Establishment of a BioequivalenceIndicating Dissolution Specification for Candesartan Cilexetil Tablets Using a Convolution Model

Hassan, Hassan Ali; Charoo, Naseem A.; Ali, Areeg Anwer; Alkhatem, Sumaiya Ser

doi:10.14227/dt220115p36

Cited by 14 publications

(13 citation statements)

References 19 publications

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“…In such cases, the addition of surfactants helps to obtain sink conditions, by enabling the drug release process at the solid-liquid interface and micelle solubilization in bulk 34 and is recommended for performing in-vitro dissolution studies 35,36 .…”

Section: Discussionmentioning

confidence: 99%

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2019

IJPSR

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The purpose of this research was to develop novel solid dispersions (SDs) of BCS class IV drug, canagliflozin hemihydrate (CFZ) using Eudragit ® E PO (EE PO) as a carrier, to enhance its solubility and dissolution rate. Solvent evaporation technique was used to prepare SDs. The SDs were evaluated for saturated solubility, in-vitro dissolution study, solidstate characterization using FTIR, DSC, XRD and SEM, and flow properties. The solubility of CFZ in SDs increased manifold as compared with pure CFZ. Low values of angle of repose, Carr"s index, and Hausner ratio indicated good flow properties. The difference factor (f 1) and similarity factor (f 2) values suggested that dissolution profiles of the SDs were dissimilar to market product and the comparative dissolution curves revealed that SDs released CFZ faster than the marketed product. XRD patterns and DSC thermographs suggested that the SDs were present in an amorphous form, unlike pure crystalline CFZ. SEM studies showed CFZ has discrete crystalline particles whereas SD2 has diffuse, irregular asymmetrical structure. The SDs was superior to pure CFZ as they showed substantial improvement in solubility and dissolution rate along with good flow properties. Hence, the amorphous form of CFZ was successfully achieved by formulating it into SDs using EE PO as the carrier, which has conferred an increase in solubility and dissolution rate.

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Section: Discussionmentioning

confidence: 99%

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2019

IJPSR

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“…In-vitro release study was achieved for all formulations in addition to pure CC suspension. The release condition monitored in 0.1 M HCl (pH 1.2) and PBS (pH 6.8) and at the same conditions with adding tween 20 (0.35%-0.7%w/w) to achieve "sink" conditions during a dissolution test for all formulations 54,55 . It was found that all formulations exhibit a lack of drug release within 24 h. The in-vitro release of the best formula (CC-NLC9) was reached to less than 5% as showed in (figure 6) but, CC suspension showed almost complete drug release (100%) within 8 h. As CC had solubility equal to 11 μg/ml in 0.1 M HCl and 1 μg/ml in PBS (pH 6.8).…”

Section: In-vitro Release Studymentioning

confidence: 99%

Screening Study for Formulation Variables in Preparation and Characterization of Candesartan Cilexetil Loaded Nanostructured Lipid Carriers

