International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (5), pp. 001-005, May, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals

Full Length Research Paper

Comparative Bioavailability of Celecoxib Formulations in Healthy Males: A Randomized Crossover Study

Muhammad Akhtar1*, Mahmood Ahmad1, Irshad Ahmad1, Naveed Akhtar1, Asad Ullah Madni1, Muhammad Usman1, Muhammad Naeem Aamir1, Sonia Khiljee1, Mohammad Sualeh2, Shujaat Ali Khan3 and Muhammad Aleem4

1Faculty of Pharmacy and Alternative Medicine, the Islamia University of Bahawalpur, Pakistan.
2Faculty of Pharmacy, Federal Urdu University, Karachi, Pakistan.
3Department of Pharmaceutical Sciences, COMSATS Institute of Information Technology, Abbottabad, Pakistan.
4Department of Statistics, the Islamia University of Bahawalpur, Pakistan.

Accepted 7 October, 2024

The purpose of this study was to assess bioequivalence of two marketed formulations of celecoxib capsules in healthy human male volunteers. The study was conducted according to a single dose, randomized sequence, open label, two-period and crossover design. Both test and reference formulations comprised labeled dose of 200 mg celecoxib and were administered to each subject after an overnight fasting on two treatment days separated by one week of washout period. After drug administration, blood samples were collected at predetermined time points for a period of 48 h. Plasma separated from blood was analyzed for celecoxib concentrations using validated reverse phase-high performance liquid chromatographic (RP-HPLC) method. Various pharmacokinetic parameters including Cmax, Tmax, AUC0-t, AUC0-∞, T1/2 and Kel were determined from the plasma concentration for both formulations. Cmax, AUC0-t and AUC0-∞, were evaluated for bioequivalence after log-transformation of data. The 90% confidence intervals for the ratio of Cm ax (93.26 to 100.70%), AUC0-t (87.00 to 117.50%) and AUC0-∞ (86.49 to 118.56%), values for the test and reference products were within the acceptance range of 80 to 125%, proposed by Food and Drug Administration (FDA) and European Medicines Evaluation Agency (EMEA). Based on these statistical inferences, it was concluded that two formulations of celecoxib are bioequivalent in their rate and extent of absorption.

Key words: Celecoxib, pharmacokinetics, bioequivalence, healthy human male volunteers.
 

International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (5), pp. 001-008, May, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals

Full Length Research Paper

Development and Biopharmaceutical Assessment of Fast Dissolving Nifedipine-Cyclodextrin Tablets

Saleh A. Al-Suwayeh1*, Jia-You Fang1,2, Ibrahim M. El-Bagory1,3, Ehab I. Taha1 and Mohsen A. Bayomi1,3

1College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
2Pharmaceutics Laboratory, Graduate Institute of Natural Products, Chang Gung University, Kweishan, Taoyuan,
Taiwan.

3Center of Excellence in Biotechnology Research, King Saud University, Box 2460 Riyadh 11451, Saudi Arabia.

Accepted 11 March, 2025

In this study, nifedipine tablets were formulated with different types of cyclodextrins (CDs) by direct compression method. Spray dried lactose and microcrystalline cellulose (MCC) were used as tablet fillers. The prepared tablets showed good appearance with acceptable crushing strength and disintegration time. The tablets showed fast dissolution within 11 to 68 min for 80% of the drugs depending on the type of CD and tablet filler. Some of the formulated tablets presented good fast release properties similar to soft gelatin capsules (USP XXIV) and based on the calculated dissolution efficiency (DE%), tablets containing hydroxypropyl- -CD and lactose as a filler were chosen for in vivo study by oral administration to beagle dogs when compared with the commercially available 10 mg soft gelatin capsule (Adalat®) and 10 mg film coated tablets (Corinfar ®). The formulated tablets showed significantly higher area under the curve (AUC0- ) than the commercial soft gelatin capsule and film coated tablets as result of increased drug absorption. It was concluded that the formulated fast release tablets could replace the nifedipine soft gelatin capsules with the advantages of ease of preparation and less restricted storage and handling conditions.

Key words: Nifedipine tablets, cyclodextrins, bioavailability, beagle dogs.
 

