scholarly journals “FORMULATION DEVELOPMENT AND EVALUATION OF GASTRORETENTIVE FLOATING FILMS OF LAFUTIDINE”

2019 ◽  
Vol 7 (2) ◽  
Author(s):  
Hir. R. Mehta ◽  
Vijay K. Patel
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Stability Study ◽  
Formulation Development ◽  
Casting Technique ◽  
Drug Content ◽  
Peg 400 ◽  
Weight Variation ◽  
Folding Endurance

The present invention was aimed to formulate and evaluate Lafutidine gastro retentive films. The films were prepared by solvent casting technique using different film forming polymers like HPMC and Ethyl cellulose. PEG 400 used as a plastsizer. The prepared films were evaluated for number of parameters like Physical appearance, Weight variation, Thickness, Folding endurance, Tensile strength, unfolding behavior, floating properties, drug content and In vitro drug release studies. From the trial batches the best release for gastroretentive film was shown by formulation T5 (Ethyl cellulose and PEG 400). Formulation T5 exhibited good appearance, better mechanical strength with acceptable flexibility. Also, formulation T5 was given more than 90 % drug released after 12 hr and 97.56 % Drug content.  For optimization of formulation, 32 factorial design was applied by taking Ethyl cellulose and PEG 400 as an independent variables. Drug release at 8 hour and folding endurance selected as dependent variables. Based on drug release study, L8 batch found most satisfactory in all formulation and the effect of Ethyl cellulose and PEG 400 found significant. L8 batch found stable during stability study. Key words: Lafutidine, Floating Films, Ethyl Cellulose.

scholarly journals DESIGN, DEVELOPMENT AND EVALUATION OF MOUTH DISSOLVING TABLETS OF TOFACITINIB CITRATE

2022 ◽  
pp. 238-245
Author(s):  
MEGHANA RAYKAR ◽  
MALARKODI VELRAJ
Keyword(s):  
Drug Release ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Design Development ◽  
Disintegration Time ◽  
Drug Content ◽  
Weight Variation ◽  
Wetting Time ◽  
Bulk Drug

Objective: This study aims to Formulate Mouth Dissolving Tablets (MDTs) of Tofacitinib Citrate with the increase in bioavailability and patient compliance. Methods: Mouth Dissolving Tablets (MDTs) of Tofacitinib Citrate were developed by full factorial design at 32levelsand prepared by direct compression method using super integrants like sodium starch glycolate, Ludiflash. The tablets were compressed into compacts on a 10 station tablet machine. The bulk drug was characterised by determining, MP, Solubility, pH and FTIR spectra. Results: The weight variation, hardness and diameter, thickness, friability, drug content, wetting time, in vitro disintegration time and in vitro dissolution studies, and stability study, tablet thickness, weight variation and drug content post compression parameters remained consistent and reproducible. All the formulations showed, almost 100 percent of drug release within 75 min. Formulations F1, F2 and F3 were prepared with 5 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F1<F2<F3. Formulations F4, F5 and F6 were prepared with 10 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F4<F5<F6. Formulations F7, F8 and F9 were prepared with 15 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F7<F8<F9. Conclusion: It is concluded that the amount of superdisintegrants decreases disintegration time of tablets, decreases wetting time, increases the cumulative % drug release causes better absorption.

DEVELOPMENT AND CHARACTERIZATION OF NOVEL GASTRORETENTIVE RAFT FORMING FLOATING FILM OF ATENOLOL

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (03) ◽  
pp. 15-23
Author(s):  
N Sharma ◽  
◽  
R. Awasthi
Keyword(s):  
Drug Release ◽  
Polymer Matrix ◽  
Processing Parameters ◽  
Dissolution Profile ◽  
X Ray Diffraction ◽  
Casting Technique ◽  
Floating Raft ◽  
Weight Variation ◽  
Folding Endurance

