Development of Pulsatile Drug Delivery for Chronotherapeutics of Hypertension

Kanugo, Abhishek; Kochar, Nitin I.; Chandewar, A. V.

doi:10.25258/ijddt.v7i03.9562

Cited by 3 publications

(5 citation statements)

References 2 publications

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“…The powder mass was subjected for compression and tablets were prepared on 12 station multi-tooling machine (Rimek mini press-II, Karnavati Engineering, Ahmadabad). The formulation constituents were depicted in Table 7 [27][28].…”

Section: Formulation Of Tablets From the Powder Blendsmentioning

confidence: 99%

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Neusilin US2 based Liquisolid Compact technique for the enhancement of solubility and dissolution rate of Olmesartan: Box-Behnken design approach

KANUGO¹,

THANVI²

2023

jrp

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The therapeutic efficacy of an active ingredients are imperfect owing to the poor solubility and dissolution rate. Moreover, dissolution is the rate-limiting period towards the absorption and bioavailability of the active ingredients. Olmesartan medoxomil is an angiotensin II receptor blocker (ARB) recommended for the therapy of high blood pressure as well as minimizes the chances of stroke, heart attack and kidney problems. Olmesartan medoxomil is a BCS class II molecule with only 26 % bioavailability. Hence, the current research work was focused on cost-effective Liquisolid technology for the improvement of solubility, dissolution rate and thereby achieving higher therapeutic efficacy. Liquisolid Compact is one of the best technique for improvement of solubility of potent hydrophobic molecules by utilizing non-volatile solvent. The solubility of olmesartan was estimated in several non-volatile solvents and tween 80 (95 mg/ml) was found to be best. The formed liquid medicaments were converted into the free-flowing powder blends for direct compression by the addition of carrier (Dibasic anhydrous calcium phosphate) and coating agent (Neusilin US2). The drug-excipients compatibilities were confirmed with FTIR. QbD design (Box-Behnken) was applied which comprised of independent factors (X1: DCP, X2: Neusilin US2, X3: CCS) and dependable factors were (Y1: Disintegration time, Y2: Dissolution release). The Design of expert software (DOE, Statease, Version 11) showed 12 batches which were evaluated for their flowing characteristics. The optimized batch F12 showed excellent flowing characteristics (Carr's index: 14, Angle of repose: 24.42), rapid disintegration time (2.07 min), in-vitro drug release (99.45%) and qualify under accelerated stability testing with minimal drug loss.

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Section: Formulation Of Tablets From the Powder Blendsmentioning

confidence: 99%

“…ARB has typical action against angiotensin II and modulate the blood pressure by their prompt vasoconstriction mechanism. Moreover, these agents are highly effective and good tolerability in several persons [16].…”

Section: Introductionmentioning

confidence: 99%

Neusilin US2 based Liquisolid Compact technique for the enhancement of solubility and dissolution rate of Olmesartan: Box-Behnken design approach

KANUGO¹,

THANVI²

2023

jrp

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“…The core tablets were evaluated for post-compression analysis and an optimized batch was selected based on the least disintegration time and greater dissolution release [31].…”

Section: Optimization Of Core Tabletsmentioning

confidence: 99%

“…The mechanistic approach for early morning surge is attributed due to the stimulation of the sympathetic nervous system [9]. The temporal rhythm of the body strongly impacted the number of diseases along with the pharmacokinetics and pharmacodynamics of maximum molecules in use [10]. Chronopharmaceutics include pharmaceutical applications of chronobiology in drug delivery.…”

Section: Introductionmentioning

confidence: 99%

“…Disease conditions such as early morning symptoms of blood pressure, asthma, arthritis, and ischemic heart disease, a time-controlled pulsatile drug delivery system offer more benefits [14]. A pulsatile drug delivery system (PDDS) is defined as the ''system which releases the drug rapidly and completely after a lag time, thus providing spatial and temporal delivery and increasing patient compliance'' [15]. PDDS is differentiated from conventional for offering improved bioavailability, reduced adverse effects and tolerability, no risk of dose dumping, improved stability, patient comfort and compliance and achieved a unique release pattern [16].…”

Section: Introductionmentioning

confidence: 99%

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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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Design and Development of Fast-dissolving Tablets of Apixaban using Single Coprocessed Excipient

Jaiswal,

Kanugo

2024

Scopus Indexed

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Background: Apixaban is administered orally as an anticoagulant action and minimizes the chances of strokes and systemic embolism. The conventional film-coated tablet showed less bioavailability due to its minimal solubility in the gastrointestinal tract. Rationale: The goal of designing the current analysis is to prepare a prompt release tablet using a single Coprocessed excipient which minimizes multistep processing, time, and cost effectiveness. Methods: The prompt release tablets of Apixaban were developed by direct compression technique using multifunctional material like Prosolve ODT G2 and Prosolve Easytab. Drug excipients inertness was confirmed with FTIR and DSC. Flowing characteristics of Apixaban and co-processed excipients were evaluated in terms of Carr’s index, Angle of repose, and Hausner’s ratio. These co-processed excipients indicated exceptional flowing and compression characteristics. The ready tablets were assessed for weight variation, hardness, friability, dispersion time, disintegration, and dissolution studies. Results: Among 12 batches, the least disintegration time was shown with C6 with a cumulative drug release of 99.06 % within 25 min. The optimized batch C6 was highly stable when tested under stability guidelines at 40 0 C and at 75 % relative humidity. Conclusion: Among these co-processed excipients, Prosolve Easytab SP was found the best one for direct compression intended for the immediate or fast dissolving tablets.

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Development of Pulsatile Drug Delivery for Chronotherapeutics of Hypertension

Cited by 3 publications

References 2 publications

Neusilin US2 based Liquisolid Compact technique for the enhancement of solubility and dissolution rate of Olmesartan: Box-Behnken design approach

Neusilin US2 based Liquisolid Compact technique for the enhancement of solubility and dissolution rate of Olmesartan: Box-Behnken design approach

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

Design and Development of Fast-dissolving Tablets of Apixaban using Single Coprocessed Excipient

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