Minimum Disintegration Time Research Articles

Formulation Design and Development of Fast Disintegrating Tablets of Losartan Potassium By Using Locast Bean Gum As Superdisintigrants

For patients who have trouble swallowing tablets, capsules, etc., fast dissolving drug delivery devices provide an option. Water is not necessary for the swallowing of fast dissolving pills because they dissolve instantly in the mouth. Using locust bean gum as a natural superdisintegrant, the present work set out to produce fast-dissolving tablets of losartan potassium. Perform pre formulation studies like partition coefficient, solubility and identification of drug. The influence of precompressional parameters like interaction studies and compatibility. Other tablet properties were examined, as well as the impact of formulation parameters on losartan potassium disintegration and in-vitro dissolution. The findings indicated that the 7.5% concentration of locust bean gum had good superdisintegrant qualities and produced quickly dissolving tablets. The best tablet formulation (F3) had a 20-second minimum disintegration time and a 30-minute maximum drug release of 98%. The locust bean gum was discovered to have a notable ability to be employed as a superdisintegrant, with a swelling index of 22. The DSC analysis and IR spectra demonstrated that there was no interaction of any type with the tablet's formulation ingredients. Accelerated short-term experiments on optimized formulation show no appreciable modifications to the formulation.

Formulation development, in vivo bioequivalence and pediatric PBPK modeling studies of taste-masked ciprofloxacin chewable tablets

A taste-masked chewable tablet of ciprofloxacin using ion exchange resin Kyron T-134 for enhancing compliance for the paediatric population was developed. The drug-to-resin ratio was optimized for maximum taste masking by studying the effects of soaking time (X1) and mixing time (X2) on complexation (%) using Central Composite Rotatable Design (CCRD). The resin complexes were characterized by bitterness score, DSC, FTIR, and PXRD. The complex was further formulated and optimized into chewable tablets through full factorial design, The optimized formulation was subjected to a bioequivalence study, and a virtual approach of PBPK modelling was adapted to predict the pharmacokinetics of the drug in the paediatric group. The drug resin ratio of 1:1.5 yielded an optimum drug loading of 99.05%. The optimized formulation shows minimum disintegration time with more than 99% drug release within 30 min. The formulation F-9 was found to be bioequivalent with a geometric mean ratio of Cmax, Tmax, AUC0–t, and AUC0–∞ within 90% CI. It was concluded that quality by design approach can successfully be applied to optimize the drug resin ratio and PBPK modeling is a successful predictive tool for estimating the pharmacokinetics of ciprofloxacin HCl in the paediatric population.

Formulation and Estimation of Rapidly Dissolving Sublingual Thin Film of Vildagliptin

The purpose of the present research was to develop a fast and rapidly dissolving polymeric sublingual thin film of vildagliptin due to its simplicity of use as an alternative to oral disintegrating tablets and better compliance for diabetic patients. Nine different formulations (F1-F9) of vildagliptin sublingual films were produced using diverse concentrations of polymer A and plasticizer B by solvent casting method. Several physicochemical properties, including morphological properties, weight variation test, film thickness, folding endurance, surface pH, percentage of moisture loss, in-vitro disintegration test, in-vitro dissolution test, trinocular microscopic imaging of film, differential scanning calorimetry (DSC), FTIR study and content uniformity were evaluated. The ratios of polymer A-plasticizer B were as follows (5:1), (7:1), (7.67:1), (8:1), (8.5:1), (8.67:1, (9.67:1), (10:1), (11:1) which made the film smooth, mechanically strong and easy to peel out. Among all the different formulations, the F1 formulation showed the most significant result concerning in-vitro dissolution (98.95%) in 5 minutes, minimum disintegration time (38 sec.), less film thickness (116.67 ± .58 μm) and better folding endurance (403 times). Bangladesh Pharmaceutical Journal 26(2): 212-218, 2023 (July)

OPTIMIZATION AND CHARACTERIZATION OF MELOXICAM ORODISPERSIBLE TABLETS USING MIXED HYDROTROPY FOR ENHANCED WATER SOLUBILITY