The aim of present work was to develop a gastroretentive floating raft forming film of atenolol using solvent casting technique. The films were characterized in terms of drug-excipient compatibility by FTIR, drug content, swelling, folding endurance, thermal behaviour by DSC, effect of processing parameters on drug state (amorphous or crystalline) by X-ray diffraction (XRD), and in vitro drug release profiles. The results confirm that there was no interaction between the drug-polymers and fusion of drug crystals within the polymer matrix. Results of XRD indicate partial dissolution of drug within the polymer matrix and suggested it was partly distributed in amorphous form throughout the film. The weight variation, thickness and folding endurance of films were in the range of 2.170 ± 0.05 to 2.444 ± 0.23 gm, 1.120 ± 0.032 to 1.125 ± 0.011 mm and 200 ± 5 to 400 ± 5, respectively. The pH values of the different films were between 6.8 to 7.21. After 24 h, the best selected film shows 75% and 90% of drug release in 0.1 N HCl (pH 1.2) and in phosphate buffer (pH 6.8), respectively. Based on these results it is suggested that the incorporation of drug into the hydrophilic floating film may be an appropriate strategy to improve the dissolution profile and oral bioavailability of the drug.

scholarly journals FORMULATION AND EVALUATION OF CILNIDIPINE MUCOADHESIVE BUCCAL FILM BY SOLVENT CASTING TECHNIQUE FOR THE TREATMENT OF HYPERTENSION

2021 ◽  
pp. 34-43
Author(s):  
SHIFA SHAUKAT HAJU ◽  
SHEELA YADAV
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Calcium Channel ◽  
Content Uniformity ◽  
Solvent Casting ◽  
Casting Technique ◽  
Drug Content ◽  
Buccal Drug Delivery ◽  
Folding Endurance

Objective: Buccal drug delivery is the most suited route for local as well as systemic delivery of drugs. Cilnidipine is an L/N type dihydropyridine 4th generation calcium channel blocker (CCB), which decreases hypertension by blocking the N-type calcium channel to attenuate vascular sympathetic neurotransmission. It has high first-pass metabolism leading to low bioavailability. Hence the present research work was undertaken to formulate mucoadhesive buccal film of Cilnidipine with an objective to enhance therapeutic efficacy, bioavailability and was developed to administer into the unconscious and less-co-operative patients. Methods: Cilnidipine buccal films were prepared by a solvent-casting technique using various concentrations of mucoadhesive-polymers such as Hydroxyl propyl methylcellulose (HPMC) E15 and K4M and ethyl-cellulose as backing-layer, which acts like a patch providing unidirectional drug release. Prepared films were evaluated for their weight variation, thickness, surface-pH, swelling-index, drug content uniformity, in vitro residence time, folding endurance, tensile strength, in vitro release and permeability studies. Results: The infra-red (IR) spectra showed no interaction, and Physico-chemical characteristics were found within the limit. Swelling of the film increases with increasing concentration of polymers and %drug content of all formulations found to be in the range of 92.13%±0.94% to 97.92%±0.35%. The formulation F5, showed a promising tensile strength, folding endurance and in vitro drug release of about 95.18±0.03%, thus can be selected as an optimized formulation of mucoadhesive buccal film. Conclusion: The formulation of Cilnidipine mucoadhesive buccal film was found to be satisfactory and reasonable.

FORMULATION, DEVELOPMENT AND EVALUATION OF HERBAL TRANSDERMAL PATCH FOR FRACTURE HEALING

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (09) ◽  
pp. 60-66
Author(s):  
Aadesh Kumar ◽  
Mahendra Rana ◽  
Madan Bisht ◽  
Amita Rana
Keyword(s):  
Drug Release ◽  
Bone Fracture ◽  
Antibacterial Properties ◽  
Transdermal Patch ◽  
Formulation Development ◽  
Drug Content ◽  
Zero Order Kinetics ◽  
Folding Endurance ◽  
Peristrophe Bicalyculata

Peristrophe bicalyculata posses expectorant, analgesic, anti-inflamatory, antipyretic and antibacterial properties and has been traditionally used for the management of pain, sprain, and bone fracture. In this study we have tried to incorporate bioactive components of P. bicalyculata in transdermal patches which were developed by solvent casting method. Formulated patches were further evaluated for thickness, folding endurance, moisture content and moisture reuptake. Formulations showing good folding endurance were selected for estimation of the drug content and in-vitro drug release. The patches showing drug content more than 90% and drug release 85% were selected and fitted for Zero-order kinetics. This study will help in the development of transdermal patch for the treatment of bone fracture.

