In Situ Absorption in Rat Intestinal Tract of Solid Dispersion of Annonaceous Acetogenins

In Vitro and In Situ Absorption and Metabolism of Sesquiterpenes from Petasites hybridus Extracts

Planta Medica ◽

10.1055/s-0044-100401 ◽

2018 ◽

Vol 84 (11) ◽

pp. 795-805

Author(s):

Lucia Disch ◽

Kristina Forsch ◽

Beate Siewert ◽

Jürgen Drewe ◽

Gert Fricker

Keyword(s):

Hepatic Metabolism ◽

Absorption Capacity ◽

Active Constituent ◽

In Situ Absorption ◽

Low Solubility ◽

S9 Fraction

Abstract Petasites hybridus extract is used in the treatment of seasonal allergic rhinitis. The aim of this study was to evaluate the active constituent petasin and its isomers isopetasin and neopetasin (petasins) in the P. hybridus extract Ze 339 for liberation, dissolution, absorption, and metabolism. The determination of pH-dependent thermodynamic solubility was performed via the shake-flask method. Petasins exhibited a low solubility that was pH independent. In vivo, the concentration of solute drugs is decreased continuously by intestinal absorption. Therefore, low solubility is not assumed to be critical for in vivo performance. Additionally, dissolution of an herbal medicinal product containing P. hybridus extract Ze 339 was assessed. Furthermore, high permeability through Caco-2 monolayers was evident. Using an in situ rat model, absorption capacity for petasins was found in all tested intestinal segments, namely, duodenum, jejunum, and ileum. Besides, high metabolism was evident both in Caco-2 monolayers and in the rat intestine. To compare intestinal and hepatic metabolism of petasins, in vitro enzyme assays using liver and intestinal cytosol and microsomes (S9 fraction) of rats and humans were performed. A significantly higher metabolic rate was found in the liver S9 fraction of both species compared with the intestinal S9 fraction.

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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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Formulation optimization and in situ absorption in rat intestinal tract of quercetin-loaded microemulsion

Colloids and Surfaces B Biointerfaces ◽

10.1016/j.colsurfb.2009.03.005 ◽

2009 ◽

Vol 71 (2) ◽

pp. 306-314 ◽

Cited By ~ 79

Author(s):

Yan Gao ◽

Yuqiang Wang ◽

Yukun Ma ◽

Aihua Yu ◽

Fengqun Cai ◽

...

Keyword(s):

Intestinal Tract ◽

Formulation Optimization ◽

In Situ Absorption

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Integration of In Silico, In Vitro and In Situ Tools for the Preformulation and Characterization of a Novel Cardio-Neuroprotective Compound during the Early Stages of Drug Development

Pharmaceutics ◽

10.3390/pharmaceutics14010182 ◽

2022 ◽

Vol 14 (1) ◽

pp. 182

Author(s):

Claudia Miranda ◽

Alejandro Ruiz-Picazo ◽

Paula Pomares ◽

Isabel Gonzalez-Alvarez ◽

Marival Bermejo ◽

...

Keyword(s):

Cell Lines ◽

Intestinal Permeability ◽

Oral Absorption ◽

Neuroprotective Effects ◽

In Situ Perfusion ◽

In Vitro Cell Lines ◽

Low Solubility

The main aim of this work is the biopharmaceutical characterization of a new hybrid benzodiazepine-dihydropyridine derivative, JM-20, derived with potent anti-ischemic and neuroprotective effects. In this study, the pKa and the pH-solubility profile were experimentally determined. Additionally, effective intestinal permeability was measured using three in vitro epithelial cell lines (MDCK, MDCK-MDR1 and Caco-2) and an in situ closed-loop intestinal perfusion technique. The results indicate that JM-20 is more soluble at acidic pH (9.18 ± 0.16); however, the Dose number (Do) was greater than 1, suggesting that it is a low-solubility compound. The permeability values obtained with in vitro cell lines as well as with the in situ perfusion method show that JM-20 is a highly permeable compound (Caco-2 value 3.8 × 10−5). The presence of an absorption carrier-mediated transport mechanism was also demonstrated, as well as the efflux effect of P-glycoprotein on the permeability values. Finally, JM-20 was provisionally classified as class 2 according to the biopharmaceutical classification system (BCS) due to its high intestinal permeability and low solubility. The potential good oral absorption of this compound could be limited by its solubility.

