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both the CDs, which indicated formation of the inclusion complex of TLM in 1:2 stoichiometries with Î²-CD and HP-Î²-CD. The inclusion complexes in molar ratio of 1:2 were prepared by various methods. The molecular behavior of TLM in all
samples were characterized by Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and powder X-ray diffraction studies.The result of studies showed inclusion of TLM molecule into cyclodextrin cavities.The
highest improvement in in-vitro dissolution of TLM was observed in a complex prepared with HPÎ²-CD using the kneading method. Mean dissolution time (MDT) and similarity factor (f2) indicated a significant difference between the release profile of TLM from complexes, physical mixture, and pure TLM. The highest improvement in solubility and in-vitro drug release were observed in inclusion complex prepared with HP-Î²-CD by kneading method. Improvement in solubility and in-vitro drug release of telmisartan was more with HP-Î²-CD as compared to Î²-CD
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Karlberg BE, Lins LE, Hermansson K. Efficacy and safety of telmisartan:
A selective AT1 receptor antagonist, compared with enalapril in elderly
patients with primary hypertension: TEES Study Group. J Hypertens
Ries UJ, Mihm G, Narr B, Hasselbach KM, Wittneben H, Entzeroth M,
et al. 6-Substituted benzimidazoles as new nonpeptide angiotensin
II receptor - antagonists: Synthesis, biological activity, and structure-
activity relationships. J Med Chem 1993;36:4040-51.
Mallion JM, Siche JP, LacourciÃ¨re Y. ABPM comparison of the
antihypertensive profiles of the selective angiotensin II receptor
antagonists telmisartan and losartan in patients with mild to moderate
hypertension. J Hum Hypertens 1999;13:657-64.
Benson SC, Pershadsingh HA, Ho CI, Chittiboyina A, Desai P, Pravenec
M, et al. Identification of telmisartan as a unique angiotensin II
receptor antagonist with selective PPARgamma-modulating activity.
P ro d u c t I n f o r m a t i o n : M i c a rd i s Â® H C T, t e l m i s a r t a n a n d
hydrochlorothiazide. Boehringer Ingelheim, Ridgefield, Connecticut.
(PI revised 11/2000) reviewed 1/2001.
Proudfoot S. Factors affecting bioavailability: Factors influencing
drug absorption from the gastrointestinal tract. In: Aulton ME, editor.
Pharmaceutics, the science of dosage form design. UK: Churchill
Livingstone London; 1991. p. 135-73.
Cappello B, Clelia DM, Iervolino M, A. Improvement of solubility and
stability of valsartan by hydroxypropyl-boldbeta-cyclodextrin. J Incl
Phenom Macro Chem 2006;54:289-94.
Patel R, Patel M. Solid-state characterization and dissolution properties
of lovastatin hydroxypropyl-Î²-cyclodextrin inclusion complex. Pharm
Tech 2007; February 2:72-81.
Becket G, Schep LJ, Tan MY. Improvement of the in vitro dissolution
of praziquantel by complexation with alpha, beta and gamma
cyclodextrin. Int J Pharm 1999;179:65-71.
Higuchi T, Connors K. Phase solubility techniques. Adv Anal Chem
Moore JW, Flanner H. Mathematical comparison of dissolution profiles.
Pharm Tech 1996;20:64-74.
US food and drug administration, guidance for industry SUPAC-MR:
Modified release solid oral dosage forms scale-up and postapproval
changes: Chemistry, manufacturing, and controls; In vitro dissolution
testing and in vivo bioequivalence documentation. Rockville, MD:
Human medicines evaluation unit, European agency for the Evaluation
of Medicinal Products (EMEA), Notes for guidance on quality of
modified-release products: A oral dosage forms; B transdermal dosage
forms, Section 1 (Quality). London, UK: EMEA; 1999.
Reppas C, Nicolaides E. Analysis of drug dissolution data. In: Dressman JB, Lennernaâ€™s H, editors. Oral drug absorption prediction and
assessment. New York: Marcel Decker; 2000. p. 229-54.
Vueba ML, Batista de Carvalho LA, Veiga F, Sousa JJ, Pina ME. Influence
of cellulose ether polymers on ketoprofen release from hydrophilic
matrix tablets. Eur J Pharm Biopharm 2004;58:1-59.
Costa FO, Sousa JJ, Formosinho SJ. Comparison of dissolution profiles
of Ibuprofen pellets. J Control Release 2003;89:199-212.
Rinaki E, Dokoumetzidis A, Macheras P. The mean dissolution time
depends on the dose/solubility ratio. Pharm Res 2003;20:406-8.
Loftsson T, Magnusdottir AM, Masson JF, Sigurjonsdottir. Self-association
and cyclodextrin solubilization of drugs. J Pharm Sci 2002;91:2307-16.