Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Aciclovir

Arnal, Jean-François; González‐Álvarez, Isabel; Bermejo, Marival; Amidon, Gordon L.; Junginger, Hans E.; Kopp, Sabine; Midha, K. K.; Shah, Vinod P.; Stavchansky, Salomon A; Dressman, Jennifer B.; Barends, D. M.

doi:10.1002/jps.21392

Cited by 84 publications

(65 citation statements)

References 49 publications

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“…2 These monographs do not intend to simply apply the WHO, FDA 3 and/or EMEA Guidance, 4 but aim to apply these guidances and further serve as a critical validation of these regulatory documents. Biowaiver monographs have already been published for acetaminophen (INN: paracetamol), 5 acetazolamide, 6 aciclovir, 7 amitriptyline, 8 atenolol, 1 chloroquine, 9 cimetidine, 10 ethambutol, 11 ibuprofen, 12 isoniazid, 13 metoclopramide, prednisolone, 14 prednisone, 15 pyrazinamide, 16 propranolol, 1 ranitidine, 17 and verapamil. 1 They are also available on-line at www.fip.org/bcs.…”

Section: Introductionmentioning

confidence: 99%

Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Diclofenac Sodium and Diclofenac Potassium

Chuasuwan

Binjesoh

Polli

et al. 2009

Journal of Pharmaceutical Sciences

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144

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Literature data are reviewed regarding the scientific advisability of allowing a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing either diclofenac potassium and diclofenac sodium. Within the biopharmaceutics classification system (BCS), diclofenac potassium and diclofenac sodium are each BCS class II active pharmaceutical ingredients (APIs). However, a biowaiver can be recommended for IR drug products of each salt form, due to their therapeutic use, therapeutic index, pharmacokinetic properties, potential for excipient interactions, and performance in reported BE/bioavailability (BA) studies, provided: (a) test and comparator contain the same diclofenac salt; (b) the dosage form of the test and comparator is identical; (c) the test product contains only excipients present in diclofenac drug products approved in ICH or associated countries in the same dosage form, for instance as presented in this paper; (d) test drug product and comparator dissolve 85% in 30 min or less in 900 mL buffer pH 6.8, using the paddle apparatus at 75 rpm or the basket apparatus at 100 rpm; and (e) test product and comparator show dissolution profile similarity in pH 1.2, 4.5, and 6.8.

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Section: Introductionmentioning

confidence: 99%

Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Diclofenac Sodium and Diclofenac Potassium

Chuasuwan

Binjesoh

Polli

et al. 2009

Journal of Pharmaceutical Sciences

Self Cite

144

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“…22 In this context, it is presumed that permeation of acyclovir through the biological membrane could be relatively low. Hence, the drug was first enclosed in a biodegradable polymer (PLGA) by formulating into nanoparticles.…”

Section: Resultsmentioning

confidence: 99%

Mucoadhesive Film Embedded with Acyclovir Loaded Biopolymeric Nanoparticles: In vitro Studies

Nair¹,

Al-ghannam²,

Al‐Dhubiab³

et al. 2017

JYP

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Objective: The efficiency of acyclovir, a potent antiviral agent, is mainly limited by its low permeability.The purpose of this investigation was to formulate and assess nanoparticle impregnated buccal films to improve acyclovir permeability and thereby enhance bioavailability. Methods: Acyclovir was incorporated into the polymeric materials and formulated as nanoparticles. The prepared nanoparticles were then loaded into various films (F5-F7) prepared with varying quantities of hydroxyethyl cellulose and Eudragit RL 100. The prepared films were evaluated for physico-mechanical characters, mucoadhesion, swelling, in vitro acyclovir release and ex vivo diffusion. Results: The films so prepared showed adequate mucoadhesive strength and excellent physico-mechanical properties. Rapid hydration of films (>35%) were observed in 15 min, followed by a relatively slower phase of hydration which continued till 60 min. In vitro release profile exhibited biphasic pattern, while the rate of acyclovir release was higher with film F7. Prepared films exhibited either first order (F5, control) or Higuchi model (F6, F7) kinetics. The enhancement in acyclovir permeation in F5, F6 and F7 loaded films were 2.2, 4.1 and 6.7 folds, respectively, when compared to control. Conclusion: This study concludes that the drug loaded nanoparticles impregnated buccal film could be an alternative approach to enhance the oral bioavailability of acyclovir, and need to be proved in vivo.

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“…19 ACV is categorized as a BCS class III drug when ACV is administered at a dose of 400 mg and as a BCS class IV drug at a dose of 800 mg, due to the low permeability and limited water solubility of ACV (solubility is 2.3 mg/mL in water). 20 To enhance the low oral bioavailability of ACV, prodrugs synthesized to target SLC transporters are as follows: 5 0 -amino acid ester prodrugs, 21-23 beta-glucoside-conjugated prodrug, 24 dipeptide ester prodrugs, 25,26 and bile acideconjugated prodrugs. 27 Bile acideconjugated prodrugs of ACV were synthesized using 4 bile acids, chenodeoxycholate (CDCA), deoxycholate, cholate, and ursodeoxycholate and Val as a linker.…”

Section: Bile Acid Transportermentioning

confidence: 99%

A Minireview: Usefulness of Transporter-Targeted Prodrugs in Enhancing Membrane Permeability

Murakami

2016

Journal of Pharmaceutical Sciences

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Orally administered drugs are categorized into 4 classes depending on the solubility and permeability in a Biopharmaceutics Classification System. Prodrug derivatization is one of feasible approaches in modifying the physicochemical properties such as low solubility and low permeability without changing the in vivo pharmacological action of the parent drug. In this article, prodrug-targeted solute carrier (SLC) transporters were searched randomly by PubMed. Collected SLC transporters are amino acid transporter 1, bile acid transporter, carnitine transporter 2, glucose transporter 1, peptide transporter 1, vitamin C transporter 1, and multivitamin transporter. The usefulness of transporter-targeted prodrugs was evaluated in terms of membrane permeability, stability under acidic condition, and conversion to the parent drug. Among prodrugs collected, peptide transporter-targeted prodrugs exhibited the highest number, and some prodrugs such as valaciclovir and valganciclovir are clinically available. ATP-binding cassette efflux transporter, P-glycoprotein (P-gp), reduces the intestinal absorption of lipophilic P-gp substrate drugs, and SLC transporter-targeted prodrugs of P-gp substrate drugs circumvented the P-gp-mediated efflux transport. Thus, SLC transporter-targeted prodrug derivatization seems to be feasible approach to increase the oral bioavailability by overcoming various unwanted physicochemical properties of orally administered drugs, although the effect of food on prodrug absorption should be taken into consideration.

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Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Aciclovir

Cited by 84 publications

References 49 publications

Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Diclofenac Sodium and Diclofenac Potassium

Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Diclofenac Sodium and Diclofenac Potassium

Mucoadhesive Film Embedded with Acyclovir Loaded Biopolymeric Nanoparticles: In vitro Studies

A Minireview: Usefulness of Transporter-Targeted Prodrugs in Enhancing Membrane Permeability

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