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Optimasi Hidroksipropil Metilselulosa K-4M dan Carbopol® 940 pada Sediaan Patch Dispersi Padat Piroksikam

Kartika Jurnal Ilmiah Farmasi ◽

10.26874/kjif.v5i2.133 ◽

2018 ◽

Vol 5 (2) ◽

pp. 80

Author(s):

Dwi Nurahmanto ◽

Nurul Shalikha ◽

Lidya Ameliana

Keyword(s):

Moisture Content ◽

Solid Dispersion ◽

Hydroxypropyl Methylcellulose ◽

Lattice Design ◽

Simplex Lattice Design ◽

Peg 4000 ◽

First Pass Metabolism ◽

First Pass ◽

Simplex Lattice ◽

Pass Metabolism

Abstrak Piroksikam merupakan anti inflamasi non steroid (AINS) turunan oksikam yang berkhasiat sebagai analgesik dan antiinflamasi digunakan untuk pengobatan rheumatoid arthritis dan osteoarthritis. Piroksikam menyebabkan masalah pada saluran cerna dan first pass metabolism yang dapat dihindari dengan cara pemberian transdermal patch. Salah satu komponen patch yaitu polimer yang berfungsi untuk mengontrol kecepatan pelepasan obat dari sediaan. Penelitian ini dilakukan untuk menentukan komposisi terbaik dari kombinasi polimer hidroksipropil metilselulosa (HPMC) dan Carbopol terhadap % moisture content (MC) dan flux pelepasan sediaan transdermal patch dispersi padat piroksikam dengan rancangan formula Simplex Lattice Design. Piroksikam dibuat dalam bentuk dispersi padat dengan pembawa PEG 4000 untuk meningkatkan kelarutannya. Rancangan formula patch dispersi padat piroksikam dibuat dengan menggunakan tiga polimer Etil selulosa:HPMC:carbopol dimana yang divariasikan adalah perbandingan HPMC : Carbopol yaitu 1 : 0 ; 0,5 : 0,5 ; 0 : 1. Hasil uji menunjukkan ketiga formula memenuhi persyaratan keseragaman kadar dengan rentang keseragaman 3,735 – 97,349 %. Hasil juga menunjukkan formula 3 menghasilkan patch yang lebih tebal, pH permukaan patch lebih rendah, nilai % moisture content lebih besar dan nilai flux lebih tinggi dibandingkan formula 2 dan formula 3, Formula 3 mempunyai nilai % moisture content yang memenuhi persyaratan sebesar 6,613% dan nilai flux pelepasa yang paling bagus sebesar 32,562 µg/cm2.menit1/2. Hasil penelitian juga menunjukkan formula 1 memiliki keseragaman bobot lebih baik dibandingkan formula 2 dan formula 3. Dapat disimpulkan bahwa komposisi optimum dari kombinasi polimer HPMC dan Carbopol pada sediaan patch dispersi padat piroksikam yaitu formula dengan komposisi polimer HPMC sebanyak 0 mg dan Carbopol sebanyak 75 mg. Kata kunci: Dispersi padat, patch piroksikam, HPMC, Carbopol Optimization of Hydroxypropyl Methylcellulose K-4M and Carbopol® 940 in Solid Dispersion Piroxicam Patch Abstract Piroxicam is a non-steroidal anti-inflammatory (NSA) oxysmic derivative as an analgesic and anti-inflammatory agent used for the treatment of rheumatoid arthritis and osteoarthritis. Piroxicam causes problems in the gastrointestinal tract and first pass metabolism that can be avoided by giving transdermal patches. One of the patch components is a polymer that serves to control the speed of drug release from the preparation. The present study was conducted to determine the best composition of the combination of hydroxypropyl methylcellulose (HPMC) and Carbopol polymers against% moisture content (MC) and fluxes release of the pyroxicam dispersion transdermal patch dispersion with the design of the Simplex Lattice Design formula. Piroxicam is prepared in the form of a solid dispersion with a PEG 4000 carrier to increase its solubility. The design of a pyroxicam solid dispersion patch formulation was prepared using three ethyl cellulose polymers: HPMC: carbopol wherein the HPMC ratio is computed: Carbopol is 1: 0; 0.5: 0.5; 0: 1. The test results show the three formulas meet the requirements of uniformity of the content with a uniformity range of 3.735 - 97.349%. the results also show formula 3 resulting in thicker patches, lower patch pH surfaces, greater moisture content values and higher flux values than formula 2 and formula 3, Formula 3 has a moisture content value of 6.613% the finest fl ux flux of 32,562 μg / cm2.menit1 / 2. The results also show that formula 1 has better weight uniformity than formula 2 and formula 3. It can be concluded that the optimum composition of HPMC and Carbopol polymer combinations in the preparation of piroxicam solid dispersion patch is a formula with HPMC polymer composition as 0 mg and Carbopol as much as 75 mg.. Key words: solid dispersion, piroxicam patch, HPMC, Carbopol

