Effervescent tablet containing sapropterin dihydrochloride

A technology of sapropterin hydrochloride and effervescent tablets, which is applied in the fields of pharmacy and children's orphan drugs, and can solve the problems of the drug being unstable to humidity, reducing patient compliance, and children's oral incompatibility, achieving good taste and appearance, The effect of process amplification and reproducibility is good, and the fluidity requirement is not strict

Inactive Publication Date: 2015-01-07
中盛特医食品(汕头)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Sapropterin hydrochloride has a certain pungent smell. After the currently marketed tablets are dissolved in water, children may not be able to adapt to oral administration, thus reducing the patient's compliance
At the same time, because the drug is not very stable to humidity, the speed of dissolving into a solution with ordinary tablets is not as fast as that of effervescent tablets.

Method used

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  • Effervescent tablet containing sapropterin dihydrochloride
  • Effervescent tablet containing sapropterin dihydrochloride
  • Effervescent tablet containing sapropterin dihydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 5-8

[0072]

[0073] Effervescent tablet preparation process:

[0074] Examples 5-8 adopt the wet preparation method described in Example 4 to mainly investigate the effects of fumaric acid as an acid source, lactose as a filler and the use of different alkali sources on the quality of effervescent tablets. Fumaric acid is not hygroscopic and has a certain lubricating effect, which can avoid sticking and moisture absorption, but the acidity may not be as strong as citric acid and tartaric acid, and the amount of foaming may be insufficient.

[0075] The above eight embodiments prepare 200 tablets respectively, and the key indicators of effervescent tablets are compared

[0076]

[0077] Among them, the detection conditions of the foaming amount are: take a 25ml test tube with a stopper, add 3ml of water, put it in a water bath at 37°C for 5 minutes, put this product into it, and observe the maximum foaming amount. As can be seen from the key indicators, using the pre...

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PUM

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Abstract

The invention belongs to the pharmaceutical field, and in particular relates to an effervescent tablet containing sapropterin dihydrochloride. The effervescent tablet comprises 4-12wt% of sapropterin dihydrochloride, 5-40wt% of an acid source, 9-50wt% of an alkali source, 0.1-5wt% of an antioxidant, 5-50wt% of filler, 1-5wt% of a disintegrating agent, 1-4wt% of a binding agent, 1-5wt% of a wetting agent and 0.5-5wt% of a flavoring agent. The effervescent tablet disclosed by the invention is applicable to hyperphenylalaninemia (HPA) caused by tetrahydrobiopterin (BH4) of the adult and children older than 4-years old. The effervescent tablet disclosed by the invention is quick to disintegrate, and a foaming amount is more than 10ml; a formed solution is good in appearance, and high in oral compliance to children; and compared to an originally developed preparation, absorption and in-vivo distribution are not changed.

Description

technical field [0001] The invention relates to the field of pharmacy, more particularly to the field of children's orphan drugs, in particular to an effervescent tablet containing sapropterin hydrochloride. Background technique [0002] Phenylalaninemia is a congenital disorder of amino acid metabolism characterized by elevated plasma phenylalanine concentrations caused by a deficiency of phenylalanine hydroxylase activity, often resulting in severe mental retardation. The disease is autosomal recessive and is caused by the enzyme encoding phenylalanine hydroxylase (such as phenylketonuria) or with 6R-tetrahydrobiopterin (6R-BH 4 ) synthesis or regeneration related enzymes (such as BH 4 deficiency) due to genetic mutations. BH 4 Deficiencies are encoded with BH 4 A disease caused by a genetic mutation or deletion of one of five enzymes involved in synthesis or recycling. In both cases, phenylalanine cannot be efficiently converted to tyrosine, resulting in elevated blo...

Claims

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Application Information

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IPC IPC(8): A61K9/46A61K31/519A61K47/26A61K47/32A61K47/34A61P3/00
Inventor 张永丰陈卫孙小虎
Owner 中盛特医食品(汕头)有限公司
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