Solid Dispersions of Famotidine: Physicochemical Properties and In Vivo Comparative Study on the Inhibition of Hyperacidity
- At August 09, 2020
- By Yori Yuliandra
- In Scientific Paper
36
Yori Yuliandra, Lili Fitriani, Robby Kurniawan, Fuji Yasardi, Erizal Zaini
Abstract
Famotidine is a potent histamine 2 antagonist used in the treatment of gastric acid overproduction. Famotidine belongs to Class IV in Biopharmaceutics Classification System (BCS) which has low solubility and membrane permeability. The purpose of this study was to compare the solubility and dissolution profile of solid dispersions (SDs) of famotidine with mannitol (SD‐MAN) and with hydroxypropyl methylcellulose (SD‐HPMC), and to comparatively study their in vivo effectiveness against hyperacidity. Famotidine SDs were prepared by cogrinding technique with the respective carriers in various ratios and grinding time. SDs with the best solubility underwent dissolution rate studies, solid‐state characterization, and in vivo efficacy evaluation. The in vivo evaluation was conducted in Sprague Dawley rats receiving famotidine formulations in the dose equivalent to 12 mg/kg of famotidine. The study found that the famotidine SDs could greatly improve the solubility of famotidine by 100.61 and 120.91% for SD‐MAN and SD‐HPMC, respectively. The solid‐state characterization revealed the decrease in crystallinity degree of famotidine solid dispersion systems. The comparative study on the in vivo efficacy of famotidine SDs showed that SD‐HPMC was significantly better than SD‐MAN. This study concludes that SDs can improve the solubility and in vivo effectiveness of famotidine in overproduction of gastric acid.
Read More»Multicomponent crystals of mefenamic acid–tromethamine with improved dissolution rate
Yori YULIANDRA, Riri IZADIHARI, Henni ROSAINI, Erizal ZAINI
Abstract
Mefenamic acid (MA) is a popular nonsteroidal anti-inflammatory drug classified into BCS class II which has a low solubility and dissolution rate in an aqueous medium. The present study aimed to improve the dissolution rate of MA by preparing multicomponent crystals with tromethamine (TM) through the solvent evaporation technique. The resulting powder was characterized for its solid-state properties and evaluated for the dissolution rate. The results showed that the powder X-ray diffraction pattern of the MA–TM binary system was different from its starting materials, indicating the formation of a new crystalline phase. The differential scanning calorimetry analysis of the MA–TM binary system showed a single and sharp endothermic peak at 110 °C, which was attributed to the melting point of MA–TM multicomponent crystals. The Fourier transform infrared spectroscopy analysis showed the occurrence of solid-state interaction involving proton transfer between MA and TM. The dissolution efficiency of MA–TM multicomponent crystal was 2.5-fold higher than the intact MA. The study concludes that the MA–TM binary system forms a salt-type multicomponent crystal. The multicomponent crystals can significantly increase its dissolution rate and is an alternative technique for modifying the physicochemical properties of active pharmaceutical ingredients.
Hematologic Toxicities of Chemotherapy in Lung Cancer Patients: A Retrospective Study in Dr. M. Djamil Hospital Padang, Indonesia
- At July 23, 2019
- By Yori Yuliandra
- In Scientific Paper
- 0
Yori Yuliandra, Hansen Nasif, Sabrina Ermayanti, Lilik Sulistyowati, Dian A Juwita
Abstract
The use of chemotherapeutic agents in the management of cancer is often followed by a range of toxicities to various organ systems. A retrospective study on the hematologic toxicities of chemotherapy in lung cancer patients has been carried out. The study was conducted by a cross-sectional method from medical records of four-year data in 2010-2014 at Dr. M. Djamil Hospital Padang, West Sumatra, Indonesia. Data from medical records of patients diagnosed with lung cancer and underwent chemotherapy, not suffering from primary hematologic diseases, and with normal kidney and liver function prior to chemotherapy were studied. A number of 22 medical records of lung cancer patients which met the criteria with a total of 40 chemotherapy cycles were observed. The study revealed that a combination of carboplatin-paclitaxel was the most common chemotherapy used for the patients (72.7%). The hematologic toxicities comprised anemia, leukopenia, and thrombocytopenia with the severity ranging from grade 1–3. Carboplatin-paclitaxel was the only combination that caused these three toxicities, and the only combination to cause thrombocytopenia as well. Anemia was the major hematologic toxicity experienced by more than half of the patients. The study concludes that there is a reasonably high incidence of hematologic toxicities from chemotherapy among lung cancer patients.
Keywords: anemia, chemotherapy, hematologic toxicity, leukopenia, lung cancer, thrombocytopenia
Read More»Blood pressure lowering effect of scopoletin on oxidative stress-associated hypertensive rats
- At April 01, 2019
- By Yori Yuliandra
- In Scientific Paper
- 34
Armenia ARMENIA, Rahmat HIDAYAT, Meiliani MEILIANI, Yori YULIANDRA
Abstract
Scopoletin is a coumarin derivative known for its antioxidant capacity. The present study was undertaken to investigate the blood pressure lowering effect of scopoletin in multiple models of hypertensive rats. To obtain animal models of hypertension, a number of 18 Wistar-Kyoto male rats were divided into two groups receiving a combination of oral prednisone and salt for 14 days (PN group, the endocrine hypertension model) while another half received the same inducers with an additional Nω-nitro-L-arginine methyl ester (L-NAME) for 2 days (PNL group, oxidative stress-associated hypertension model). The rats were anesthetized with propofol and subdivided into 3 groups receiving control, scopoletin 10 mg/kg, and tempol 100 μmol/kg. The systolic blood pressure (SBP), diastolic blood pressure (DBP), mean arterial blood pressure (MAP) and heart rate (HR) were recorded for 120 minutes after a single dose of drug commencement. The serum concentration of nitric oxide (NO) was measured before and at the end of the experiment. The data were analyzed using two-way ANOVA followed by Tukey’s HSD with 95% confidence interval. The results showed that scopoletin decreased the SBP, DBP, and MAP of the rats significantly (p<0.05) without any significant effect on the animal HR (p>0.1). The concentration of NO in animals receiving scopoletin and tempol was greater as compared control, but there was no significant difference in blood NO between both hypertensive models (p>0.1). The study concludes that scopoletin is effective as blood pressure lowering agent on oxidative stress-associated hypertensive rats.
