Quality evaluation of extemporaneous delayed-release liquid formulations of lansoprazole

Melkoumov, Alexandre; Soukrati, Amina; Elkin, Igor; Forest, Jean‐Marc; Hildgen, Patrice; Leclair, Grégoire

doi:10.2146/ajhp100634

Cited by 9 publications

(5 citation statements)

References 11 publications

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“…In addition, some investigations that assessed the effects of early therapeutic interventions showed that about 55% of the infants are free of any clinical symptoms by the time they are 10 months old and this increases to 81% by 18 months old [2]. That notwithstanding, it is still vital to identify which children exhibit gastro-oesophageal reflux-associated disease to allow selection of the most effective therapy for treating the manifestations of the disease [3].…”

Section: Introductionmentioning

confidence: 99%

Effects of Cyclodextrins (β and γ) and l-Arginine on Stability and Functional Properties of Mucoadhesive Buccal Films Loaded with Omeprazole for Pediatric Patients

Khan

Boateng

2018

Polymers

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Omeprazole (OME) is employed for treating ulcer in children, but is unstable and exhibits first pass metabolism via the oral route. This study aimed to stabilize OME within mucoadhesive metolose (MET) films by combining cyclodextrins (CD) and L-arginine (L-arg) as stabilizing excipients and functionally characterizing for potential delivery via the buccal mucosa of paediatric patients. Polymeric solutions at a concentration of 1% w/w were obtained by dispersing the required weight of metolose in 20% v/v ethanol as solvent at a temperature of 40 • C using polyethylene glycol (PEG 400) (0.5% w/w) as plasticizer. The films were obtained by drying the resulting polymer solutions at in an oven at 40 • C. Textural (tensile and mucoadhesion) properties, physical form (differential scanning calorimetry (DSC), X-ray diffraction (XRD) and Fourier transform infrared (FTIR) spectroscopy), residual moisture content (thermogravimetric analysis (TGA)) and surface morphology (scanning electron microscopy (SEM)) were investigated. Optimized formulations containing OME, CDs (β or γ) and L-arg (1:1:1) were selected to investigate the stabilization of the drug. The DSC, XRD, and FTIR showed possible molecular dispersion of OME in metolose film matrix. Plasticized MET films containing OME:βCD:L-arg 1:1:1 were optimum in terms of transparency and ease of handling and therefore further functionally characterized (hydration, mucoadhesion, in vitro drug dissolution and long term stability studies). The optimized formulation showed sustained drug release that was modelled by Korsmeyer-Peppas equation, while the OME showed stability under ambient temperature conditions for 28 days. The optimized OME loaded MET films stabilized with βCD and L-arg have potential for use as paediatric mucoadhesive buccal delivery system, which avoids degradation in the stomach acid as well as first pass metabolism in the liver.

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Section: Introductionmentioning

confidence: 99%

Effects of Cyclodextrins (β and γ) and l-Arginine on Stability and Functional Properties of Mucoadhesive Buccal Films Loaded with Omeprazole for Pediatric Patients

Khan

Boateng

2018

Polymers

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“…At room temperature 10% lansoprazole loss occurred in 8 hours; while refrigerated the sample showed 4% loss in 14 days and 12% loss after 21 days. Melkoumov et al 43 also evaluated a liquid formulation of lansoprazole and found a maximum stability of 7 days when stored at 4.5–5.5°C, but an extemporaneous formulation consisting of lansoprazole microgranules in Ora-Blend maintained acceptable quality attributes when stored for only 3 days at 4.5–5.5°C. However, in both studies the sample preparations were significantly different from our work as they did not use crushed pellets for sample preparation; we used this form of raw material as it is more representative of common compounding practice.…”

Section: Resultsmentioning

confidence: 99%

Compatibility of proton pump inhibitors in a preservative-free suspending vehicle

