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Preparation, physicochemical characterization, dissolution and formulation studies of telmisartan cyclodextrin inclusion complexes
Kane Rajesh,Kuchekar Bhanudas
Asian Journal of Pharmaceutics , 2010,
Abstract: The objective of this research was to prepare, characterize, and to study dissolution properties of inclusion complexes of telmisartan (TLM), with β-cyclodextrin and hydroxypropyl-β-cyclodextrin and to study effect of complexation on aqueous solubility and rate of dissolution in dissolution media. The phase solubility curve was classified as an A P type for both the CDs, which indicated formation of the inclusion complex of TLM in 1:2 stoichiometries with β-CD and HP-β-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 HPβ-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-β-CD by kneading method. Improvement in solubility and in-vitro drug release of telmisartan was more with HP-β-CD as compared to β-CD
Research: COMPARATIVE STUDY OF ANTIHYPERTENSIVE ACTIVITY OF TELMISARTAN WITH TELMISARTAN-HYDROXYPROPYL-β-CYCLODEXTRIN INCLUSION COMPLEXES
Shashikant N Dhole*,Bhanudas S Kuchekar
Pharmacie Globale : International Journal of Comprehensive Pharmacy , 2011,
Abstract: Telmisartan is an angiotensin II receptor antagonist used in the treatment of hypertension. According to BCS, (biopharmaceutical classification system) telmisartan belongs to class II drug, and it is practically insoluble in water and it shows low dissolution profile and poor absorption and reduced oral bioavailability. The aim of work was to develop telmisartan-hydroxypropyl-β-cyclodextrin inclusion complexes in order to improve its water solubility and bioavailability. The complexes were prepared by the physical mixture, spray drying and freeze-drying techniques. The improvement in the solubility and bioavailability was evaluated by virtue of comparison of antihypertensive activity of the plain telmisartan (1 mg/kg) with the inclusion complexes equivalent to (1 mg/kg) of telmisartan using two kidney one clip (2K1C) induced renal hypertension model. The results showed that the inclusion complexes of the telmisartan were more significant in reducing the mean arterial blood pressure of the hypertensive rats as compared to the plain telmisartan showing the enhanced solubility and bioavailability of the drug by virtue of the complexes.
Pharmaceutical equivalence of gabapentin tablets with various extragranular binders Pharmaceutical equivalence of gabapentin tablets with various extragranular binders
SWATI C. JAGDALE,BHANUDAS KUCHEKAR,JIBANANANDA SATAPATHY,ANIRUDDHA CHABUKSWAR
Revista de Ciências Farmacêuticas Básica e Aplicada , 2010,
Abstract: Gabapentin is a high-dose drug widely used as an oral anti-epilepticagent. Due to high crystalline and has poor compaction properties it is difficult to form tablets by direct compression. The aim of this study was to develop gabapentin tablets, pharmaceutically equivalent to the reference product Neurontin (marketed in USA). Gabapentin 800mg tablets were produced by wet granulation by keeping intragranular binder as well as its concentration constant and by changing with various extragranular binders with its concentration (A = PVPK 30, B = HPMC 15 cps, C = Kollidon VA 64, D =Klucel EXF).The tablet having no weight, thickness and hardness variation and having appropriate, friability as well as disintegration profile were coated with a 3% film coating solution .Seven formulations F1 (A in lower concentration) F2 (A in higher concentration), F3 (B in lower concentration) and F4 (B in higher concentration), F5 (C in lower concentration), F6 (C in higher concentration), F7 (D in lower concentration) were formulated. Among them F6 demonstrated adequate hardness, friability, disintegration, uniformity of content, and total drug dissolution after 45minutes. The dissimilarity factor (f1) is 5.93 and the similarity factor (f2) is 67.85. So F6 was found to be equivalent to Neurontin. Gabapentin is widely used as an oral anti-epileptic agent. However, owing to its high crystallinity and poor compaction properties, it is difficult to form tablets of this drug by direct compression. The aim of this study was to develop gabapentin tablets, pharmaceutically equivalent to the brand-name pioneer product Neurontin (marketed in USA). Gabapentin 800mg tablets were produced by wet granulation with a constant concentration of intragranular binder and a varying concentration of extragranular binders (A = polyvinylpyrrolidone K30, B = hydroxypropylmethylcellulose 15 cps, C = Kollidon VA64, D =Klucel EXF). The tablets that did not vary in weight, thickness or hardness and had appropriate friability and disintegration profiles were coated with a 3% film-coating solution. Seven formulations F1 (A 3%), F2 (A 6%), F3 (B 3%), F4 (B 6%), F5 (C 3%), F6 (C 3%) and F7 (D 3%) were prepared. Among these, F6 exhibited adequate hardness, friability, disintegration, uniformity of content and total drug dissolution after 45minutes. Comparing the F6 dissolution profile with that of the brand-name tablets, the difference factor (f1) was 5.93 and the similarity factor (f2) 67.85. Hence, formulation F6 was found to be equivalent to Neurontin . Keywords: Dissolution. Gabapentin. Tablet. Binder.