Introduction: In order to attain rapid discharge in saliva and enhanced absorption, drug was incorporated in a fast-dissolving dosage form (ODTs) as a solid dispersion. In this present work ODTs of Meloxicam were prepared by sublimation techniques where different subliming agents were used with super disintegrant. Materials and Methods: Hydrotropic solid dispersions were prepared using different ratios (1:2, 1:4 and 1:6) of drug and hydrotropic blends (Niacinamide, Anhy. Sodium citrate, Sodium Salicylate and Sodium benzoate). Best hydrotropic solid dispersion was selected to prepare ODTs comprising of croscarmellose sodium and camphor in different concentration along with other pharmaceutical excipients. From the primary trial batches, T3 was selected for optimization experimental designs due to lowest disintegration time and highest in vitro drug release. Secondary batches (F1-F9) were prepared by using 32 full factorial design with different concentration of croscarmellose sodium (12, 14 and 16 mg) and camphor (8, 10 and 12 mg) as two independent variables while disintegration time and percent friability were considered as two dependent response variables. These formulations were subjected to study of various post compression evaluation parameters like hardness, thickness, friability, weight variation, disintegration time (25-117 sec) and in-vitro drug release (99.09%).
 Result and Discussion: Equilibrium solubility studies were reported that by utilizing hydrotropy, the solubility of Meloxicam got enhanced from 20.5 to 140.96 times as compared to its aqueous solubility. The desirability fraction was used to optimize the response variables for specific targets, i.e., minimum disintegration time and maximum dissolution, and the responses obtained were consistent for experimental values.

DEVELOPMENT AND CHARACTERIZATION OF TRANDOLAPRIL IMMEDIATE RELEASE TABLETS USING DIFFERENT SUPERDISINTEGRATING AGENTS

A potent non-sulfhydryl prodrug, trandolapril is transformed into the active substance, trandolaprilat, in the liver. For obese individuals with mild-to-moderate essential hypertension, Trandolapril is effective and safe. The elimination t1/2 of trandolapril and trandolaprilat are approximately 6 hours and 16–24 hours, respectively. The goal of present work is to develop the Trandolapril immediate release tablet using various superdisintegrants. Crospovidone, Sodium starch glycolate and Croscarmellose sodium in concentrations of 2%, 4%, and 6% were used as superdisintegrating agents for the optimization. Direct compression technique was used to make nine formulations (IRTR 1 to IRTR 9). The powder blends of all batches were evaluated for different parameters to know the powder flow characteristics and it was found that the powder blend had excellent flow and compressibility characteristics. Then, compressed tablets were tested for quality control parameters as per the IP. In formulation IRTR1-IRTR9, disintegration time was observed 30.23 to 71.67 Sec and more than 70% drug was released in 30 min. Thus, based on evaluation results, it is concluded that formulation of immediate release (IR) tablets of Trandolapril were successfully developed. Minimum disintegration time 30.23 seconds 90.56% drug release in 30 min was obtained with IRTR3. KEYWORDS: Trandolapril, Immediate release, Crospovidone, Sodium starch glycolate, crocarmellose sodium

Perbandingan karakteristik pektin kulit buah kakao dan kulit buah kopi dalam sediaan cangkang kapsul

Cocoa peels and coffee peels as food industry have low economic value but have great potential because of the high levels of pectin in them. This research used microwave assistant extraction (MAE) method from kako peel and coffee peel waste and has assessed their potential as a source of raw material for capsule shells. This research included observing the optimization of pectin extraction techniques, standardizing pectin, and observing the quality of the resulting capsule shells. The pectin used comes from cocoa peel and coffee peel waste in West Java. The test results showed that the quality of the pectin obtained from cocoa shells and coffee husks complied with IPPA (International Pectin Produce Association) standards so that these pectins could be used for industrial purposes. While the capsule shells obtained have met the organoleptic standards and the disintegration time of the capsule shells according to the Indonesian Pharmacopoeia. Some of the parameters that meet these standards were the size of the capsule shell, both the uniformity of the size of the capsule cap, the uniformity of the size of the capsule body and the minimum disintegration time. Meanwhile, the weight uniformity standards have not met the requirements. The coffee peel capsule shells also meet the Indonesian Pharmacopoeia standards in terms of uniformity of capsule cap size, uniformity of capsule body size, minimum disintegration time, and uniformity of weight. In addition, capsule shells made from cocoa peel and coffee peel meet the requirements for the characteristics of good capsule shell materials where the results of the elongation strength and tensile strength tests meet the quality requirements. So it can be seen that the pectin from cocoa and coffee peels waste have good character to be developed as a source of pectin for pharmaceutical raw materials with the addition of other excipients, such as CMC-Na and carrageenan

