Immediate Release Tablets of Telmisartan Using Superdisintegrant-Formulation, Evaluation and Stability Studies

Sekar, Vasanthakumar; Chellan, Vijaya Raghavan

doi:10.1248/cpb.56.575

Cited by 26 publications

(17 citation statements)

References 5 publications

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“…Additionally Sekar et al (2008) reported the TLM as an insoluble in water; hence the drug may be slowly or incompletely dissolved in the gastro intestinal tract. So the rate of dissolution and therefore its bioavailability is less (bioavailability 42%).…”

Section: Resultsmentioning

confidence: 99%

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: Resultsmentioning

confidence: 99%

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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“…From this stock solution, further dilutions were performed for each formulation. Absorbance was measured and the concentration of the drug in the tablet was determined, using the calibration curve of pure drug in 0.1N HC1 spectrophotometrically at 236 nm, using 0.1N HC1 as blank (Kaushik et al, 2004;Malke et al, 2008;Sekar et al, 2008).…”

Section: Assay Methodsmentioning

confidence: 99%

Formulation and in vitro evaluation of taste-masked oro-dispersible dosage form of diltiazem hydrochloride

Jagdale¹,

Gawali²,

Kuchekar³

et al. 2011

Braz. J. Pharm. Sci.

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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.Uniterms: Diltiazem hydrochloride. Cyclodextrin. Drugs/taste-masking. Freeze-drying.O cloridrato de diltiazem é bloqueador do canal de cálcio geralmente indicado para o tratamento de angina e de hipertensão e é extensamente biotransformado devido ao metabolismo hepático. A formulação do cloridrato de diltiazem em orodispersão pode prover rápida liberação com maior biodisponibilidade. O sabor amargo do fármaco deve ser mascarado para ser formulado em forma palatável. No presente trabalho tentou-se mascarar o sabor pela técnica de complexação, com uma orodispersão, usando superdesintegrantes, como Doshio P544, crospivodina (CP) e glicolato de amido sódico (SSG). Os complexos de cloridrato de diltiazem com β-CD (razão molar 1:1) foram preparados por mistura, coevaporação, comoagem, liofilização e métodos de fusão. A solubilidade de fase mostrou estabilidade constante de 819,13 M -1 . Os complexos de inclusão preparados foram avaliados com relação ao mascaramento do sabor e caracterizados por IV, Difração de Raios X e DSC. Empregando-se o fármaco complexado com β-CD, prepararam-se comprimidos dispersíveis e avaliaram-se os mesmos quanto à dureza, friabilidade, variação de peso, espessura, tempo de desintegração (DT), taxa de dissolução e sabor. Formulações com 4% de Doshion, 8% de CP e 4% de SSG mostraram DT de 0,54, 0,35 e 1,23 minutos, respectivamente. Unitermos: Cloridrato de diltiazem. Ciclodextrina. Fármacos/mascaramento de sabor. Liofilização.

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“…Lubricants remove grittiness and assist in the drug transport mechanism from the mouth down into the stomach. 7,8,17 : A disintegrant is an excipient, which is added to a tablet or capsule blend to aid in the breakup of the compacted mass when it is put into a fluid environment.…”

Section: Advantages Of Immediate Release Drug Delivery Systemmentioning

confidence: 99%

“…Drug release studies were carried out in eight stage dissolution test apparatus using specified volume of dissolution media maintained at 37±2 The tablets are kept in the cylindrical basket and rotated at 100 rpm 5ml of the sample from the dissolution medium are withdrawn at each time interval (5,10,15,20,30,45, 50 & 60) minutes) and 5ml of fresh medium was replaced each time. The samples were filtered and from the filtrate 1ml was taken and diluted to 10ml 17 . One hand, The dissolution profiles were carried out by USP apparatus 2 (paddle) at 50 rpm in 1000 ml 0.1 N HCl and distilled water 10ml of the sample from the dissolution medium are withdrawn at each time interval (5,10,15,20,30, 45 & 60 minutes) and 10ml of fresh medium was replaced each time.…”

Section: Disintegration Testmentioning

confidence: 99%

Untitled

2013

IJPSR

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Tablet is the most popular among all dosage forms existing today because of its convenience of self-administration, compactness and easy manufacturing; however in many cases immediate onset of action is required than conventional therapy. There are novel types of dosage forms that act very quickly after administration. The basic approach used in development tablets is the use of superdisintegrants like Cross linked carboxymelhylcellulose (Crosscarmellose), Sodium starch glycolate (Primogel), Kollidon Cl etc. which provide instant disintegration of tablet after administration. A new dosage form allows a manufacturer to extend market exclusivity, while offering its patient population a more convenient dosage form or dosing regimen. In this regard, immediate release formulations are similar to many sustained release formulations that are now commonly available.

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Immediate Release Tablets of Telmisartan Using Superdisintegrant-Formulation, Evaluation and Stability Studies

Cited by 26 publications

References 5 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

Formulation and in vitro evaluation of taste-masked oro-dispersible dosage form of diltiazem hydrochloride

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