Dissolution Testing for Bioavailability of Over-the-Counter (OTC) Drugs—a Technical Note

Gao, Ziwen; Yu, Lawrence X.; Clark, Stephanie; Trehy, Mike; Moore, Terry W.; Westenberger, Benjamin J.; Buhse, Lucinda F.; Kauffman, John F.; Bishop, B.; Velazquez, Lydia; Furness, Scott

doi:10.1208/s12249-015-0297-x

Cited by 6 publications

(4 citation statements)

References 8 publications

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“…Therefore, its solubility and ionization are reduced at alkaline pH and increased at acidic pH. This may be due to the conversion of the hydrochloride salt to its less soluble free base [ 15 ]. Similar pH dependent Meclizine HCl release was also observed by Mahrous et al [ 2 ].…”

Section: Discussionmentioning

confidence: 99%

“…Meclizine HCl, a Biopharmaceutics classification system (BCS) class II agent, is attributed with low solubility and high permeability [15]. Increased bioavailability and prolonged drug delivery of Meclizine HCl can be achieved by preparation of lipids bearing extruded-spheronized pellets because of the resemblance of lipids to in vivo components and its unique set of physiochemical properties [16].…”

Section: Introductionmentioning

confidence: 99%

“…In oral drug delivery system, lipids are successfully used to enhance swallowability, shelf life, provision of modified release profiles, taste masking, reduction of gastric irritation and to improve bioavailability of poorly soluble drugs [ 14 ]. Meclizine HCl, a Biopharmaceutics classification system (BCS) class II agent, is attributed with low solubility and high permeability [ 15 ]. Increased bioavailability and prolonged drug delivery of Meclizine HCl can be achieved by preparation of lipids bearing extruded-spheronized pellets because of the resemblance of lipids to in vivo components and its unique set of physiochemical properties [ 16 ].…”

Section: Introductionmentioning

confidence: 99%

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Lipids bearing extruded-spheronized pellets for extended release of poorly soluble antiemetic agent—Meclizine HCl

et al. 2017

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BackgroundAntiemetic agent Meclizine HCl, widely prescribed in vertigo, is available only in immediate release dosage forms. The approved therapeutic dose and shorter elimination half-life make Meclizine HCl a potential candidate to be formulated in extended release dosage form. This study was aimed to develop extended release Meclizine HCl pellets by extrusion spheronization using natural and synthetic lipids. Influence of lipid type, drug/lipid ratio and combinations of different lipids on drug release and sphericity of pellets were evaluated.MethodsThirty two formulations were prepared with four different lipids, Glyceryl monostearate (Geleol®), Glyceryl palmitostearate (Precirol®), Glyceryl behenate (Compritol®) and Carnauba wax, utilized either alone or in combinations of drug/lipid ratio of 1:0.5–1:3. Dissolution studies were performed at variable pH and release kinetics were analyzed. Fourier transform infrared spectroscopy was conducted and no drug lipid interaction was found.ResultsSphericity indicated by shape factor (eR) varied with type and concentration of lipids: Geleol® (eR = 0.891–0.997), Precirol® (eR = 0.611–0.743), Compritol® (eR = 0.665–0.729) and Carnauba wax (eR = 0.499-0.551). Highly spherical pellets were obtained with Geleol® (Aspect ratio = 1.005–1.052) whereas irregularly shaped pellets were formed using Carnauba wax (Aspect ratio = 1.153–1.309). Drug release was effectively controlled by three different combinations of lipids: (i) Geleol® and Compritol®, (ii) Geleol® and Carnauba wax and (iii) Geleol®, Compritol® and Carnauba wax. Scanning electron microscopy of Compritol® pellets showed smooth surface with pores, whereas, irregular rough surface with hollow depressions was observed in Carnauba wax pellets. Energy dispersive spectroscopy indicated elemental composition of lipid matrix pellets. Kinetics of (i) Geleol® and Compritol® pellets, explained by Korsmeyer-Peppas (R2 = 0.978–0.993) indicated non-Fickian diffusion (n = 0.519-0.597). Combinations of (ii) Geleol® and Carnauba wax and (iii) Geleol®, Compritol® and Carnauba wax pellets followed Zero-order (R2 = 0.991–0.995). Similarity test was performed using combination of Geleol® and Compritol® (i) as a reference.ConclusionsMatrices for the extended release of Meclizine HCl from extruded-spheronized pellets were successfully formed by using three lipids (Geleol®, Compritol® and Carnauba wax) in different combinations. The encapsulated pellets of Meclizine HCl can be effectively used for treatment of motion sickness, nausea and vertigo for extended period of time.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Lipids bearing extruded-spheronized pellets for extended release of poorly soluble antiemetic agent—Meclizine HCl