Effect of starch, cellulose and povidone based superdisintegrants in a QbD-based approach for the development and optimization of Nitazoxanide orodispersible tablets: Physicochemical characterization, compaction behavior and in-silico PBPK modeling of its active metabolite Tizoxanide

The objective of the study was to develop a QbD based orodispersible Nitazoxanide 200 mg tablets its in-silico PBPK modeling. The central composite design was applied to study the effect of four different superdisintegrant i.e., starch and cellulose based (sodium starch glycolate, pre-gelatinized starch, croscarmellose sodium), and crospovidone with microcrystalline cellulose as independent variables on disintegration time and % drug release. The Heckel analysis was applied to determine the compression behavior of the formulations which revealed a yield pressure in the range of ∼119 MPa–∼138 MPa. Moreover, the hardness of the tablets increased with the compression force and was largely independent of the disintegration time (<3 min for a maximum pressure of ∼138 MPa) owing to the role of superdisintrgrants in the formulations. The quality attributes suggest that the formulations containing microcrystalline cellulose (11–15%) with sodium starch glycolate (8%), pregelatinized starch (7.185%), croscarmellose sodium (2.755%), and crospovidone (5%) at the maximum desirability (0.799–0.902) exhibited minimum disintegration time and maximum % drug release. Their dissolution data (pH 1.2) were applied to predict the pediatric plasma profile of the active metabolite Tizoxanide by PBPK modeling. The QbD-based approach was successfully applied in designing Nitazoxanide 200 mg orodispersible tablets.

Formulation and evaluation of polyherbal anti-diabetic tablet for oral drug delivery system

The Present Investigation was aimed to develop a Polyherbal tablet formulation for effective treatment of diabetes mellitus. Polyherbal tablets containing various Herbal extracts were prepared using different super disintegrants in varying concentrations to achieve minimum disintegration time. Pre-compression Parameters for all blends were within acceptable range of pharmacopoeial specifications. Formulation F4 showed minimum disintegration time of 14.20 minutes. Hence, it was selected as an optimised formulation and subjected to stability study. Stability study results revealed that, formulation F4 was a stable formulation having better disintegration time and % friability and could be used for effective treatment of diabetes mellitus.

Formulation, Evaluation and Optimization of Sublingual Tablet of Clonidine Hcl

Clonidine hydrochloride (CHL) is a centrally acting alpha two adrenergic agonist. It crosses the blood brain barrier and acts in hypothalamus to induce a decrease in blood pressure. The objective of the present study was to develop and evaluate sublingual tablet of Clonidine Hcl for rapid action and to improve patient compliance to therapy. Wet granulation method was used to prepare sublingual tablet of Clonidine HCL. 32 factorial designs were used to study the effect of binder concentration on dependent variables such as friability disintegration time and wetting time. The prepared formulations were evaluated for various parameters such diameter, thickness, weight variation, hardness, friability, wetting time, drug content, in vitro disintegration time and stability studies Results (Hausner’s ratio 1.24, Carrs index less than 13% and angle of repose 29? ) revealed that all pre compression parameters meet the standard values indicating good flow properties. The average weight, friability and hardness were within compendial limits which showed that all formulations possessed good mechanical strength. The formulation F8 containing 5 % binder and 6 % disintegrant showed minimum disintegration time and wetting time, good friability, drug content and rapid drug release. Prepared sublingual tablets of Clonidine Hcl, were able to provide rapid drug release (94% drug release in 10 minutes) which is a prerequisite for the treatment of hypertension.&#x0D;

Formulation Development and In vitro Evaluation of Memantine Hydrochloride Fast Dissolving Oral Films employing different grades of Hydroxy Propyl Methyl Cellulose

