Journal of Applied Pharmaceutical Research

An overview on fundamentals of immediate release drug delivery system

2022-11-01T12:18:17+0530

Tablet is most popular among all dosage forms today because of its convenience, ease of administration, greater flexibility in dosage form design, ease of production, and low cost and non-invasive therapy. Formulation of tablets requires API along with excipients. Excipients include lubricants, diluents, binders, glidants, disintegrants, sweetening agents, flavoring agents, etc. Recent trends indicate that multi-particulate drug delivery systems are suitable for achieving extended-release oral formulation with a low risk of dose dumping, mixing flexibility to attain difference release patterns, and reproducible and short gastric residence time. Modern technology in immediate-release tablets, such as novel granulation techniques and electrostatic dry powder coating techniques, are prevalent nowadays. Recently, the immediate-release formulation has been similar to various sustained-release formulations that are currently readily attainable.

A brief overview of sustained released drug delivery system

2022-11-02T13:53:40+0530

The most popular and patient-friendly method of drug administration is often thought to be the oral route of administration. Compared to conventional release formulations, advancements in formulation technology, including modified release dosage forms or sustained release oral dosage forms, have been extensively accepted. A sustained release dosage form provides a prolonged release of the drug over an extended period, thereby giving better patient compliance and enhanced bioavailability. Sustain release systems are considered a wiser approach for drugs with short half-lives requiring repeated dosing. Sustained release drug delivery has a range of advantages over conventional dosage forms, including increased patient compliance due to less frequent drug administration, significantly reduced steady state drug level fluctuations, maximum drug utilization, the increased safety margin of potent drugs, lower healthcare costs due to improved therapy, and shorter treatment times. The present review focuses on design, fabrication, and various factors that influence the performance of sustained-release dosage forms.

Analgesic effect of intravenous versus intraperitoneal dexmedetomidine as an adjuvant to intraperitoneal bupivacaine (0.125%) in laparoscopic cholecystectomy: a randomized, double blind, interventional study

2022-11-02T14:08:16+0530

Background and Aims: Laparoscopic cholecystectomy has emerged as a gold standard technique for gall bladder stones. The aim of the present study was to compare the analgesic effect of intravenous (IV) vs intraperitoneal (IP) dexmedetomidine as an adjuvant to intraperitoneal (IP) bupivacaine in laparoscopy. Methods: A prospective, randomized, double blind, interventional study was conducted on 100 patients undergoing laparoscopic cholecystectomy where they were divided into following 2 groups: Group A: Patients received IV 1µg/kg dexmedetomidine diluted to 30 ml with normal saline over 10 min and 40 ml of 0.125% bupivacaine IP after removal of gall bladder. Group B: Patients received IV 30 ml of normal saline and 1µg/kg IP dexmedetomidine in 40 ml of 0.125% IP bupivacaine after removal of gall bladder. The primacy outcome was noted as a difference in mean duration for need of first rescue analgesia. The total consumption of analgesic in first 24hours was recorded and compared between the two groups. Results: Both the groups were comparable in terms of demographic profile and intraoperative hemodynamic parameters with no statistical difference. Comparison of time to first analgesic requirement between the two groups showed statistically significant results with unpaired t test The time of first rescue analgesia in Group A was 151.80 min ± 76.624. and in Group B was 94.80min ± 21.499. The total analgesic requirement in 24 hours in Group A was 136.64 ± 31.251 and in Group B was 144.12 ± 21.49. Conclusion: In our study we concluded that intravenous dexmetomidine provided superior analgesia as compared to intraperitoneal dexmetomidine when used as an adjuvant with Bupivacaine intraperitoneally.

Effects of dexmedetomidine on perioperative monitoring parameters and recovery in patients undergoing laparoscopic cholecystectomy in a 300 bedded hospital, Jaipur

