Bioequivalence Dissolution Test Criteria for Formulation Development of High Solubility-Low Permeability Drugs
Chem Pharm Bull (Tokyo). 2023;71(3):213-219. doi: 10.1248/cpb.c22-00685.ABSTRACTThe purpose of the present study was to provide the experimental and theoretical basis of bioequivalence (BE) dissolution test criteria for formulation development of high solubility-low permeability drugs. According to the biowaiver scheme based on the biopharmaceutics classification system (BCS), for BCS class III drugs, a test formulation and a reference formulation are predicted to be BE when 85% of the drug dissolves within 15 min (T85% < 15 min) in the compendial dissolution test. However, previous theoretical simulation studies have s...
Source: Chemical and Pharmaceutical Bulletin - March 1, 2023 Category: Drugs & Pharmacology Authors: Asami Ono Rena Kurihara Katsuhide Terada Kiyohiko Sugano Source Type: research

Bioequivalence Dissolution Test Criteria for Formulation Development of High Solubility-Low Permeability Drugs
Chem Pharm Bull (Tokyo). 2023;71(3):213-219. doi: 10.1248/cpb.c22-00685.ABSTRACTThe purpose of the present study was to provide the experimental and theoretical basis of bioequivalence (BE) dissolution test criteria for formulation development of high solubility-low permeability drugs. According to the biowaiver scheme based on the biopharmaceutics classification system (BCS), for BCS class III drugs, a test formulation and a reference formulation are predicted to be BE when 85% of the drug dissolves within 15 min (T85% < 15 min) in the compendial dissolution test. However, previous theoretical simulation studies have s...
Source: Chemical and Pharmaceutical Bulletin - March 1, 2023 Category: Drugs & Pharmacology Authors: Asami Ono Rena Kurihara Katsuhide Terada Kiyohiko Sugano Source Type: research

Bioequivalence Dissolution Test Criteria for Formulation Development of High Solubility-Low Permeability Drugs
Chem Pharm Bull (Tokyo). 2023;71(3):213-219. doi: 10.1248/cpb.c22-00685.ABSTRACTThe purpose of the present study was to provide the experimental and theoretical basis of bioequivalence (BE) dissolution test criteria for formulation development of high solubility-low permeability drugs. According to the biowaiver scheme based on the biopharmaceutics classification system (BCS), for BCS class III drugs, a test formulation and a reference formulation are predicted to be BE when 85% of the drug dissolves within 15 min (T85% < 15 min) in the compendial dissolution test. However, previous theoretical simulation studies have s...
Source: Chemical and Pharmaceutical Bulletin - March 1, 2023 Category: Drugs & Pharmacology Authors: Asami Ono Rena Kurihara Katsuhide Terada Kiyohiko Sugano Source Type: research

Bioequivalence Dissolution Test Criteria for Formulation Development of High Solubility-Low Permeability Drugs
Chem Pharm Bull (Tokyo). 2023;71(3):213-219. doi: 10.1248/cpb.c22-00685.ABSTRACTThe purpose of the present study was to provide the experimental and theoretical basis of bioequivalence (BE) dissolution test criteria for formulation development of high solubility-low permeability drugs. According to the biowaiver scheme based on the biopharmaceutics classification system (BCS), for BCS class III drugs, a test formulation and a reference formulation are predicted to be BE when 85% of the drug dissolves within 15 min (T85% < 15 min) in the compendial dissolution test. However, previous theoretical simulation studies have s...
Source: Chemical and Pharmaceutical Bulletin - March 1, 2023 Category: Drugs & Pharmacology Authors: Asami Ono Rena Kurihara Katsuhide Terada Kiyohiko Sugano Source Type: research

Bioequivalence Dissolution Test Criteria for Formulation Development of High Solubility-Low Permeability Drugs
Chem Pharm Bull (Tokyo). 2023;71(3):213-219. doi: 10.1248/cpb.c22-00685.ABSTRACTThe purpose of the present study was to provide the experimental and theoretical basis of bioequivalence (BE) dissolution test criteria for formulation development of high solubility-low permeability drugs. According to the biowaiver scheme based on the biopharmaceutics classification system (BCS), for BCS class III drugs, a test formulation and a reference formulation are predicted to be BE when 85% of the drug dissolves within 15 min (T85% < 15 min) in the compendial dissolution test. However, previous theoretical simulation studies have s...
Source: Chemical and Pharmaceutical Bulletin - March 1, 2023 Category: Drugs & Pharmacology Authors: Asami Ono Rena Kurihara Katsuhide Terada Kiyohiko Sugano Source Type: research

Bioequivalence Dissolution Test Criteria for Formulation Development of High Solubility-Low Permeability Drugs
Chem Pharm Bull (Tokyo). 2023;71(3):213-219. doi: 10.1248/cpb.c22-00685.ABSTRACTThe purpose of the present study was to provide the experimental and theoretical basis of bioequivalence (BE) dissolution test criteria for formulation development of high solubility-low permeability drugs. According to the biowaiver scheme based on the biopharmaceutics classification system (BCS), for BCS class III drugs, a test formulation and a reference formulation are predicted to be BE when 85% of the drug dissolves within 15 min (T85% < 15 min) in the compendial dissolution test. However, previous theoretical simulation studies have s...
Source: Chemical and Pharmaceutical Bulletin - March 1, 2023 Category: Drugs & Pharmacology Authors: Asami Ono Rena Kurihara Katsuhide Terada Kiyohiko Sugano Source Type: research

