Applications of Cellulose and Cellulose Derivatives in Immediate Release Solid Dosage

Background: The better control of the drug release with immediate effect is the major concern to achieve better therapeutic action and patient compliance. The failure of the solid dispersion complex during storage as well as in-vivo is another concern for the oral solid dosage form. Objective: The prime objective of the present study was to optimize the biphasic minitablet incorporating quality by design approach using the combination of waxy erodible and water-impermeable excipients. Exploration of Soluplus as a precipitation inhibitor and Dexolve as a solubility enhancer in oral solid dosage form was the secondary objective. Methods: The drug-Excipient compatibility study was assessed by FTIR. Clozapine was chosen as a model drug that has poor aqueous solubility. The complex was formulated using B-cyclodextrin or HP B-CD or Dexolve by kneading method. The screening of solubility enhancers and their amount were performed based on phase solubility study. The precipitation inhibitor was screened as per the parachute effect study. Immediate release minitablets were formulated using a direct compression method using different disintegrating agents. The IR minitablets were evaluated for different evaluation parameters. The sustained release minitablets was formulated by hot-melt granulation technique incorporating the Precirol ATO 5 as a waxy excipient and ethyl cellulose as water impermeable excipient. The SR minitablet was optimized using a central composite design. The amount of Precirol ATO 5 and ethyl cellulose were chosen as independent variables and % drug release at 1, 6, and 10 h was selected as responses. The designed batches were evaluated for different pre and post compressional parameters. The IR and SR minitablets were filled in a capsule as per dose requirement and evaluated for in-vitro drug release. The in-vivo plasma concentration was predicted using the Back calculation of the Wagner – Nelson approach. Results: Drug – Excipient study revealed that no significant interaction was observed. Dexolve was screened as a solubility enhancer for the improvement of the solubility of clozapine. The Soluplus was chosen as a precipitation inhibitor from the parachute effect study. The immediate-release tablet was formulated using Prosolv EASYtab SP yield less disintegration time with better flowability. The sustained release mini-tablet was formulated using Precirol ATO 5 and ethyl cellulose. Two-dimensional and three-dimensional plots were revealed the significant effect of the amount of Precirol ATO 5 and ethyl cellulose. The overlay plot locates the optimized region. The in-vitro drug release study revealed the desired drug release of the final combined formulation. The in-vivo plasma concentration-time confirms the drug release up to 12h. Conclusion: The biphasic mini-tablets were formulated successfully for better control of drug release leads to high patient compliance. The use of soluplus as a precipitation inhibitor is explored in the oral solid dosage form for a poorly aqueous drug. Prosolv EASYtab SP was incorporated in the formulation as super disintegrant. The amount of Precirol ATO 5 and ethyl cellulose had a significant effect on drug release in sustained-release minitablet. The approach can be useful in the industry.

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An Effective Technology for the Development of Immediate Release Solid Dosage Forms Containing Low-Dose Drug: Fused Deposition Modeling 3D Printing

Pharmaceutical Research ◽

10.1007/s11095-019-2655-y ◽

2019 ◽

Vol 36 (9) ◽

Cited By ~ 13

Author(s):

Hazal Ezgi Gültekin ◽

Serdar Tort ◽

Füsun Acartürk

Keyword(s):

3D Printing ◽

Fused Deposition Modeling ◽

Low Dose ◽

Immediate Release ◽

Dosage Forms ◽

Solid Dosage Forms ◽

Solid Dosage ◽

Fused Deposition ◽

Effective Technology ◽

Deposition Modeling

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A comparative in vitro dissolution study of generic moxifloxacin immediate-release film coated tablets and referent pharmaceutical product

Macedonian Pharmaceutical Bulletin ◽

10.33320/maced.pharm.bull.2018.64.02.003 ◽

2019 ◽

Vol 64 (02) ◽

pp. 27-34

Author(s):

Emilija Janeva ◽

Liljana Anastasova ◽

Irena Slaveska Spirevska ◽

Tatjana Rusevska ◽

Tanja Bakovska Stoimenova ◽

...