Polonini¹,

Silva²,

Loures³

et al. 2016

Eur J Hosp Pharm

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ObjectivesTo evaluate the microbiological and physicochemical compatibility of commonly used proton pump inhibitors (PPIs) esomeprazole, lansoprazole, omeprazole and pantoprazole compounded at a single concentration using SyrSpend SF Alka and stored at refrigerated temperatures (omeprazole was also stored at room temperature because it has the most widespread use).MethodsCompatibility was assessed by measuring the per cent recovery at varying time points throughout a 90-day period. Quantification of the APIs was performed by a validated high performance liquid chromatography (HPLC-UV) method. This same assay was also used to determine the dosage content uniformity of the suspensions. Microbiological stability (‘test in use’) was assessed during 60 days and total aerobic microbial count (TAMC), total combined yeasts and moulds count (TYMC), detection of Escherichia coli and pH determination were performed. Antimicrobial effectiveness testing was determined following European Pharmacopoeia guidelines.ResultsBeyond-use dates of maximum 60 days for omeprazole (5 mg/mL), pantoprazole (3 mg/mL) and esomeprazole (3 mg/mL) were established. All suspensions that met the physicochemical criteria for stability also met the content uniformity criteria. The suspensions showed no antimicrobial efficiency against bacteria, yeasts and moulds as SyrSpend SF Alka is an unpreserved vehicle, but the ‘test in use’ showed that the suspensions can remain microbiologically stable for up to 60 days.ConclusionsSyrSpend SF Alka can be used to compound palatable (taste-masking properties) preservative-free oral suspensions with almost all commonly used PPIs.

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“…The researchers found that the oral liquid prepared extemporaneously from pantoprazole tablets in an 8.4% sodium bicarbonate solution was stable in dark glass bottles for 62 days under refrigeration conditions [ 158 ]. Melkoumov et al [ 159 ] investigated the stability of lansoprazole microgranules (Prevacid FasTab) after suspending them in the Ora-Blend ® vehicle. Ora-Blend ® is a flavored colloidal medium with slightly acidic pH.…”

Section: Ppis’ Pharmaceutical Formulations Available On the Marketmentioning

confidence: 99%

“…Ora-Blend ® is a flavored colloidal medium with slightly acidic pH. It was found that the extemporaneous formulation with lansoprazole remained stable for 3 days at 4.5–5.5 °C [ 159 ]. Ferron et al [ 160 ] reported the results of an open-label, randomized, two-period crossover study comparing the bioavailability of pantoprazole administered as a suspension in 8.4% sodium bicarbonate solution and as delayed-release tablets.…”

Section: Ppis’ Pharmaceutical Formulations Available On the Marketmentioning

confidence: 99%

Formulation of Dosage Forms with Proton Pump Inhibitors: State of the Art, Challenges and Future Perspectives

2022

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Since their introduction to pharmacotherapy, proton pump inhibitors (PPIs) have been widely used in the treatment of numerous diseases manifested by excessive secretion of gastric acid. Despite that, there are still unmet needs regarding their availability for patients of all age groups. Their poor stability hinders the development of formulations in which dose can be easily adjusted. The aim of this review is to describe the discovery and development of PPIs, discuss formulation issues, and present the contemporary solutions, possibilities, and challenges in formulation development. The review outlines the physicochemical characteristics of PPIs, connects them with pharmacokinetic and pharmacodynamic properties, and describes the stability of PPIs, including the identification of the most important factors affecting them. Moreover, the possibilities for qualitative and quantitative analysis of PPIs are briefly depicted. This review also characterizes commercial preparations with PPIs available in the US and EU. The major part of the review is focused on the presentation of the state of the art in the development of novel formulations with PPIs covering various approaches employed in this process: nanoparticles, microparticles, minitablets, pellets, bilayer, floating, and mucoadhesive tablets, as well as parenteral, transdermal, and rectal preparations. It also anticipates further possibilities in the development of PPIs dosage forms. It is especially addressed to the researchers developing new formulations containing PPIs, since it covers the most important formulary issues that need to be considered before a decision on the selection of the formula is made. It may help in avoiding unnecessary efforts in this process and choosing the best approach. The review also presents an up-to-date database of publications focused on the pharmaceutical technology of formulations with PPIs.

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Quality evaluation of extemporaneous delayed-release liquid formulations of lansoprazole

Abstract: An extemporaneous formulation consisting of lansoprazole microgranules in Ora-Blend maintained acceptable quality attributes when stored for three days at 4.5-5.5 °C.

Cited by 9 publications

References 11 publications

Effects of Cyclodextrins (β and γ) and l-Arginine on Stability and Functional Properties of Mucoadhesive Buccal Films Loaded with Omeprazole for Pediatric Patients

Effects of Cyclodextrins (β and γ) and l-Arginine on Stability and Functional Properties of Mucoadhesive Buccal Films Loaded with Omeprazole for Pediatric Patients

Compatibility of proton pump inhibitors in a preservative-free suspending vehicle

Formulation of Dosage Forms with Proton Pump Inhibitors: State of the Art, Challenges and Future Perspectives

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