et al. 2017

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“…AAP is the most widely used non-prescription analgesic globally and is considered safe in therapeutic doses producing negligible therapeutically significant drug interaction even though overdose can cause hepatotoxicity [ 3 , 4 ]. AAP is categorized as Biopharmaceutical Classification System (BCS) class I, which is highly soluble and highly permeable [ 5 , 6 , 7 , 8 ]. The absorption of BCS class I drugs can be influenced mainly by gastric emptying rate rather than dissolution or formulation parameters unless the dissolution rate is slower than gastric emptying time [ 9 ].…”

Section: Introductionmentioning

confidence: 99%

Bioavailability of the Common Cold Medicines in Jellies for Oral Administration

Kim¹,

Jun²,

Lee

2020

Pharmaceutics

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Jellies for oral administration have been suggested as alternative dosage forms to conventional tablets for improved palatability and compliances for pediatric and geriatric patients. To evaluate the effect of jelly formulation on the bioavailability of cold medicines, two types of jellies were prepared for a fixed-dose combination of acetaminophen (AAP), chlorpheniramine maleate (CPM), dextromethorphan hydrobromide (DMH), and dl-methylephedrine hydrochloride (MEH). Jelly-S and Jelly-H were fabricated using carrageenan and locust bean gum in the absence and presence of xanthan gum, respectively. In vitro dissolution and in vivo absorption of the four drugs in the jellies were compared with other conventional formulations, a syrup and two types of immediate-release (IR) tablets with different hardness, Tablet-S (15 kPa) and Tablet-H (20 kPa). All the formulations exhibited more than 80% dissolution rate within 2 h even though the syrup, Jelly-S, and Tablet-S showed higher 30-min dissolution compared to Jelly-H and Tablet-H. The dissolution rates from the jellies decreased with increasing pH, which resulted in the slowest dissolution in pH 6.8 compared to the syrup and IR tablets. When administered orally to beagle dogs, all five formulations were determined not to be bioequivalent. However, Jelly-S and Jelly-H showed 0.82–1.05 of the geometric mean ratios (GMRs) of AUC0-t for all four drugs compared to the syrup suggesting comparable absorption. In two IR tablets, GMRs of AUC0-t were in a range of 0.55–0.95 indicating a tendency of lower absorption than the syrup and jellies. In conclusion, jelly can be a patient-centered formulation with comparable bioavailability to syrup.

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Comprehensive study of medications solubility in supercritical CO2 with and without co-solvent; Laboratory, theoretical, and intelligent approaches

Hsu,

Jasim,

Bansal

et al. 2024

Journal of Molecular Liquids

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Dissolution Testing for Bioavailability of Over-the-Counter (OTC) Drugs—a Technical Note

Cited by 6 publications

References 8 publications

Lipids bearing extruded-spheronized pellets for extended release of poorly soluble antiemetic agent—Meclizine HCl

Lipids bearing extruded-spheronized pellets for extended release of poorly soluble antiemetic agent—Meclizine HCl

Bioavailability of the Common Cold Medicines in Jellies for Oral Administration

Comprehensive study of medications solubility in supercritical CO2 with and without co-solvent; Laboratory, theoretical, and intelligent approaches

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