2022-09-29T10:52:23+0530

Background: Laparoscopic cholecystectomy has emerged over the open cholecystectomy as gold standard for surgical treatment of symptomatic gall stones. Although pain after laparoscopic cholecystectomy is less intense, but many patients may experience considerable pain during first 24 hours in post-operative period. Intravenous (i.v.) use of dexmedetomidine in perioperative period lead to 90% decrease in the serum catecholamine levels, and further diminishing the haemodynamic response and sedating the patient and decrease analgesic requirements in the post-operative period. The efficacy of dexmedetomidine in providing hemodynamic stability during perioperative period and anesthesial recovery in patients undergoing laparoscopic cholecystectomy is studied. Methods: 60 patients of ASA grade I and II and of either sex (20–50 years) allocated in one of two parallel groups containing 30 patients each. In Group A- Dexmedetomidine (i.v.) bolus over 10min and continuous maintenance infusion 0.5µg/kg/h and in group B-0.9% normal saline i.v. bolus and continuous maintenance infusion was done. Parameters noted were heart rate, mean arterial pressure, oxygen saturation, post-operative pain were evaluated using VAS and analgesic requirement. Results: Both the groups were similar results in terms of age, sex, weight, ASA status, duration of surgery and hemodynamic parameters. SBP, DBP, MAP, SpCO₂, EtCO₂ values for both the groups were similar at all the intervals of time. No significant side effects were noted. Conclusion: Dexmedetomidine, pre-anaesthetic medication and its intraoperative infusion, further reducing the intraoperative anaesthetic requirement, sympathoadrenal response to intubation, maintains intraoperative cardiovascular stability, smooth extubation, sedation, and reduction in postoperative complications.

In-silico ADME prediction and molecular docking study of novel benzimidazole-1,3,4-oxadiazole derivatives as CYP51 inhibitors for antimicrobial activity

2022-11-02T16:21:52+0530

A class of innovative benzimidazole-1,3,4-Oxadiazole derivatives is a significant heterocyclic molecule for therapeutic development. In heterocyclic chemistry, the novel 1,3,4-Oxadiazole nucleus has a wide range of uses, including antibacterial, treatment. Molecular docking is frequently employed in contemporary drug design to comprehend drug-receptor interaction. Swiss dock, PyRx, and discovery studio visualizer (DSV) tools were used to predict in-silico ADME properties. In the current investigation, substituted benzimidazole-1,3,4-Oxadiazole derivatives were taken for docking studies against 6AYB an Naegleria fowleri CYP51-ketoconazole complex. The main objective of the study is to perform docking of the selected benzimidazole-1,3,4-oxadiazole derivatives on the protein and compare the docking score with standard ketoconazole. The molecular docking study was conducted using PyRx and the discovery studio visualizer (DSV) program, Naegleria fowleri CYP51-ketoconazole complex (6AYB) was obtained from the protein data bank (PDB) site. It was found that the docking score of all sixteen 1,3,4-Oxadiazole compounds ranged from -8.1 to -8.9 Kcal/mol. The novel benzimidazole with 1,3,4-Oxadiazole derivatives has been found to possess antibacterial properties, many substituted 1,3,4-Oxadiazole derivatives have been reported for the activity

Effect of priming in preventing myoclonic movements after intravenous induction with etomidate in adult patients undergoing cardiac surgery: a randomised controlled interventional study

2022-09-27T16:34:17+0530

Etomidate is a hypnotic drug used as an intravenous anaesthetic induction agent. Etomidate causes myoclonic movements in 50-80% patients after induction which makes it less desirable for induction. Aim: Present study was to determine the effect of priming in preventing myoclonic movements after intravenous injection with etomidate in adult patients undergoing cardiac surgery. Materials and Methods: 108 patients ASA grade III scheduled for elective cardiac surgery were allocated randomly in two groups- Group A (n=54): Patients received induction dose of 0.3mg/kg I.V. etomidate, Group B (n=54): Patients received a priming dose of 0.03mg/kg etomidate I.V. followed after 1 minute by induction dose of 0.3 mg/kg I.V. etomidate over 20 seconds. 3 minutes after the start of induction with etomidate, patients in both groups were given injection fentanyl 4mcg/kg followed by injection Rocuronium (1mg/kg bodyweight) to facilitate tracheal intubation. The occurrence and intensity of myoclonus were observed for 3 min from the start of injection of the induction dose and graded clinically by a blinded observer as: 0=no myoclonus, 1=mild myoclonus, 2=moderate myoclonus and 3=severe myoclonus. Result: The average dose of etomidate used during induction and demographic variables were similar in both the groups. The incidence of myoclonus in priming Group (27/54 [50%] was significantly lower than in control Group (45/54 [83.33%].Myoclonus of moderate or severe grade occurred in significantly more patients in control Group (68.3%) than in priming Group (36.5%).Conclusion: Pre-treatment with etomidate (0.03 mg/kg), given 60 seconds before induction of anaesthesia is more effective in reducing the incidence of etomidate-induced myoclonus without related side-effects.