Development, optimization and pharmacokinetic evaluation of biphasic extended-release osmotic drug delivery system of trospium chloride for promising application in treatment of overactive bladder

Gundu, Ramakanth; Pekamwar, Sanjay S.; Shelke, Santosh; Kulkarni, Deepak; Shep, Santosh

doi:10.1186/s43094-021-00311-6

Cited by 7 publications

(7 citation statements)

References 38 publications

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“…The impact of orifice diameter on in vitro rivastigmine release was studied by mechanically drilling various orifices of about 0.4, 0.5, and 0.6 mm on the optimized formulation. 43 Subsequently the drilled tablets were subjected to dissolution.…”

Section: Impact Of Orifice Diametermentioning

confidence: 99%

Development and Characterization of Rivastigmine Hydrogen Tartrate Elementary Osmotic Tablets

Naz,

CVS Subrahmanyam,

Rachamalla

2023

Int J. Pharm. Investigation

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Background: The present study aims to develop an Elementary Osmotic tablet (EOP) of Rivastigmine Hydrogen Tartrate (RHT). EOP consists of a core tablet suitably coated with a polymeric solution, and an orifice drilled on one side of the tablet. Materials and Methods: The influence of core variables, including sodium chloride (osmogen) concentration and Polyvinyl Pyrrolidine K30 (PVP K30) concentration, have been investigated and optimized by factorial design. The effect of membrane (coating) variables, including polyethylene glycol 400 (PEG 400) amount and percent coating weight gain have been studied. The rivastigmine release of the optimized system has been investigated in various dissolution media, at different stirring rates, at variable pH, and variable osmotic pressure. Results: It was observed that PEG 400 incorporated in the coating membrane improved drug release. The sodium chloride had a profoundly positive influence, and PVP K30 had a negative influence on the rivastigmine release. The finding reveals that the core tablet containing sodium chloride (50 mg) and PVP K30 (2.5 mg) coated with the solution containing 20% PEG 400 and 5% weight gain was optimized. Conclusion: The developed EOP provides the RHT release for up to 24 hr with improved bioavailability. The results instigated a controlled release of rivastigmine.

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Section: Impact Of Orifice Diametermentioning

confidence: 99%

Development and Characterization of Rivastigmine Hydrogen Tartrate Elementary Osmotic Tablets

Naz,

CVS Subrahmanyam,

Rachamalla

2023

Int J. Pharm. Investigation

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“…FTIR spectra of pure drug and final Formulation carried out using the K.B.R. disc method as graphs of FTIR shown in results section [32,33,36].…”

Section: Ftir Studymentioning

confidence: 99%

“…spectra of a mixture of drug and polymers, which indicate physical compatibility between L.H. and all ingredients used in the final Formulation of the transdermal matrix patch [36].…”

Section: Ftir Studymentioning

confidence: 99%

“…The same way results of the folding endurance study showed that the patch would not break and maintain their integrity with general skin folding applied. The results are listed in (Table 7) [35,36,51,52].…”

Section: Physicochemical Evaluations Of Lh Containing Transdermal Mat...mentioning

confidence: 99%

“…DSC peak of Lercanidipine hydrochloride shown in Fig 7. and DSC curve of P9 formulation shown in Fig 8. The DSC peak elucidations for drug alone and powder mixture are represented in Table 6[36].…”

mentioning

confidence: 99%

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Fabrication of Transdermal Matrix Patch of Lercanidipine Hydrochloride Using Natural Polymer and Essential Oil

Jani

Puri

Chakraborthy

et al. 2022

JPRI

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The goal of the present research work was to develop and characterize a transdermal matrix patch of Lercanidipine hydrochloride (L.H.) for controlled drug delivery using the solvent evaporation method. To achieve controlled drug release, polymers such as Psyllium and HPMC K15M were optimized. Moreover, the skin permeation effect of essential oils such as linseed oil, jojoba oil, and pumpkin seed oil was investigated on Wistar rat skin. A 32 full factorial design was applied to optimize two formulation variables: concentration of essential oil as a permeation enhancer and polymer fixed-weight ratio. To study drug-excipients incompatibility, Fourier Transform Infrared Spectroscopy (FTIR) had employed, which showed the absence of chemical interaction. All formulations were evaluated for Physico-chemical parameters, ex-vivo drug release study, an in-vivo skin-irritation study on Wistar rats, and stability study. Developed matrix patch showed optimum Physico-chemical properties with the absence of skin irritation. An Ex-vivo drug release study revealed that both formulation variables show an effect on drug release from matrix patches. The effectiveness of the oils as the permeation enhancer was found to be in the following descending order: Pumpkin seed oil > Linseed oil > Jojoba oil. Therefore, pumpkin seed oil was selected as a permeation enhancer in the final Formulation that shows the highest flux (164.09±1.49 µg/cm2/h) and desired drug release for transdermal administration. Stability study shows that the patch was stable up to 6 months at 40±2 ˚C and 75±5 % R.H. and 30±2 ˚C and 65±5 % R.H. The present investigation demonstrates that the prepared matrix patch can deliver therapeutically effective controlled release dose of lercanidipine hydrochloride (L.H.) via transdermal route using pumpkin seed oil as the permeation enhancer.

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Development and pharmacokinetic evaluation of osmotically controlled drug delivery system of Valganciclovir HCl for potential application in the treatment of CMV retinitis

Gundu

Pekamwar

Shelke³

et al. 2022

Drug Deliv. and Transl. Res.

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Valganciclovir HCl (VGH) is the widely used drug for the treatment of Cytomegalovirus (CMV) retinitis infection with an induction dose of 900mg twice a day and a maintenance dose of 900mg. This required dose of the drug also leads to multiple side effects due to repeated administration. The research was highlighted to develop, formulate, optimize and evaluate Single-Core Osmotic Pump (SCOP) tablet of VGH with the dose of 450mg to reduce dosing frequency and associated side effects. . The decrease in dose also minimize the hepatic and nephrotic load. The optimized batch of formulation was subjected to comparative in vitro and in vivo evaluation. The tablet core composition is the primary in uencer of the drug delivery fraction in a zero-order, whereas the membrane characteristics control the drug release rate. In-vivo pharmacokinetic studies revealed that the newly developed osmotic formulation has controlled zero-order release for 24 hours with a single dose of 450mg while the marketed formulation requires twice administration within 24 hours to maintain the plasma concentration in the therapeutic window. The developed formulation can be the promising option for the treatment of CMV retinitis with the minimum dose and dosing frequency. MaterialsVGH was obtained as a free sample from Wockhardt Research Centre, Aurangabad (M.S), India, and lactose monohydrate was obtained from DFE Pharma, India.

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Development, optimization and pharmacokinetic evaluation of biphasic extended-release osmotic drug delivery system of trospium chloride for promising application in treatment of overactive bladder

Cited by 7 publications

References 38 publications

Development and Characterization of Rivastigmine Hydrogen Tartrate Elementary Osmotic Tablets

Development and Characterization of Rivastigmine Hydrogen Tartrate Elementary Osmotic Tablets

Fabrication of Transdermal Matrix Patch of Lercanidipine Hydrochloride Using Natural Polymer and Essential Oil

Development and pharmacokinetic evaluation of osmotically controlled drug delivery system of Valganciclovir HCl for potential application in the treatment of CMV retinitis

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