Effect of amorphization method on telmisartan solubility and the tableting process

Lepek, P.; Sawicki, Wiesław; Wlodarski, K.; Wojnarowska, Ż.; Paluch, Marian; Guzik, Łukasz

doi:10.1016/j.ejpb.2012.09.019

Cited by 41 publications

(21 citation statements)

References 15 publications

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“…Our findings are in line with Lepek et al, (2013), who reported TLM (TLM) as a poor water-soluble angiotensin II receptor antagonist in crystalline form. That was transformed into the amorphous state by the melt quench technique, as well as a cryogenic grinding method, in order to improve its physiochemical properties.…”

Section: Resultssupporting

confidence: 81%

Role of Chitosan, Carboxy Methyl Cellulos, Polyvinyl Pyrrolidone, Kyron T134 and Primogel to Design the Mouth Disintegrating Telmisartan Tablet With Extended Release Profile

Akram

Taha²,

Nazir³

2017

Indonesian J. Pharm.

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The Mouth Disintegrating Extended Release Telmisartan (MDERT) tablets are designed for adequate pharmacokinetic profile to avoid the unusual peaks and troughs. Although, there are extensive advance techniques used to deliver drugs. But oral route is still remains effective in most of the therapeutical situations. Thus we aimed this study to formulate a dosage form with dual character of orodispersion as well as extended effectiveness. MDERTS dosage form was prepared by direct compression method. The major components of this preparation were Telmisartan (TLM), Carboxy methyl cellulose polyvinyl Pyrrolidone, Chitosan, Talc, Mg-stearate, Lactose. The MDERTS dosage form was characterized with different determinants. While, the drug release curves of all 6 formulations upto 12h, DSC spectra of TLM, Kyron T 134 , Primogel, TLM+Kyron T 134 +Primogel, Chitosan, CMC and different excepients are presented as comprehensive scientific figures. DSC and FTIR spectroscopic studies indicate the compatibility of drugs with each other and with excipients. Moreover, the formulation F2 containing more than 10% of Kyron T had shown best results. Whereas, the overall results had shown that Kyron T containing tablets had best, in vitro dispersion time, wetting time and wetting volume, water absorption ratio. The order in which superdisintegrants and polymers had produced desirable effect is Kyron T134 > Kyron T134134 + primogel > primogel and for polymers chitosan> chitosan+CMC> chitosan +PVP> CMC> CMC+PVP> PVP. Thus, Kyron T is the best superdisintegrant of others which were used in present study and direct compression method is the best used to prepare extended release mouth disintegrating tablets.

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Section: Resultssupporting

confidence: 81%

Role of Chitosan, Carboxy Methyl Cellulos, Polyvinyl Pyrrolidone, Kyron T134 and Primogel to Design the Mouth Disintegrating Telmisartan Tablet With Extended Release Profile

Akram

Taha²,

Nazir³

2017

Indonesian J. Pharm.

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“…Melting temperature (peak maximum), T fus , and enthalpy, DH fus , of valsartan, telmisartan and irbesartan determined in the present work, compared with values reported in the literature ; 263; 24 264; 25 268;26,27 269; 28 272 29 183 a ; 184; 30 185 31,32 DH fus /kJ mol À1…”

mentioning

confidence: 54%

Thermal behavior and molecular mobility in the glassy state of three anti-hypertensive pharmaceutical ingredients

Ramos

2017

RSC Adv.

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“…TS belongs to BCS class II drug and the solubility of TS is extremely low (0.09 mg/ml in water) and pH-dependent. Accordingly, TS shows variable oral bioavailability of 42-58%, leading to inadequate and varying pharmacological effects [18][19][20][21][22]. So far several attempts have been made to ameliorate the oral bioavailability of several poorly soluble actives [23][24][25][26][27].…”

Section: Introductionmentioning

confidence: 99%

Development and biological evaluation of vesicles containing bile salt of telmisartan for the treatment of diabetic nephropathy

Ahad

Raish

Ahmad

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

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The aim of present study was to develop and evaluate vesicles containing bile salt formulation of telmisartan for the treatment of diabetic nephropathy. Different vesicles containing bile salt formulations were developed by varying ratios of soybean phosphatidylcholine and sodium deoxycholate. Prepared formulations were characterized for their size, polydispersity index, zeta potential, morphology and entrapment efficiency. Further, the renoprotective outcome of optimized formulation was studied in streptozotocin-induced diabetic nephropathy rat model. Results of the present study demonstrated that the average vesicles size, polydispersity index, zeta potential and entrapment efficiency were found to be in the range of 64.98 ± 1.40 to 167.60 ± 6.46 nm, 0.02 ± 0.04 to 0.31 ± 0.01, -24.30 ± 1.39 to -42.60 ± 6.67 mV and 29.68 ± 1.08% to 77.21 ± 0.52%, respectively. Further, the best chosen formulation F4 presented vesicles size, polydispersity index, zeta potential and entrapment efficiency of 64.98 ± 1.40 nm, 0.24 ± 0.02, -35.40 ± 1.48 mV and 77.21 ± 0.52%, respectively. In addition, formulation F4 improved the biological indices in streptozotocin-induced diabetic nephropathy in rats. It was concluded that prepared formulation exerts a valuable results on diabetic nephropathy and it may be a potential pharmaceutical dosage form for the treatment of diabetic nephropathy.

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Effect of amorphization method on telmisartan solubility and the tableting process

Cited by 41 publications

References 15 publications

Role of Chitosan, Carboxy Methyl Cellulos, Polyvinyl Pyrrolidone, Kyron T134 and Primogel to Design the Mouth Disintegrating Telmisartan Tablet With Extended Release Profile

Role of Chitosan, Carboxy Methyl Cellulos, Polyvinyl Pyrrolidone, Kyron T134 and Primogel to Design the Mouth Disintegrating Telmisartan Tablet With Extended Release Profile

Thermal behavior and molecular mobility in the glassy state of three anti-hypertensive pharmaceutical ingredients

Development and biological evaluation of vesicles containing bile salt of telmisartan for the treatment of diabetic nephropathy

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