"Enhancement of solubility of a poorly soluble antiplatelet aggregation drug by cogrinding technique"

Bayoumi, Asmaa A

doi:10.22159/ajpcr.2018.v11i10.27136

Cited by 9 publications

(5 citation statements)

References 8 publications

(9 reference statements)

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“…Twenty (20) tablets were randomly selected from both formulations and the weight variation test was performed using digital weighing balance. The results were compared with the official limits provided in US Pharmacopoeia ( Bayoumi, 2018 ). The weight variation was calculated in percentage by:

where W.V is the weight variation and I w and A w were individual and average weight respectively.…”

Section: Methodsmentioning

confidence: 99%

Synthesis of Thiol-Modified Hemicellulose, Its Biocompatibility, Studies, and Appraisal as a Sustained Release Carrier of Ticagrelor

et al. 2021

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Background: Nature has always been considered as the primary source of pharmaceutical ingredients. A variety of hemicelluloses, as well as their modified forms, have been under investigation. Herein, a study was designed to explore the biocompatibility of hemicellulose and its modified form (thiolated hemicellulose) as well as its potential as a pharmaceutical excipient.Method: For thiol modification thiourea was used as the thiol donor, HCl as the catalytic reagent, and methanol was used for washing purposes. Modified polymers were characterized for physicochemical characteristics, including surface morphology, the amorphous or crystalline nature of the particles, modification of polymer by FTIR, and biocompatibilities. For acute oral toxicity study, a single dose of 2 g/kg was administered to albino rats of 200 g average weight (n = 3). Polymers were evaluated as pharmaceutical excipients by preparing compressed tablets of antiplatelet drug (Ticagrelor), followed by various quality control tests, such as swelling index, thickness and diameter, disintegration, and in-vitro drug release.Results: From the results, it was observed that thiol modification has been successfully accomplished as characteristic peaks belonging to –SH group appeared at 2667.7691 cm−1 in FTIR scan. The modified polymer was found safe in the use concentration range, confirming their safe use for in vivo analysis. No significant effect has been observed in the behavior, biological fluid (blood), or on vital organs. Thiolated hemicellulose was found to be an excellent drug retarding polymer as 8 h of dissolution studies showed that 67.08% of the drug has been released.Conclusion: Conclusively, incorporation of thiol moiety made the polymer more mucoadhesive with, and a worthy carrier of, the drug with good biocompatibilities.

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where W.V is the weight variation and I w and A w were individual and average weight respectively.…”

Section: Methodsmentioning

confidence: 99%

Synthesis of Thiol-Modified Hemicellulose, Its Biocompatibility, Studies, and Appraisal as a Sustained Release Carrier of Ticagrelor

et al. 2021

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“…The solubility enhancement may be a result of the formation of a Ticagrelor-PVP K25 soluble complex. 5 Ticagrelor SNEDDS was formulated as a novel formulation to enhance solubility and dissolution rate. Ticagrelor was formulated into SNEDDS using surfactants polyoxyethylene sorbitan monooleate (Tween 80) and medium-chain triglyceride (MCT) oil, while Labrafil M1944CS was used as co-surfactant.…”

