Pharmacokinetic Interaction Study Between Saxagliptin and Omeprazole, Famotidine, or Magnesium and Aluminum Hydroxides Plus Simethicone in Healthy Subjects: An Open‐Label Randomized Crossover Study

Ren, Song; Boulton, David W.

doi:10.1002/cpdd.634

Cited by 4 publications

(13 citation statements)

References 18 publications

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“…The clinical PK data of saxagliptin and 5-hydroxy saxagliptin were retrieved from the literature, [8][9][10][11][12] as shown in Table S3.…”

Section: Clinical Pk Datamentioning

confidence: 99%

Physiologically Based Pharmacokinetic Modeling Characterizes the Drug‐Drug Interaction Between Saxagliptin and Rifampicin in Patients With Renal Impairment

Lin

et al. 2023

The Journal of Clinical Pharma

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The aim of the present study is to develop physiologically based pharmacokinetic (PBPK) models for saxagliptin and its active metabolite, 5‐hydroxy saxagliptin, and to predict the effect of coadministration of rifampicin, a strong inducer of cytochrome P450 3A4 enzymes, on the pharmacokinetics of saxagliptin and 5‐hydroxy saxagliptin in patients with renal impairment. The PBPK models of saxagliptin and 5‐hydroxy saxagliptin were developed and validated in GastroPlus for healthy adults with or without rifampicin and adults with varying renal functions. Then, the effect of renal impairment combined with drug‐drug interaction on saxagliptin and 5‐hydroxy saxagliptin pharmacokinetics was investigated. The PBPK models successfully predicted the pharmacokinetics. For saxagliptin, the prediction suggests that rifampin greatly weakened the effect of renal impairment on reducing clearance, and the inductive effect of rifampin on parent drug metabolism seems to be increased with an increase in the degree of renal impairment severity. For patients with the same degree of renal impairment, rifampicin would have a slightly synergistic effect on the increase of 5‐hydroxy saxagliptin exposure compared with dosed alone. There is an unsignificant decline for the saxagliptin total active moiety exposure values in patients with the same degree of renal impairment. It seems that patients with renal impairment are unlikely to require additional dose adjustments when coadministered with rifampicin, compared with saxagliptin alone. Our study provides a reasonable approach to explore unknown DDI potential in renal impairment.

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“…The clinical PK data of saxagliptin and 5-hydroxy saxagliptin were retrieved from the literature, [8][9][10][11][12] as shown in Table S3.…”

Section: Clinical Pk Datamentioning

confidence: 99%

Physiologically Based Pharmacokinetic Modeling Characterizes the Drug‐Drug Interaction Between Saxagliptin and Rifampicin in Patients With Renal Impairment

Lin

et al. 2023

The Journal of Clinical Pharma

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“…Setelah melalui lambung dan masuk dalam lumen usus halus yang bersifat alkali, salut enterik tersebut akan larut dan prekursor obat tersebut kemudian diserap. Resorpsinya lengkap, dalam waktu 2-5 jam pompa protonnya tinggi yakni 95% (Mansjoer, 2010). Golongan Antasida sebanyak 40,20%, Antasida jarang digunakan sebagai obat utama, tetapi sering digunakan oleh pasien untuk meringankan gejala dispepsia.…”

Section: Populasi Dan Sampelunclassified

“…Populasi dalam penelitian ini adalah seluruh resep pasien yang terdiagnosa penyakit gastritis di Apotek Amalga. (Mansjoer, 2010).…”

Section: Populasi Dan Sampelunclassified

“…Antasida mampu mengurangi rasa nyeri di lambung dengan cepat. Dengan penggunaan 3 x sehari 1 -2 tablet dapat memberikan efek yang mampu bertahan 20-60 menit, bila di minum pada perut kosong dan sampai 3 jam bila diminum 1 jam setelah makan (Mansjoer, 2010).…”

Section: Populasi Dan Sampelunclassified

“…Konsentrasi plasma puncak dicapai dalam waktu 2 -3 jam, setelah pemberian oral tunggal 150mg konsentrasi serum dibutuhkn untuk menghambat 50% dari sekresi asam lambung dirangsang diselenggarakan hingga 12 jam. Paruh waktu 1,5 -3 jam, dosis terapi 3-4 x sehari 1 tab (Mansjoer, 2010).…”

Section: Populasi Dan Sampelunclassified

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Profil Peresepan Obat Gastritis Pada Pasien Dewasa Di Apotek Amalga Kecamatan Darma Kabupaten Kuningan Periode Januari – Desember 2020

