Optimasi Hidroksipropil Metilselulosa dan Polivinil Pirolidon dalam Sediaan Mucoadhesive Buccal Film Diltiazem Hidroklorida

Diltiazem HCl is a class of benzodiazepine calcium channel blockers used to treat angina pectoris, arrhythmias, and hypertension. Diltiazem HCl improves first-pass metabolism, a short half time of 3-5 hours, and bioavailability of diltiazem for oral administration of about 40%. Mucoadhesive buccal film diltiazem HCl releases the drug to the buccal mucosa, so the first pass metabolism can be avoided because of its absorption through the venous system that flows from the cheek. This study aimed to study HPMC polymers and polyvinyl pyrrolidone (PVP) polymers on swelling index, residence time, mucoadhesive strength of mucoadhesive buccal film diltiazem HCl, FTIR, and drug release. The prepared film was evaluated for swelling index, mucoadhesive strength, and mucoadhesive residence time. The optimal amount for HPMC was 35 mg, and PVP was 15 mg. The combination of polymers with this amount can produce a swelling index was 3,00, mucoadhesive strength was 41,87 gF, and mucoadhesive residence time was 330,66. FTIR test indicated that there was no interaction between active function clusters of Diltiazem HCl and other excipients. The release of the optimum formula in the 360th minute was about 97.847%, following in the zero-order release model and Higuchi.

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OPTIMASI POLIVINILPIROLIDON DAN CARBOPOL PADA SEDIAAN PATCH DISPERSI PADAT PIROKSIKAM

Jurnal Ilmiah Manuntung ◽

10.51352/jim.v3i2.129 ◽

2018 ◽

Vol 3 (2) ◽

pp. 197

Author(s):

Dwi Nurahmanto ◽

Friska Wira Sabrina ◽

Lidya Ameliana

Keyword(s):

Solid Dispersion ◽

Lattice Design ◽

Simplex Lattice Design ◽

Peg 4000 ◽

First Pass Metabolism ◽

First Pass ◽

Inflammatory Drugs ◽

Simplex Lattice ◽

Optimum Formula ◽

Pass Metabolism

Piroxicam, a non steroidal anti inflammatory drugs (NSAID), is an oxicam derivative which can be used for treatment of various rheumatic diseases, such as rheumatoid arthritis and osteoarthritis. Piroxicam patch is an affective approach evading piroxicam’s side effect such as peptic ulcer and first pass metabolism. One of the patch components is polymer that the function is to control the speed of drug release from the patch. The aims of this study were to determine the optimum formula of a combination of polyvinylpyrolidone (PVP) and Carbopol to % moisture content (MC) and the flux release in solid dispersion piroxicam patch using Simplex Lattice Design. Piroxicam was prepared in the form of a solid dispersion in PEG 4000 to increase its solubility. The design formula of solid dispersion piroxicam patch made with the ratio PVP : Carbopol, that were 1 : 0; 0.5 : 0.5; 0 : 1. The optimum formula was chosen with the ratio PVP : Carbopol, 1: 0, which gave the best result of % MC and flux release. The result of % MC was 6.91% and the result of flux release was 35.543 µg/cm2.menit1/2.

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An Optimasi Polivinil Pirolidon dan Kitosan dalam Sediaan Mucoadhesive Buccal Film Diltiazem HCl

Pustaka Kesehatan ◽

10.19184/pk.v7i3.11543 ◽

2020 ◽

Vol 7 (3) ◽

pp. 177

Author(s):

Viddy Agustian Rosyidi ◽

Ulfia Dwi Novita ◽

Lusia Lusia Oktora Ruma Kumala Sari

Keyword(s):

