scholarly journals Solubility Enhancement of Budesonide and Statistical Optimization of Coating Variables for Targeted Drug Delivery

2014 ◽  
Vol 2014 ◽  
pp. 1-13 ◽  
Author(s):  
Himanshu Bhatt ◽  
Bhargavi Naik ◽  
Abhay Dharamsi
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Statistical Design ◽  
Aqueous Solubility ◽  
Stability Study ◽  
Design Variables ◽  
Accelerated Stability ◽  
Eudragit S100 ◽  
Enteric Polymers

The purpose of the research was to present Budesonide (BUD) as a novel formulation showing improved aqueous solubility, which may decrease variability in Cmax⁡ and Tmax⁡ found in inflammatory bowel disease (IBD) patients, and drug targeting to colon. To improve aqueous solubility, solid dispersion (SD) of the BUD with poloxamer 188 was prepared by melting method. Physical characterization of solid dispersion was performed. The SD was used to prepare tablet equivalent to 9 mg of BUD. The tablet was coated with enteric polymers Eudragit S100 and Eudragit L100 to target colon. The ratio of polymers and percentage coating was optimized using statistical design. Variables studied in design were ratio of enteric polymers and the effect of percentage coating on in vitro drug release. Dissolution at different pH showed that drug release in colon could be modified by optimizing the ratio of polymers and percentage coating. The dissolution data showed that the percentage coating and ratio of polymers are very important to get lag time and optimum formulation. The optimized batch from statistical design was kept under accelerated condition for three months. After accelerated stability study, there was no significant change in the drug release.

scholarly journals Enrichment of aqueous solubility and dissolution profile of mesalamine: In vitro evaluation of solid dispersion

2021 ◽  
Vol 9 (2) ◽  
pp. 127-135
Author(s):  
Anil Raosaheb Pawar ◽  
Pralhad Vitthalrao Mundhe ◽  
Vinayak Kashinath Deshmukh ◽  
Ramdas Bhanudas Pandhare ◽  
Tanaji Dilip Nandgude
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Peg 4000

The aim of the present study was to formulate solid dispersion (SD) of Mesalamine to enrich the aqueous solubility and dissolution rate. Mesalamine is used in the management of acute ulcerative colitis and for the prevention of relapse of active ulcerative colitis. In the present study, Solid dispersion of Mesalamine was prepared by Fusion and Solvent evaporation method with different polymers. SD’s were characterized by % practical yield, drug content, Solubility, FT-IR, PXRD (Powder X- ray diffractometry), SEM (Scanning electron microscopy), in vitro dissolution studies and Stability studies. The percent drug release of prepared solid dispersion of Mesalamine by fusion and solid dispersion method (FM47, FM67, SE47 and SE67) in 1:7 ratio was found 81.36±0.41, 86.29±0.64, 82.45±0.57and 87.25±1.14 respectively. The aqueous solubility and percent drug release of solid dispersion of Mesalamine by both methods was significantly increased. The PXRD demonstrated that there was a significant decrease in crystallinity of pure drug present in the solid dispersions, which resulted in an increased aqueous solubility and dissolution rate of Mesalamine.The significant increase in aqueous solubility and dissolution rate of Mesalamine was observed in solid dispersion as the crystallinity of the drug decreased, absence of aggregation and agglomeration, increased wetability and good dispersibility after addition of PEG 4000 and PEG 6000.

Design, Development and Optimization of Pulsatile Core in Cup Tablets of Naproxen

2017 ◽  
Vol 7 (03) ◽  
Author(s):  
Rutu H. Patel ◽  
ImadHadi Hameed ◽  
Kunal N. Patel ◽  
Madhabhai M. Patel
Keyword(s):  
Drug Release ◽  
Lag Time ◽  
Major Effect ◽  
Stability Study ◽  
Design Development ◽  
In Vitro Drug Release ◽  
Box Behnken Design ◽  
Accelerated Stability ◽  
Excipient Compatibility

The aim of the present study to prepare Pulsatile release tablet of naproxen for the treatment of rheumatoid arthritis. The drug delivery system was designed to deliver the drug at a time when it could be most needful for the patient. Drug excipient compatibility studies were carried out using DSC and found to be compatible with each other. Pulsatile tablet was prepared by direct compression method using different type and amount of superdisintegrants and coating polymers and evaluated for pre and post compression parameters. Box Behnken design was applied to optimize responses. Concentrations of Sodium starch glycolate (SSG) (X1), Ethyl cellulose (EC) (X2), and HPMC K100M (X3) were selected as independent variables while Lag time (Y1) and % drug release at 8 hrs (Y2) were selected as dependent variables. The prepared tablets were evaluated for post compression parameters and results indicated that concentration of SSG has major effect on in vitro drug release while concentration of EC and HPMC K100M has major effect on Lag time. Batch BE13 prepared with SSG 35mg, EC 175mg, and HPMC K100M 75 mg was found to be best batch as it achieves predetermined lag time of 5 hr 02 min and 99.32% of drug release. There was no significant variation in formulation at the end of six month accelerated stability study.

scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF ELEMENTARY OSMOTIC TABLET OF LISINOPRIL DIHYDRATE

2017 ◽  
pp. 20-27
Author(s):  
BHUSHAN A. BHAIRAV ◽  
PRADNYA M. KHANDAGALE ◽  
R. B. SAUDAGAR
Keyword(s):  
Sodium Chloride ◽  
Drug Release ◽  
Release Rate ◽  
Flow Property ◽  
Stability Study ◽  
Formulation Development ◽  
Drug Release Rate ◽  
Accelerated Stability ◽  
Response Percentage

Objective: Lisinopril Dihydrate is one of the antihypertensive drug used to control the high blood pressure. Osmotically Controlled release tablet of Lisinopril Dihydrate was performed for reducing dosing frequency and patient compliance.Methods: Elementary osmotic tablets of Lisinopril Dihydrate were developed using Sodium chloride as a key ingredient which gives osmogent property which provides driving force inside the core tablet and which leads to release of the drug. Microcrystalline cellulose used as a release retardant material in the present work. Different formulations were prepared by varying the concentrations using 32 factorial designs. It was applied to see the effect of variables Sodium chloride (X1) and MCC (X2) on the response percentage drug release as a dependent variable. These formulations were evaluated for, Hardness, Flow property, Thickness, Friability, Drug content and In vitro drug release. Tablets were coated with a semipermeable membrane using 5% w/v cellulose acetate(CA) in acetone and PEG 400(1%) used as Plasticizer. Coated Elementary osmotic tablets were drilled for delivery orifice using a standard micro drill of diameter size 0.8 mm.Results: Drug release rate was increased as the increase in the concentration of sodium chloride and release rate decreased on increasing the concentration of MCC. Drug release rate was directly proportional to delivery orifice size. SEM Study carried out for detection of diameter size of the delivery orifice. The FTIR studies demonstrate that there was no interaction between polymer and drug.Conclusion: The optimized formulation was stable for 3 mo of accelerated stability study

scholarly journals Solubility enhancement of glimperide: Development of solid dispersion by solvent melt method, characterization and dosage form development

2018 ◽  
Author(s):  
Suchitra Kaushik ◽  
Kamla Pathak
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Dosage Form ◽  
Solid Dispersions ◽  
Immediate Release ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Accelerated Stability ◽  
Form Development

The aim of the present work was to develop immediate release dosage form of the solid dispersion of glimperide (GLIM) for potential enhancement in the bioavailability. The solid dispersions of GLIM were prepared with PEG6000, PVP K30 and Poloxamer 188, in 1:1, 1:3 and 1:5 %w/w ratio by using solvent wetting and solvent melt method. The in vitro dissolution parameters (%DE10min, %DE30min, %DE60min, T50% and DP30) were used to select the optimized solid dispersion that was characterized by IR, PXRD, DSC and SEM. The optimized solid dispersion of GLIM (GSDSM3) was used as drug component for immediate release (IR) tablets that were evaluated for physical and pharmacopoeial parameters. The in vitro drug release studies identified G4 as the optimized tablet with a cumulative drug release (CDR) of 99.34% in 30 min in phosphate buffer, pH 7.4. The CDR was higher than the marketed tablet (91.15%, Amaryl®, Sanofiaventis), However, the f1 and f2 were 10.6 and 52 respectively, which confirmed similarity of the dissolution profile(s). Accelerated stability studies confirmed stability up to 6 months at 40°C/75% condition in the HDPE bottle pack.

Enhancement of Dissolution Rate of Quercetin Using Solid Dispersion Approach: In Vitro and In Vivo Evaluation

2020 ◽  
Vol 10 (3) ◽  
pp. 330-349
Author(s):  
Raghvendra Chaubey ◽  
Nimisha Srivastava ◽  
Apoorva Singh
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Dissolution Profile ◽  
In Vivo Evaluation ◽  
Rat Paw Edema ◽  
Anti Inflammatory