Cancer nanotechnology
Jagdale Swati,Shah Tejas,Kuchekar Bhanudas,Chabukswar Aniruddha
Asian Journal of Pharmaceutics , 2009,
Abstract: Cancer nanotechnology is the latest trend in cancer therapy. It helps the pharmacist to formulate the product with maximum therapeutic value and minimum or negligible range side effects. Cancer is the disease in which the abnormal cells are quite similar to the normal cell with just minute functional or genetic change. Thus, it is very hard to target the abnormal cells by the conventional method of the drug delivery system. Nanotechnology is probably the only method that can be used for site-specific action without causing the side effects by killing the normal cells. This review article describes the possible way to exploit the nanotechnology to targeted drug therapy in cancer. The various methods used are: systemic delivery systems, passive targeting, active targeting, intracellular delivery, subcellular localization, and nanoparticle drugs. Different cancer detection techniques like carbon nanotubes, nanorods, and biosensors are also available. This review article gives an idea about the possible potential of nanotechnology in drug delivery, drug targeting, and the diagnosis of cancer.
Formulation and evaluation of chewable tablet of levamisole
Swati Jagdale, Mahesh Gattani, Dhaval Bhavsar, Bhanudas Kuchekar, Aniruddha Chabukswar
International Journal of Research in Pharmaceutical Sciences , 2010,
Abstract: Levamisole is a synthetic imidazothiazole derivative that has been widely used in treatment of worm infestations in both humans and animals. As an anthelmintic, it probably works by targeting the nematode nicotinergic acetylcholine receptor. In the market, levamisole tablets are available in the form of tablets. Geriatric and paediatric patients find it difficult to swallow these tablets. So in order to avoid this problem, chewable tablets are most preferable. The chewable tablets of levamisole were prepared by using lactose or mannitol along with sodium starch glycolate in concentration ratios especially for paediatric use. Sodium saccharin and vanilla were used as sweetening agent and flavouring agent respectively. From the disintegration studies, it was observed that the formulation containing 1.6% w/w of sodium starch glycolate shows minimum disintegration time whereas formulation having no or less concentration of sodium starch glycolate shows increase in disintegration time. It was observed that the formulation containing lactose shows less disintegration time than formulation containing mannitol.
Physicochemical characterization and solubility enhancement studies of allopurinol solid dispersions
Changdeo, Jagdale Swati;Vinod, Musale;Shankar, Kuchekar Bhanudas;Rajaram, Chabukswar Anuruddha;
Brazilian Journal of Pharmaceutical Sciences , 2011, DOI: 10.1590/S1984-82502011000300009
Abstract: allopurinol is a commonly used drug in the treatment of chronic gout or hyperuricaemia associated with treatment of diuretic conditions. one of the major problems with the drug is that it is practically insoluble in water, which results in poor bioavailability after oral administration. in the present study, solid dispersions of allopurinol were prepared by solvent evaporation, kneading method, co-precipitation method, co-grinding method and closed melting methods to increase its water solubility. hydrophilic carriers such as polyvinylpyrrolidone, polyethylene glycol 6000 were used in the ratio of 1:1, 1:2 and 1:4 (drug to carrier ratio). the aqueous solubility of allopurinol was favored by the presence of both polymers. these new formulations were characterized in the liquid state by phase solubility studies and in the solid state by differential scanning calorimetry, powder x-ray diffraction, uv and fourier transform infrared spectroscopy. solid state characterizations indicated that allopurinol was present as an amorphous material and entrapped in polymer matrix. in contrast to the very slow dissolution rate of pure allopurinol, the dispersion of the drug in the polymers considerably enhanced the dissolution rate. solid dispersion prepared with polyvinylpyrrolidone showed highest improvement in wettability and dissolution rate of allopurinol. mathematical modeling of in vitro dissolution data indicated the best fitting with korsemeyer-peppas model and the drug release kinetics primarily as non-fickian diffusion. therefore, the present study showed that polyvinylpyrrolidone and polyethylene glycol 6000 have a significant solubilizing effect on allopurinol.
