Tags

Type your tag names separated by a space and hit enter

Indinavir-loaded pH-sensitive microparticles for taste masking: toward extemporaneous pediatric anti-HIV/AIDS liquid formulations with improved patient compliance.
AAPS PharmSciTech. 2009; 10(1):1-6.AP

Abstract

The aim of this work was to develop indinavir pediatric anti-HIV/AIDS formulations enabling convenient dose adjustment, ease of oral administration, and improved organoleptic properties by means of the generation of drug-loaded microparticles made of a polymer that is insoluble under intake conditions and dissolves fast in the stomach in order to completely release the active agent. Indinavir-loaded microparticles made of a pH-dependent polymeric excipient soluble at pH < 5, Eudragit E100, were prepared using a double emulsion solvent diffusion technique and the in vitro release profiles characterized. Finally, taste masking properties were evaluated in blind randomized sensory experiments by ten healthy human volunteers. The use of a w/o/o emulsion system resulted in indinavir loads around 90%. Thermal analysis of the microparticles by differential scanning calorimetry revealed that indinavir appeared mainly dispersed at the molecular level. Concentrations of residual organic solvents as determined by gas chromatography were below the upper limits specified by the European Pharmacopeia for pharmaceutical oral formulations. Then, the behavior of drug-containing microparticles in aqueous media at different pH values was assessed. While they selectively dissolved in gastric-like medium, in tap water (intake conditions), the matrix remained almost unchanged and efficiently prevented drug dissolution. Finally, sensoring taste tests performed by volunteers indicated that systems with indinavir loads approximately 15% displayed acceptable taste. This work explored the production of indinavir-containing microparticles based on a common pharmaceutical excipient as a means for the improvement of medicines of drugs involved in the treatment of HIV/AIDS. For systems containing about 15% drug, taste studies confirmed the acceptability of the formulation. In pediatric regimes, this composition would require an acceptable amount of formulation (0.7-1.5 g).

Links

PMC Free PDF
PMC Free Full Text

Authors+Show Affiliations

Chiappetta DA
Department of Pharmaceutical Technology, Faculty of Pharmacy and Biochemistry, University of Buenos Aires, 956 Junín Street, Buenos Aires, CP1113, Argentina.
Carcaboso AM
No affiliation info available
Bregni C
No affiliation info available
Rubio M
No affiliation info available
Bramuglia G
No affiliation info available
Sosnik A
No affiliation info available

MeSH

AcrylatesAdministration, OralCalorimetry, Differential ScanningChemistry, PharmaceuticalChildDrug CarriersDrug CompoundingEmulsionsGastric JuiceHIV Protease InhibitorsHumansHydrogen-Ion ConcentrationIndinavirKineticsMedication AdherenceParticle SizePilot ProjectsPolymersSolubilityTasteTechnology, Pharmaceutical

Pub Type(s)

Journal Article
Randomized Controlled Trial
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

19127436

Citation

Chiappetta, Diego A., et al. "Indinavir-loaded pH-sensitive Microparticles for Taste Masking: Toward Extemporaneous Pediatric anti-HIV/AIDS Liquid Formulations With Improved Patient Compliance." AAPS PharmSciTech, vol. 10, no. 1, 2009, pp. 1-6.
Chiappetta DA, Carcaboso AM, Bregni C, et al. Indinavir-loaded pH-sensitive microparticles for taste masking: toward extemporaneous pediatric anti-HIV/AIDS liquid formulations with improved patient compliance. AAPS PharmSciTech. 2009;10(1):1-6.
Chiappetta, D. A., Carcaboso, A. M., Bregni, C., Rubio, M., Bramuglia, G., & Sosnik, A. (2009). Indinavir-loaded pH-sensitive microparticles for taste masking: toward extemporaneous pediatric anti-HIV/AIDS liquid formulations with improved patient compliance. AAPS PharmSciTech, 10(1), 1-6. https://doi.org/10.1208/s12249-008-9168-z
Chiappetta DA, et al. Indinavir-loaded pH-sensitive Microparticles for Taste Masking: Toward Extemporaneous Pediatric anti-HIV/AIDS Liquid Formulations With Improved Patient Compliance. AAPS PharmSciTech. 2009;10(1):1-6. PubMed PMID: 19127436.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Indinavir-loaded pH-sensitive microparticles for taste masking: toward extemporaneous pediatric anti-HIV/AIDS liquid formulations with improved patient compliance. AU - Chiappetta,Diego A, AU - Carcaboso,Angel M, AU - Bregni,Carlos, AU - Rubio,Modesto, AU - Bramuglia,Guillermo, AU - Sosnik,Alejandro, Y1 - 2009/01/06/ PY - 2008/05/21/received PY - 2008/11/21/accepted PY - 2009/1/8/entrez PY - 2009/1/8/pubmed PY - 2009/6/24/medline SP - 1 EP - 6 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 10 IS - 1 N2 - The aim of this work was to develop indinavir pediatric anti-HIV/AIDS formulations enabling convenient dose adjustment, ease of oral administration, and improved organoleptic properties by means of the generation of drug-loaded microparticles made of a polymer that is insoluble under intake conditions and dissolves fast in the stomach in order to completely release the active agent. Indinavir-loaded microparticles made of a pH-dependent polymeric excipient soluble at pH < 5, Eudragit E100, were prepared using a double emulsion solvent diffusion technique and the in vitro release profiles characterized. Finally, taste masking properties were evaluated in blind randomized sensory experiments by ten healthy human volunteers. The use of a w/o/o emulsion system resulted in indinavir loads around 90%. Thermal analysis of the microparticles by differential scanning calorimetry revealed that indinavir appeared mainly dispersed at the molecular level. Concentrations of residual organic solvents as determined by gas chromatography were below the upper limits specified by the European Pharmacopeia for pharmaceutical oral formulations. Then, the behavior of drug-containing microparticles in aqueous media at different pH values was assessed. While they selectively dissolved in gastric-like medium, in tap water (intake conditions), the matrix remained almost unchanged and efficiently prevented drug dissolution. Finally, sensoring taste tests performed by volunteers indicated that systems with indinavir loads approximately 15% displayed acceptable taste. This work explored the production of indinavir-containing microparticles based on a common pharmaceutical excipient as a means for the improvement of medicines of drugs involved in the treatment of HIV/AIDS. For systems containing about 15% drug, taste studies confirmed the acceptability of the formulation. In pediatric regimes, this composition would require an acceptable amount of formulation (0.7-1.5 g). SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/19127436/Indinavir_loaded_pH_sensitive_microparticles_for_taste_masking:_toward_extemporaneous_pediatric_anti_HIV/AIDS_liquid_formulations_with_improved_patient_compliance_ L2 - https://dx.doi.org/10.1208/s12249-008-9168-z DB - PRIME DP - Unbound Medicine ER -