A Novel Multicompartment Dissolution Apparatus for Evaluation of Floating Dosage Form Containing Poorly Soluble Weakly Basic Drug

Parikh, Rajesh K.; Parikh, Dhaivat; Delvadia, Renish R.; Patel, Sanjay M.

doi:10.14227/dt130106p14

Cited by 20 publications

(10 citation statements)

References 14 publications

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“…Parikh et al (20) prepared a floating tablet of CNZ using HPMC K100 and sodium bicarbonate and tested in a multicompartment dissolution apparatus. Complete release was reported within 24 h with nearly zero-order release rate and no precipitation observed in the intestinal compartment, giving 100% of CNZ transferred to absorption compartment.…”

Section: In Vitro Drug Releasementioning

confidence: 99%

In Vitro Release Kinetics and Bioavailability of Gastroretentive Cinnarizine Hydrochloride Tablet

Nagarwal

Ridhurkar²,

Pandit

2010

AAPS PharmSciTech

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Abstract. An oral sustained release dosage form of cinnarizine HCl (CNZ) based on gastric floating matrix tablets was studied. The release of CNZ from different floating matrix formulations containing four viscosity grades of hydroxypropyl methylcellulose, sodium alginate or polyethylene oxide, and gasforming agent (sodium bicarbonate or calcium carbonate) was studied in simulated gastric fluid (pH 1.2). CNZ release data from the matrix tablets were analyzed kinetically using Higuchi, Peppas, Weibull, and Vergnaud models. From water uptake, matrix erosion studies, and drug release data, the overall release mechanism can be explained as a result of rapid hydration of polymer on the surface of the floating tablet and formation of a gel layer surrounding the matrix that controls water penetration into its center. On the basis of in vitro release data, batch HP1 (CNZ, HPMC-K100LV, SBC, LTS, and MgS) was subjected to bioavailability studies in rabbits and was compared with CNZ suspension. It was concluded that the greater bioavailability of HP1 was due to its longer retention in the gastric environment of the test animal. Batch no. HP1 of floating tablet in rabbits demonstrated that the floating tablet CNZ could be a 24-h sustained release formulation.

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Section: In Vitro Drug Releasementioning

confidence: 99%

In Vitro Release Kinetics and Bioavailability of Gastroretentive Cinnarizine Hydrochloride Tablet

Nagarwal

Ridhurkar²,

Pandit

2010

AAPS PharmSciTech

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“…Cinnarizine is furthermore used as an agent to reduce motion sickness 13. It is a weak base with a p K a1 = 2.0 and p K a2 = 7.514 having higher solubility at lower pH (0.29 mg/mL in 0.1 N HCl) and lower solubility at higher pH (0.002 mg/mL in phosphate buffer pH 7.2) 15. Finally cinnarizine has a log P of 5.8 and is a lipophilic compound having a solubility in oleic acid of 237 mg/g 16…”

Section: Introductionmentioning

confidence: 99%

Precipitation of a Poorly Soluble Model Drug during In Vitro Lipolysis: Characterization and Dissolution of the Precipitate

Sassene

Knopp

Hesselkilde

et al. 2010

Journal of Pharmaceutical Sciences

139

115

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“…Carr's compressibility index was calculated from the bulk and tapped densities using a tap density apparatus. [17,18] …”

Section: Characterization Of Granules Propertiesmentioning

confidence: 99%

Untitled

Shinde

2017

AJP

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Aim: An attempt has been made to improve drug concentration in the stomach by preparing gastroretentive, swellable, matrix-based sustained release tablets of diltiazem hydrochloride that due to their size would be retained in the upper part of gastrointestinal tract. Materials and Methods: A 3 2 full factorial design was employed for the formulation of expandable tablets; two variables were evaluated. In the present investigation, the amounts of HPMC K100M and sodium carboxymethyl cellulose were selected as independent variables and effect of these variables, on swelling index (SI) and drug release was studied. Tablets were prepared and characterized by physical properties of compressed tablets such as hardness, friability, weight variation, content uniformity, SI, and drug release were determined. Results and Discussion: The SI of optimized batch varied between 114.21% and 220.41%. The percentage drug release of optimized batch was 15.60 at 1 h and 71.97% at 12 h. From the drug release kinetic study, Peppas model was found to be the best fit. Infrared spectrum and differential scanning calorimetric thermograms showed that there was no interaction between drug and polymers in the formulation. Expandable gastroretentive tablets were achieved a size more than the diameter of the pylorus and are not able to pass through the pylorus, thus causing prolongation of gastric residence time. Conclusion: The study indicates that development of diltiazem hydrochloride tablet can be beneficial in the treatment of hypertension. It releases drug in sustained manner for an extended period of time to reduce frequency of administration and improve patient compliance.

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A Novel Multicompartment Dissolution Apparatus for Evaluation of Floating Dosage Form Containing Poorly Soluble Weakly Basic Drug

Cited by 20 publications

References 14 publications

In Vitro Release Kinetics and Bioavailability of Gastroretentive Cinnarizine Hydrochloride Tablet

In Vitro Release Kinetics and Bioavailability of Gastroretentive Cinnarizine Hydrochloride Tablet

Precipitation of a Poorly Soluble Model Drug during In Vitro Lipolysis: Characterization and Dissolution of the Precipitate

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