Bioequivalence Dissolution Test Criteria for Formulation Development of High Solubility-Low Permeability Drugs
Chem Pharm Bull (Tokyo). 2023;71(3):213-219. doi: 10.1248/cpb.c22-00685.ABSTRACTThe purpose of the present study was to provide the experimental and theoretical basis of bioequivalence (BE) dissolution test criteria for formulation development of high solubility-low permeability drugs. According to the biowaiver scheme based on the biopharmaceutics classification system (BCS), for BCS class III drugs, a test formulation and a reference formulation are predicted to be BE when 85% of the drug dissolves within 15 min (T85% < 15 min) in the compendial dissolution test. However, previous theoretical simulation studies have s...
Source: Chemical and Pharmaceutical Bulletin - March 1, 2023 Category: Drugs & Pharmacology Authors: Asami Ono Rena Kurihara Katsuhide Terada Kiyohiko Sugano Source Type: research

Apple (Malus domestica  Borkh) leaves attenuate indomethacin-induced gastric ulcer in rats
Biomed Pharmacother. 2023 Feb 1;160:114331. doi: 10.1016/j.biopha.2023.114331. Online ahead of print.ABSTRACTMalus domestica Borkh, the apple tree, exhibited numerous pharmacological properties including antioxidant, neuroprotective, anti-inflammatory, anticancer and antimicrobial activities. The present work aimed to annotate the secondary metabolites from a butanol fraction of apple leaves (BLE), evaluate the gastro-protective and healing effects of this fraction against indomethacin-induced gastric ulcers in rats and to identify its mechanism of action. BLE (100, and 200 mg/kg) was orally administered in rats as an acut...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - February 3, 2023 Category: Drugs & Pharmacology Authors: Mona F Mahmoud Walied Abdo Mohamed Nabil Badreddine Drissi Assem M El-Shazly Mohamed A O Abdelfattah Mansour Sobeh Source Type: research

Promoting Activity of Terpenes on Skin Permeation of Famotidine
Chem Pharm Bull (Tokyo). 2023;71(2):111-119. doi: 10.1248/cpb.c22-00568.ABSTRACTFamotidine (FMT) is a competitive histamine-2 (H2) receptor antagonist that inhibits gastric acid secretion for the treatment of Gastroesophageal reflux disease. To study the promoting effect and mechanism of terpenes, including l-menthol, borneol, and geraniol, as chemical enhancers, FMT was used as a model drug. Attenuated total reflectance-Fourier transform IR spectroscopy (ATR-FTIR) and differential scanning calorimetry (DSC) were used to explore the effects of terpenes on the skin. Hairless mouse skin was mounted on Franz-type diffusion ce...
Source: Chemical and Pharmaceutical Bulletin - February 1, 2023 Category: Drugs & Pharmacology Authors: Qihui Xu Yifan Wu Hiroki Saito Yuki Ofuchi Haruna Setoyama Takayuki Furuishi Kaori Fukuzawa Etsuo Yonemochi Yasuko Obata Source Type: research

Masking the Taste of Fixed-Dose Combination Drugs: Particular NSAIDs Can Efficiently Mask the Bitterness of Famotidine
This study aimed to evaluate the bitterness of famotidine (FAM) combined with each of three non-steroidal anti-inflammatory drugs (NSAIDs): ibuprofen (IBU), flurbiprofen (FLU), and naproxen (NAP), which have potential as fixed-dose combination (FDC) drugs. We evaluated the bitterness of FAM and each NSAID by taste sensor AN0 and C00, respectively. FAM showed high sensor output representing sensitivity to bitterness, whereas three NSAIDs did not show large sensor output, suggesting that the bitterness intensities of three NSAIDs were lower than that of FAM. The bitterness of FAM on sensor AN0 was suppressed in a concentrati...
Source: Chemical and Pharmaceutical Bulletin - February 1, 2023 Category: Drugs & Pharmacology Authors: Rio Uno Kyoko Ohkawa Honami Kojima Tamami Haraguchi Minoru Ozeki Ikuo Kawasaki Miyako Yoshida Masaaki Habara Hidekazu Ikezaki Takahiro Uchida Source Type: research

