CN1415297A - Pharmic compsn. of local administration for treating herpes zoster - Google Patents
Pharmic compsn. of local administration for treating herpes zoster Download PDFInfo
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- CN1415297A CN1415297A CN 02146255 CN02146255A CN1415297A CN 1415297 A CN1415297 A CN 1415297A CN 02146255 CN02146255 CN 02146255 CN 02146255 A CN02146255 A CN 02146255A CN 1415297 A CN1415297 A CN 1415297A
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- pharmaceutical composition
- acyclovir
- composition according
- lignocaine
- liniment
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Abstract
An antiviral composite medicing for locally appling it is composed of one or more antiviral medicines, one or more local anesthetics, and medical carrier. It features less irritation and antiviral and antalgic action.
Description
Technical field
The present invention relates to a kind of pharmaceutical composition for the treatment of the topical of herpes zoster.
Background technology
Herpes zoster is a kind of infectious skin disease that varicella zoster virus causes, shows as pain or superficial sensory disturbance, and pain is one of primary disease feature, and especially for the gerontal patient, pain can be violent unusually.Some patient still leaves over pain after erythra disappears fully, sustainable several months, even longer time.The Therapeutic Principle that this is sick: antiviral, pain relieving, the antiinflammatory protection is local, protects from infection.
Antiviral drugs commonly used is acyclovir, ribavirin, valaciclovir; The present invention be more particularly directed to antiviral drug is acyclovir, it is the purine nucleosides material, broad-spectrum antiviral drug, external and body is interior to comprise herpes simplex virus HSV-1, HSV-2 to the herpes virus hominis, varicella zoster virus (VIV), Epstein-Barr virus (EBV), cytomegalovirus (CMV) etc. has inhibitory action, has efficient, low toxicity, characteristics that selectivity is strong, be the drug of first choice of preventing and treating herpesvirus infection at present, concentration is 0.1%-10%.Become local administration preparation can directly act on lesions position these medication preparation, the performance optimum curative effect, but local use at these medicines, can not suppress the pain that varicella zoster virus causes, simultaneously owing to directly act on lesions position, can produce bigger zest, cause bigger misery to patient, patient is reluctant to accept.
Summary of the invention
It is little and have antiviral simultaneously and the pharmaceutical composition of the topical of the effect of relieving the pain to the purpose of this invention is to provide a kind of zest that is used for the treatment of herpes zoster.
For achieving the above object, the present invention adopts following technical scheme:
A kind of pharmaceutical composition that is used for the treatment of the topical of herpes zoster, this pharmaceutical composition is made up of one or more antiviral drugs and one or more local anesthetics and pharmaceutical carrier.
Described antiviral drug is acyclovir, ribavirin, valaciclovir.
Described local anesthetic is tetracaine, tetracaine, lignocaine, dyclonine, procaine and benzocaine, and with the anesthetis of the form of salt.
The content of described antiviral drug is 0.1wt%～10wt%, and the content of local anesthetic is 0.1wt%～5.0wt%, the pharmaceutical carrier surplus.
Described pharmaceutical composition is a liniment, and described pharmaceutical carrier is polymer substance, plasticizer and solvent.This pharmaceutical composition can be ointment, the gel that contains one or more antiviral drugs and one or more local anesthetics, can use conventional ointment base, comprises oleaginous base, emulsion-type substrate, aqueous matrix.Preferably the form of liniment contains one or more antiviral drugs and one or more local anesthetics.
Described polymer substance is one or more in sodium alginate, polyvinylpyrrolidone (PVP) and the Polyethylene Glycol (PEG).
Described plasticizer is a glycerol.
Described solvent comprises distilled water or ethanol or alcoholic acid aqueous solution.
Described pharmaceutical composition is a liniment, and described pharmaceutical carrier is one or more in ethanol, distilled water and hard ester acid, glycerol, Tween 80, octadecanol, potassium sorbate and the vaseline.