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PENGARUH PENAMBAHAN POLIETILEN GLIKOL 6000 PADA TABLET IBUPROFEN DISPERSI PADAT TERHADAP ABSORBSI IBUPROFEN SECARA IN SITU

Jurnal Riset Kefarmasian Indonesia ◽

10.33759/jrki.v3i3.167 ◽

2021 ◽

Vol 3 (3) ◽

pp. 211-222

Author(s):

Antetti Tampubolon

Keyword(s):

Polyethylene Glycol ◽

Solid Dispersion ◽

Male Rats ◽

In Situ Methods ◽

In Situ Absorption ◽

Polyethylene Glycol 6000 ◽

Drug Solution

Drug absorption can be decided by various methods, namely in vitro methods, in situ methods, and in vivo methods. The in situ method is a procedure that is very close to the in vivo method. The aim of this study was to identify the effect of accumulation of polyethylene glycol 6000 (PEG 6000) on solid dispersion of ibuprofen tablets on the in-situ absorption of the drug. This research was conducted through an experiment to determine the effect of adding polyethylene glycol 6000 to the absorption of ibuprofen in situ by flowing the solution from solid dispersion ibuprofen tablets, solutions from generic ibuprofen tablets and standard ibuprofen solutions. The solid dispersion system was carried out by melting ibuprofen and polyethylene glycol 6000 in a ratio of 1:05. The drug solution was flowed through the lumen of the small intestine of male rats. Unabsorbed ibuprofen was measured by an ultraviolet spectrophotometer at a wavelength of 225.5 nm. Next, the absorbed level of ibuprofen was calculated. The results showed that ibuprofen from solid dispersion tablets was absorbed more than ibuprofen from generic tablets and standard ibuprofen. It can be concluded that polyethylene glycol 6000 has an effect on the absorption of ibuprofen in situ.

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Optimasi Hidroksipropil Metilselulosa K-4M dan Carbopol® 940 pada Sediaan Patch Dispersi Padat Piroksikam

Kartika Jurnal Ilmiah Farmasi ◽

10.26874/kjif.v5i2.121 ◽

2017 ◽

Vol 5 (2) ◽

pp. 80

Author(s):

Dwi Nurahmanto ◽

Nurul Shalikha ◽

Lidya Ameliana

Keyword(s):