Read More»Reversible Hepatotoxicity of Cassytha filiformis Extract: Experimental Study on Liver Function and Propofol-Induced Sleep in Mice
- At January 20, 2019
- By Yori Yuliandra
- In Scientific Paper
- 37
Yori Yuliandra, Armenia Armenia*, Rahmad Arief, Mifta Hul Jannah, Helmi Arifin
Abstract
Objective: To study the liver toxicity of Cassytha filiformis L. extract and its reversibility in mice. Methods: A total of 108 male mice were used to investigate the hepatotoxicity of Cassytha filiformis extract (CFE) and the reversibility of its toxicity to the liver. Seventy-two mice were treated with CFE orally for 7 consecutive days. A half of these animals were used to study the sleep time on propofol-induced sleep that comprised the sleep onset time (SOT) and duration of sleep (DOS), while another half was used for the quantitation of serum alanine transaminase (ALT) activity. To investigate the reversibility of the liver toxicity, thirty-six mice were treated with daily CFE for 7 days. Activities of ALT and alkaline phosphatase (ALP) were determined and the liver weight ratio was measured on day 0, 1, 3 and 7 after the termination of the CFE treatment. Data of liver toxicity determination were analyzed by two-way ANOVA followed by Duncan’s multiple range test, while data of the reversibility was analyzed by Pearson’s correlation. The significance level was taken at 95% of confidence interval. Results: CFE shortened the SOT and prolonged the DOS significantly compared with control (p<0.05). The activity of ALT was increased due to the toxicity of CFE. However, the ALT/ALP activities decreased and liver weight ratio increased gradually after the extract treatment was discontinued. The trend of these data was correlated significantly (p<0.05). Conclusion: Cassytha filiformis L. extract is toxic to the liver but the toxicity is reversible depending on doses.
Read More»Pharmacodynamics effect of methylprednisolone tablets on the serum concentration of annexin A1: in vivo comparative study between generic and innovator drug
- At January 01, 2019
- By Yori Yuliandra
- In Scientific Paper
- 36
HANSEN NASIF, HENNY LUCIDA , YANWIRASTI YANWIRASTI, YUFRI ALDI, YORI YULIANDRA
Abstract
Objective: The aims of this study were to investigate the comparative pharmacodynamics effect of methylprednisolone (MP) innovator, MP branded generic, and MP generic products to the serum concentration of annexin A1 (AnxA1).
Methods: It was conducted by two-way crossover design in male rabbits. AnxA1 was measured at 0, 0.5, 1, 2, 3, 5, 7, and 9 h after the administration of the drugs. The peak concentration (Cmax), the time at which the peak concentration was achieved (Tmax), and the area under the plasma concentration-time curve (AUC) were also determined.
Results: The highest concentration and widest AUC of AnxA1 were obtained in MP innovator drug. MP innovator and branded generic reaches the peak time (Tmax) at the third 3rd h, while the MP generic reaches the peak time at the 5th h. The results showed that there was no significant difference in the serum concentration of AnxA1 between MP tablets after analyzed with a one-way analysis of variance.
Conclusion: It could be concluded that the innovator drug of MP tablet gave the same effect on the serum concentration of AnxA1 than its generic counterparts, but an onset of action MP innovator and branded generic is faster than the generic product.
Effect of Eleutherine americana Merr. bulb extract on blood pressure and heart rate in anesthetized hypertensive rats
- At August 31, 2018
- By Yori Yuliandra
- In Scientific Paper
- 36
Yori Yuliandra, Rizki Oktarini, Armenia Armenia
Abstract
The effect of ethanolic extract of Eleutherine americana Merr. on the blood pressure and heart rate has been investigated. A number of 25 Sprague-Dawley male rats were induced with prednisone 1.5 mg/kg in combination with saline solution 2.5% for 14 days to obtain hypertension model. The rats were anesthetized and prepared for the recording of blood pressure and heart rate. The rats were divided into five groups receiving 100, 200, and 400 mg/kg of the extract, vehicle control, and captopril 30 mg/kg as the reference. The treatment was administered three times with 30 minutes interval. The systolic (SBP), diastolic (DBP), mean arterial pressure (MAP), and heart rate (HR) were recorded. The data were analyzed with two-way analysis of variance (ANOVA) followed by Duncan’s MRT (95% confidence interval). The study revealed that the extract exhibited a blood pressure lowering effect. The best antihypertensive activity of the extract was shown by the dose of 100 mg/kg. Meanwhile, HR was also affected inversely by the treatment, in which the lowest dose caused the highest increase. The study suggests that the extract of Eleutherine americana exhibits antihypertensive activity that may be potential for future development of drugs.
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