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Compositions For Delivering Acyclovir

a technology of compositions and acyclovir, applied in the field of acyclovir formulations, can solve the problems of inability to respond to acyclovir therapy, inability to improve the bioavailability of acyclovir, and difficulty in compliance with oral acyclovir formulations

Inactive Publication Date: 2008-06-05
NOVO NORDISK NORTH AMERICA OPERATIONS AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0010]The present invention provides a composition (e.g., a pharmaceutical composition) comprising (a) at least one delivery agent compound and (b) acyclovir or a salt, ester, or prodrug thereof. Preferably, the composition includes a therapeutically effective amount of acyclovir and the delivery agent compound. The composition of the present invention facilitates the delivery of acyclovir and increases its bioavailability compared to administration without the delivery agent compound. The composition is particularly well suited for oral administration. Preferably, the composition provides bioavailability (i.e., AUC) substantially equivalent to the current acyclovir formulations marketed as Zovirax® (U.S. FDA NDA No. 18828, 19909, or 20089) when:

Problems solved by technology

Failure to respond to acyclovir therapy may arise from an inadequate dose (frequency of dose or total daily dose); patient noncompliance; malabsorption in the intestine; or, resistant viral strains.
The need for readily absorbed oral antiviral agents has been identified as imperative for treatment of viral diseases to both patient populations since long term IV treatment is restrictive and compliance with currently available oral acyclovir formulations is difficult.
The tablets, however, do not improve the bioavailability of the acyclovir.
Although, previous attempts have been made to improve the delivery and bioavailability of acyclovir, these attempts have had limited success.

Method used

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  • Compositions For Delivering Acyclovir
  • Compositions For Delivering Acyclovir
  • Compositions For Delivering Acyclovir

Examples

Experimental program
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Effect test

example 1

Solid Oral Delivery of Acyclovir in Rats

[0136]The dose of Acyclovir used was 25 mg / kg body weight. The dose of delivery agent was either 50 or 75 mg / kg body weight.

[0137]Approximately 6.25 mg / tablet of acyclovir was blended with either 12.5 or 18.75 mg / tablet (50 and 75 mg / kg, respectively) of delivery agent compound. Upper punch, lower punch and die of a Carver 4350 manual pellet press with a Caplet shape model sold by Natoli Engineering Company, Inc. were treated with magnesium stearate (0.1%). Approximately 6.25 mg (Acyclovir alone), 18.75 mg (Acyclovir+50 mg / kg delivery agent compound), or 25 mg (Acyclovir+75 mg / kg delivery agent compound) of mixed powder was fed into the die and a mini bead shape tablet was made at about 1000 PSI bar pressure. The resulting solid dosage forms were 2.65 mm in diameter and approximately 8.40 mm in length for the 25 mg tablets, 6.3 mm in length for the 18.75 mg tablets, and 2.1 mm in length for the 6.25 mg tablets.

[0138]Male Sprague Dawley rats (˜...

example 2

Delivery of Acyclovir in Dogs

[0141]Six different oral dosage forms (tablets) were administered to dogs: (1) unitary solid oral dosage forms comprising 80 mg of acyclovir and 240 mg of the delivery agent, the monosodium salt of N-(8-[2-hydroxybenzoyl]-amino)caprylic acid (SNAC), (2) a solid oral dosage form comprising 400 mg of acyclovir (Zovirax™, commercially available from GlaxoSmithKline), (3) a solid oral dosage form comprising 800 mg dosage of (Zovirax™, commercially available from GlaxoSmithKline), (4) a solid oral dosage form comprising 500 mg dosage of valacyclovir (Valtrex™, commercially available from GlaxoSmithKline) and (6) unitary solid oral dosage comprising 240 mg of acyclovir and 240 mg of the delivery agent SNAC. Oral administration of acylcovir alone and with a delivery agent was compared to an interveneous dosage form comprising 80 mg of acyclovir (Zovirax™ for injection, commercially available from GlaxoSmithKline).

[0142]Unitary dosages of acyclovir and delivery ...

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Abstract

The present invention relates to an acyclovir formulation having improved bioavailability resulting in better efficacy and / or requiring less frequent administration.

Description

[0001]This application claims the benefit of U.S. Provisional Application No. 60 / 573,003, filed May 19, 2004, which is hereby incorporated by reference.FIELD OF THE INVENTION[0002]The present invention relates to an acyclovir formulation having improved bioavailability resulting in improved efficacy and / or requiring less frequent administration.BACKGROUND OF THE INVENTION[0003]Acyclovir (9-((2-hydroxyethoxy)methyl)guanine) is an antiviral which inhibits human herpes viruses, including herpes simplex types 1 (HSV-1) and 2 (HSV-2), varicella zoster, Epstein-Barr virus (EBV) and cytomegalovirus (CMV). The inhibitory activity of acyclovir is highly selective for these viruses. O'Brien and Campoli-Richards, Drugs, 37:233-309 (1989). The chemical composition of acyclovir is reported in Shaffer, et al. (J. Med. Chem. 14:367 (1971)), U.S. Pat. No. 4,199,574, and UK Patent Specification No. 1,523,865, all of which are hereby incorporated by reference.[0004]Acyclovir has been demonstrated to ...

Claims

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Application Information

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IPC IPC(8): A61K31/522A61P31/12
CPCA61K9/0019A61K9/08A61K47/18A61K31/522A61K47/12A61K9/2013A61P11/00A61P15/00A61P27/02A61P31/12A61P31/22A61P35/00A61P43/00A61K47/14
Inventor ADAMS, AMY C.SINGH, BRAHMA N.DHOOT, NIKHILMAJURU, SHINGAI
Owner NOVO NORDISK NORTH AMERICA OPERATIONS AS
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