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Preparation method and new clinic application of penciclovir injection solution

A technology for penciclovir and injection, which is applied in the direction of medical preparations of non-active ingredients, pharmaceutical formulas, powder delivery, etc., and can solve the problem of production and clinical application of injection liquid injections and penciclovir injections that have not yet been seen. The treatment of condyloma acuminatum has not been reported, and the pain caused by patients has achieved the effect of controlling subclinical infection, increasing the safety of medication, and reducing pain

Active Publication Date: 2011-04-20
SHANDONG DANHONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the dosage forms of penciclovir on the market at home and abroad are only cream and powder injection for intravenous injection, and there are no reports on the production and clinical application of injection water injection
Moreover, penciclovir cream is an external preparation with relatively slow action and low bioavailability; clinically, when dermatologists face the complications of severe herpes zoster patients and immunocompromised patients, they need to use injection to Quickly control the disease with medicine
And the pH value of the listed penciclovir freeze-dried powder injection is more than 11 (referring to patent CN101108169A), which is easy to bring pain to the patient during injection
Chinese patent application number: 02113790.0 discloses the addition of Tween and poloxamer for solubilization, but since Tween or poloxamer is not available for injection, this brings unsafe factors to the medication
[0005] And about penciclovir injection treatment aspect condyloma acuminatum also does not have report yet

Method used

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  • Preparation method and new clinic application of penciclovir injection solution
  • Preparation method and new clinic application of penciclovir injection solution
  • Preparation method and new clinic application of penciclovir injection solution

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Exploration experiment of embodiment 1 penciclovir and amino acid formula

[0031] This experiment studies the solubility of penciclovir alone or in combination with amino acids in pure water. We experimented with amino acids of different types and molar ratios, and found that the combination of different types of amino acids produced significantly different solubilization effects. The specific results are shown in Table 1.

[0032] Table 1 Solubility of Penciclovir alone or in combination with different kinds of amino acids

[0033]

[0034] According to the above experiments, considering the cost of medication and other factors, the comprehensive effect of arginine, ornithine and glycine is the best.

Embodiment 2

[0035] The preparation of embodiment 2 penciclovir sodium chloride injection

[0036] prescription:

[0037] Penciclovir 25g

[0038] Sodium chloride 22.5g

[0039] Arginine 34.4g

[0040] 6mol / L hydrochloric acid appropriate amount

[0041]

[0042] Water for injection (add to) 25L sub-package of 100 bottles

[0043] Preparation method:

[0044] The sodium chloride of prescription quantity adds water for injection and is made into 10% (weight) solution, adds the arginine of prescription quantity, after stirring and dissolving, add 25g gac and stir and boil for 30 minutes, cool, filter and remove carbon. Add 10L of water for injection to the filtrate, add the prescribed amount of penciclovir, heat and stir at 80°C to dissolve, then cool to room temperature, adjust the pH value to 5.03 with 6mol / L hydrochloric acid solution, then make up water for injection to 25L, and then Pass through 0.45μm and 0.22μm filter membranes to obtain a c...

Embodiment 3

[0045] The quality influence of embodiment 3 different pH values ​​to penciclovir sodium chloride injection

[0046] The prescription in Example 2 is adjusted to four different pH values ​​(3.0, 4.0, 5.0, 8.0, 9.0) with a pH regulator (hydrochloric acid or sodium hydroxide), prepared as an injection, and subjected to an accelerated test at a temperature of 80°C , the stability of the injection was investigated through items such as color, clarity, pH value, content, and related substances. The specific results are shown in Table 2.

[0047] Table 2 Different pH values ​​affect the quality of Penciclovir Sodium Chloride Injection (80°C)

[0048]

[0049]

[0050] As can be seen from Table 2, the quality of penciclovir sodium chloride injection is relatively stable in the pH range of 4.0 to 8.0, but within this pH range, the solubility of penciclovir itself is relatively low, so it is not suitable for preparation For injection, it is especially not suitable to be formulat...

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Abstract

The invention discloses a preparation method and new clinic application of a penciclovir injection solution. The preparation method comprises the steps of: (1) mixing and dissolving penciclovir, one or more amino acids selected from alanine, glycocoll, cysteine hydrochloride, valine, glutamic acid, lysine and arginine, and pharmaceutically acceptable injection auxiliaries in water, wherein the concentration of the penciclovir is larger than 1.5mg / ml; (2) adjusting the pH value to be 4.0-8.0, preferably 4.5-6.5; and (3) adding water to adjust the concentration of the penciclovir to be 0.1-1.2mg / ml, preferably 0.4-1.1mg / ml, or randomly adjusting the pH value and then carrying out freeze-drying. The penciclovir injection solution can be used for safely, effectively and rapidly preventing and treating venereal diseases, such as herpes progenitalis, condyloma acuminatum and the like.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular, the present invention relates to a method for preparing penciclovir injection preparations and intermediate preparations thereof and prepared preparations, which can prevent and treat venereal diseases safely, effectively and quickly, such as genital Herpes and genital warts etc. Background technique [0002] Genital warts (Condylomata Acuminata CA), also known as genital warts and venereal warts, are sexually transmitted diseases caused by human papillomavirus (human papilloma virus, HPV) infection. It occurs in the vulva, perianal, penis, vaginal mucosa. According to the survey, the incidence of condyloma acuminatum in the UK increased from 30 / 100,000 in 1970 to 260 / 100,000 in 1988, an increase of almost 8 times, and the incidence of the disease in the United States increased 6 times from 1966 to 1984. Epidemiological surveys show that the incidence of genital warts in the Uni...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K9/19A61K31/52A61K47/16A61K47/26A61P31/20
Inventor 张登科
Owner SHANDONG DANHONG PHARMA
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