Solubility enhancement, physicochemical characterization and formulation of fast-dissolving tablet of nifedipine-betacyclodextrin complexes
Jagdale, Swati Changdeo;Jadhav, Vinayak Narhari;Chabukswar, Aniruddha Rajaram;Kuchekar, Bhanudas Shankar;
Brazilian Journal of Pharmaceutical Sciences , 2012, DOI: 10.1590/S1984-82502012000100015
Abstract: the main objective of the study was to enhance the dissolution of nifedipine, a poorly water soluble drug by betacyclodextrin complexation and to study the effect of the preparation method on the in vitro dissolution profile. the stoichiometric ratio determined by phase solubility analysis for inclusion complexation of nifedipine with β-cyclodextrin was 1:1. binary complex was prepared by different methods and was further characterized using xrd, dsc and ft-ir. a saturation solubility study was carried out to evaluate the increase in solubility of nifedipine. the optimized complex was formulated into fast-dissolving tablets by using the superdisintegrants doshion p544, pregelatinized starch, crospovidone, sodium starch glycolate and croscarmellose sodium by direct compression. tablets were evaluated for friability, hardness, weight variation, disintegration and in vitro dissolution. tablets showed an enhanced dissolution rate compared to pure nifedipine.
Formulation and in vitro evaluation of taste-masked oro-dispersible dosage form of diltiazem hydrochloride
Jagdale, Swati Changdeo;Gawali, Vaibhav Uttam;Kuchekar, Bhanudas Shankar;Chabukswar, Aniruddha Rajaram;
Brazilian Journal of Pharmaceutical Sciences , 2011, DOI: 10.1590/S1984-82502011000400028
Abstract: diltiazem hydrochloride is a calcium channel blocker generally indicated for the treatment of angina and hypertension, and it is extensively metabolized due to the hepatic metabolism. formulation of diltiazem hydrochloride into an oro-dispersible dosage form can provide fast relief with higher bioavailability. the bitter taste of the drug should be masked to formulate it in a palatable form. in the present work, an attempt was made to mask the taste by complexation technique, with a formulation into an oro-dispersible dosage form, using superdisintegrants doshion p544, crospovidone (cp) and sodium starch glycolate (ssg). the complexes of diltiazem hydrochloride with β-cd (1:1 molar ratio) were prepared by kneading, co-evaporation, co-grounding, freeze-drying and melting methods. phase solubility showed stability constant 819.13m-1. prepared inclusion complexes were evaluated for taste masking and characterized by i.r, xrd, dsc. using the drug β-cd complex, oro-dispersible tablets were prepared and evaluated for hardness, friability, weight variation, thickness, disintegrating time (dt), dissolution rate and taste. formulations with 4 % doshion, 8 % cp and 4 % ssg showed dt of 0.54, 0.35 and 1.23 minutes, respectively.