The aim of this present research work is to formulate and evaluate mouth dissoving films using Memantine hydrochloride as a model drug which is used for facilitating rapid onset of action in Alzheimer’s patients who are mentally ill. The films were designed to dissolve upon contact with a wet surface, such as tongue, within a few seconds especially for these patients who are unable to swallow. In this present research work various trials were carried out using different grades of HPMC E3, E5 and E15 by solvent casting method. The prepared films were eva1uated for morphological properties, weight variation, drug content uniformity, thickness uniformity, folding endurance, surface pH, In-vitro disintegration time,In-vitro dissolution studies and stability studies of the satisfactory formulation. Films prepared using HPMC E5 and E15 showed better morphohogical properties when compred with grade E3. Best formulations F4 and F8 prepared using HPMC E5 and E15 respectively with polymer concentration 45% showed minimum disintegration time and maximum dissolution rate. A slight increase in drug dissolution rate with F8 was observed but there is no significant difference between these two formulations was identified. These findings suggest that the fast dissolving film containing Memantine is considered to be potentially useful for the treatment of Alzheimer’s where geriatric patients feel difficulty to swallow a dosage form.

Quality by Design Approach for Design, Development and Optimization of Orally Disintegrating Tablets of Montelukast Sodium

Background: The goal of this research was to use the Quality by Design (QbD) approach to develop orally disintegrating tablets of Montelukast sodium, a leukotriene receptor antagonist used to treat asthma. Characterizing the reference product, defining the quality target product profile (QTPP), identifying critical quality attributes (CQAs), and performing initial testing are all parts of the QbD approach and relating the critical material attributes (CMAs) and critical process parameter (CPP) to drug product CQAs, as a result to develop the design space and defining control strategy. Method: Montelukast sodium tablets were designed using direct compression technique. Formulation were designed by using (DOE software v 13.2) 23 full factorial design in which three variables namely croscarmellose sodium (CCS), microcrystalline cellulose (MCC) and magnesium stearate were varied at two levels by considering one center point. Results: The disintegration time and in vitro dissolution were considered as responses and the prepared tablets have been evaluated for various quality control tests. Formulation F5 was considered as optimized as it showed minimum disintegration time and maximum drug release profile. Conclusion: The CMAs classified as high or medium risk in the initial risk assessment were mitigated to low risk based on the experimentation. Finally, a control strategy was defined giving better control over drug product development.

Formulation and Evaluation of Salbutamol Sulphate Taste Masked Oral Disintegrating Tablets

Salbutamol is a short acting, selective beta2-adrenergic receptor agonist used in the treatment of astama and COPD. The aim of this study is to formulate oral disintegrating tablets of salbutamol sulphate to achieve rapid dissolution, absorption and further improving the bioavailability of the drug. Oral disintegrating tablets of salbutamol sulphate were designed with a view to enhance the patient compliance and provide a quick onset of action. The oral disintegrating tablets were prepared by using different synthetic polymers by direct compression method. Development of the formulation in the present study was based on the concentration of superdisintegrants and the properties of the drug. Nine batches of tablets were formulated and evaluated for various parameters: drug content, weight variation, water absorption ratio, wetting time, in vitro disintegration, hardness, friability, thickness uniformity, and in vitro dissolution. A fourier-transform infrared spectroscopy (FTIR) study showed that there were no significant interactions between the drug and the excipients. The prepared tablets were good in appearance and showed acceptable results for hardness and friability. The in vitro disintegrating time of the formulated tablets was found to be 14.39-32.41 sec and the drug content of tablets in all formulations was found to be between 87.48-99.96 %, which complied within the limits established in the Indian pharmacopeia. The study concluded that taste of the drug was masked with the help of sodium saccarhin, flavor and the concentration of super disintegrating agent increases the disintegration time of tablets get decreases. The formulation (F9) had a minimum disintegration time of 14.39 sec and 99.96 % of the drug was released within 20 min.

