Solubility and Dissolution Rate Enhancement of Telmisartan by Solid Dispersion and Pelletization Techniques Using Soluplus as Carrier

Kunam, Viswanadh; Garikapati, Devala Rao; Vidyadhara, S.; Mandava, Venkata Basaveswara Rao; Janga, Ramesh Babu; Sunkara, Siva Prasad

doi:10.22159/ijap.2020v12i1.35620

Cited by 3 publications

(2 citation statements)

References 5 publications

(5 reference statements)

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“…Another mechanism involved may be that, soluplus being hydrophilic makes a wet layer around the drug molecule which allows the transfer of solvent to the surface of the drug molecule which makes the drug molecule solubilize [19].…”

Section: Discussionmentioning

confidence: 99%

Development of Amorphous Binary and Ternary Solid Dispersions of Nateglinide for Improved Solubility and Dissolution

2020

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Objective: Nateglinide is a commonly used oral hypoglycemic, biopharmaceutical classification system Class II drug, which shows relatively poor water solubility and variable bioavailability. The objective of the present investigation was to develop the binary and ternary solid dispersions of nateglinide for improved solubility and dissolution. Methods: Nateglinide solid dispersions were prepared by a common solvent evaporation method. Polymers like soluplus, kolliphor P188, sylloid 244FP, gelucire 48/16, affinisol (HPMCAS), HPβCD, βCD were used in different combinations. The physicochemical characterization of the optimized ternary dispersion was studied by using FT-IR, DSC, and PXRD. Solubility and dissolution behavior of all dispersions were studied. Result: From all prepared ternary solid dispersions, nateglinide dissolution was significantly faster than pure nateglinide. With ternary solid dispersion of NTG, soluplus and kolliphor P188 there was a big improvement in solubility and dissolution. This combination enhanced the solubility of NTG by 23 folds. Another ternary dispersion of NTG with soluplus and gelucire 48/16 enhanced solubility by 25 fold. Conclusion: Ternary solid dispersion found superior over binary dispersions. For the ternary dispersions, showing the best solubility, tablets were prepared. Dissolution and drug release from the formulated tablet was as good as a marketed product.

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Section: Discussionmentioning

confidence: 99%

Development of Amorphous Binary and Ternary Solid Dispersions of Nateglinide for Improved Solubility and Dissolution

2020

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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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Solubility and Dissolution Rate Enhancement of Telmisartan by Solid Dispersion and Pelletization Techniques Using Kollidon Va 64 as Carrier

et al. 2022

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Objective: In the present investigation, an attempt was made to improve the surface characters and solubility of the drug by solid dispersion and coating it on the nonpareil sugar beads as pellets. Methods: Telmisartan solid dispersions were prepared by solvent evaporation technique using Kollidon VA64 as binder and solubility enhancer, Crospovidone as disintegrant and ethanol was used as the solvent. Telmisartan pellets were prepared by dissolving telmisartan, kollidonVA64, Crospovidone in ethanol in different ratios and coated on nonpareil sugar beads as a drug layer by pan coating technique. All the formulations were further evaluated for physicochemical parameters such as particle size, friability, angle of repose and drug content. In vitro dissolution studies were carried out in pH 7.5 phosphate buffer by using USP apparatus II. Results: It was observed that the dissolution rate of the solid dispersion formulation TSD5 showed a better dissolution rate to the extent of 1.113 folds and 1.979 folds when compared to a marketed formulation and pure drug, respectively. Similarly, the formulation TPL3containing 1:3 ratio of Telmisartan to Kollidon VA64 showed an improved dissolution rate to the extent of 1.150 folds and 2.045 folds when compared to the marketed formulation and pure drug, respectively. Majority of the formulations displayed first-order release kinetics and were found to be linear with R2 values in the range of 0.905 to 0.994. FTIR analysis and DSC analysis revealed that there was no major interaction between the drug and the excipients used in the design of the formulation. SEM analysis was performed for solid dispersions, pellet formulations and its polymers to determine the surface characteristics. Conclusion: From the present study, it was observed that the solubility of Telmisartan was enhanced by Kollidon VA 64 in pellet formulations when compared to solid dispersions.

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Solubility and Dissolution Rate Enhancement of Telmisartan by Solid Dispersion and Pelletization Techniques Using Soluplus as Carrier

Cited by 3 publications

References 5 publications

Development of Amorphous Binary and Ternary Solid Dispersions of Nateglinide for Improved Solubility and Dissolution

Development of Amorphous Binary and Ternary Solid Dispersions of Nateglinide for Improved Solubility and Dissolution

Novel Pharmaceutical Cocrystal of Telmisartan and Hydrochlorothiazide

Solubility and Dissolution Rate Enhancement of Telmisartan by Solid Dispersion and Pelletization Techniques Using Kollidon Va 64 as Carrier

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