et al. 2020

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The current study inspects the screening of the formulation components further, evaluates the physicochemical properties of the nanostructured lipid carriers (NLCs) for the antihypertensive drug as Candesartan Cilexetil (CC). The sequence screening of all excipients required for the preparation of NLCs should be performed. Firstly, the solubility of CC in different solid and liquid lipids is the major parameter for the selection of the best one. Precirol® ATO 5, Compritol ® 888 ATO and Glyceryl Monostearate (GMS) were showed the maximum solubility of the CC (1000±4.12 mg, 1500±4.15 mg and 1750±3.16 mg), respectively. Hence, they were selected as the solid lipids for the development of NLCs. Liquid lipids Transcutol® HP (30±2.21 mg/ml), Labrasol® ALF (25±1.32 mg/ml) and CapryolTM 90 (18±1.34 mg/ml) were observed to have good affinity for the drug on systematic screening of different liquid lipids. However, Precirol® ATO 5 was found to has good physical compatibility with Transcutol® HP, Compritol ATO 888 was found to has high physical miscibility with Labrasol® ALF and last GMS was appeared in good affinity and compatibly with CapryolTM 90. Hence, the following binary lipid mixtures (Precirol® ATO 5 - Labrasol® ALF), (Compritol® 888 ATO-Transcutol® HP) and (GMS - CapryolTM 90) were selected for the preparation of NLCs. The liquid–solid lipid mixture in the ratio up to 30:70 was observed to have sufficient melting point (55-59 0C). Lutrol F-68, Lutrol F-127, Cremophore EL and Cremophore® RH. In addition to, the combination of (Lutrol® F68:Cremophore® EL) and (Lutrol® F127: Cremophore® RH) were selected as the main surfactants for the preparation of NLCs formulations because of its good emulsification efficacy and homogeneity for the solid-liquid lipid mix. The prepared formulations were investigated for the different quality issues. All designed formulations observed in nanometer size of particles ranged from (408.9±11.5 to 114.6±8.3 nm) with high encapsulation efficiency around 99%. Also, the obtained results revealed that the ZP of the various formulations was consistently negative surface charge in between ((-13 ±2.3 to27.3±3.7 mV). Finally, formula number nine of CC (CC-NLC9) which composed of GMS (solid lipid), CapryolTM 90 (liquid lipid) and Lutrol® F127: Cremophore® RH (surfactants combination) was selected as the best formulation after the rank order for further investigations in the next work. Peer Review History: UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency. Received file Average Peer review marks at initial stage: 5.0/10 Average Peer review marks at publication stage: 7.5/10 Reviewer(s) detail: Name: Dr. Mohammed Abdel-Wahab Sayed Abourehab Affiliation: Umm Al-Qura University; Makkah Al-Mukarramah, Saudi Arabia E-mail: maabourehab@uqu.edu.sa Name: Dr. Maha Khalifa Ahmed Khalifa Affiliation: Al-Azhar Universit - Cairo, Egypt E-mail: mahakhalifa.ahmed@hotmail.com Name: Dr. Evren Alğin Yapar Affiliation: Turkish Medicines and Medical Devices Agency, Turkiye E-mail: evren.yapar@yahoo.com Comments of reviewer(s): Similar Articles: FORMULATION AND CHARACTERIZATION OF TOPICAL NANO EMULGEL OF TERBINAFINE A REVIEW ON GOLD NANOPRTICLES SYNTHESIS AND CHARACTERIZATION FORMULATION AND EVALUATION OF ELASTIC LIPOSOMES OF DECITABINE PREPARED BY ROTARY EVAPORATION METHOD

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“…Hydrophobic APIs will display absorption kinetics based on the rate-limiting step of dissolution, and those APIs with insufficient permeability will demonstrate permeation -rate limited absorption kinetics [1]. Noyes-Whitney equation suggests that the aqueous solubility of an API is directly related to the its rate of dissolution and consequently it is a significant variable that regulates the rate of dissolution and thereby the absorption [2].…”

Section: Introductionmentioning

confidence: 99%

Solid Dispersions: Resuscitating Oral Delivery of Hydrophobic Drugs

Agrawal¹,

Raza²,

Patel³

2019

Asian J Pharm Clin Res

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Objective: This review article explores solid dispersions (SDs) as one of the suitable approaches to formulate poorly water-soluble drugs. The objective of this review on SD techniques is to explore their utility as a feasible, simple, and economically viable method for augmentation of dissolution of hydrophobic drugs. Methods: Various types of SDs are classified and compared. Use of surfactants to stabilize the SDs and their potential advantages and disadvantages has been discussed. Different techniques for preparing and evaluating SDs are appraised along with discussions on scalability and industrial production. Review of the current research on SD along with future trends is also offered. Results: Based on the various researches, SDs offer an efficient means of improving bioavailability while concurrently contributing to lower toxicity and dose-reduction. Conclusion: Solid-dispersions have been and continue to be one of the key technologies for solving the issue of poor solubility for newer hydrophobic molecules which are being discovered. This would give a new lease of life for such drugs enabling them to be delivered in an effective way.

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Establishment of a BioequivalenceIndicating Dissolution Specification for Candesartan Cilexetil Tablets Using a Convolution Model

Cited by 14 publications

References 19 publications

Untitled

Untitled

Screening Study for Formulation Variables in Preparation and Characterization of Candesartan Cilexetil Loaded Nanostructured Lipid Carriers

Solid Dispersions: Resuscitating Oral Delivery of Hydrophobic Drugs

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