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A co-crystal of penciclovir and 3,5-dihydroxybenzoic acid and its preparation method

A technology of dihydroxybenzoic acid and penciclovir, which is applied in the field of medicinal chemistry, can solve the problems of easy-to-cause phlebitis in clinical application, poor water solubility of penciclovir, and great irritation to human body, and achieve easy control of the crystallization process. Good performance and simple process

Active Publication Date: 2020-08-28
TIANJIN UNIVERSITY OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Penciclovir has poor water solubility, is difficult to be absorbed orally, and is not easy to be made into liquid preparations such as injections and eye drops. At present, most of the commercially available dosage forms at home and abroad are ointments
Abroad has developed the freeze-dried powder injection of penciclovir sodium salt, although making it into penciclovir sodium salt can significantly improve the solubility in water, but the pH value of its aqueous solution reaches 11, which is more irritating to human body, It is easy to cause phlebitis and its clinical application is limited

Method used

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  • A co-crystal of penciclovir and 3,5-dihydroxybenzoic acid and its preparation method
  • A co-crystal of penciclovir and 3,5-dihydroxybenzoic acid and its preparation method
  • A co-crystal of penciclovir and 3,5-dihydroxybenzoic acid and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043]Weigh 63.3mg of penciclovir and 308.2mg of 3,5-dihydroxybenzoic acid, add 1mL of 50% ethanol (the volume ratio of ethanol and water is 1:1) to obtain a suspension, and place the suspension in Stir at room temperature for 24 hours, filter with suction, wash the resulting white solid with an appropriate amount of 50% ethanol, and then dry at 40°C for 48 hours to obtain a solid sample of penciclovir and 3,5-dihydroxybenzoic acid cocrystal.

Embodiment 2

[0045] Weighed 63.3 mg of penciclovir and 231.2 mg of 3,5-dihydroxybenzoic acid, added 1 mL of ethanol to obtain a suspension, stirred the suspension at room temperature for 2 h, and filtered it with suction. The resulting white solid was dried and obtained a spray Solid sample of co-crystal of ciclovir and 3,5-dihydroxybenzoic acid.

Embodiment 3

[0047] Weigh 63.3 mg of penciclovir and 231.2 mg of 3,5-dihydroxybenzoic acid, add 1 mL of methanol to obtain a suspension, stir the suspension at room temperature for 12 hours, filter with suction, and dry the obtained white solid to obtain Solid sample of co-crystal of penciclovir and 3,5-dihydroxybenzoic acid.

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Abstract

The invention discloses a penciclovir and 3,5-dihydroxybenzoic acid eutectic crystal and a preparation method thereof. In the penciclovir and 3,5-dihydroxybenzoic acid eutectic crystal, the molar ratio of penciclovir to 3,5-dihydroxybenzoic acid is 1:1. The preparation method of the penciclovir and 3,5-dihydroxybenzoic acid eutectic crystal is simple in process, the crystallization process is easyto control, the reproducibility is good, and the penciclovir and 3,5-dihydroxybenzoic acid eutectic crystal is suitable for industrial production. Compared with penciclovir, the penciclovir and 3,5-dihydroxybenzoic acid eutectic crystal has the advantages that the dissolution rate is higher, the apparent solubility is higher, the bioavailability of the penciclovir is favorably improved, and a material basis is provided for successfully developing oral preparations and liquid preparations of penciclovir.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to a co-crystal of penciclovir and 3,5-dihydroxybenzoic acid and a preparation method thereof. Background technique [0002] Pharmaceutical active ingredients usually exist in crystalline forms, such as polymorphs, hydrates, solvates, salts, and co-crystals. For the same pharmaceutical active ingredient, different crystalline forms have different physical and chemical properties. Therefore, obtaining a suitable crystalline form of a drug is of great importance in the pharmaceutical industry. The drug exists in the form of co-crystal, which can have significant advantages in improving the stability, solubility and permeability of the active ingredient of the drug. Therefore, pharmaceutical co-crystals are usually an effective means to improve the physical and chemical properties of pharmaceutical active ingredients. [0003] The chemical name of Penciclovir is 9-[4-hyd...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D473/18C07C65/03C07C51/41C07C51/43A61K31/522A61P31/22A61P31/20
CPCA61P31/20A61P31/22C07B2200/13C07C65/03C07D473/18
Inventor 陈嘉媚元昭君戴霞林鲁统部
Owner TIANJIN UNIVERSITY OF TECHNOLOGY
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