Formulation of Nanoparticles of Telmisartan Incorporated in Carboxymethylchitosan for the Better Drug Delivery and Enhanced Bioavailability

Yadav, Upasana; Chowdhuri, Angshuman Ray; Sahu, Sumanta Kumar; Husain, Nuzhat; Rehman, Qamar

doi:10.22159/ajpcr.2017.v10i9.19162

Cited by 3 publications

(3 citation statements)

References 36 publications

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“…Previous studies, to improve the aqueous solubility of TEL, show the possibility of preparing solid dispersions [14][15][16], amorphous formulation [17], immediate release tablets [18], nanoparticles [19,20], and self-nanoemulsifying drug delivery systems [21,22]. However, the cocrystallization approach, for improving the aqueous solubility of TEL, has been investigated by Chadha et al [23] and by Alatas et al [24].…”

Section: Research Articlementioning

confidence: 99%

Novel Pharmaceutical Cocrystal of Telmisartan and Hydrochlorothiazide

Kulkarni¹,

Shete²,

Hol³

et al. 2020

Asian J Pharm Clin Res

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Objective: Telmisartan (TEL), commonly used antihypertensive, is poorly soluble in water and has limited and variable bioavailability. Commercially, TEL is available as a single drug and in combination with hydrochlorothiazide (HYZ). Researchers have developed cocrystals of TEL with coformers, namely, oxalic acid, glutaric acid, and saccharin. An attempt was made to prepare the cocrystals of TEL with HYZ, an active pharmaceutical ingredient (API) itself so that both the APIs are available in a single tablet. The present study was aimed at enhancement in solubility of TEL by formation of its cocrystals. Methods: The cocrystals of TEL with HYZ, in different stoichiometric ratios (1:0.5, 1:1, and 1:2), were prepared by solvent coevaporation and liquid-assisted grinding methods. The cocrystals, consisting of TEL:HYZ (in 1:0.5 ratio and 1:1 ratio), depicted maximum yield, drug content, saturation solubility, and flow properties. These cocrystals were characterized by X-ray analysis, infrared spectroscopy, and thermal analysis. Results: The crystal structure of TEL-HYX revealed that it was a cocrystal, since no proton was transferred between the TEL and HYZ molecules. It was predicted that two molecules are associated through a hydrogen bond between an acidic group of TEL and sulfonamido group of HYZ. The cocrystallization improved the solubility of TEL 7 times. In vitro release rate of tablets of cocrystals was higher than that of marketed TEL tablets. HYZ has a potential to form the cocrystals of TEL. Conclusion: The objective of improvement in the solubility of TEL was successfully achieved by the formation of cocrystals of TEL: HYZ.

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Section: Research Articlementioning

confidence: 99%

Novel Pharmaceutical Cocrystal of Telmisartan and Hydrochlorothiazide

Kulkarni¹,

Shete²,

Hol³

et al. 2020

Asian J Pharm Clin Res

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“…The solid was filtered and rinsed in 70-90% ethyl alcohol, and vacuum dried at room temperature. The resulted product was the sodium salt of CMC [17].…”

Section: Preparation Of Carboxymethyl Chitosan (Cmc)mentioning

confidence: 99%

Formulation of Nanoparticles of Eprosartan Mesylate for the Better Drug Delivery by Improving Solubility

