Formulation of Tablets in Capsule system: Statistical optimization for chronotherapeutic drug delivery of propranolol hydrochloride

Gowthami, Buduru; Krishna, S.; Rao, D. Subba

doi:10.1016/j.jddst.2021.102398

Cited by 10 publications

(4 citation statements)

References 26 publications

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“…Hard gelatin capsules of size 1 were selected, and then caps and bodies were separated. Coating solution of prepared by using 10% w/v ethyl cellulose in methanol and 0.5% 0.5% dibutyl phthalate (plasticizer) was added [ 53 ]. Only bodies were allowed to dip in the prepared coating solution.…”

Section: Methodsmentioning

confidence: 99%

Development of Nanocrystal Compressed Minitablets for Chronotherapeutic Drug Delivery

Sreeharsha

Naveen²,

Anitha³

et al. 2022

Pharmaceuticals

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The present work aimed to develop a chronotherapeutic system of valsartan (VS) using nanocrystal formulation to improve dissolution. VS nanocrystals (VS-NC) were fabricated using modified anti-solvent precipitation by employing a Box–Behnken design to optimize various process variables. Based on the desirability approach, a formulation containing 2.5% poloxamer, a freezing temperature of −25 °C, and 24 h of freeze-drying time can fulfill the optimized formulation’s requirements to result in a particle size of 219.68 nm, 0.201 polydispersity index, and zeta potential of −38.26 mV. Optimized VS-NC formulation was compressed (VNM) and coated subsequently with ethyl cellulose and HPMC E 5. At the same time, fast dissolving tablets of VS were designed, and the best formulation was loaded with VNM into a capsule size 1 (average fill weight—400–500 mg, lock length—19.30 mm, external diameter: Cap—6.91 mm; Body—6.63 mm). The final tab in cap (tablet-in-capsule) system was studied for in vitro dissolution profile to confirm the chronotherapeutic release of VS. As required, a bi-pulse release of VS was identified with a lag time of 5 h. The accelerated stability studies confirmed no significant changes in the dissolution profiles of the tab in cap system (f2 similarity profile: >90). To conclude, the tab in cap system was successfully developed to induce a dual pulsatile release, which will ensure bedtime dosing with release after a lag-time to match with early morning circadian spikes.

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Section: Methodsmentioning

confidence: 99%

Development of Nanocrystal Compressed Minitablets for Chronotherapeutic Drug Delivery

Sreeharsha

Naveen²,

Anitha³

et al. 2022

Pharmaceuticals

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“…The randomly selected 6 tablets were kept in the disintegration test apparatus and the time required to pass all the particles from the sieves was noted. This test was carried out at 37±0.5° C using 900 ml of simulated gastric fluid [28].…”

Section: Disintegrationmentioning

confidence: 99%

pH-dependent pulsatile delivery of Ambrisentan for the treatment of hypertension

KANUGO¹,

DHAGE²

2023

jrp

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The greatest number of mortality in the world occurred due to hypertension. Several bodily functions are based on circadian rhythm including hypertension. The stimulation of the sympathetic nervous system in the early morning hours resulted in accelerating blood pressure which is a highly dangerous condition. This lead to cardiac failure and damage to the vital organs of the body. The current research focuses on pulsatile delivery of Ambrisentan for the treatment of high blood pressure which released the medicament at the right time and the right place. Primarily, core tablets were prepared with Ambrisentan. The compatibility of Ambrisentan with excipients was confirmed by FTIR analysis. The core tablets were evaluated for flowing characteristics which showed better flowing behavior and optimized core batch CT6 showed consolidation index 16.07±0.11 and angle of repose 27.02±0.14. Moreover, due to the least disintegration time (2.23±0.10) and greater dissolution release of 99.70 % ±0.49, CT6 was selected as an optimized core tablet for pulsatile delivery. Further, the combination of Eudragit L100 and ethyl cellulose were utilized for coating purposes in different proportion were utilized for achieving the desired lag time of 6 hrs. The optimized batch PC6 (Eudragit L100: EC 10) which comprised of 25:75 proportion showed a lag time of 6 hours, cumulative release of 99.25 % and content uniformity of 99.29±0.82. The dissolution release profile predicted zero-order release for Ambrisentan pulsatile tablets. The accelerated stability testing showed minimal loss of drug content when exposed at 40 0 C and 75 % relative humidity without altering lag time.

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“…These polymers according to table no 2 as CF1 to CF6 were mixed, 2/3 rd portion of the mixture was introduced in the die cavity, then the core tablet was placed and added the remaining 1/3rd portion, then compressed using 8mm punch. In the next step the buoyant compositions in Table no 5 using Ispaghula gum and Methocel K100M as major polymers for delayed oating were blended and compressed over the prepared compression coated tablet by using 9mm punch to obtain the coated oating tablets as BL1 to BL8 and nally the immediate release layer was compressed (9,10) Factorial Design of Buoyant Formulation:…”

Section: Identi Cation Of Drug and Spectral Studies By Ftirmentioning

confidence: 99%

Design, Formulation, Evaluation and Statistical Optimization of Coated Floating Pulsatile Tablets for Modified Chronopharmacotherapy of Rheumatoid Arthritis

jyothirmayi

2023

Preprint

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Objective The main aim of designing Coated Floating Pulsatile Tablets (CFPT) of Tramadol hcl for statistical optimization and to perform in vitro and in vivo buoyancy evaluation for modified chronopharmacotherapy of rheumatoid arthritis. Methods The formulation was designed with the immediate core covered with a compression coat followed by the upper buoyant layer. Best formulations of Immediate burst release core tablets were compression coated with polymer HPMC K15M, Ispaghula gum (IG), and Tamarindus gum (TG) to assign suitable lag time to formulation. HPMC K100M, Ispaghula gum, and their combination were compressed as the buoyant layers. Parameters such as BLT, TFT, %SI,% CDR were Statistical optimized by surface and contour plots AND invivo buoyancy was also done. Results Immediate release core tablets were optimized with formulation IF2 which contains sodium starch Glycolate 8% as immediate release agent, and then in compression coated buoyant formulation CFPT was optimized by DoE optimization showing BF4 and BF8 exhibiting good floating behavior and lag time, drug release for a period of 11 hrs. Abdominal X-ray imaging of rabbits after oral administration of the tablets, confirmed the floating behavior and lag time. Conclusion As the formulation showed delay in drug release both in in vitro and showed in vivo buoyancy, hence nighttime administration could be beneficial to reduce the rheumatoid arthritis complications in the early morning.

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Formulation of Tablets in Capsule system: Statistical optimization for chronotherapeutic drug delivery of propranolol hydrochloride

Cited by 10 publications

References 26 publications

Development of Nanocrystal Compressed Minitablets for Chronotherapeutic Drug Delivery

Development of Nanocrystal Compressed Minitablets for Chronotherapeutic Drug Delivery

pH-dependent pulsatile delivery of Ambrisentan for the treatment of hypertension

Design, Formulation, Evaluation and Statistical Optimization of Coated Floating Pulsatile Tablets for Modified Chronopharmacotherapy of Rheumatoid Arthritis

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