Promoting Activity of Terpenes on Skin Permeation of Famotidine
Chem Pharm Bull (Tokyo). 2023;71(2):111-119. doi: 10.1248/cpb.c22-00568.ABSTRACTFamotidine (FMT) is a competitive histamine-2 (H2) receptor antagonist that inhibits gastric acid secretion for the treatment of Gastroesophageal reflux disease. To study the promoting effect and mechanism of terpenes, including l-menthol, borneol, and geraniol, as chemical enhancers, FMT was used as a model drug. Attenuated total reflectance-Fourier transform IR spectroscopy (ATR-FTIR) and differential scanning calorimetry (DSC) were used to explore the effects of terpenes on the skin. Hairless mouse skin was mounted on Franz-type diffusion ce...
Source: Chemical and Pharmaceutical Bulletin - February 1, 2023 Category: Drugs & Pharmacology Authors: Qihui Xu Yifan Wu Hiroki Saito Yuki Ofuchi Haruna Setoyama Takayuki Furuishi Kaori Fukuzawa Etsuo Yonemochi Yasuko Obata Source Type: research

Masking the Taste of Fixed-Dose Combination Drugs: Particular NSAIDs Can Efficiently Mask the Bitterness of Famotidine
This study aimed to evaluate the bitterness of famotidine (FAM) combined with each of three non-steroidal anti-inflammatory drugs (NSAIDs): ibuprofen (IBU), flurbiprofen (FLU), and naproxen (NAP), which have potential as fixed-dose combination (FDC) drugs. We evaluated the bitterness of FAM and each NSAID by taste sensor AN0 and C00, respectively. FAM showed high sensor output representing sensitivity to bitterness, whereas three NSAIDs did not show large sensor output, suggesting that the bitterness intensities of three NSAIDs were lower than that of FAM. The bitterness of FAM on sensor AN0 was suppressed in a concentrati...
Source: Chemical and Pharmaceutical Bulletin - February 1, 2023 Category: Drugs & Pharmacology Authors: Rio Uno Kyoko Ohkawa Honami Kojima Tamami Haraguchi Minoru Ozeki Ikuo Kawasaki Miyako Yoshida Masaaki Habara Hidekazu Ikezaki Takahiro Uchida Source Type: research

Promoting Activity of Terpenes on Skin Permeation of Famotidine
Chem Pharm Bull (Tokyo). 2023;71(2):111-119. doi: 10.1248/cpb.c22-00568.ABSTRACTFamotidine (FMT) is a competitive histamine-2 (H2) receptor antagonist that inhibits gastric acid secretion for the treatment of Gastroesophageal reflux disease. To study the promoting effect and mechanism of terpenes, including l-menthol, borneol, and geraniol, as chemical enhancers, FMT was used as a model drug. Attenuated total reflectance-Fourier transform IR spectroscopy (ATR-FTIR) and differential scanning calorimetry (DSC) were used to explore the effects of terpenes on the skin. Hairless mouse skin was mounted on Franz-type diffusion ce...
Source: Chemical and Pharmaceutical Bulletin - February 1, 2023 Category: Drugs & Pharmacology Authors: Qihui Xu Yifan Wu Hiroki Saito Yuki Ofuchi Haruna Setoyama Takayuki Furuishi Kaori Fukuzawa Etsuo Yonemochi Yasuko Obata Source Type: research

Masking the Taste of Fixed-Dose Combination Drugs: Particular NSAIDs Can Efficiently Mask the Bitterness of Famotidine
This study aimed to evaluate the bitterness of famotidine (FAM) combined with each of three non-steroidal anti-inflammatory drugs (NSAIDs): ibuprofen (IBU), flurbiprofen (FLU), and naproxen (NAP), which have potential as fixed-dose combination (FDC) drugs. We evaluated the bitterness of FAM and each NSAID by taste sensor AN0 and C00, respectively. FAM showed high sensor output representing sensitivity to bitterness, whereas three NSAIDs did not show large sensor output, suggesting that the bitterness intensities of three NSAIDs were lower than that of FAM. The bitterness of FAM on sensor AN0 was suppressed in a concentrati...
Source: Chemical and Pharmaceutical Bulletin - February 1, 2023 Category: Drugs & Pharmacology Authors: Rio Uno Kyoko Ohkawa Honami Kojima Tamami Haraguchi Minoru Ozeki Ikuo Kawasaki Miyako Yoshida Masaaki Habara Hidekazu Ikezaki Takahiro Uchida Source Type: research

Masking the Taste of Fixed-Dose Combination Drugs: Particular NSAIDs Can Efficiently Mask the Bitterness of Famotidine
This study aimed to evaluate the bitterness of famotidine (FAM) combined with each of three non-steroidal anti-inflammatory drugs (NSAIDs): ibuprofen (IBU), flurbiprofen (FLU), and naproxen (NAP), which have potential as fixed-dose combination (FDC) drugs. We evaluated the bitterness of FAM and each NSAID by taste sensor AN0 and C00, respectively. FAM showed high sensor output representing sensitivity to bitterness, whereas three NSAIDs did not show large sensor output, suggesting that the bitterness intensities of three NSAIDs were lower than that of FAM. The bitterness of FAM on sensor AN0 was suppressed in a concentrati...
Source: Chemical and Pharmaceutical Bulletin - February 1, 2023 Category: Drugs & Pharmacology Authors: Rio Uno Kyoko Ohkawa Honami Kojima Tamami Haraguchi Minoru Ozeki Ikuo Kawasaki Miyako Yoshida Masaaki Habara Hidekazu Ikezaki Takahiro Uchida Source Type: research