The invention has the advantages that: by in pharmaceutical composition, adding local anesthetic, can reduce medicine irritation, and have antiviral and the effect of relieving the pain simultaneously, increase patient's compliance.
The specific embodiment
Embodiment 1: compound recipe acyclovir lignocaine liniment
Acyclovir 5.0g
Lignocaine 1.0g
PVP(44-08) 1.0g
Glycerol 5.0g
Ethanol 60.0g
Distilled water an amount of (adding to cumulative volume is 100ml)
Preparation method: by recipe quantity acyclovir is dissolved in the ethanol, PVP, glycerol, the lignocaine of recipe quantity is dissolved in an amount of distilled water, the alcoholic solution of acyclovir is slowly joined in the aqueous solution of PVP and glycerol, the limit edged stirs, mix homogeneously is diluted to prescribed volume, gets final product.Checking this liniment to contain acyclovir through reversed-phase liquid chromatography is 5.0% (W/V), contains lignocaine 1.0% (W/V).
Embodiment 2: compound recipe acyclovir benzocaine liniment
Acyclovir 5.0g
Benzocaine 1.0g
Sodium alginate 8.0g
Glycerol 5.0g
Ethanol 60.0g
Distilled water an amount of (adding to cumulative volume is 100ml)
Preparation method: acyclovir is dissolved in the ethanol by recipe quantity, sodium alginate, glycerol, the benzocaine of recipe quantity are dissolved in an amount of distilled water, the alcoholic solution of acyclovir is slowly joined in the aqueous solution of sodium alginate and glycerol, the limit edged stirs, mix homogeneously, be diluted to prescribed volume, get final product.Checking this liniment to contain acyclovir through reversed-phase liquid chromatography is 5.0% (W/V), contains benzocaine 1.0% (W/V).
Embodiment 3: compound recipe acyclovir dyclonine gel
Acyclovir 20.0g
Dyclonine 10.0g
Cross linked sodium polyacrylate (SDB-L-400) 10.0g
PEG-4000 80.0g
Glycerol 100.0g
Benzalkonium bromide 10.0ml
Distilled water adds to 1000g
Preparation method: take by weighing PEG-400, glycerol and put the beaker slight fever to dissolving fully, add acyclovir, dyclonine mixing, after in mortar, grinding well in the SDB-L-400 adding 800ml water (60 ℃), with substrate and PEG-400, glycerol, acyclovir, dyclonine mixing, add water to 1000g, promptly, this product is a hydrophilic gel, through check, this product content is that every 10g gel contains acyclovir 0.2g, dyclonine 0.1g, gained gel viscosity (insertion degree 265) is qualified, and coating has good uniformity.
Embodiment 4: the Compound Ribavirin dyclonine
Ribavirin 50.0g
Dyclonine 50.0g
Cross linked sodium polyacrylate (SDB-L-400) 10.0g
PEG-4000 80.0g
Glycerol 100.0g
Benzalkonium bromide 10.0ml
Distilled water adds to 1000g
Preparation method: take by weighing PEG-400, glycerol and put the beaker slight fever to dissolving fully, add ribavirin, dyclonine mixing, after in mortar, grinding well in the SDB-L-400 adding 800ml water (60 ℃), with substrate and PEG-400, glycerol, acyclovir, dyclonine mixing, add water to 1000g, promptly, this product is a hydrophilic gel, through check, this product content is that every 10g gel contains ribavirin 0.5g, dyclonine 0.5g, gained gel viscosity (insertion degree 265) is qualified, and coating has good uniformity.
