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1.
Pak J Pharm Sci ; 34(3(Supplementary)): 1069-1074, 2021 May.
Article in English | MEDLINE | ID: mdl-34602434

ABSTRACT

The purpose of the current studies was to develop ocular insert of betaxolol hydrochloride (BXH), using arabinoxylan (AX) as a film former. The inserts were prepared by sandwiching I mg of BXH between two films of AX. Six different formulations of ocular inserts were prepared in such a way that first three formulations contained varying concentrations of AX along with glycerol as plasticizer, whereas, rest of the formulations were added with 0.5mg of sodium alginate, sandwiched between two films of AX along with 1mg of BXH. Chemical compatibilities of the ingredients were assessed by using FTIR. Prepared ocular inserts were subjected to various physicochemical characterizations. The dissolution studies showed that ocular inserts containing sodium alginate with the AX showed sustained release effect better than the formulations with AX alone. Addition of sodium alginate resulted in inhibition of sudden release in initial phase and further sustained the release of drug from ocular inserts. Ocular inserts were pH compatible to the eyes as well as there was no interaction among the drug and excipients, suggesting that the selected excipients were suitable for the development of sustained release ocular inserts of BXH.


Subject(s)
Adrenergic beta-1 Receptor Antagonists/administration & dosage , Alginates , Betaxolol/administration & dosage , Glycerol , Plantago , Xylans , Administration, Ophthalmic , Adrenergic beta-1 Receptor Antagonists/pharmacokinetics , Betaxolol/pharmacokinetics , Delayed-Action Preparations , Drug Liberation , Glaucoma, Open-Angle/drug therapy
2.
Pak J Pharm Sci ; 34(6(Supplementary)): 2357-2364, 2021 Nov.
Article in English | MEDLINE | ID: mdl-35039274

ABSTRACT

The current study was conducted to fabricate Metoclopramide HCL (MCH) and Sumatriptan succinate (SS) instant release buccal films (IRBF) without using any super disintegrant. The solvent casting method was used for the preparation of IRBFs and prepared IRBFs were physicochemically evaluated. Spectrophotometric analysis was done to determine the lambda max followed by the linearity determination of both drugs. Different concentrations such as 100, 125, and 150mg of hydrophilic polymer (HPMC E5) were employed but the concentration of glycerol was variable. Comparatively better results were observed for the formulation with 150mg of HPMC E5 and 30% glycerol. Formulated IRBFs showed good tensile strength with a mean disintegration time of 12.4-28.4 seconds and rapid dissolution with more than 50% drug release within 2 minutes. It was concluded that the chosen combination of polymers was appropriate for the fabrication of MCH and SS buccal strips.


Subject(s)
Dopamine D2 Receptor Antagonists/chemistry , Glycerol/chemistry , Hypromellose Derivatives/chemistry , Metoclopramide/chemistry , Serotonin 5-HT1 Receptor Agonists/chemistry , Sumatriptan/chemistry , Administration, Buccal , Dopamine D2 Receptor Antagonists/administration & dosage , Dosage Forms , Drug Compounding , Drug Liberation , Kinetics , Metoclopramide/administration & dosage , Serotonin 5-HT1 Receptor Agonists/administration & dosage , Solubility , Spectrophotometry, Ultraviolet , Sumatriptan/administration & dosage , Tensile Strength
3.
Pak J Pharm Sci ; 32(4(Supplementary)): 1773-1779, 2019 Jul.
Article in English | MEDLINE | ID: mdl-31680072

ABSTRACT

Current study was designed with the aim to employ quasi emulsification, and double emulsification techniques for the development of Flurbiprofen (FLB) loaded micro sponges, followed by their physicochemical evaluation. FTIR interpretations exhibited compatibility of ingredients, while crystallographic analysis revealed crystalline nature of pure drug, which was masked upon incorporation into microsponges. Optical microscope and SEM have exposed spherical and spongy surfaces of prepared micro sponges. Micromeritics suggested that the flow properties are excellent and microsponges have remarkable drug entrapment efficiency (98.55±0.08%). In-vitro dissolution studies demonstrated good control over release of FLB until 8th h from the prepared microsponges. However, a difference in cumulated amount of released drug was noticed i.e. EC based formulation has released about 99.3±0.10%, while XG facilitated EC based formulations offered 92.7±2.1% release of the drug. Zeta potential indicated access of negative charge while zeta sizer has described the range of the particle size between 2.6 to 3.5µm. Conclusively the results have advocated the suitability of selected ingredients for incorporation of FLB into microsponges for its sustained delivery.