Keyword(s):

Immediate Release ◽

Dosage Forms ◽

Pharmaceutical Product ◽

Generic Product ◽

In Vitro Dissolution ◽

Dissolution Behavior ◽

Solid Dosage Forms ◽

Solid Dosage ◽

Similarity Factor

Dissolution testing of generic immediate release solid dosage forms represents a valuable tool to obtain dissolution profiles and to establish the similarity/dissimilarity between tested dosage forms. In this study, the in vitro dissolution profiles of generic immediate-release moxifloxacin (MOX) film coated tablets and a referent pharmaceutical product were compared and evaluated. The dissolution behavior of the generic product was investigated in three different dissolution media (pH=1.2, 4.5 and 6.8). The amount of dissolved MOX was determined using validated UV spectrophotometric method. For comparison of the dissolution behavior, the similarity factor, f2, was used. The dissolution profile of the generic product showed a release of >85 % MOX in the time frame of 30 min, in all the tested dissolution media. The similarity factor, f2, calculated from the comparison of the dissolution profiles of the generic and the referent pharmaceutical product in pH=1.2 dissolution medium was 50, 58, thus the products were established as similar. Based on the results of our study, the dissolution similarity between the generic MOX immediate-release film coated tablet and the referent product could be successfully used as a part of the approach to ensure their in vivo bioequivalence. Keywords: moxifloxacin, immediate-release solid dosage forms, dissolution, in vitro similarity

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FACTORIAL DESIGN USED IN OPTIMIZATION IMMEDIATE RELEASE SOLID DOSAGE RANITIDINE HYDROCHLORIC

Estudos de Biologia ◽

10.7213/reb.v28i62.22714 ◽

2006 ◽

Vol 28 (62) ◽

Author(s):

Antonio Zenon Antunes Teixeira ◽

Garima Saini ◽

Alexander Macgregor

Keyword(s):

Drug Release ◽

Factorial Design ◽

Immediate Release ◽

Drug Dissolution ◽

Drug Release Profile ◽

Solid Dosage ◽

Significant Difference ◽

The Difference ◽

32 Factorial Design ◽

The Times

The aims of this study were to develop a predictive immediate release tablet formulation system for soluble drugs. Ranitidine hydrochloride, silicifiedmicrocrystallinecellulose (SMCC), polyplasdone XL and hydroxyprophylmethylcellulose (HPMC) E6 were evaluated for powder properties. The effects of binder (HPMC E6) and disintegrant (Polyplasdone XL) were investigated. A 32 factorial design was applied to optimize the drug release profile. The amount of binder and disintegrant were selected as independent variables. The times required for 50% (t50) and 80% (t80) drug dissolution and similarity factor (f2) were chosen as dependent variables. The results of factorial design indicated that a high amount of binder and low amount of disintegrate favored the preparation of drug release. The difference (f1) and similarity (f2) factors were used to measure the relative error and the closeness (similarity) between the factorial design batches and brand name drugs. No significant difference was observed between the brand drug and ranitidine batches F1, F2, F5, F6 and F9. Ranitidine batch F2 yielded the highest value of f2(71%)and the lowest of f1(10%). This research indicates that the proper amount of binder and disintegrant can produce drug dissolution profiles comparable to their brands.

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Formulation and Evaluation of Immediate Release Tablet Dosage Form of Linagliptin and Metformin Hydrochloride

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v11i3-s.4831 ◽

2021 ◽

Vol 11 (3-S) ◽

pp. 61-64

Author(s):

Rakesh Kumar Jat ◽

Sukanta Chatterjee

Keyword(s):

Dosage Form ◽

Drug Product ◽

Scale Up ◽

Immediate Release ◽

Fixed Dose ◽

Metformin Hydrochloride ◽

Solid Dosage ◽

Model Drug ◽

The Individual ◽

Tablet Dosage

The aim of the current study work was to formulate and assess a fixed dose mixture tablet of instant release oral solid dosage form comprising two anti-diabetic drugs (linagliptin and metformin hydrochloride) for managing of diabetes mellitus type 2.The innovator drug product (Jentadueto Tablet) was evaluated for the various evaluation parameters, which have been taken into consideration during the drug product development. Pre-formulation evaluation was accomplished to safeguard better parameters of formulated drug product. On the result of pre-formulation evaluation and innovator drug product characterization, the model drug product was recognized in various steps. The established formulation was augmented for different excipients. The instant release film covered tablet of linagliptin and metformin HCl was expressed and augmented at laboratory scale. The individual steps (procedures) were improved for the same and the scale-up contemplation have been engaged into account certify the product performance at pilot plant-up to commercial scale-up. Keywords: anti-diabetic, linagliptin, metformin

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Understanding Direct Powder Extrusion for Fabrication of 3D Printed Personalised Medicines: A Case Study for Nifedipine Minitablets

Pharmaceutics ◽

10.3390/pharmaceutics13101583 ◽

2021 ◽

Vol 13 (10) ◽

pp. 1583

Author(s):

Sergio A. Sánchez-Guirales ◽

Noelia Jurado ◽

Aytug Kara ◽

Aikaterini Lalatsa ◽

Dolores R. Serrano

Keyword(s):