Objective: The objective of present study was to enhance the potential activities of Quercetin by improving its solubility and dissolution profiles through solid dispersion approach. Method: A three level full factorial design (32) was adopted to study the possible combinations of polyethylene glycol (PEG) 6000 & pluronic F 127 (PF 127). The solid dispersions were prepared by solvent evaporation method and evaluated for percentage yield, drug content, aqueous solubility and drug release. For in vivo evaluations SD4 was incorporated into Carbopol base gel and subjected to anti-inflammatory activity using carrageenan-induced rat paw edema method. Results: SD4 batch with drug to carrier ratio 1:1 showed release of 82.96 ± 1.76 % in 240 min following Higuchi’s model. It was 5.54 fold increment in solubility as compared to quercetin. SD4 batch was further evaluated by FTIR, DSC, PXRD and SEM. The crystallinity was significantly reduced and drug was homogeneously dispersed in the carrier as shown by the results of DSC, PXRD and SEM. The DPPH scavenging assay showed significance in the IC50 value of SD4 as compared to pure quercetin and ascorbic acid when subjected to one way ANOVA at 0.05 level of significance (P<0.0001). In vivo anti-inflammatory study showed 78.17 ± 0.156 % inhibition of edema by SD4 and 58.64 ± 0.640 % by pure quercetin which is significantly lower (P<0.05). Conclusion: These findings demonstrate that the solid dispersion of quercetin shows increased solubility, dissolution profile, drug release and significant potential in enhancing the antiinflammatory activity of drug.

scholarly journals ALGINATE BASED GASTRO-RETENTIVE RAFT FORMING TABLETS FOR ENHANCED BIOAVAILABILITY OF TINIDAZOLE

2016 ◽  
Vol 9 (1) ◽  
pp. 16
Author(s):  
Sreejan Manna ◽  
Kanchi Jayasri ◽  
Kancherla Radha Annapurna ◽  
Lakshmi Kanta Kanthal
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Hydroxypropyl Methylcellulose ◽  
Aqueous Solubility ◽  
Lag Time ◽  
In Vitro Dissolution ◽  
Major Barrier ◽  
Gastric Residence Time ◽  
Gastro Retentive

Objective: Tinidazole, a nitroimidazole derivative is having low aqueous solubility which is a major barrier for systemic drug absorption. The aim of the present research was to develop gastro retentive raft forming tablets of tinidazole to achieve prolonged gastric residence time and thus higher bioavailability.Methods: Solid dispersion of tinidazole was prepared by kneading method by using methanol and polyvinylpyrrolidone (PVP). Different concentration of sodium alginate and hydroxypropyl methylcellulose (HPMC) was used to formulate a suitable raft forming tablets and then evaluated for drug content, floating lag time, raft strength, raft volume, raft weight, drug release and release kinetics.Results: Fourier transform infra-red (FT-IR) study confirms compatibility between drug and polymer. The floating lag time was found in the range of 40±4 to 60±5 s for all the formulation. Raft strength for all the formulations was within the range from 3.03±0.12 to 5.92±0.06 g. The raft volume for all the formulation was found within the range of 7.37±1.86 to 9.84±2.76 ml. Raft weight was measured after completion of raft formation for each formulation and was found in the range of 5.21±1.17 to 7.88±1.95 g. In vitro dissolution was carried up to 8 h and percentage of drug release was found to vary between 79.71±2.18 to 94.32±1.79 %.Conclusion: It can be concluded that the combination of solid dispersion and raft formation increases the bioavailability of tinidazole in tablet formulation.

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.

scholarly journals EVALUATION OF STABILITY OF ROPINIROLE HYDROCHLORIDE AND PRAMIPEXOLE DIHYDROCHLORIDE MICROSPHERES AT ACCELERATED CONDITION

2018 ◽  
Vol 10 (4) ◽  
pp. 82
Author(s):  
Koyel Kar ◽  
R. N. Pal ◽  
Gouranga Nandi
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Surface Morphology ◽  
Shelf Life ◽  
Stability Study ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Ropinirole Hydrochloride ◽  
Pramipexole Dihydrochloride