FABRICATION OF MICROEMULSION LOADED SUBLINGUAL FILM FOR RAPID ABSORPTION OF FENTANYL CITRATE IN TRANSIENT BREAKTHROUGH PAIN

Objective: The present research work aims to develop a microemulsion loaded sublingual film for rapid absorption of fentanyl citrate in transient breakthrough pain.&#x0D; Methods: The Fentanyl citrate microemulsion loaded sublingual film was prepared using Capmul MCM C8 (oil), tween 20 (surfactant) and propylene glycol (co-surfactant) with different grades of film-forming polymer (HPMC) using a film casting machine. The films were evaluated for in vitro disintegration study, tensile strength, folding endurance, content uniformity, drug content, in vitro dissolution, pH, thickness and weight variation, scanning electron microscopy, ex vivo permeation study, droplet size, polydispersity index, zeta potential, % moisture content and stability study were evaluated.&#x0D; Results: The optimized film formulation showed desired mechanical properties (tensile strength of 0.291 kg/cm2) and a minimum disintegration time of 20 s. The optimized sublingual film formulation exhibited 43.16 % of FC microemulsion loading. Morphological study showed the absence of drug crystals on the polymeric surface. Permeation studies through goat sublingual mucosa indicated 89% fentanyl citrate release through fentanyl citrate microemulsion loaded sublingual film, whereas only 40% fentanyl citrate release was obtained when it was directly added to film without microemulsion strategy.&#x0D; Conclusion: The present study indicated that extend of permeation of fentanyl citrate when added to the sublingual film in microemulsion form was around 2.225 folds higher than when added directly to film without microemulsion. The present microemulsion embedded film technology could be a promising alternative to conventional drug delivery systems and traditional routes of administration for breakthrough pain management.

Formulation and evaluation of orally disintegrating tablet containing taste masked mirtazapine

Objective: This study aims to prepare the taste-masked granules of Mirtazapine by mass extrusion technique and formulate it into an oral dispersible tablet using different super disintegrates. Methods: Taste masked granules of mirtazapine were prepared by mass extrusion technique using Eudragit EPO in different ratios. The drug-polymer ratio was optimized based on the percent drug release in SSF and SGF. Taste masking efficacy of drug-polymer complex was determined by developing the bitterness threshold value of Mirtazapine. The selected drug-polymer complex was formulated into an oro-dispersible tablet by direct compression method. A randomized design was used to investigate individual effect of three different super disintegrates each in different concentrations. Ten formulations were developed including a controlled formulation without the addition of superdisintegrants. A comparative study was done based on various pre-compression and post-compression parameters. Results: Eudragit EPO was able to mask the bitter taste of Mirtazapine effectively in 1:2 ratio by mass extrusion method. The minimum disintegration time and wetting time was found to be 13.6±2.7 and 18.13±0.24 seconds with the formulation containing crospovidone 5% (F9). It was found that the wetting time and disintegration time followed the order SSG&gt;CCS&gt;CPV. The selected best formulation was subjected to an incompatibility study design. The IR spectrum showed that all the excipients were chemically compatible. Conclusion: Thus, in this study unpalatable taste of Mirtazapine was masked using Eudragit EPO polymer by mass extrusion technique, and superdisintegrants were added to prepare orally disintegrating tablets of Mirtazapine. This research work suggests a rapid, simple and cost effective method for formulating Mirtazapine ODT.

FABRICATION OF AN ABUSE DETERRENT AND MICROEMULSION-BASED SUBLINGUAL FILM OF BUPRENORPHINE HYDROCHLORIDE FOR BREAKTHROUGH PAIN MANAGEMENT

