• Journal of Pharmaceutical Investigation
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• v.36 no.6
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• pp.393-399
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• 2006

This study was aimed to design, formulate and characterize the moisture-activated patches containing acyclovir for antiviral action. Gel intermediates for film-type patches were prepared with mucoadhesive polymer, viscosity builders, enhancers and acyclovir. Patches containing acyclovir were characterized by in vitro measurement of drug release rates through a cellulose barrier membrane, and of drug flux through the hairless mouse skin. Film-type patches obtained were uniform in the thickness and showed a mucoadhesive property when contacted with moisture. The formulation was optimized, which consisted of $Cantrez^{\circledR}$ AN-169(2%), $Kollidon^{\circledR}$ VA 64(1%), $Natrosol^{\circledR}$(1%), hydroxypropyl-$\beta$-cyclodextrin(1%) and dimethylsulfoxide(0.5%). Release rates of acyclovir patches increased dose-dependently. The addition of terpenes such as d-limonene or cineole increased release rates of acyclovir, but decreased permeation rates. The permeation rates were enhanced by 2 and 2.5 times by the addition of glycyrrhizic acid ammonium salt and sodium glycocholate, respectively, compared with that of no enhancer. These results suggest that it may be feasible to deliver acyclovir through the skin or gingival mucosa from the moisture-activated patches.

• Clinical and Experimental Pediatrics
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• v.46 no.9
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• pp.939-943
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• 2003

Neonatal herpes simplex virus(HSV) infections result in significant morbidity and mortality. Although acyclovir treatment has improved survival, severe neurological sequelae can occur in the majority of survivors. HSV infections limited to the skin, eyes and mouth(SEM) can cause neurologic impairment. A direct correlation exists between the development of neurologic deficits and the frequency of cutaneous HSV recurrences. National Institutes of Allergy and Infectious Diseases(NIAID) Collaborative Antiviral Study Group conducted a phase I/II trial of continuous oral acyclovir therapy for the suppression of cutaneous recurrences. We describe a preterm infant who had two recurrences after neonatal SEM disease had been treated with intravenous acyclovir, and there were no more recurrences after continuous oral acyclovir suppressive therapy for six months. We report this case with a review of related literature.

• Annals of Clinical Neurophysiology
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• v.3 no.2
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• pp.122-127
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• 2001

Background : Bell's palsy(BP) is defined as an idiopathic peripheral facial paralysis of sudden onset and account more than 50% of facial paralysis. It's etiology is unclear, but herpes simplex virus type-1(HSV-1) has been the most suspicious causative agent of BP that ever been studied. We evaluated the effect of add-on acyclovir in acute stage of BP. Methods : Subject consisted of 35 patients who developed acute idiopathic unilateral facial nerve palsy(16 men and 19 women with age 9-78 years old). The treatments were started within 10 days after onset of BP. Facial nerve function was assessed by the House-Brackman facial nerve grading scale and facial nerve conduction study including blink reflex. Follow-up evaluation were made 2 month after onset. Twenty of 35 patients were treated with combined therapy of acyclovir and prednisone. As a control group, 15 patients were treated with prednisone only. We compared the improvement of neurologic defects at recovery phase. Results : Compared with two groups, difference in grading scale at recovery phase is statistically significant(p<0.01). So, acyclovir-prednisone group showed a significant improvement in grading scale at recovery phase compared with prednisone group. Conclusion : We identified the benefits of add-on acyclovir in the acute stage of BP.

• YAKHAK HOEJI
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• v.34 no.3
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• pp.155-160
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• 1990

An oral adhesive tablet of acyclorir [9-(2-hydroxyethoxymethyl) guanine] for herpetic stomatitis was prepared and its physical properties were evaluated. 300 mg weighed tablets containing 30 mg of acyclovir were prepared with six kinds of polymers from direct compression, and the stickiness, fracture resistance and dissolution in pH 6.8 buffer solution were tested. HPMC and MC showed good stickiness and fracture resistance, and their dissolution rates were significantly different from each other. Three factors-HPMC:MC ratio, acyclovir content, compression force-were chosen as an important factor of manufacture and factorial analyses for these three factors were carried out. Eight kinds of formulations from different combination of three factors were prepared and tested in stickiness, fracture resistance and dissolution in pH 6.8 buffer solution. Dissolution rate was significantly affected by polymer ratio, fracture resistance was affected by compression force, and stickiness was not significantly affected by acyclovir content and polymer ratio.

