An Oral Single-dose, Randomized, Balanced, Open-label, Two-sequence, Two-treatment, Two-period, Crossover Bioequivalence Study of Sitagliptin Hydrochloride / Metformin Hydrochloride Extended Release Film Coated Tablets 50 mg / 500 mg (FDC) of Galenicum Health S.L.U., Spain With That of JANUMET® XR (Sitagliptin Phosphate / Metformin Hydrochloride) Extended-release Coated Tablets 50 mg / 500 mg (FDC) of Merck Sharp & Dohme Pharmaceuticals Ltd., Brazilin Healthy Adult Male and Female Subjects Under Fed Conditions.

The objective of this study was to evaluate and compare the bioavailability and therefore to assess the bioequivalence of two different formulations of sitagliptin/metformin extended release tablets after a single oral dose administration under fed conditions.

开始日期2023-01-16

申办/合作机构

Galenicum Health SL

NCT06124495 / Completed临床1期

An Oral Single-dose, Randomized, Balanced, Open-label, Two-sequence, Two-treatment, Two-period, Crossover Bioequivalence Study of Sitagliptin Hydrochloride / Metformin Hydrochloride Extended-release Film Coated Tablets 50 mg / 500 mg (FDC) of Galenicum Health S.L.U., Spain With That of JANUMET® XR (Sitagliptin Phosphate / Metformin Hydrochloride) Extended-release Coated Tablets 50 mg / 500 mg (FDC) of Merck Sharp & Dohme Pharmaceuticals Ltd., Brasil in Healthy Adult Male and Female Subjects Under Fasting Conditions.

开始日期2023-01-13

申办/合作机构

Galenicum Health SL

NCT06124573 / Completed临床1期

An Oral Single-dose, Randomized, Balanced, Open-label, Two-sequence, Two-treatment, Two-period, Crossover Bioequivalence Study of Sitagliptin Hydrochloride / Metformin Hydrochloride Extended-release Film Coated Tablets 100 mg /1000 mg (FDC) of Galenicum Health S.L.U., Spain With That of JANUMET® XR (Sitagliptin Phosphate / Metformin Hydrochloride) Extended-release Coated Tablets 100 mg / 1000 mg (FDC) of Merck Sharp & Dohme Pharmaceuticals Ltd., Brasil in Healthy Adult Male and Female Subjects Under Fed Conditions.

开始日期2022-11-07

申办/合作机构

Galenicum Health SL

100 项与盐酸二甲双胍/盐酸西格列汀相关的临床结果

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100 项与盐酸二甲双胍/盐酸西格列汀相关的转化医学

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100 项与盐酸二甲双胍/盐酸西格列汀相关的专利（医药）

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项与盐酸二甲双胍/盐酸西格列汀相关的文献（医药）

2022-07-03·Pharmaceutical Development and Technology

Exploiting synergistic effects of brittle and plastic excipients in directly compressible formulations of sitagliptin phosphate and sitagliptin hydrochloride

Article

作者: Papaioannou, Markos ; Edinger, Peter ; Zakowiecki, Daniel ; Hess, Tobias ; Terlecka, Anna ; Kubiak, Bartlomiej

Direct compression (DC) is the simplest and most economical way to produce pharmaceutical tablets. Ideally, it consists of only two steps: dry blending of a drug substance(s) with excipients followed by compressing the powder mixture into tablets. In this study, immediate-release film-coated tablets containing either Sitagliptin phosphate or Sitagliptin hydrochloride were developed using DC technique. After establishing the optimum ratio of ductile and brittle excipients, five formulations were compressed into tablets using a rotary press and finally film coated. Both powders and tablets were examined by standard pharmacopoeial methods. It has been shown that the simultaneous use of excipients with different physical properties, i.e. ductile microcrystalline cellulose and brittle anhydrous dibasic calcium phosphate, produces a synergistic effect, allowing preparation of Sitagliptin DC tablets with good mechanical strength (tensile strength over 2 N/mm²), rapid disintegration (shorter than 2 min), and fast release of the drug substance (85% of the drug is dissolved within 15 min). It was found that the type of calcium phosphate excipient used had a large effect on the properties of the sitagliptin tablets. All formulations developed showed good chemical stability, even when stored under stress conditions (50 °C/80% RH).

2021-04-20·Turkish Journal of Pharmaceutical Sciences

Development of an <i>In Vitro-In Vivo</i> Correlation for Sitagliptin and Metformin Prolonged-release Tablet Formulations

Article

作者: Vadla, Harikiran Chary ; Rallabandi, Balaramesha Chary ; Kothamasu, Umamaheshwar ; Boddu, Rajkumar ; Prathap, Vamshi Ramana ; Gannu, Ramesh

ObjectivesThe objective of this study was to establish and validate an in vitro-in vivo correlation (IVIVC). To investigate the safety of a fixed-dose combination (FDC) versus the reference formulations (Januvia^® 100 mg Filmtabletten co-administered with Glucophage^® SR 1000 mg prolonged-release tablets), a bioequivalence study was conducted in the fasted and fed states, and the data generated were used to establish the correlation.Materials and MethodsThe formulations used in the bioequivalence study were a FDC (sitagliptin hydrochloride equivalent to 100 mg of sitagliptin and metformin hydrochloride 1000 mg prolonged release) and Januvia^® 100 mg co-administered with Glucophage^® SR 1000 mg. The plasma profiles from the bioequivalence study and respective dissolution data were then utilized to establish "level A" IVIVC. The procedure comprises pharmacokinetic modeling to derive the empirical constants for further use in deconvolution and convolution procedures. Levy plots were constructed to understand the relationship between in vitro and in vivo properties. The internal and external predictabilities were evaluated by comparing the predicted pharmacokinetics with the observed values from the bioequivalence study.ResultsThe formulations showed approximately 91%-95% and 89%-91% dissolution, respectively in fasted and fed-state dissolution media for sitagliptin. The dissolution of metformin was 96%-98% and 89%-95%, respectively, in fasted and fed-state media. The regression coefficients of all the Levy plots were more than 0.900, indicating a linear correlation between in vitro release and in vivo parameters. The prediction error value of internal and external predictabilities was below 10 and met the US Food and Drug Administration criteria. Therefore, it can be stated that the correlation models are validated and can be used for predictions and to setting the dissolution specifications. The safety and tolerability of the FDC was found to be superior to those of the reference formulations, as fewer adverse events occurred following administration of the FDC.ConclusionCorrelation models can be useful for the prediction of FDCs during the management life cycle of the product. The models can also serve as a surrogate for in vivo studies. The FDC was tolerable, and the adverse events were mild and similar to those observed with the reference products. Therefore, the FDC is safe for use in human subjects.

100 项与盐酸二甲双胍/盐酸西格列汀相关的药物交易

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