International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (5), pp. 001-009, May, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals

Full Length Research Paper
        
Determination of Acetylator Status in Pakistani Population: A Study of Sulphamethazine Metabolism in Male and Female Volunteers

Naheed Akhter, Tahira Iqbal* and Amer Amil
Department of Chemistry and Biochemistry, University of Agriculture, Faisalabad, Pakistan.
Accepted 09 January, 2025

The acetylation polymorphism is one of the most common inherited variations in the biotransformation of drugs and chemicals and large number of studies has been done to determine the distribution of acetylator phenotypes among populations of different geographic origin. The aim of this study was to investigate the acetylator phenotypes of the Pakistani population and compare it between male and female healthy volunteers. The polymorphic acetylation of sulphamethazine has been investigated in male and female volunteers (50 each) of Pakistani population. Sulphamethazine was administered orally in Capsule form as 500 mg to each healthy male and female volunteer. Sulphamethazine and acetylsulphamethazine were determined in the six hour plasma samples by high-pressure liquid chromatography (HPLC). Acetylator phenotype was determined from the metabolic ratio of acetylsulphamethazine to sulphamethazine in the plasma samples. The acetylation of sulphamethazine by arylamine N-acetyltransferase 2 (NAT2) showed bimodal population frequency distribution. 60% of the female volunteers were found to be fast and 40% to be slow acetylators while that of male volunteers were 62% fast and 38% slow acetylators.

Key words: NAT2 acetylation phenotype, sulphamethazine, male & female volunteers, HPLC assay.
 

International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (5), pp. 001-007, May, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals

Full Length Research Paper

Antimicrobial Prescribing Practices in Otorhinolaryngology: A Tertiary Care Hospital Study

Farhan Ahmad Khan1*, Sheikh Nizamuddin2 and Mohammad Tariq Salman3

1Department of Pharmacology, Teerthanker Mahaveer Medical College and Research Centre,
Moradabad-244001, India.
2Department of Ear Nose and Throat (ENT), Teerthanker Mahaveer Medical College and Research Centre,
Moradabad-244001, India.

3Department of Pharmacology, Era's Lucknow Medical College, Sarfarazganj, Hardoi Road, Lucknow.-226003. India.

Accepted 12 September, 2024

The objective of this research is to study the pattern of antimicrobial prescription in outpatient (OPD) and inpatient (IPD) of the Department of Otolaryngology in a tertiary care teaching hospital of North India. This was a prospective study conducted at the Teerthanker Mahaveer Medical College and Research Centre, over a period of 12 months. All the patients who attended the Ear Nose and Throat (ENT) OPD and IPD were included. The results show that out of 4800 patients, only 54% (n=2600) of patients were included in the study on the basis of inclusion and exclusion criteria and 31.25 % (n=1500) were defaulters. Majority of the patients were male 60% (n = 1560). Majority of the patients had suffered from ear disorders, 55% (n=1430). The most frequently prescribed antibacterials were - Lactams (75.68%) followed by aminoglycosides (9.43%). Among the penicillin group, the commonest drug prescribed was a combination of amoxicillin and clavulanic acid (9.58%), in cephalosporins was cefixime (37.98%) and in aminoglycosides was gentamicin (6.25%). In the concomitant medications antihistaminic were prescribed in 11.53%, proton pump inhibitors in 20.38% cases and NSAIDS in 7.26% cases. The average number of drugs used in each prescription was 2.70. All the drugs were prescribed with trade names. The average cost per prescription per day in OPD and IPD patients were Rs.45 and Rs.185, respectively. Out of 2600 patients; culture sensitivity tests were performed for only 71 patients (inclusive of OPD and IPD). Of which only 43 patients depicted a positive culture sensitivity tests. Our study showed that antimicrobials were mostly prescribed in patients of ear diseases while it was least in throat disorders. Proton pump inhibitors were the most common concomitant drug used. The cost of treatment in IPD patients were 4.11 times more than the OPD patients.

Key words: Antibacterial agents, drug utilization, ear nose and throat (ENT) infections, prescribing pattern, pharmacoepidemiology.

International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (4), pp. 001-006, April, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals

Full Length Research Paper

Fluvastatin Reduces Amyloid Beta Production in Rat Brain by Modulating APP Processing and Secretase Expression

Yun Shi1, Min Yao1, Lian-Guo Hou1, Jing Li1, Hai-Bao Zhu2, Jie Liu1, and Ling-Ling Jiang1*

1Department of Biochemistry and Molecular Biology, Hebei Medical University, Shijiazhuang 050017, PR China.
2Department of Neurology, Chengde Central Hospital, Chengde 067000, PR China.

Accepted 5 March, 2025

The aim of the present study was to determine the effects of fluvastatin, a relatively hydrophilic 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMGR) inhibitor, on endogenous amyloid beta (A ) production and if such effects would be associated with changes in brain total cholesterol in rats. Wistar male rats were treated with fluvastatin at a dose of 20 mg/kg/day or vehicle (controls) by oral gavage for 28 days. We examined serum and brain cholesterol levels by CHOD-PAP method, brain A levels by radioimmunoassay, mRNA levels of HMGR and cholesterol 24S-hydroxylase (CYP46) involving in cholesterol balance, -secretase (BACE1) and -secretase (ADAM10) involving in amyloid beta precursor protein (A PP) processing by RT-PCR and protein levels of A PP by immunohistochemistry. Serum total cholesterol and brain A levels were significantly reduced in fluvastatin-treated rats. There was no change in total cholesterol levels, HMGR and CYP46 mRNA levels in the brain of fluvastatin-treated rats. Fluvastatin reduced A PP protein levels and up-regulated ADAM10 but down-regulated BACE1 mRNA expression in rat brain under used condition. These results suggest that reduction of brain A levels by fluvastatin is associated with changes in level of A PP and A PP cleavage-related enzyme mRNA, and is independent of brain total cholesterol. It may contribute to one of neuroprotective effects of fluvastatin and reveal that administration of fluvastatin could be beneficial in the preventation of AD.