Moisture Content ◽

Solid Dispersion ◽

Hydroxypropyl Methylcellulose ◽

Lattice Design ◽

Simplex Lattice Design ◽

Peg 4000 ◽

First Pass Metabolism ◽

First Pass ◽

Simplex Lattice ◽

Pass Metabolism

Abstrak Piroksikam merupakan anti inflamasi non steroid (AINS) turunan oksikam yang berkhasiat sebagai analgesik dan antiinflamasi digunakan untuk pengobatan rheumatoid arthritis dan osteoarthritis. Piroksikam menyebabkan masalah pada saluran cerna dan first pass metabolism yang dapat dihindari dengan cara pemberian transdermal patch. Salah satu komponen patch yaitu polimer yang berfungsi untuk mengontrol kecepatan pelepasan obat dari sediaan. Penelitian ini dilakukan untuk menentukan komposisi terbaik dari kombinasi polimer hidroksipropil metilselulosa (HPMC) dan Carbopol terhadap % moisture content (MC) dan flux pelepasan sediaan transdermal patch dispersi padat piroksikam dengan rancangan formula Simplex Lattice Design. Piroksikam dibuat dalam bentuk dispersi padat dengan pembawa PEG 4000 untuk meningkatkan kelarutannya. Rancangan formula patch dispersi padat piroksikam dibuat dengan menggunakan tiga polimer Etil selulosa:HPMC:carbopol dimana yang divariasikan adalah perbandingan HPMC : Carbopol yaitu 1 : 0 ; 0,5 : 0,5 ; 0 : 1. Hasil uji menunjukkan ketiga formula memenuhi persyaratan keseragaman kadar dengan rentang keseragaman 3,735 – 97,349 %. Hasil juga menunjukkan formula 3 menghasilkan patch yang lebih tebal, pH permukaan patch lebih rendah, nilai % moisture content lebih besar dan nilai flux lebih tinggi dibandingkan formula 2 dan formula 3, Formula 3 mempunyai nilai % moisture content yang memenuhi persyaratan sebesar 6,613% dan nilai flux pelepasa yang paling bagus sebesar 32,562 µg/cm2.menit1/2. Hasil penelitian juga menunjukkan formula 1 memiliki keseragaman bobot lebih baik dibandingkan formula 2 dan formula 3. Dapat disimpulkan bahwa komposisi optimum dari kombinasi polimer HPMC dan Carbopol pada sediaan patch dispersi padat piroksikam yaitu formula dengan komposisi polimer HPMC sebanyak 0 mg dan Carbopol sebanyak 75 mg. Kata kunci: Dispersi padat, patch piroksikam, HPMC, Carbopol Optimization of Hydroxypropyl Methylcellulose K-4M and Carbopol® 940 in Solid Dispersion Piroxicam Patch Abstract Piroxicam is a non-steroidal anti-inflammatory (NSA) oxysmic derivative as an analgesic and anti-inflammatory agent used for the treatment of rheumatoid arthritis and osteoarthritis. Piroxicam causes problems in the gastrointestinal tract and first pass metabolism that can be avoided by giving transdermal patches. One of the patch components is a polymer that serves to control the speed of drug release from the preparation. The present study was conducted to determine the best composition of the combination of hydroxypropyl methylcellulose (HPMC) and Carbopol polymers against% moisture content (MC) and fluxes release of the pyroxicam dispersion transdermal patch dispersion with the design of the Simplex Lattice Design formula. Piroxicam is prepared in the form of a solid dispersion with a PEG 4000 carrier to increase its solubility. The design of a pyroxicam solid dispersion patch formulation was prepared using three ethyl cellulose polymers: HPMC: carbopol wherein the HPMC ratio is computed: Carbopol is 1: 0; 0.5: 0.5; 0: 1. The test results show the three formulas meet the requirements of uniformity of the content with a uniformity range of 3.735 - 97.349%. the results also show formula 3 resulting in thicker patches, lower patch pH surfaces, greater moisture content values and higher flux values than formula 2 and formula 3, Formula 3 has a moisture content value of 6.613% the finest fl ux flux of 32,562 μg / cm2.menit1 / 2. The results also show that formula 1 has better weight uniformity than formula 2 and formula 3. It can be concluded that the optimum composition of HPMC and Carbopol polymer combinations in the preparation of piroxicam solid dispersion patch is a formula with HPMC polymer composition as 0 mg and Carbopol as much as 75 mg.. Key words: solid dispersion, piroxicam patch, HPMC, Carbopol