scholarly journals Development of Fast Dissolving Oral Films Containing Vitamin B6 for Nausea and Vomiting of Pregnancy (NVP)

2019 ◽  
Vol 9 (3) ◽  
pp. 51-59
Author(s):  
JESINDHA BEYATRICKS ◽  
, Dhananjaya
Keyword(s):  
Drug Release ◽  
Vitamin B6 ◽  
Stability Study ◽  
Infrared Study ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Folding Endurance ◽  
The Fourier Transform ◽  
The Stability

The aim of this study was to formulate and evaluate the oral fast-dissolving film of Vitamin B6 for the effective management of motion sickness and vomiting during pregnancy. Fast-dissolving films were prepared by the solvent-casting method using different polymers, HPMC-15 and Pullulan, along with Propylene glycol as a plasticizer. The Fourier-transform infrared study for the drug-polymer interaction was carried out. Evaluation of physical parameters such as physical appearance, surface texture, uniformity of weight, uniformity of strip thickness, surface pH, folding endurance, uniformity of drug content and percentage of moisture absorption were performed. Kinetic data analysis for the release study and the stability study were also performed. Results of uniformity of weight, thickness, folding endurance, surface pH, percentage drug content, tensile strength and percentage elongation of all the films were found to be satisfactory. The Fourier-transform infrared study indicated that there was no interaction between the drug and the polymers. The in-vitro drug release study showed that a better rate of drug release was achieved by formulations F4 and F8 compared with other formulations. The stability study did not show any significant difference in the external appearance, the drug content and the in-vitro drug release. In conclusion present study suggested that fast dissolving films has a better ability to cross the sublingual barrier at a faster rate, and hence the delivery system was found to be promising as it has the potential of overcoming the drawbacks associated with tablet formulations available in the market presently. Keywords: Fast-dissolving film, Vitamin B6, HPMC-15, Pullulan gum, Mango peel pectin, Crospovidone, solvent casting

scholarly journals Formulation design and characterization of osmotically controlled tablet of Ramipril

2017 ◽  
Vol 4 (1) ◽  
pp. 1 ◽  
Author(s):  
Bhabani Shankar Nayak ◽  
P. Ellaiah ◽  
Suprava Sethy ◽  
Monalisha Nayak ◽  
Subham Sourajit
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Enzyme Inhibitor ◽  
Release Kinetic ◽  
Flow Properties ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Weight Variation ◽  
Ft Ir

Objective: Ramipril is a long-acting angiotensin-converting enzyme inhibitor. The study aimed to design, formulate and evaluate the oral osmotic drug delivery dosage form of an anti-hypertensive drug, ramipril.Methods: The tablet was formulated using ramipril and different polymers like PVP- K30 and Ethyl cellulose. The microcrystalline cellulose (MCC - diluent), Potassium chloride, Mannitol (osmogen) and Magnesium stearate (lubricant) were used in all the formulations. All the tablets were manufactured by wet granulation method followed by film coating. Compatibility of the drug with excipients was determined by FT-IR spectral analysis. The granules were evaluated for bulk density, Carr’s index and Hausner’s ration to determine flow properties. The prepared compressed and coated tablets were evaluated for weight variation, thickness, hardness, friability, and drug content and in vitro drug release and release kinetic studies.Results: The FT-IR study revealed that drug was compatible with excipients.  The flow properties of granules of most formulation were excellent. All osmotic tablet formulations had good tablet physiochemical properties as per Pharmacopeia. The drug content of all tablet batches was satisfactory. The in vitro drug release study revealed that the formulation F7 containing 100 mg of ethyl cellulose release 100% of drug in 24 h with zero order release kinetics.Conclusions: Ramipril osmotic tablet could be used for safe management of hypertension with greater novelty.

scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF pH TRIGGERED IN SITU OPHTHALMIC GEL OF BESIFLOXACIN HYDROCHLORIDE