Yadav

Husain

Rehman

2018

Asian J Pharm Clin Res

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Objective: In the present study, we have made an attempt to the developed formulation of nanoparticles (NPs) of eprosartan mesylate (EM) incorporated in carboxymethyl chitosan using reverse micelle technique for the better drug delivery by improving solubility.Methods: The NPs size and morphology were investigated by high-resolution transmission electron microscopy and field emission scanning electron microscopy, respectively. The physical and chemical aggregation state of eprosartan was analyzed using ultraviolet spectroscopy, and Fourier transforms infrared spectroscopy.Results: To increase the solubility of eprosartan by reverse micelle technique of the drug through polymeric NPs is an alternative efficient, option for increasing the solubility. Eprosartan nanosuspension was successfully formulated for dissolution and bioavailability enhancement of the drug. The percentage drug release pattern of both formulations was compared against that of pure drug. It shows that in 10 min 39% and 17% of drug was released from the NPs made by RM method and microemulsion method, respectively, as compared to that of 1.3% of the pure drug. In 50 min almost more than half 51% of the drug was released from NPs by microemulsion method whereas only 2.5% of the drug was released from NPs containing the pure drug. In 120 min 67% of the drug was released from NPs by microemulsion method whereas only 5.8% of drug release was shown by NPs with the pure drug. We are paying attention on evaluating the influence of particle size and crystalline state on the in vitro performance of eprosartan.Conclusion: In summary, we have developed a new approach toward the delivery of poorly water-soluble drug eprosartan by reverse micellar method. The particle size of NPs obtained by the reverse micellar method was significantly reduced as compared to the other method.

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“…Being anionic, chitosan succinate has favorable characteristics for the oral delivery system and has wide solubility in alkaline media and decreased solubility in acid. The change in solubility occurs because of the decreased amount of amino group and substitution with carboxylic groups during the substitution reaction [5][6][7][8]. This characteristic indicates that modifying chitosan with succinic acid gives it the potential to be a useful polymer for enteric-coated tablets [9].…”

Section: Introductionmentioning

confidence: 99%

Preparation and Characterization of Chitosan Succinate as Coating Polymer for Enteric-Coated Tablet

Surini

Prakoso

2018

Int J App Pharm

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Objective: This present study was aimed to evaluate the potential of chitosan succinate as a coating polymer.Methods: In this study, chemical modification of chitosan was performed by substituting a succinate group into chitosan's amine group. This reaction used a water-solvent method to obtain chitosan succinate. Chitosan succinate was characterized and used as a coating agent in enteric-coated tablet dosage forms containing sodium diclofenac as the drug model at concentrations of 3% and 4% and combined it with hydroxypropyl methylcellulose phthalate (HPMCP) in ratios of 3:1 and 2:1 (3%). The obtained tablets were evaluated based on their physical appearance, uniformity of weight and size, thickness film, disintegration time for an hour in acid, and dissolution profile. Results:Although the enteric-coated tablets with 3% and 4% chitosan succinate dissolved after 1 h in acid, they could not hold drug release in the acid medium under 10%. The enteric-coated tablet combined with chitosan succinate and HPMCP (3:1 and 2:1) at 3% did not dissolve after 1 h in the acid medium and could hold drug release up to 8.53% in acid. Conclusion:A combination of chitosan succinate and HPMCP (3:1 and 2:1) at 3% has a better ability to hold drug release in acid medium and met the requirement as a coating in enteric-coated tablet dosage forms. Chitosan succinate preparationAbout 4 g of chitosan (deacetylated degree of 94.2%, Surindo Biotech, Indonesia) was dissolved in 400 ml of 1% acetic acid. Succinic anhydride (Merck, Germany) was dissolved in 400 ml of methanol and added into a beaker with the chitosan solution by dropping method. We increased the pH by adding 1.0 N NaOH until the solution neutralized and prepared the precipitated mixture. This mixture was then filtered to remove the solvent and was then washed with methanol. The precipitate was dialyzed for 24 h and dried at 40°C in an oven (Modena ® ) for 24 h. Then, the dried material was filtered with 60-mesh sieve. Characterization Physical appearanceThe products were evaluated based on their shape, color, and odor.

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Formulation of Nanoparticles of Telmisartan Incorporated in Carboxymethylchitosan for the Better Drug Delivery and Enhanced Bioavailability

Cited by 3 publications

References 36 publications

Novel Pharmaceutical Cocrystal of Telmisartan and Hydrochlorothiazide

Novel Pharmaceutical Cocrystal of Telmisartan and Hydrochlorothiazide

Formulation of Nanoparticles of Eprosartan Mesylate for the Better Drug Delivery by Improving Solubility

Preparation and Characterization of Chitosan Succinate as Coating Polymer for Enteric-Coated Tablet

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