Development and validation of dissolution test for lopinavir, a poorly water-soluble drug, in soft gel capsules, based on in vivo data

Lercanidipine hydrochloride (HCl) is L-type calcium channel blocker widely used in the management of hypertension. According to the BCS classification system, it is classified under BCS class II drugs, showing low solubility and high permeability. The dissolution profile and thus the in vivo performance of this class of drugs widely depend on their solubility and hence their behaviour in dissolution medium. Lercanidipine HCl is not official in any pharmacopeia, so no official dissolution method is available. The present work is mainly focussed on development and validation of a dissolution test that can be used as a quality control test for lercanidipine HCl tablets and formulations. Saturation solubility and sink conditions that can be achieved in different media suggested that 0.1 N HCl, acetate buffer pH 4.5, and phosphate buffer pH 6.8 can be used as a dissolution medium. Dissolution tests of lercanidipine HCl tablets were carried out in these different media at different rotation speeds using a USP type II (paddle) apparatus. The most suitable dissolution conditions were 0.1 N HCl pH 1.2 (900 mL at 37 ± 0.5 °C) as a dissolution medium and a paddle apparatus at 100 rpm for 60 min. The analysis of released lercanidipine HCl was done by ultraviolet spectrophotometry. The developed method was validated according to ICH guidelines. This method showed linearity with an r 2 value of 0.999 within the concentration range of 2-20 µg/mL. The method was found to be accurate with recoveries ranging from 98.50% to 103.72%. The interday and intraday precision was below RSD 2%. The developed method can effectively be used for quality control evaluation of lercanidipine HCl tablets.

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“…After selecting the optimum dissolution test conditions, the dissolution method was validated (26,27).…”

Section: Validation Of Dissolution Methodsmentioning

confidence: 99%

Dissolution Method Development and Validation for Lercanidipine Hydrochloride Tablets

Shaikh¹,

Patel²,

Patel³

et al. 2018

Dissolution Technol.

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“…The author concluded that BCS class-II compounds will behave as class-I compounds when administered in optimized SMEDDS formulation. Similar Level A IVIVC correlations were established for various poorly water-soluble drugs such as ritonavir and lopinavir administered as lipid formulations in soft gelatin capsules 90 , 91 . Various IVIVC examples from the literature using in vitro dispersion/dissolution/precipitation and in vivo data are presented in Table 3 .…”

Section: Ivivc Potential For Lipid-based Formulationsmentioning

confidence: 58%

Pharmacokinetic aspects and in vitro–in vivo correlation potential for lipid-based formulations

Kollipara

Gandhi

2014

Acta Pharmaceutica Sinica B

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Lipid-based formulations have been an attractive choice among novel drug delivery systems for enhancing the solubility and bioavailability of poorly soluble drugs due to their ability to keep the drug in solubilized state in the gastrointestinal tract. These formulations offer multiple advantages such as reduction in food effect and inter-individual variability, ease of preparation, and the possibility of manufacturing using common excipients available in the market. Despite these advantages, very few products are available in the present market, perhaps due to limited knowledge in the in vitro tests (for prediction of in vivo fate) and lack of understanding of the mechanisms behind pharmacokinetic and biopharmaceutical aspects of lipid formulations after oral administration. The current review aims to provide a detailed understanding of the in vivo processing steps involved after oral administration of lipid formulations, their pharmacokinetic aspects and in vitro in vivo correlation (IVIVC) perspectives. Various pharmacokinetic and biopharmaceutical aspects such as formulation dispersion and lipid digestion, bioavailability enhancement mechanisms, impact of excipients on efflux transporters, and lymphatic transport are discussed with examples. In addition, various IVIVC approaches towards predicting in vivo data from in vitro dispersion/precipitation, in vitro lipolysis and ex vivo permeation studies are also discussed in detail with help of case studies.