Section: Recent Advancements For Solubility Enhancement Of Ticagrelormentioning

confidence: 99%

A Review on Different Solubility Enhancement Techniques of Ticagrelor

Srivastava

Khan

Bedi

et al. 2022

Int J. Pharm. Investigation

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Solubility is characterized as the sum of substance that passes into the solution to form a saturated solution at steady temperature and pressure. Solubility can be framed in terms of the maximum volume or mass of the solute that breaks up in a given volume or mass of a solvent. 2 An increase in solubility can be achieved by various methods such as Salt formation, Complexation, Micronization, 4 Solid Dispersion, altering the pH, co-solvency, co-crystals, polymeric micelles, etc. 5 A highly efficacious technique is the conversion of a crystalline drug to its amorphous form. Amorphous drugs have better solubility than crystalline drugs due to their structure, increased surface area, and better wettability. 6 The amorphous state has better solubility as it has higher entropy, enthalpy, volume, and free energy when compared to its crystalline structure. 7 TICAGRELORTicagrelor is classified as an anti-platelet aggregator, which reversibly binds to the P2Y12 receptor and acts by antagonizing the binding of adenosine phosphate to the P2Y12 receptor resulting in decreased uptake of adenosine. It is a direct-acting and immediate-release drug taken orally. Both the active drug ABSTRACT Ticagrelor is a BCS class IV drug that inhibits platelet action by reversibly binding to the P2Y12 receptor. One of the major challenges faced by the class IV (low solubility, low permeability) drug is the lower dissolution rate leading to low bioavailability. The bioavailability of the marketed formulation of ticagrelor is approximately 36%. Researchers have come up with various techniques to improve the BCS class II and IV drug formulations as an integral part of the development of the pharmaceutical sciences. An increase in solubility can be achieved by various methods such as Salt formation, Complexation, Micronization, Solid Dispersion, altering the pH, Co-solvency, co-crystals, polymeric micelles, etc. A highly efficacious technique is converting a crystalline drug to its amorphous form. An extensive literature search was conducted using various databases like science direct, Taylor and Francis, Springer to extract relevant articles. Keywords like "Ticagrelor", "low permeability", "P2Y12 receptor inhibitor" were used for the literature search. Relevant articles were screened and referred for further study. This article discusses the techniques employed to increase the solubility of ticagrelor, thus highlighting the research conducted and reported. The increase in bioavailability of ticagrelor could be seen when formulated as nanoparticles, co-crystals, ticagrelor loaded self-micro emulsifying and nano emulsifying drug delivery system, solid dispersion, etc. the conversion of the crystalline drug into amorphous drug is a highly recommended approach to increase the solubility of ticagrelor which can be seen in cases of co-crystals and solid dispersion formulation.

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“…The average weight of 20 tablets from all formulations (F1 and F2) was recorded for the purpose of finding any weight variation among formulations and were compared to the acceptable range mentioned in USP pharmacopoeia [28]. The weight variation was calculated in percentage by:…”

Section: Weight Variation Testmentioning

confidence: 99%

Synthesis and characterization of thiol modified beta cyclodextrin, its biocompatible analysis and application as a modified release carrier of ticagrelor

Zaman

Bajwa²,

Saeed³

et al. 2020

Biomed. Mater.

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Thiol modification of beta cyclodextrin (β-CD) was carried out using thiourea, which served as a thiol donor. The chemical reaction was mediated using HCl. Polymer prepared via thiolation was further subjected to physicochemical and biocompatible analysis. Acute oral toxicity and compatibility was determined in albino rats. Furthermore, compressed tablets of ticagrelor (TCG) were prepared using modified and unmodified polymers and evaluated via various quality control tests. Thiolation was successfully achieved and confirmed by the FTIR scan, as a significant corresponding peak was observed at 2692 cm−1 wavenumber, demonstrating the attachment of –SH group. In vivo analysis has confirmed the safe use of β-CD, as none of the vital organs showed any kind of toxic effects. Dissolution studies revealed that Tβ-CD was able to release 96.62% of the drug within 1 h of the study, hence providing an immediate release. Conclusively, a thiol moiety was successfully attached to the polymeric backbone and was found safe to be used as a pharmaceutical excipient.

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"Enhancement of solubility of a poorly soluble antiplatelet aggregation drug by cogrinding technique"

Cited by 9 publications

References 8 publications

Synthesis of Thiol-Modified Hemicellulose, Its Biocompatibility, Studies, and Appraisal as a Sustained Release Carrier of Ticagrelor

Synthesis of Thiol-Modified Hemicellulose, Its Biocompatibility, Studies, and Appraisal as a Sustained Release Carrier of Ticagrelor

A Review on Different Solubility Enhancement Techniques of Ticagrelor

Synthesis and characterization of thiol modified beta cyclodextrin, its biocompatible analysis and application as a modified release carrier of ticagrelor

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