Objective: The present research work aims to develop an abuse deterrent rapidly dissolving buprenorphine microemulsion loaded sublingual film for the treatment of breakthrough pain.&#x0D; Methods: The Buprenorphine microemulsion loaded sublingual films were prepared using Capmul MCM C8 (oil), tween 20 (surfactant) and propylene glycol (co-surfactant) with different grades of film-forming polymer (HPMC) using film casting machine. The films were evaluated for in vitro disintegration and dissolution study, tensile strength, folding endurance, content uniformity, surface pH, thickness and weight variation, % loading of buprenorphine microemulsion in sublingual film, scanning electron microscope, ex vivo permeation study, droplet size and polydispersity index, Zeta potential, % moisture content, stability and abuse deterrent potential were evaluated.&#x0D; Results: The optimized film formulation showed desired mechanical properties with minimum disintegration time of 21s and exhibited 34.45 % loading of Buprenorphine microemulsion. Permeation studies through goat sublingual mucosa, indicated 87% Buprenorphine release, through Buprenorphine microemulsion loaded sublingual film, whereas only 30% Buprenorphine release when it was directly added to film without microemulsion strategy.&#x0D; Conclusion: The present study concludes that abuse deterrent and fast acting buprenorphine microemulsion-incorporated sublingual film of buprenorphine HCL and naloxone HCL is a promising alternative to mostly marketed buprenorphine injectable delivery systems and a non-invasive route of administration for breakthrough pain management.

Formulation And Evaluation of Fast Dissolving Oral Films Incorporated With Ramipril and β-Cyclodextrin Complex

Ramipril being ACE inhibitor belongs to BCS class II drug with low solubility and undergoes first-pass metabolism that leads to reduced bioavailability of 28%. The current research is aimed at formulating and evaluating ramipril fast dissolving oral films (FDOF). Solubility enhancement of ramipril was done by formation of inclusion complex with β-cyclodextrin in 3 ratios (1:0.5, 1:1, 1:2). Based on higher drug content and dissolution values the physical mixture of ramipril with β-cyclodextrin in 1:1 ratio (IC2) was chosen for further studies. Total 12 formulations of ramipril FDOF containing IC2 prepared with various polymers and evaluated for physicochemical properties. The optimized formulation F9 shown better tensile strength (11.6 g/cm2), significant % elongation (9.8) and maximum % drug content of 99.98 %. The formulation F9 exhibited minimum disintegration time of 9 sec that is desirable for immediate onset of action and maximum drug release. The FTIR data of F9 assured the compatibility of drug and formulation excipients, found to be stable for 180 days at accelerated conditions. The study confirmed that ramipril FDOF lead to quicker onset of action and enhanced therapeutic efficiency in comparison to marketed product.

Investigating the Potential of Transmucosal Delivery of Febuxostat from Oral Lyophilized Tablets Loaded with a Self-Nanoemulsifying Delivery System.

Gout is the most familiar inflammatory arthritis condition caused by the elevation of uric acid in the bloodstream. Febuxostat (FBX) is the latest drug approved by the United States Food and Drug Administration (US FDA) for the treatment of gout and hyperuricemia. FBX is characterized by low solubility resulting in poor gastrointestinal bioavailability. This study aimed at improving the oral bioavailability of FBX by its incorporation into self-nanoemulsifying delivery systems (SNEDS) with minimum globule size and maximum stability index. The SNEDS-incorporated FBX was loaded into a carrier substrate with a large surface area and lyophilized with other excipients to produce a fluffy, porous-like structure tablet for the transmucosal delivery of FBX. The solubility of FBX was studied in various oils, surfactants, and cosurfactants. Extreme vertices design was utilized to optimize FBX-SNEDS, and subsequently loaded into lyophilized tablets along with suitable excipients. The percentages of the main tablet excipients were optimized using a Box–Behnken design to develop self-nanoemulsifying lyophilized tablets (SNELTs) with minimum disintegration time and maximum drug release. The pharmacokinetics parameters of the optimized FBX-SNELTs were tested in healthy human volunteers in comparison with the marketed FBX tablets. The results revealed that the optimized FBX-SNELTs increased the maximum plasma concentration (Cmax) and decreased the time to reach Cmax (Tmax) with a large area under the curve (AUC) as a result of the enhanced relative oral bioavailability of 146.4%. The significant enhancement of FBX bioavailability is expected to lead to reduced side effects and frequency of administration during the treatment of gout.