Superdisintegrant Selection for Tramadol Dispersible Tablets Superdisintegrant Selection for Tramadol Dispersible Tablets
SWATI JAGDALE,NISHA C. FERNANDES,ANIRUDDHA R. CHABUKSWAR,BHANUDAS S. KUCHEKAR
Revista de Ciências Farmacêuticas Básica e Aplicada , 2010,
Abstract: The selection of a suitable superdisintegrant for a rapidly disintegrating dosage form is of utmost importance, since disintegration time is a critical parameter. An experimental design was designed so as to find out the effect of superdisintegrants (sodium starch glycollate, crospovidone, croscarmellose sodium and Methacrylic copolymer with divinyl benzene) at 2, 4, 6% w/w and its effect on hardness with respect to disintegration time. 4% w/w methacrylic copolymer with divinyl benzene is selected as the best superdisintegrant, effective enough for Tramadol. With increase in hardness, there was a considerable increase disintegration time with all concentrations of superdisintegrants. Crospovidone and Methacrylic copolymer with divinyl benzene in combination showed a remarkable drop in disintegration time upto 0.33 min. Stability Studies of the batch with lowest disintegration time was also carried out and suggests that there was no degradation with respect to time. The selection of a suitable superdisintegrant for a rapidly disintegrating dosage form is of the utmost importance, since disintegration time (DT) is a critical parameter. An experimental design was implemented, to find out the effects of superdisintegrants (sodium starch glycolate, crospovidone, croscarmellose sodium and methacrylic copolymer with divinyl benzene), at 2, 4, 6% w/w, on tablet hardness, with respect to DT. Methacrylic copolymer with divinyl benzene (at 4 wt%) was selected as the best superdisintegrant, adequate for the formulation of dispersible Tramadol tablets. With increasing hardness, there was a considerable increase in DT at all concentrations of superdisintegrants. A combination of crospovidone and methacrylic copolymer with divinyl benzene showed a remarkable drop in DT to 0.33 min. The stability of the batch with lowest DT was also tested under various conditions and the results suggested that there was no degradation over the test period. Keywords: Tramadol. Sodium Starch Glycolate. Crospovidone. Croscarmellose Sodium. Superdisintegrants.
Dissolution Rate Enhancement, Design and Development of Buccal Drug Delivery of Darifenacin Hydroxypropyl β-Cyclodextrin Inclusion Complexes
Swati C. Jagdale,Prachyasuman Mohanty,Aniruddha R. Chabukswar,Bhanudas S. Kuchekar
Journal of Pharmaceutics , 2013, DOI: 10.1155/2013/983702
Abstract: Darifenacin is a urinary antispasmodic. The oral absorption of darifenacin is poor due to its low solubility and poor bioavailability (15–19%). Darifenacin was complexed with hydroxylropyl beta-cyclodextrin (Hpβ-CD). The best results were obtained with the coevaporation that interacts in a 1?:?1 drug?:?cyclodextrin molar ratio. The solid inclusion complexes were found to be amorphous in the characterization. The dissolution rate of darifenacin from the Hpβ-CD solid inclusion complex was increased compared to the powdered drug. The controlled release buccoadhesive patches for the delivery of darifenacin were prepared using HPMC K100M CR and HPMC K15. The coevaporation complex of the drug was used in the formulation due to its increased saturation solubility and increased ease of dissolution. The patches were evaluated for their surface pH, folding endurance, swelling, mucoadhesive properties, in vitro residence time, vapour transmission test, and in vitro and ex vivo release studies. Formulations Hb2 (2%) and Pb4 (4%) were found to be optimized. These two formulations can be used for buccal delivery of darifenacin which avoids first pass effect and leads to increased bioavailability of darifenacin. 1. Introduction Cyclodextrin is capable of forming inclusion complexes with many drugs by taking up a whole drug molecule, or a part of it, into the cavity of the cyclodextrin molecule. Drug cyclodextrins complexes can improve the clinical usage of drugs by increasing their aqueous solubility, dissolution rate, and pharmaceutical availability [1]. Hpβ-CD can be used to solubilise poorly water-soluble drugs by complexation and then delivery via the buccal or sublingual mucosa may be advantageous for increasing drug absorption. The buccal route has high acceptance due to avoidance of first pass metabolism and possibility of being accessible for controlled drug release. Various bioadhesive mucosal dosage forms have been developed which include adhesive tablets, gels, ointments, and more recently patches. Buccal patches are preferred over adhesive tablets in terms of flexibility and patients comfort.Nowadays bioadhesive polymers receive considerable attention as platforms for buccal controlled delivery due to their ability to localize the dosage form in specific regions to enhance drug bioavailability [2, 3]. Buccal mucosa is a potential site for the delivery of drugs to the systemic circulation. A drug administered through the buccal mucosa enters directly the systemic circulation, thereby minimizing the first-pass hepatic metabolism and adverse gastrointestinal
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