• Journal of Pharmaceutical Investigation
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• v.23 no.3
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• pp.139-144
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• 1993

Microencapsulation of acyclovir, an effective antiviral agent which acts as a specific inhibitor of herpes DNA polymerase, by carbopol-gelatin complex coacervation has been carried out to develop an oral controlled release preparation, which could improve the absorption characteristics in GI tract. After dissolving carbopol and gelatin separately in distilled water at $40^{\circ}C$, gelatin solution was mixed with carbopol solution while stirring at the same temperature. The pH of the mixture was lowered gradually by dropwise addition of 10% HCI with continuous stirring, and then, at pH 3.5, positively charged gelatin molecules were attracted to negatively charged carbopol. These coacervation processes were observed by optical microscopy during preparation. Plasma concentrations of acyclovir in rats after an oral administration of microcapsule suspension were assayed by HPLC, and pharmacokinetic parameters were calculated based on the model-independent analyses. Two standard formulations, oral solution and intravenous bolus injection, were used as references to compare the bioavailability. It has been revealed that $C_{max}$, $T_{max}$, and MRT of microcapsule suspension were greater than those of oral solution, which results in about two-fold increases in bioavailability. Therefore, in conclusion, the carbopol-gelatin microcapsule of acyclovir might be evaluated as an effective oral controlled release preparation which could increase the bioavailability of acyclovir.

• Proceedings of the PSK Conference
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• 2000.04a
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• pp.145.3-146
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• 2000

• Natural Product Sciences
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• v.5 no.2
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• pp.107-111
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• 1999

To investigate less toxic antiviral agents from Basidiomycetes, EA, the water soluble substance, was isolated from the carpophores of Elfvingia applanata (pers.) Karst. Anti-varicella zoster virus (Oka strain; anti-VZV/Oka) activity of EA was examined in MRC-5 cells by plaque reduction assay in vitro. And the combined antiviral effects of EA with nucleoside anti-VZV agents, acyclovir and vidarabine, were examined on the multiplication of VZV/Oka. EA exhibited a concentration-dependent reduction in the plaque formation of VZV/Oka with a 50% effective concentration $(EC_{50})$ of $464.14\;{\mu}g/ml$. The results of combination assay were evaluated by the combination index (CI) that was calculated by the multiple drug effect analysis. The combination of EA with acyclovir showed more potent synergism with CI values of $0.18{\sim}0.62$ for $50{\sim}90%$ effective levels than that of EA with vidarabine with CI values of $0.67{\sim}1.04$.

• Pediatric Infection and Vaccine
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• v.11 no.1
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• pp.121-125
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• 2004

Chickenpox is a common childhood infection that generally resolves without complications. But maternal chickenpox near term, or soon after delivery, can cause severe or fatal illness in the newborn. The severity of neonatal chickenpox is closely related to the time of maternal infection and the fatality is reported up to 30%. Although chickenpox is thought to be a mild disease, complications are frequent in neonates and immunocompromised children. The diagnosis of neonatal chickenpox is usually based on the typical clinical feature, the characteristic point in time and the maternal history of chickenpox. Serologic methods have been widely used to confirm clinical diagnosis. To prevent severe neonatal chickenpox, passive immunization is indicated. If varicella occurs, acyclovir treatment has to be done promptly. But the use of acyclovir in symptomatic healthy infant is controversial. We report a case of neonatal chickenpox that was infected by an asymptomatic infected mother and rapid improvement of varicella skin lesions without complications after intravenous acyclovir administration.

• Annals of Clinical Neurophysiology
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• v.15 no.1
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• pp.34-36
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• 2013

• Journal of Pharmaceutical Investigation
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• v.36 no.6
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• pp.401-403
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• 2006

Topical preparations such as cream for Acyclovir(ACV), a potent anti-viral agent for the treatment of herpes simplex and herpes zoster, have been marketed in the world since 1993. However, the skin penetration rate of ACV from generic cream formulations sold in Europe has been found to be lower than the original $Zovirax^{\circledR}$ cream. In this study, we formulated ACV into a novel organogel system and compared the skin penetration characteristics with $Zovirax^{\circledR}$ cream. The rate and amount of skin penetration of ACV from the organogels were 6.3-fold greater than those obtained with $Zovirax^{\circledR}$ at an ACV concentration of 5%. The solubilizing effect of oil phase and anti-nucleation effect exhibited by sodium alginate contained in water phase are most likely attributed to enhanced ACV skin penetration property.