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Faculty Opinions recommendation of Modeling the influence of cyclodextrins on oral absorption of low-solubility drugs: I. Model development.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1166614.627630 ◽

2009 ◽

Author(s):

Marival Bermejo

Keyword(s):

Oral Absorption ◽

Model Development ◽

Low Solubility ◽

Low Solubility Drugs

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Antiviral Essential Oils Incorporated in Nanocarriers: Strategy for Prevention from COVID-19 and Future Infectious Pandemics

Pharmaceutical Nanotechnology ◽

10.2174/2211738508666201016151850 ◽

2020 ◽

Vol 8 (6) ◽

pp. 437-451

Author(s):

Malkiet Kaur ◽

Gayatri Devi ◽

Manju Nagpal ◽

Manjinder Singh ◽

Gitika A. Dhingra ◽

...

Keyword(s):

Phenolic Compounds ◽

Antiviral Activity ◽

Essential Oils ◽

Bacterial Infections ◽

Biological Properties ◽

Vital Role ◽

Chinese Herbs ◽

Active Constituents ◽

Prevention And Treatment ◽

Low Solubility

Background: Coronavirus has become a life-threatening disease and it is caused by severe acute respiratory syndrome (SARS). This new strain of coronavirus is not completely understood and to date, there is no treatment for coronavirus. Traditional ayurvedic medicines, mainly essential oils and Chinese herbs, have always played a vital role in the prevention and treatment of several epidemics and pandemics. In the meantime, guidelines of the ministry of AYUSH (Ayurveda, yoga, unani, siddha and homoepathy) include a traditional medicinal treatment for flu and fever and also recommended to boost immunity to prevent the spread of coronavirus. It is not possible to find which essential oil will offer the best level of protection. However, it is likely to assume that some essential oils are likely to offer a measurable level of defense in the same way they do with many other known viruses. Methods: Literature relevant to various essential oils having antiviral activity has been collected and compiled. Various nanocarriers of essential oils have also been stated. The database was collected using various search engines such as J-Gate, Google Scholar, Sci-Hub, PubMed, ScienceDirect, etc. Results: Essential oils contain active constituents such as phenolic compounds, terpenoids, alkaloids, phenyl propanoids, etc., which are responsible for their biological properties such as antiviral, antibacterial, antimicrobial, antioxidant activities and many more. However, the use of essential oils has always been limited due to poor solubility, solvent toxicity, volatility and low solubility. Many nanotechnology based carriers especially, liposomes, dendrimers, nanoparticles, nanoemulsion and microemulsion, etc. have been evidenced to overcome limitations associated with essential oils. Conclusion: Several essential oils possess potent antiviral activity and are characterized by fewer side effects and are safe for human use. The nanocarrier systems of these oils have proved the potential to treat viral and bacterial infections. Lay Summary: Current COVID-19 era demands traditional treatment for immunity boost up as support therapy. Traditional ayurvedic medicines, mainly essential oils and Chinese herbs, have always played a vital role in the prevention and treatment of several epidemics and pandemics. Therefore, authors have summarized various essential oils having antiviral activity in current manuscript. Various nanocarriers of essential oils have been reported. Essential oils contain active constituents such as phenolic compounds, terpenoids, alkaloids, phenyl propanoids, etc., which are responsible for their biological properties such as antiviral, antibacterial, antimicrobial, antioxidant activity. However, the use of essential oils has always been limited due to poor solubility, solvent toxicity, volatility and low solubility. Many nanotechnology based carriers especially, liposomes, dendrimers, nanoparticles, nanoemulsion and microemulsion, etc. have been evidenced to overcome limitations associated with essential oils. The nanocarrier systems of these oils have proved the potential to treat viral and bacterial infections.

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