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“…In a recent clinical trial, the dietary supplement glucosol in a soft gel capsule showed a 30% decrease in blood glucose levels compared to a 20% drop seen with dry-powder filled two-piece hard gelatin capsule formulation, suggesting that soft gel formulation made of glucosol improved its bioavailability 23 . This is further illustrated by Lissyet al (2010) in the pharmacokinetic comparison of an oral diclofenac potassium liquid-filled soft gelatin capsule (DPSGC) with a diclofenac potassium tablet, study which showed that, DPSGC, 25mg and 50mg were more rapidly and consistently absorbed than diclofenac potassium 50-mg comparator tablets.…”

Section: Modification Of Drug Delivery Increase Bioavailabilitymentioning

confidence: 99%

Formulation and modifying drug release from Hard and Soft Gelatin Capsules for Oral drug delivery

Prasad

2017

IJRDPL

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Available online on:15.06.2017@http://ijrdpl.com http://dx.doi.org/10.21276/IJRDPL.227 8-0238.2017.6(4). [2663][2664][2665][2666][2667][2668][2669][2670][2671][2672][2673][2674][2675][2676][2677] ABSTRACT: Capsule is the most versatile of all dosage forms. Capsules are solid dosage forms in which one or more medicinal and inert ingredients are enclosed in a small shell or container usually made of gelatin. There are two types of capsules, "hard" and "soft". The hard capsule is also called "two pieces" as it consists of two pieces in the form of small cylinders closed at one end, the shorter piece is called the "cap" which fits over the open end of the longer piece, called the "body". The soft gelatin capsule is also called as "one piece". Capsules are available in many sizes to provide dosing flexibility. Unpleasant drug tastes and odors can be masked by the tasteless gelatin shell. The administration of liquid and solid drugs enclosed in hard gelatin capsules is one of the most frequently utilized dosage. This proves the oral bioavailability of poorly soluble compounds, delivery of low and ultra-low doses of a compound using softgel also ensures decreased plasma variability. This has led to the commercial pharmaceutical and nutraceutical industries opting for the development of alternative shell forming materials instead of the traditional capsule shell material gelatin. This review discusses establishment and the ongoing development of the manufacturing technology for liquid and semisolid capsules with focus on progress and challenges of soft and hard gelatin capsules formulation in oral administration for improved solubility and as an absorption-enhancing technique. These considerations form a basis for new applications in oral drug delivery.⇑ Corresponding author at: (4).2663-2677ABSTRACT: Capsule is the most versatile of all dosage forms. Capsules are solid dosage forms in which one or more medicinal and inert ingredients are enclosed in a small shell or container usually made of gelatin. There are two types of capsules, "hard" and "soft". The hard capsule is also called "two pieces" as it consists of two pieces in the form of small cylinders closed at one end, the shorter piece is called the "cap" which fits over the open end of the longer piece, called the "body". The soft gelatin capsule is also called as "one piece". Capsules are available in many sizes to provide dosing flexibility. Unpleasant drug tastes and odors can be masked by the tasteless gelatin shell. The administration of liquid and solid drugs enclosed in hard gelatin capsules is one of the most frequently utilized dosage. This proves the oral bioavailability of poorly soluble compounds, delivery of low and ultra-low doses of a compound using softgel also ensures decreased plasma variability. This has led to the commercial pharmaceutical and nutraceutical industries opting for the development of alternative shell forming materials instead of the traditional capsule shell material gelatin. This review discusses establishment and the ongoing ...

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Development and validation of dissolution test for lopinavir, a poorly water-soluble drug, in soft gel capsules, based on in vivo data

Cited by 27 publications

References 12 publications

Dissolution Method Development and Validation for Lercanidipine Hydrochloride Tablets

Dissolution Method Development and Validation for Lercanidipine Hydrochloride Tablets

Pharmacokinetic aspects and in vitro–in vivo correlation potential for lipid-based formulations

Formulation and modifying drug release from Hard and Soft Gelatin Capsules for Oral drug delivery

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