is bromide-17-(cyclopropylmethyl)-4,5α-epoxy-3,14-dihydroxy-17-methyl-6-oxo morphinan. Jointly researched and developed by a subsidiary of Wyeth Pharmaceutical Company of the United States and Progenics Pharmaceuticals, it is a peripheral μ opioid receptor antagonist that does not cross the blood-brain barrier, can maintain the normal gastrointestinal function of patients, and improve the quality of life of advanced patients. This product is indicated for the treatment of opioid-induced constipation in patients with progressive disease receiving palliative care who have not responded to laxative medications. [0003] [0004] In April 2008,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/485A61K47/12A61K47/20A61K47/18A61K47/04A61K9/20A61P1/10
Inventor 常天安周晓星刘大鹏钱丽娜金晶王珍程稳项斌王晓星
Owner 江苏国丹生物制药股份有限公司
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