2018 ◽  
Vol 8 (5) ◽  
pp. 313-321 ◽  
Author(s):  
Vishakha Waghulde ◽  
Ravindranath Saudagar
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Drug Release ◽  
Stability Study ◽  
Gelling Agent ◽  
Formulation Development ◽  
Drug Content ◽  
Wide Range

The aim of the present work was to formulation and evaluation of pH Triggered in-situ Ophthalmic Gel of Besifloxacin Hydrochloride to overcome the drawbacks obtained by conventional eye drop. There are two independent variables were used i.e. Carbopol 934 and HPMC K100. Carbopol 934 were used as gelling agent and HPMC K100 were used as bioadhesive polymer. Besifloxacin Hydrochloride shows activity against a wide range of Gram-positive and negative ocular pathogens: examples are  Corynebacterium pseudodiphtheriticum, Moraxella lacunata, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae and Streptococcus salivarius. The in situ gelling system involves sol-to-gel transition in the cul-de-sac upon instillation to avoid pre corneal elimination. The formulations were prepared by 32 factorial design. The prepared formulations were evaluated for clarity, pH, viscosity, Bioadhesive strength of gel, gel strength gel, Drug Content, In-vitro Drug Release Study, Antibacterial Activity, Isotonicity Evaluation, HET-CAM Test and stability studies. The drug content was in the range of 97-99.57 %. Formulation F5 selected as optimized on the basis of evaluation. It shows highest drug release upto 8hrs. It shows good antibiotic activity against Staphylococcus aureus. The optimized formulation was isotonic with blood cells. It passes sterility test. The optimized formulation passes the ocular irritancy test i.e. HET-CAM Test. The formulation kept for the stability study for 3 months. Short term stability study indicates that room temperature 400±20 was appropriate storage condition for formulations. Keywords: pH Triggered, bioadhesive polymer, Carbopol 934, HPMC K100, HET-CAM Test, Antibacterial Activity.

Formulation and Evaluation of Orally Disintegrating Tablets of Lamotrigine

2015 ◽  
Vol 8 (2) ◽  
pp. 2881-2888
Author(s):  
Sudarshan Singh ◽  
S S Shyale ◽  
P Karade
Keyword(s):  
Drug Release ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Disintegration Time ◽  
Orally Disintegrating Tablet ◽  
Drug Content ◽  
Weight Variation ◽  
Wetting Time ◽  
Croscarmellose Sodium

The aim of this study was to design orally disintegrating tablet (ODT) of Lamotrigine. It is an Antiepileptic drug which is widely used in epilepsy. It is also used in simple and complex partial seizures and secondary generalized tonic-clonic seizures. It is poorly water soluble drug (0.46 mg/ml). Thus, an attempt was made to enhance the water solubility by complexation with β-cyclodextrin (1:1 molar ratios). The orally disintegrating tablet of lamotrigine was prepared by direct compression method using different concentration of superdisintegrants such as Sodium starch glycollate, croscarmellose sodium by sublimating agent such as camphor. The formulations were evaluated for weight variation, hardness, friability, drug content, wetting time, in vitro disintegration time and in vitro dissolution studies. The prepared tablets were characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry. The disintegration time for the complexed tablets prepared by different concentration of superdisintegrants was found to be in range of 32.54 ± 0.50 to 55.12 ± 0.57 sec and wetting time of the formulations was found to be in range of 28.47 ± 0.67 to 52.19 ± 0.72 sec. All the formulation showed almost 100 percent of drug release within 15 min. Among all the formulation F6 and F7 prepared with 18% croscarmellose sodium and camphor shows faster drug release, respectively 10 min, F6 gives good result for disintegration time, drug release, wetting time and friability. Further formulations were subjected to stability testing for 30 days at temperature of 40 ± 5 ºC/75 ± 5 %RH. Tablets showed no appreciable changes with respect to physical appearance, drug content, disintegration time and dissolution profiles. Results were statistically analyzed by one-way ANOVA at a p < 0.05. It was found that, the data at any point of time are significant at p < 0.05.

scholarly journals FORMULATION AND EVALUATION OF CHLOROTHALIDONE LOADED MOUTH DISSOLVING FILM-A BIOAVAILABILITY ENHANCEMENT APPROACH USING MULTILEVEL CATEGORIC DESIGN