Key words: Alzheimer’s disease, cholesterol, amyloid, amyloid-protein precursor, fluvastatin, statin.

International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (4), pp. 001-005, April, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals

Full Length Research Paper

Diabetic Wound Healing: Stimulatory Effects of Omega-3 and Omega-6 Polyunsaturated Fatty Acids in Rats

Jafari Naveh H. R.1, Taghavi M. M.1*, Shariati M.1,2, Vazeirnejad R.3 and Rezvani M. E.4

1Department of Anatomy, School of Medicine, Rafsanjan University of Medical Sciences, Rafsanjan, Iran.
2Department of Anatomy, School of Medicine, Mashhad University of Medical Sciences, Mashhad, Iran.

3Department of Medical society, School of Medicine, Rafsanjan University of Medical Sciences, Rafsanjan, Iran. 4Department of Physiology and Pharmacology, School of Medicine, Rafsanjan University of Medical Science, Rafsanjan, Iran.

Accepted 7 September, 2024

The potential role of omega-3 ( -3) and omega-6 ( -6) fatty acids on wound healing in chronic diabetic diseases is of interest and controversial. In this experimental study, the effect of topical application of fish and corn oils containing -3 and -6 fatty acids on skin wound healing in chronic diabetic rat has been evaluated. Rats were randomly divided into five groups (n = 7). First group was served as normal or control group. In diabetic groups, one group was non-treated group (shame group) and two groups received fish and corn oil (FO-group and CO-group), respectively. The last diabetic group was treated with both fish and corn oil (FCO-group) . Treatment was done from 4 weeks after the induction of diabetes till complete wound healing. All animals were wounded by a 2 cm2 incision in their dorsum. Wound surface area and required time for full healing were measured at various post-operated periods. The histological characteristics were studied by using hematoxilin and Eosin (H & E) method. Our results showed that surface area of wound in FCO- group was lesser than that non-treated group at 11th, 15th and 20th post-operative days significantly. Moreover the percentage of the wound healing in FCO-treated and non-treated groups was 98 and 70% at the 20th day, respectively. Histological studies showed that epidermal growth, cellular diffusion, density of collagen in FCO-group approximately were the same as control group. Topical application of fish and corn oil together may result in an acceleration of skin wound healing in chronic diabetic rats.

Key words: Fish oil, corn oil, wound healing, chronic diabetes.
 

International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (4), pp. 001-010, April, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals

Full Length Research Paper

Inotropic Activity Assessment of a Newly Synthesized Estradiol Derivative Using Isolated Rat Heart Preparations

Figueroa-Valverde L.1*, Díaz-Cedillo F.2, López-Ramos M.1, García-Cervera E1 and Pool-Gómez E.1

1Laboratory of Pharmaco-Chemistry, Faculty of Chemical Biological Sciences, Universidad Autonóma de Campeche, Av. Agustín Melgar s/n, Col Buenavista C.P.24039 Campeche Cam., México. 2Escuela Nacional de Ciencias Biológicas del Instituto Politécnico Nacional. Prol. Carpio y Plan de Ayala s/n Col. Santo Tomas, México, D.F. C.P. 11340.

Accepted 8 January, 2025

Several studies indicate that some steroid derivatives have inotropic activity; nevertheless, there is scarce information about the effects of the estradiol derivatives at cardiovascular level. Therefore, in this study, estradiol derivative was synthetized with the objective of evaluating its inotropic activity. In this first stage, the Langendorff technique was used to measure perfusion pressure and coronary resistance changes in isolated rat heart in absence or presence of estradiol derivative. In second stage, the inotropic activity of estradiol derivative was evaluated by measuring left ventricular pressure in absence or presence of following compounds; tamoxifen, prazosin, metoprolol, indomethacin and nifedipine. The results showed that the estradiol derivative significantly increase the perfusion pressure and coronary resistance in isolated heart. Additionally, other data indicate that estradiol derivative increase left ventricular pressure in a dose-dependent manner [10-9 to 10 -4 mmol]; nevertheless, this phenomenon was significantly inhibited by nifedipine at a dose of 1 × 10-6 mmol. In conclusion, these data suggest that the estradiol derivative induces positive inotropic activity through of activation the L-type calcium channel.

Key words: Estradiol derivative, Langendorff, inotropic activity.