Marini

Pratiwi²

2023

JurnalFarmaku

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Gastritis adalah peradangan pada dinding lambung terutama pada selaput lendir lambung dan merupakan penyakit lambung yang banyak ditemukan di masyarakat. Angka kejadian gastritis di Jawa Barat mencapai (31,2%). Penelitian ini bertujuan untuk mengetahui profil peresepan obat gastritis pada pasien dewasa di Apotek Amalga Kecamatan Darma Kabupaten Kuningan periode Januari – Desember 2020. Penelitian ini merupakan penelitian observasional deskriptif menggunakan metode retrospektif terhadap resep-resep pasien gastritis di Apotek Amalga Kecamatan Darma Kabupaten Kuningan. Jumlah populasi dalam penelitian ini adalah 1.878 resep. Sampel dalam penelitian ini diambil sebanyak 330 resep dengan teknik pengambilan sampel menggunakan System Random Sampling. Hasil penelitian berdasarkan jenis kelamin pasien terdiagnosa gastritis terbanyak adalah berjenis kelamin perempuan sebesar 55,75%, berdasarkan rentang usia terbanyak adalah 36-45 tahun sebesar 29,69%, berdasarkan penggolongan obat yang banyak digunakan adalah obat golongan antasida sebesar 40,20%, berdasarkan penggunaan obat generik paling banyak adalah obat omeprazole sebesar 10,81%, merupakan salah satu obat gastritis golongan PPI (Proton Pump Inhibitor) dan berdasarkan peresepan kombinasi obat gastritis paling banyak yaitu kombinasi antara Antasida dan PPI (Omeprazole) sebesar 21,05%.

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Influence of Gegenqinlian decoction on pharmacokinetics and pharmacodynamics of saxagliptin in type 2 diabetes mellitus rats

Yu,

Cui,

Yin

et al. 2023

Biopharm & Drug Disp

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Gegenqinlian decoction (GQD) is a classic prescription of traditional Chinese medicine (TCM), which originated from Shanghanlun. The combination of GQD and hypoglycemic drugs (saxagliptin, Sax, metformin) is often used to treat Type 2 diabetes mellitus (T2DM) in TCM clinics. However, the herb–drug interactions (HDIs) between GQD and hypoglycemic drugs are still unclear. In order to determine the safety of the combination, we assessed the influences of GQD on the pharmacokinetics and pharmacodynamics of Sax in T2DM rats. The plasma concentration of Sax (5 mg/kg) pretreated with GQD (freeze‐dried powder, 1.35 g/kg) or not was determined by high‐performance liquid chromatography (HPLC), and pharmacokinetics parameters were calculated. The influence of GQD on the pharmacodynamics of Sax was investigated by detecting the levels of weight, (see abbreviations list) OGTT, TC, TG, LDL‐C, HDL‐C, FBG, FINS, HOMA‐IR, QUICKI, AST, ALT, and the liver coefficient. The Cmax, AUC0‐t,and AUC0‐∞ of Sax increased significantly in the combination group whether in normal or T2DM rats. The results of pharmacodynamics showed that the weight of rats in each treatment group increased. FBG, TC, TG, LDL‐C, and HOMA‐IR decreased, HDL‐C, FINS, and QUICKI increased significantly (p < 0.05) compared with the model control group. The result showed that the combination of GQD and Sax could not only improve the hypoglycemic effect but also increase the plasma exposure of Sax. The potential HDIs between GQD and Sax should be taken into consideration in clinics. Moreover, for the complexity of the human compared with experimental animals, as well as genetic differences, the in‐depth study should be carried out to assess the uniformity of the pharmacokinetics and pharmacodynamics between rats and humans.

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Pharmacokinetic Interaction Study Between Saxagliptin and Omeprazole, Famotidine, or Magnesium and Aluminum Hydroxides Plus Simethicone in Healthy Subjects: An Open‐Label Randomized Crossover Study

Cited by 4 publications

References 18 publications

Physiologically Based Pharmacokinetic Modeling Characterizes the Drug‐Drug Interaction Between Saxagliptin and Rifampicin in Patients With Renal Impairment

Physiologically Based Pharmacokinetic Modeling Characterizes the Drug‐Drug Interaction Between Saxagliptin and Rifampicin in Patients With Renal Impairment

Profil Peresepan Obat Gastritis Pada Pasien Dewasa Di Apotek Amalga Kecamatan Darma Kabupaten Kuningan Periode Januari – Desember 2020

Influence of Gegenqinlian decoction on pharmacokinetics and pharmacodynamics of saxagliptin in type 2 diabetes mellitus rats

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