FORMULATION AND EVALUATION OF FAST DISSOLVING TABLET OF APREPITANT BY USING NATURAL AND SYNTHETIC SUPERDISINTEGRANTS

Objective: The present study was aimed to formulate fast dissolving tablets (FDTs) of Aprepitant (APT) using natural and synthetic superdisintegrants with the desired onset of action, increased bioavailability by reducing the frequency of dosage and also reduce the first-pass metabolism of the drug.&#x0D; Methods: In this research, the gum isolated from cordia dichotoma was investigated as super disintegrants in fast dissolving tablets (FDTs). The aprepitant tablets were prepared separately using cordia dichotoma (natural), sodium starch glycolate and croscarmellose sodium (synthetic) as superdisintegrants by direct compression method. The tablets were evaluated for various precompression and post-compression parameters.&#x0D; Results: The optimized formulation (APT F3) of cordia dichotoma (8%) showed satisfactory physicochemical properties, minimum disintegration time (34 seconds) and highest dissolution rate (86.52%) in 10 min than the other synthetic superdisintegrants. Also, the pharmacokinetic study of the optimized formulation showed effective results as compared with marketed product of aprepitant.&#x0D; Conclusion: The developed formulation can improve the onset of action as well as improve patient compliance.

Systematic Scrutinisation of Vital Factors for Fabrication and Evaluation of PGS-MCC Based Drug Loaded Pellets by Extrusion Spheronization Technique

Objective: The prime objective was to formulate pellet formulation incorporating a newer extrusion- pelletisation aid, Pregelatinised Starch (PGS) and to scrutinise the factors that can affect the quality of the pellets and to overcome the slower disintegration of Microcrystaline Cellulose (MCC). Methods: Pellets were prepared initially using PGS, MCC, water, ethanol, HPMC K 4 M and Febuxostat was employed as model drug. Optimisation of formulation was done by employing Quality by design (QbD) and Design of experiment (DoE) approach. Ratio of PGS and MCC, ratio of binder and spheronisation speed were selected as independent variables and disintegration time and % cumulative drug release as dependent variables. In vitro in vivo correlation of the optimised batch was carried out using Wagner nelson method. Incompatibility studies have indicated compatibility of drug and excipients. Results: From the experiments, it was proved that the batch comprising 3:1 ratio of PGS and MCC, 1:1 binder solution and 1500 speed yielded good pellets with decreased disintegration time and improved dissolution rate as compared to pure Febuxostat. IVIVC studies indicated one to one correlation between in vitro and in vivo parameters. Conclusion: Pellets with good quality, minimum disintegration time and improved dissolution of model drug were successfully prepared with maximum amount of PGS. Optimisation using QbD approach was worth fruitful that affected the quality of pellets.

Preparation and Evaluation of Palonosetron Hydrochloride Oral Thin Film

The purpose of the current study was to develop a fast dissolving polymeric oral thin film containing palonosetron hydrochloride having good mechanical properties, fast disintegration, dissolution and good drug content uniformity. Solvent casting method was used to prepare the films. Compatibility between drugs and excipients were studied using FTIR and HPLC. Nine different formulations of film from F1 to F9 were prepared using different concentration of polymer A at drug-polymer A ratio (1:26), (1:28), (1:30), (1:32), (1:34), (1:36), (1:38), (1:40), (1:42) and at polymer A-plasticizer B of (65:10), (70:10), (75:10), (40:10), (42.5:10), (45:10), (47.5:10), (50:10), (52.5:10), respectively. The in vitro dissolution study was carried out in phosphate buffer (pH 6.8) at 37±0.5oC and 50 rpm using USP XXIV paddle method. Physicochemical evaluations of all the batches were performed including weight variation, thickness, folding endurance, pH, in vitro disintegration and drug release, FTIR and content uniformity test. Maximum and minimum drug dissolution were found in F6 (108.7%) and in F1 (98.5%), respectively. The maximum and minimum disintegration time were in F9 (43.8 sec) and F1 (25 sec), respectively which demonstrated that disintegration of the film was directly proportional to the polymer A and plasticizer B concentration. It is quite evident from the present research work that the film prepared using polymer A-plasticizer B were smooth, mechanically strong and easy to peel out. Among all the batches, formulation F5 showed best results with respect to disintegration (33 sec), drug dissolution (105%), content uniformity (98.51%) and folding endurance (731). Therefore, it can be said that combination of polymer A and plasticizer B can be prospectively used for the preparation of palonosetron hydrochloride oral thin film. Bangladesh Pharmaceutical Journal 22(2): 228-234, 2019