Molecular properties of ciprofloxacin-indion 234 complexes

Pisal, Sambhaji S.; Zainnuddin, Rana; Nalawade, Pradeep; Mahadik, Kakasaheb R.; Kadam, Shivajirao

doi:10.1208/pt050462

Cited by 41 publications

(40 citation statements)

References 17 publications

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“…The molecular state of drugs prepared as drug resin complexes was changed from crystalline state to amorphous state. This shows that entrapped drug molecules are monomolecularly dispersed in resin beads (Pisal et al 2004). …”

Section: X-ray Diffractionmentioning

confidence: 78%

Novel ion exchange resin-based combination drug-delivery system for treatment of gastro esophageal reflux diseases

Bhalekar¹,

Kadam²,

Patil³

et al. 2010

Braz. J. Pharm. Sci.

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The present study involves preparation and characterization of a combination tablet of ranitidine in immediate release form and domperidone in sustained release form, using ion exchange resins. Ranitidine lowers acid secretion, while domperidone release over a prolonged period improves gastric motility thus justifying this combination in gastro esophageal reflux diseases (GERD) and ensuring patient compliance. Drug loading was carried out by batch method & resinates were characterized using FTIR, XRPD. Resinates were formulated as a combination tablet and evaluated for tablet properties & in vitro drug release. Resinates provided sustained release of domperidone and immediate release of ranitidine. IR and X-ray studies indicate complexation of drug and resin along with monomolecular distribution of drugs in amorphous form in the resin matrix. The tablets of resinate combination showed good tablet properties. In-vitro drug release gave desired release profiles and ex-vivo drug absorption studies carried out by placing everted rat intestine in dissolution medium indicated statistically significant similarity in absorption from test and marketed formulation. The novelty of this study is that the retardation in release of domperidone from resinates is achieved by presence of weak resin in the formulation.Uniterms: Drugs/delivery system. Ranitidine/tablets/immediate release. Domperidone/tablets/sustained release. Tablets/delivery system. Ion exchange resins/use/ drugs delivery system. O presente estudo envolve a preparação e a caracterização de associação do comprimido de ranitidina de liberação imediata e domperidona de liberação prolongada, utilizando resinas de troca iônica. A ranitidina diminui a secreção ácida, enquanto a liberação prolongada de domperidona melhora a motilidade gástica, justificando, dessa forma, a associação em doenças de refluxo gastroesofágico (DRGE) e garantindo a adesão do paciente. A carga de fármaco foi efetuada pelo método em batelada e os resinatos, caracterizados utilizando-se FTIR e XRPD. Os resinatos foram formulados como comprimido da associação e avaliados com relação às propriedades dos comprimidos e liberação do fármaco in vitro. Os resinatos proporcionaram a liberação prolongada da domperidona e a liberação imediata da ranitidina. IV e estudos de difração de raios X indicaram a complexação do fármaco e da resina junto com a distribuição monomolecular dos fármacos, em estado amorfo, na matriz da resina. Os comprimidos da associação do resinato apresentaram boas propriedades. Obtiveram-se os perfis de liberação in vitro e os estudos de absorção dos fármacos ex vivo realizados com intestino de rato em meio de dissolução indicaram semelhança significativa na absorção entre as formulações teste e comercializada. A inovação do trabalho é que o retardamento da liberação da domperidona dos resinatos é atingido pela presença de resina fraca na formulação.

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Section: X-ray Diffractionmentioning

confidence: 78%

Novel ion exchange resin-based combination drug-delivery system for treatment of gastro esophageal reflux diseases

Bhalekar¹,

Kadam²,

Patil³

et al. 2010

Braz. J. Pharm. Sci.

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“…The results can be attributed to the fact that ofloxacin hydrochloride has a pKa between 6.08 hence will have maximum solubility and complete ionization near to this pH value. The decreased complexation at lower pH is due to excess H + ions in the solution, which have more binding affinity to the -COO -groups of resin and compete with the drug for binding (Pisal et al, 2004). Since maximum loading of ofloxacin on both the resins, Tulsion 335 and Indion 204 was seen at pH 6, it was selected for complexation of ofloxacin.…”

Section: Resultsmentioning

confidence: 99%

“…Methods of taste masking employ pH sensitive polymers like Eudragit E 100 (aminoalkylmethacrylate copolymers) (Shishu, Kapoor, Kamalpreet, 2009), polyacrylic acid ion exchange resin Indion 204, Indion 214, Indion 234, Indion CRP 244 and CRP 254, Tulsion 335, Amberlite IRP64 (Cation exchange resins) (Venkatesh, Jha, Karki, 2009;Mundada et al, 2008;Avari, Bhalekar, 2008;Pisal et al, 2004;Manek, Kamat, 1981;Tawakkul, 2009;Amin et al, 2005;Leonard, Cooper, 1998;Metcalf, Purdy, 2001).…”

Section: Introductionmentioning

confidence: 99%

Development and evaluation of ofloxacin orally disintegrating tablets

Mohite

Chafle

Somasundaram

et al. 2012

Braz. J. Pharm. Sci.