Embodiment 5: compound recipe valaciclovir lignocaine liniment
Valaciclovir 5.0g
Lignocaine 0.5g
Sodium alginate 8.0g
Glycerol 5.0g
Ethanol 60.0g
Distilled water an amount of (adding to cumulative volume is 100ml)
Preparation method: valaciclovir is dissolved in the ethanol by recipe quantity, sodium alginate, glycerol, the lignocaine of recipe quantity are dissolved in an amount of distilled water, the alcoholic solution of valaciclovir is slowly joined in the aqueous solution of sodium alginate and glycerol, the limit edged stirs, mix homogeneously, be diluted to prescribed volume, get final product.Checking this liniment to contain valaciclovir through reversed-phase liquid chromatography is 5.0% (W/V), contains lignocaine 1.0% (W/V).
Embodiment 6: the skin irritation test
Experimental animal: Japan large rabbit 20 examples (Beijing Zhaoyan New Drug Research Center's experimental animal room provides)
Experimental technique: get compound recipe acyclovir lignocaine liniment 0.5ml, evenly coat rabbit and do not have on the fur skin, observe in the 72h.
The result: show speckle edema etc. does not stimulate phenomenon.
Conclusion: nonirritant.
Embodiment 7: acute eye irritation test
Experimental animal: Japan large rabbit 20 examples (Beijing Zhaoyan New Drug Research Center's experimental animal room provides)
Test method: get compound recipe acyclovir lignocaine liniment 0.1ml, slowly splash in the rabbit conjunctival of getting home, the about 1s of eyelid that gently sleeps then, an other eye does not deal with, in contrast.
The result: cornea, iris, to estimate film all normal, do not see any irritative symptoms.
Conclusion: nonirritant.
Embodiment 8: the local anesthesia experiment
Experimental animal: selecting body weight for use is male guinea pig (Beijing Zhaoyan New Drug Research Center's experimental animal room provides) about 300～350g, two every group, shaves clean its back hair, one in the hair of positive middle front part skin, all 3cm
2About make skin region exposed.
Test method: Cavia porcellus is used etherization, and the volt position is fixed on the operating-table.Damage this place's skin with the scratch method.With compound recipe acyclovir lignocaine liniment, be applied to 10 minutes after, adopt the skin pain sensation reaction (thorn test place skin region has shrinkage phenomenon when remaining as the pain sensation) of lancing test agents area to compare different pharmaceutical pain sensation reaction times in the ratio of testing time, adopt distilled water as negative control simultaneously, 0.2% lidocaine ointment the results are shown in following table as positive control
Result of the test: testing time pain sensation reaction times ratio (%) the results are shown in following table.
The local anesthesia result of the test
Testing time pain paradoxical reaction number of times ratio (%) compound recipe acyclovir lignocaine liniment 12 00 distilled water 12 12 100 lidocaine ointments 12 1 8.3
Conclusion: compound recipe acyclovir lignocaine liniment local anesthesia effect is obvious.
Embodiment 9: clinical treatment observation
Case and grouping: collect case 20 examples, the affected part all is positioned at the intercostal nerves district, is divided into two groups of A, B at random, every group 10 example.
Test sample: compound recipe acyclovir lignocaine liniment
Positive reference substance: Ah Cao Lip river Wei ointment (3%)
Therapeutic Method: therefrom mind-set external spiral formula is cleaned wound surface, wound surface periphery with 75% alcohol disinfecting with the normal saline cotton balls on the herpes surface, the reuse asepsis injector is extracted herpes surface vesicle gently out, embrocates the affected part with compound recipe acyclovir lignocaine liniment, acyclovir ointment respectively again.
Curative effect and criterion as a result:
Produce effects: be coated with the back 0.5～1d that applies medicinal lotion or ointment, play is itched or pain disappears, the very fast atrophy of herpes, and vesicle reduces subsequent drying gradually, incrustation, 3～4d cures.
Effectively: be coated with the back 1～2d that applies medicinal lotion or ointment, play is itched or pain relief, and it is few that vesicle is subdued, but at it other or near the position new focus appears again, 4～5 recoveries from illness continue to change dressings.
The clinical treatment observation result: the result shows that use compound recipe acyclovir lignocaine liniment obviously reduces varicella zoster virus patient's pain, brings into play the antivirus action of acyclovir simultaneously, increases patient's compliance, and patient is generally reflected well.