Subject(s)
Flurbiprofen/chemistry , Delayed-Action Preparations/chemistry , Drug Compounding/methods , Drug Delivery Systems/methods , Particle Size
4.
Pak J Pharm Sci ; 31(6 (Supplementary): 2743-2747, 2018 Nov.
Article in English | MEDLINE | ID: mdl-30587489

ABSTRACT

This study was schemed to comprehend the latest kaleidoscopic trends of bacterial resistance in neonatal pathogens against all those antibiotics commonly employed as empirical therapy in neonates. The methodological approach included; isolation and subsequent identification of those pathogens having caused bacterial infections in neonates, application of antibiotic sensitivity testing and finally construing the conclusion depicting patterns of antibiotic resistance by various pathogens, isolated from neonatal biological samples. Antibiotic resistance patterns was evident in gram-positive as well as in gram-negative bacteria in all the eight species identified in this study. Even antibiotic drugs which are being commonly relied upon for treating multi-resistant bacterial infections, found to be in effective against many newly emerged resistant bacteria, when used alone. Resistance Antibiotics drugs against which most prominent resistance pattern emerged include; Amikacin sulphate, Linezolid, Piperacillin / Tazobactam, Amoxicillin / Clavulanic acid, Vencomycin, Cefoperazone / Sulbactam, Ceftriaxone sodium, Ciprofloxacin, Cefixime trihydrate and Imipenem. The inferred upshot suggests that antibiotic resistance is emerging fast and ever-changing phenomenon of antibiotic resistance has significantly reduced the therapeutic space to maneuver, particularly, in treating neonatal infections.


Subject(s)
Anti-Bacterial Agents/therapeutic use , Bacterial Infections/drug therapy , Drug Resistance, Bacterial/drug effects , Anti-Bacterial Agents/pharmacology , Bacterial Infections/diagnosis , Cross Infection/diagnosis , Cross Infection/drug therapy , Cross Infection/microbiology , Drug Resistance, Bacterial/physiology , Humans , Infant, Newborn
5.
Acta Pol Pharm ; 74(2): 489-495, 2017 Mar.
Article in English | MEDLINE | ID: mdl-29624254

ABSTRACT

Single centered crossover, two cycles volunteer study was performed on 12 healthy male volunteers. Both reference and test, immediate release nimesulide formulation was given in a randomized manner with a washout period of 15 days and 5 mL of blood samples were drawn at 0.5, 1, 1.5, 2, 4, 8, 12 and 24 h. Plasma after centrifugation and deproteination, 100 µL of the sample was injected using already validated HPLC method. In plasma LOQ was 0.01 ± 0.012 µg/mL, LOD was 0.001 µg/mL and linearity was observed from 10 to 0.001 pg/mL. Pharmacokinetic parameters including in vivo bioequivalence were studied by using Kinetica 4.4.1. software. The average values of AUC,, was found to be 23.654 ± 0.688 and 23.532 ± 0.662 mg/L x h while C.. values were 6.101 ± 0.403 and 6.072 ± 0.403 pg/mL, respectively. Mean clearance and volume of distribution of reference formulation were 64.062 ± 3.086 mL/h/kg and 9.416 ± 4.767 L, respectively. The disposition rate constant in reference formulation was 0.339 ± 0.598 h' while in immediate release it was 0.467 ± 0.481 h-'. Absorption rate constant and distribution rate constant for reference brand were 1.409 ± 0.251 h- and 1.201 ± 0.283 h' while in immediate release formulation these values were 1.420 ± 0.214 h-' and 1.227 ± 0.263 h', respectively. Bioequivalence results showed 90% confidence of interval for compartmental parameters like Cmax was 99.1 to 100.3%, Tmax. was 98.198 to 99.658% and AUClast, was 99.88 to 100.08% and all were within range.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics , Sulfonamides/pharmacokinetics , Administration, Oral , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/blood , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Area Under Curve , Chromatography, High Pressure Liquid , Cross-Over Studies , Half-Life , Healthy Volunteers , Humans , Male , Metabolic Clearance Rate , Models, Biological , Pakistan , Sulfonamides/administration & dosage , Sulfonamides/blood , Sulfonamides/chemistry , Tablets , Therapeutic Equivalency , Young Adult
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