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Bitter taste of ofloxacin, a broad spectrum bactericidal agent, is masked and orally disintegrating tablets were formulated. The bitter taste is masked by forming complex between drug and weak cation exchange resins, Tulsion 335 and Indion 204. Effect of pH and drug:resin ratio on the drug loading was studied. Maximum drug loading was observed at pH 6. Ratio of 1:2 of drug:resin masked almost complete bitterness of ofloxacin. Formation of complexes was confirmed by IR spectroscopy. Physical characterization of taste masked complexes was carried out. Present work envisages the taste masking of ofloxacin and development of orally disintegrating tablets. The effect of pH and resin quantities on drug loading were studied to find the optimum conditions of drug loading for complete taste masking. Effect of superdisintegrants like sodium starch glycolate, croscarmellose sodium and polyplasdone XL at varying level on physical parameters of compressed tablets was also assessed. The formulations containing 5 % w/w polyplasdone XL showed about 90 % of drug release within 5 minutes. No significant differences were observed in the physical parameters of resinates as well as tablets prepared from Tulsion 335 and Indion 204. O gosto amargo de ofloxacina, agente bactericida de largo espectro, é mascarado e formularam-se comprimidos dispersíveis. O sabor amargo é mascarado pela formação de complexo entre o fármaco e resinas de troca catiônica fraca, Tulsion 335 e Indion 204. Efeito do pH e da proporção fármaco: resina sobre a carga de fármaco foi estudada. Carga de fármaco máxima foi observada em pH 6. Proporção 1:2 do fármaco: resina mascarou quase completamente o gosto amargo de ofloxacina. A formação de complexos foi confirmada por espectroscopia no IV. Caracterização física dos complexos de sabor mascarado foi realizada. O presente trabalho preconiza o mascaramento do gosto de ofloxacina e desenvolvimento decomprimidos por via oral, se desintegrando. O efeito do pH e da resina quantidades de carga de fármaco foram estudadas paraencontrar as condições óptimas de carga de fármaco para dissimulação do saborcompleto. Efeito da superdisintegrants como amido glicolato de sódio, croscarmelose sódica e Polyplasdone XL em diferentes níveis de parâmetros físicos de comprimidos também avaliados foi avaliada. As formulações contendo 5 %w/w Polyplasdone XL mostraram cerca de 90% de libertação do fármaco no prazo de 5 minutos. Não foram observadas diferenças significativas nos parâmetros físicos de resinatosbem como comprimidos preparados a partir de Tulsion 335 e Indion 204.

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“…Confirmation of Complexation (9,11,12) FTIR studies. Tramadol HCl, Tulsion 335, and physical mixture of both and DRC were subjected to Fourier transform infrared spectroscopy (FTIR) studies.…”

Section: Characterization Of Drcmentioning

confidence: 93%

“…Optimization of various parameters for maximum drug loading (9,10). Drug loading process was optimized for maximum drug loading considering parameters like effect of activation, resin swelling time, and pH.…”

Section: Taste Masking Of Tramadol Hclmentioning

confidence: 99%

Formulation Design and Optimization of Novel Taste Masked Mouth-Dissolving Tablets of Tramadol Having Adequate Mechanical Strength

Madgulkar¹,

Bhalekar²,

Padalkar³

2009

AAPS PharmSciTech

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Abstract. The purpose of this work was to develop novel taste masked mouth-dissolving tablets of tramadol that overcomes principle drawback of such formulation which is inadequate mechanical strength. Tramadol is an opioid analgesic used for the treatment of moderate to severe pain. Mouthdissolving tablets offer substantial advantages like rapid onset of action, beneficial for patients having difficulties in swallowing and in conditions where access to water is difficult. The crucial aspect in the formulation of mouth-dissolving tablets is to mask the bitter taste and to minimize the disintegration time while maintaining a good mechanical strength of the tablet. Mouth-dissolving tablets of tramadol are not yet reported in the literature because of its extreme bitter taste. In this work, the bitter taste of Tramadol HCl was masked by forming a complex with an ion exchange resin Tulsion335. The novel combination of a superdisintegrant and a binder that melts near the body temperature was used to formulate mechanically strong tablets that showed fast disintegration. A 3 2 full factorial design and statistical models were applied to optimize the effect of two factors, i.e., superdisintegrant (crospovidone) and a mouth-melting binder (Gelucire 39/01). It was observed that the responses, i.e., disintegration time and percent friability were affected by both the factors. The statistical models were validated and can be successfully used to prepare optimized taste masked mouth-dissolving tablets of Tramadol HCl with adequate mechanical strength and rapid disintegration.

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Molecular properties of ciprofloxacin-indion 234 complexes

Cited by 41 publications

References 17 publications

Novel ion exchange resin-based combination drug-delivery system for treatment of gastro esophageal reflux diseases

Novel ion exchange resin-based combination drug-delivery system for treatment of gastro esophageal reflux diseases

Development and evaluation of ofloxacin orally disintegrating tablets

Formulation Design and Optimization of Novel Taste Masked Mouth-Dissolving Tablets of Tramadol Having Adequate Mechanical Strength

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