Calcium Channel ◽

Calcium Channel Blocker ◽

Channel Blocker ◽

First Pass Metabolism ◽

First Pass ◽

Diltiazem Hcl ◽

Pass Metabolism

Diltiazem HCl adalah golongan benzoatiazepin penghambat kanal kalsium (calcium channel blocker) yang digunakan dalam pengobatan angina pektoris, aritmia, dan hipertensi. Diltiazem HCl mengalami first pass metabolism di hati, waktu paruh yang pendek yakni 3-5 jam dan bioavailabilitas diltiazem pada pemberian oral sekitar 40%. Sediaan mucoadhesive buccal film diltiazem HCl melepaskan obat ke mukosa buccal sehingga dapat menghindari first pass metabolism karena absorpsinya melalui sistem vena yang mengalir dari pipi. Tujuan penelitian ini adalah untuk mengetahui pengaruh polimer polivinil pirolidon (PVP) dan kitosan terhadap swelling index, waktu tinggal dan kekuatan mucoadhesive diltiazem HCl dalam sediaan mucoadhesive buccal film diltiazem HCl. Sediaan film dilakukan evaluasi swelling index, kekuatan mucoadhesive dan waktu tinggal mucoadhesive. Jumlah optimum untuk PVP adalah 1 mg dan kitosan sebesar 25 mg. Kombinasi polimer dengan jumlah tersebut dapat menghasilkan swelling index, kekuatan mucoadhesive, dan waktu tinggal mucoadhesive yaitu 3,641; 63,867 gF; dan 352,667 menit dan nilai desirability tertinggi yaitu 0,727. Kata kunci: mucoadhesive buccal film, diltiazem HCl, PVP, kitosan

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Identification of a Cranberry Juice Product Capable of Inhibiting Enteric CYP3A-Mediated First-Pass Metabolism in Humans

Planta Medica ◽

10.1055/s-2008-1075176 ◽

2008 ◽

Vol 74 (03) ◽

Author(s):

N Ngo ◽

Z Yan ◽

TN Graf ◽

DR Carrizosa ◽

EC Dees ◽

...

Keyword(s):

Cranberry Juice ◽

First Pass Metabolism ◽

First Pass ◽

Pass Metabolism

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Development, Characterization and Optimization of Mucoadhesive Tablet for Buccal Delivery of Domperidone

Drug Delivery Letters ◽

10.2174/2210303108666181108120840 ◽

2019 ◽

Vol 9 (1) ◽

pp. 37-49

Author(s):

Jagdale Sachin ◽

Panbude Aishwarya ◽

Navasare Priya

Keyword(s):

Drug Release ◽

Factorial Design ◽

Research Work ◽

Wet Granulation ◽

Buccal Delivery ◽

Scanning Calorimetry ◽

Mucoadhesive Polymers ◽

First Pass Metabolism ◽

First Pass ◽

Pass Metabolism

Background and Objective: Upon oral administration domeperidone is rapidly absorbed, but subjected to the first pass effect which lowers systemic bioavailability to 15%. Mucoadhesive tablet can remain attached to buccal mucosa and becomes capable of bypassing hepatic first-pass metabolism to improve absorption directly into systemic circulation. The present research work was carried with an aim to develop, evaluate and optimize mucoadhesive tablet containing domperidone (DOME) for buccal delivery using different bio-adhesive polymeric combinations. </P><P> Methods: The buccal tablets were formulated by wet granulation method using isopropyl alcohol. The preliminary formulations were prepared using combinations of HPMC K4, HPMC K15, HPMC K100, HPMC E5 as mucoadhesive polymers. 32 full factorial design was applied to determine the effect of independent variables like concentration of mucoadhesive polymers (HPMC K15 and HPMC K100) over dependent variables like mucoadhesive properties (swelling index, bioadhesive strength and in vitro drug release). The prepared mucoadhesive tablets were evaluated for their tablet properties and mucoadhesive properties. The interactions between drug and polymers were studied by Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC). </P><P> Results: All formulations of factorial design showed satisfactory physicochemical, mechanical and bioadhesive characteristics. The formulation F9 exhibited maximum cumulative drug release, mucoadhesive strength and swelling index. Conclusion: The developed buccal tablet of domperidone might prove alternative to bypass the hepatic first pass metabolism and to avoid degradation which in turn may result in reducing the frequency of administration. Thus, mucoadhesive tablet of domeperidone may become viable alternative overcoming the side effects; achieving greater therapeutic effectiveness and improving the patient compliance.

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