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Water solution of penciclovir and its prepn. method

A penciclovir and aqueous solution technology, applied in the field of antiviral drug aqueous solution and preparation, can solve the problems of easily causing phlebitis, limited use of freeze-dried powder injection, and high aqueous solution

Inactive Publication Date: 2003-12-17
XICHUAN INST OF ANTIBIOTIC IND NAT MEDICINE SUPERVISION BUREAU
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the freeze-dried powder injection of penciclovir sodium salt has been developed abroad, but the pH of its aqueous solution is relatively high, about 11, which is easy to cause phlebitis. limited use
[0003] In addition, there are few types of antiviral eye drops available clinically in my country, and the development of ocular dosage forms for the treatment of ocular herpes simplex infection is also urgently needed clinically.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0012] According to the efficacy concentration and solubility of penciclovir, the inventors first selected penciclovir with a concentration of 0.1% as the research object. Since penciclovir contains -OH, penciclovir can be salted with a pharmaceutically acceptable base to increase its solubility in water. The base can be sodium hydroxide, potassium hydroxide, sodium carbonate, bicarbonate Inorganic bases such as sodium; it can also be organic bases such as sodium citrate, sodium phosphate, basic amino acids, meglumine, etc. In addition, penciclovir has -NH 2 , so it can be reacted with a suitable acid to make a clear solution. The acid can be inorganic acids such as hydrochloric acid, sulfuric acid and phosphoric acid, or organic acids such as citric acid; add the rest of the auxiliary materials to make a pH4-9 aqueous solution. This includes the use of buffers such as phosphate, acetate, borax salt, and citrate.

[0013] The specific composition is as follows:

[0014] Penc...

experiment example 2

[0020] The selection of cosolvent in experimental example 2 penciclovir aqueous solution

[0021] The composition of penciclovir aqueous solution is as follows:

[0022] Penciclovir 10-100mg

[0023] Distilled water 50ml

[0024] Polyvinylpyrrolidone 0.01-20g

[0025] Add distilled water to 100ml

[0026] Preparation:

[0027] Weigh 10-100mg of penciclovir, add 50ml of distilled water, then add 0.5-20g of polyvinylpyrrolidone, heat and dissolve until clear, and finally add water until 100ml.

[0028] Polyvinylpyrrolidone can be K15, K25, K29 / 30, K90 and S-630, preferably K15, K25 and K29 / 30, and the concentration is preferably 1%-10%. A suitable acid-base regulator can be added to adjust its pH in the range of 4-9.

[0029] The prepared penciclovir aqueous solution was placed under an environment of 10° C., observed after 1 month, and no precipitation was seen in more than 4% polyvinylpyrrolidone penciclovir aqueous solution. Polyvinylpyrrolidone with a concentration of...

experiment example 3

[0030] The selection of surfactant solubilizer in experimental example 3 penciclovir aqueous solution

[0031] The composition of penciclovir aqueous solution is as follows:

[0032] Penciclovir 10-100mg

[0033] Distilled water 5ml

[0034] Surfactant 0.05-20g

[0035] Add distilled water to 100ml

[0036] Preparation:

[0037] Weigh 10-100mg of penciclovir, add 100ml of distilled water, then add 0.05-20g of surfactant, heat and dissolve until clear. Finally add distilled water until 100ml.

[0038] Surfactants can be Tween-20, 40, 60, and 80, or poloxamer. The penciclovir aqueous solution prepared has a pH between 5-8 and is placed at 25°C for a long time for one and a half years. It has good internal stability and can be placed at 4°C for about a week. Even if it precipitates, its solution will automatically convert to a clear solution in an environment of 20°C, and the content remains unchanged.

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PUM

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Abstract

A water soluble of Penxiluowei contains the Penxiluowei or its salt, solubilizer, cosolvent and pH regulator. It can be used to prepare injection, eye drops and nose drops for treating the diseases caused by herpes simple virus, herpes zoster virus and hepatitis B virus.

Description

technical field [0001] The invention relates to an antiviral drug aqueous solution and a preparation method. Background technique [0002] Penciclovir (penciclovir), an antiviral drug developed by SmithKline Beecham, has inhibitory activity against HSV-1, HSV-2 and Epstein-Barr virus. It was first listed in the UK in June 1996, and the dosage form is ointment Agent, mainly for cold sores. The pharmacological action shows that penciclovir generates monophosphate under the action of viral thymidine kinase, which is further phosphorylated by cellular enzymes to generate the active metabolite penciclovir triphosphate. When the cell penciclovir triphosphate When the ester reaches a high concentration, it interacts with the viral DNA polymerase, thereby inhibiting the synthesis of viral DNA and killing the virus. However, the oral bioavailability of penciclovir aqueous solution is only 10-20%, and the medicine is made into an oral dosage form to treat herpes simplex, varicella z...

Claims

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Application Information

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IPC IPC(8): A61K31/522A61P31/12
Inventor 丁涛蒋宁曹嘉
Owner XICHUAN INST OF ANTIBIOTIC IND NAT MEDICINE SUPERVISION BUREAU
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