Example digital display effect enabledisable zest compound recipe acyclovir lignocaine group 10 examples 91 0-acyclovir group 10 examples 73 0+
Annotate: " " after the expression medication, pain alleviates immediately, and does not have obvious irritation in whole therapeutic process, in the therapeutic process after "+" expression medication obvious irritation is arranged.
Claims (8)
1, a kind of pharmaceutical composition that is used for the treatment of the topical of herpes zoster is characterized in that: this pharmaceutical composition is made up of one or more antiviral drugs and one or more local anesthetics and pharmaceutical carrier.
2, pharmaceutical composition according to claim 1 is characterized in that: described antiviral drug is acyclovir, ribavirin, valaciclovir.
3, pharmaceutical composition according to claim 1 and 2 is characterized in that: described local anesthetic is tetracaine, tetracaine, lignocaine, dyclonine, procaine and benzocaine, and with the anesthetis of the form of salt.
4, pharmaceutical composition according to claim 3 is characterized in that: the content of described antiviral drug is 0.1wt%～10wt%, and the content of local anesthetic is 0.1wt%～5.0wt%, the pharmaceutical carrier surplus.
5, pharmaceutical composition according to claim 4 is characterized in that: described pharmaceutical composition is a liniment, and described pharmaceutical carrier is polymer substance, plasticizer and solvent.
6, pharmaceutical composition according to claim 5 is characterized in that: described polymer substance is one or more in sodium alginate, polyvinylpyrrolidone (PVP) and the Polyethylene Glycol (PEG).
7, pharmaceutical composition according to claim 6 is characterized in that: described plasticizer is a glycerol.
8, pharmaceutical composition according to claim 7 is characterized in that: described solvent comprises distilled water or ethanol or alcoholic acid aqueous solution.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02146255 CN1221264C (en) | 2002-10-17 | 2002-10-17 | Pharmic compsn. of local administration for treating herpes zoster |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02146255 CN1221264C (en) | 2002-10-17 | 2002-10-17 | Pharmic compsn. of local administration for treating herpes zoster |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1415297A true CN1415297A (en) | 2003-05-07 |
| CN1221264C CN1221264C (en) | 2005-10-05 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 02146255 Expired - Fee Related CN1221264C (en) | 2002-10-17 | 2002-10-17 | Pharmic compsn. of local administration for treating herpes zoster |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1221264C (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104415050A (en) * | 2013-08-31 | 2015-03-18 | 何伊仁 | External spray for treating viral herpes |
| CN104434885A (en) * | 2014-11-12 | 2015-03-25 | 天津大学 | Water-soluble polymeric membrane capable of quickly releasing drugs and preparation method thereof |
| CN104922130A (en) * | 2015-05-22 | 2015-09-23 | 济南新斯诺生物技术有限公司 | Gel for treating herpes zoster and preparation method thereof |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20240197670A1 (en) * | 2022-12-19 | 2024-06-20 | Pagari Life Science Corp | Treatment of herpes zoster with topical tetracaine |
-
2002
- 2002-10-17 CN CN 02146255 patent/CN1221264C/en not_active Expired - Fee Related
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104415050A (en) * | 2013-08-31 | 2015-03-18 | 何伊仁 | External spray for treating viral herpes |
| CN104434885A (en) * | 2014-11-12 | 2015-03-25 | 天津大学 | Water-soluble polymeric membrane capable of quickly releasing drugs and preparation method thereof |
| CN104922130A (en) * | 2015-05-22 | 2015-09-23 | 济南新斯诺生物技术有限公司 | Gel for treating herpes zoster and preparation method thereof |
| CN104922130B (en) * | 2015-05-22 | 2018-05-01 | 济南新斯诺生物技术有限公司 | It is a kind of to be used to treat gelling agent of herpes zoster and preparation method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1221264C (en) | 2005-10-05 |
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