2020 ◽  
pp. 34-41
Author(s):  
SHUBHAM BIYANI ◽  
SARANG MALGIRWAR ◽  
RAJESHWAR KSHIRSAGAR ◽  
SAGAR KOTHAWADE
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Aqueous Dispersion ◽  
Onset Of Action ◽  
Polyethylene Glycol 400 ◽  
Bioavailability Enhancement ◽  
Disintegration Time ◽  
Peg 400 ◽  
Folding Endurance

Objective: The intension of the present study includes fabrication and optimization of mouth dissolving film loaded with Chlorothalidone by solvent evaporation techniques using two components and their three levels as multilevel Categoric design. Methods: Major problem associated with the development of film loaded with BCS class II drug is to increase its solubility. Here the Chlorothalidone solubility achieved by co-solvents, such as methanol. After dissolving the drug in co-solvent, this drug solution is poured into an aqueous dispersion of Hydroxypropyl Methylcellulose E5 (HPMC E5) and Polyethylene glycol 400 (PEG 400). The two independent variables selected are factor A (concentration of HPMC E5) and factor B (concentration of PEG 400) was selected on the basis of preliminary trials. The percentage drug release (R1), Disintegration time in sec (R2) and folding endurance (R3) were selected as dependent variables. Here HPMC E5 used as a film former, PEG 400 as plasticizer, mannitol as bulking agent, Sodium starch glycolate as a disintegrating agent, tween 80 as the surfactant, tartaric acid as saliva stimulating agent, sodium saccharin as a sweetener and orange flavour etc. These fabricated films were evaluated for physicochemical properties, disintegration time and In vitro drug release study. Results: The formulation F6 has more favorable responses as per multilevel categoric design is % drug release about 98.95 %, average disintegration time about 24.33 second and folding endurance is 117. Thus formulation F6 was preferred as an optimized formulation. Conclusion: The present formulation delivers medicament accurately with good therapeutic efficiency by oral administration, this mouth dissolving films having a rapid onset of action than conventional tablet formulations.

DESIGN, CHARACTERIZATION AND EVALUATION OF MUCOADHESIVE NASAL IN SITU GELLING FORMULATIONS OF VENLAFAXINE HYDROCHLORIDE FOR BRAIN TARGETTING

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (01) ◽  
pp. 25-31
Author(s):  
M Priyanka ◽  
◽  
F. S. Dasankoppa ◽  
H. N Sholapur ◽  
NGN Swamy ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Linear Regression Analysis ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Drug Content ◽  
Venlafaxine Hydrochloride ◽  
In Situ Gelling

The poor bioavailability and the therapeutic effectiveness exhibited by the anti-depressant venlafaxine hydrochloride on oral administration is overcome by the use of ion-activated gel forming systems that are instilled as drops; these undergo gelation in the nasal cavity. The present study describes the design, characterization and evaluation of mucoadhesive nasal in situ gelling drug delivery of venlafaxine hydrochloride using different polymers like sodium alginate, HPMC and pectin in various concentrations. DSC studies revealed compatibility of the drug and excipients used. The in situ gels were characterized for physicochemical parameters, gelling ability, rheological studies, drug content, drug entrapment efficiency, in vitro mucoadhesive strength, water holding capacity, gel expansion coefficient and in vitro drug release studies. The amount of polymer blends was optimized using 23 full factorial design. The influence of experimental factors on percentage cumulative drug release at the end of 2 and 8 hours were investigated to get optimized formulation. The responses were analyzed using ANOVA and polynomial equation was generated for each response using multiple linear regression analysis. Optimized formulation, F9, containing 1.98% w/V sodium alginate, 0.64% w/V hydroxylpropyl methylcellulose, 0.99% w/V pectin showed percentage cumulative drug release of 19.33 and 80.44 at the end of 2 and 8 hours, respectively, which were close to the predicted values. The optimized formulation was subjected to stability study for three months at 300C /75% RH. The stability study revealed no significant change in pH, drug content and viscosity. Thus, venlafaxine hydrochloride nasal mucoadhesive in situ gel could be successfully formulated to improve bioavailability and to target the brain.

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