Objective: The objective of the present work was to conduct accelerated stability study as per international council for harmonisation (ICH) guidelines and to establish shelf life of controlled release dosage form of ropinirole hydrochloride and pramipexole dihydrochloride microspheres for a period of 6 mo.Methods: Most optimized batch of ropinirole hydrochloride and pramipexole dihydrochloride (F12 and M12 respectively) were selected and subjected to exhaustive stability testing by keeping the sample in stability oven for a period of 3 and 6 mo. Various parameters like surface morphology, particle size, drug content, in vitro drug release and shelf life were evaluated at 3 and 6 mo period. The surface morphology of the formulated microspheres was determined by scanning electron microscopy (SEM). The particle size of the microspheres was estimated by optical microscopy method. The drug content was assayed by the help of ultra-violet spectrophotometer (UV). The in vitro drug release was performed by using Paddle II type dissolution apparatus and the filtrate was analyzed by UV spectrophotometer. The shelf life of the optimized microspheres was calculated by using the rate constant value of the zero-order reaction.Results: A minor change was recorded in average particle size of F12 and M12 microspheres after storage for 6 mo. For F12 and M12, initially the particle size was 130.00 µm and 128.92 µm respectively and after 6 mo it was found to be 130.92 µm and 128.99 µm respectively. There was no change in surface morphology of F12 and M12 microspheres after 6 mo of storage. The shape of microspheres remained spherical and smooth after 6 mo. An insignificant difference of drug content was recorded after 6 mo compared to the freshly prepared formulation. For F12 and M12, 94.50% and 93.77% of the drug was present initially and after 6 mo 94.45% and 93.72% of the drug was recorded. In vitro drug release was recorded after 6 mo for F12 and M12. Initially, 97.99% and 97.69% of the drug was released till 14th hour respectively for F12 and M12. After 6 mo, 98.23% and 97.99% of the drug was released respectively. The percentage residual drug content revealed that the degradation of microspheres was low. Considering the initial percentage residual drug content as 100%, 99.94% of the drug was recorded for both F12 and M12. The shelf life for F12 and M12 was found to be 10 y 52 d and 10 y 70 d respectively which were determined by the zero-order kinetic equation.Conclusion: A more or less similar surface morphology, particle size, drug content and percent of drug release before and after stability study confirmed the stability of F12 and M12 microspheres after storage for 6 mo and prove the efficacy of the microspheres in the site-specific delivery of drugs in Parkinson’s disease.

scholarly journals Design, Development and Evaluation of Instant Release Oral Thin Films of Flunarizine

2021 ◽  
Vol 71 (1) ◽  
Author(s):  
Asfiya Fatima ◽  
Mamatha Tirunagari ◽  
Divya Theja Chilekampalli
Keyword(s):  
Thin Films ◽  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Rapid Onset ◽  
In Vitro Dissolution ◽  
Design Development ◽  
Onset Of Action ◽  
Weight Variation ◽  
Accelerated Stability

The main objective of the present study was to prepare and evaluate the instant release oral thin films of Flunarizine, in order to enhance the bioavailability of the drug and to provide rapid onset of action thereby improving patient compliance. The instant release oral thin films of Flunarizine were prepared by solvent casting method using film forming polymer like Hydroxypropyl Methylcellulose E-15. The film was evaluated for various physicochemical parameters that include thickness, weight variation, folding endurance, tensile strength, drug content and in vitro drug release studies. No differences were observed in in vitro dissolution of drug from the formulated film F1-F9 as the film instantly gets wet by dissolution medium. The drug release for F5 formulations was about 98.1%. The accelerated stability studies for the optimized film formulations F5 were performed that indicates that the formulated instant release oral thin films were unaffected after initial and 3 months storage under accelerated conditions.

scholarly journals ENHANCEMENT OF SOLUBILITY AND OPTIMIZATION OF ORALLY DISINTEGRATING FILMS OF ACYCLOVIR

2018 ◽  
Vol 11 (9) ◽  
pp. 280 ◽  
Author(s):  
Bikash Pandey ◽  
Arshad Bashir Khan
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Antiviral Agent ◽  
Disintegration Time ◽  
Casting Technique ◽  
Accelerated Stability ◽  
Full Factorial

Objective: The objective of this work was to prepare and optimize orally disintegrating films of acyclovir (ACV), which is a known antiviral agent. To enhance the solubility of ACV, solid dispersions of ACV were made.Methods: The films were prepared using a solvent casting technique. Full factorial design was utilized for the optimization of the effect of independent variables such as the amount of hydroxypropyl methylcellulose 5 cps, sodium starch glycolate, and propylene glycol on the disintegration time. Other evaluation tests such as drug release, drug content, thickness, and folding endurance of film were also conducted.Results: Compatibility studies by Fourier transform infrared showed that there was no significant interaction between the drug and excipients used. Disintegration time was found to be 43 s for the optimized batch. The in vitro release profile of formulation response disintegrating time in phosphate buffer pH 6.8 revealed that there was a significant increment in drug release of the optimized batch in comparison to the screening batches. Further, short-term accelerated stability studies carried out for 4 weeks for the optimized formulation which proved that the formulated films were stable at the accelerated conditions of temperature and humidity (40±2°C/75±5% RH).Conclusions: It was concluded that such ACV solid dispersion films could be beneficial in enhancement of dissolution and consequently the oral bioavailability of ACV.

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