Drug Loading ◽

Methyl Cellulose ◽

Controlled Drug Release ◽

Immediate Release ◽

Magnesium Stearate ◽

Dosage Forms ◽

Single Step ◽

Solid Dosage Forms ◽

Solid Dosage ◽

3D Printed

Fuse deposition modelling (FDM) has emerged as a novel technology for manufacturing 3D printed medicines. However, it is a two-step process requiring the fabrication of filaments using a hot melt extruder with suitable properties prior to printing taking place, which can be a rate-limiting step in its application into clinical practice. Direct powder extrusion can overcome the difficulties encountered with fabrication of pharmaceutical-quality filaments for FDM, allowing the manufacturing, in a single step, of 3D printed solid dosage forms. In this study, we demonstrate the manufacturing of small-weight (<100 mg) solid dosage forms with high drug loading (25%) that can be easily undertaken by healthcare professionals to treat hypertension. 3D printed nifedipine minitablets containing 20 mg were manufactured by direct powder extrusion combining 15% polyethylene glycol 4000 Da, 40% hydroxypropyl cellulose, 19% hydroxy propyl methyl cellulose acetate succinate, and 1% magnesium stearate. The fabricated 3D printed minitablets of small overall weight did not disintegrate during dissolution and allowed for controlled drug release over 24 h, based on erosion. This release profile of the printed minitablets is more suitable for hypertensive patients than immediate-release tablets that can lead to a marked burst effect, triggering hypotension. The small size of the minitablet allows it to fit inside of a 0-size capsule and be combined with other minitablets, of other API, for the treatment of complex diseases requiring polypharmacy within a single dosage form.

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Optimisation of aceclofenac fast dissolving tablets employing starch xanthate using 23 factorial design

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v9i2.2556 ◽

2019 ◽

Vol 9 (2) ◽

pp. 222-230

Author(s):

Rada Santosh Kumar ◽

T. Naga Satya Yagnesh

Keyword(s):

Factorial Design ◽

Immediate Release ◽

Disintegration Time ◽

23 Factorial Design ◽

Solid Dosage ◽

Drug Content ◽

Poorly Soluble ◽

Croscarmellose Sodium ◽

Dissolution Efficiency ◽

Good Flow

The present study involves in the evaluation of starch xanthate as a superdintegrant in the formulation of fast dissolving tablets of poorly soluble drugs employing 23factorial design. By using gelatinization process starch xanthate was synthesized. Then the synthesized starch xanthate was evaluated under physical and micromeritic methods. To develop starch xanthate as a superdisintegrant, fast dissolving tablet of aceclofenac was prepared by direct compression method employing starch xanthate in different proportions in each case employing 23 factorial design. All the prepared fast dissolving tablets were evaluated for drug content, hardness, friability, disintegration time and other dissolution characteristics like PD10, DE5 and K1. The prepared starch xanthate was found to be fine, free flowing slightly crystalline powder. Starch xanthate shown good swelling in water. The swelling index was 50% and all micrometric properties shown good flow and compressibility needed for solid dosage from manufacturing. All the formulated fast dissolving tablets employing starch xanthate were of good quality with regard to drug content, hardness and friability and fulfilled the official (IP/USP) requirements of compressed tablets with regard to the above mentioned physical properties. Starch xanthate was found to be a superdisintegrant which enhanced the dissolution efficiency when combined with croscarmellose sodium, with the aceclofenac and hence it could be utilized in the formulation of fast dissolving tablets to provide immediate release of the contained drug within 10 minutes. Keywords: Fast Dissolving, Superdisintegrant, Starch xanthate, Dissolution efficiency

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PULSATILE DRUG DELIVERY SYSTEM-A TECHNIQUE OF DELIVERING DRUG IN ACCORDANCE WITH BIOLOGICAL CLOCK - A REVIEW

International Journal of Advanced Research ◽

10.21474/ijar01/12813 ◽

2021 ◽

Vol 9 (4) ◽

pp. 101-124

Author(s):

Chiluvuru Vani ◽

◽

K. Srinivas Reddy ◽

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Biological Clock ◽

Biological Rhythms ◽

Immediate Release ◽

Dosage Forms ◽

The Body ◽

Solid Dosage ◽

Pulsatile Drug Delivery

Over last 30 years pulsatile drug delivery system has achieved a lot of importance in drug delivery technology. And the reason why this pulsatile drug delivery is gaining importance is because of its strategy of delivering drug molecule at right place, right time. There are certain diseases which are controlled by biological clock of our body and follow circadian rhythms like congestive heart failure, asthma, rheumatoid arthritis ,osteoarthritis, inflammatory disorders and other hormonal disorders, for this type of diseases conventional solid dosage forms like immediate release tablets or modified dosage forms like sustained, controlled release tablets cant give the required therapeutic response and also for such diseases delivering the drug at right time in right amount is very important. And that task is accomplished by this pulsatile drug delivery system. These pulsatile drug delivery framework is planned by the organic mood i.e., biological rhythms of the body, and medication conveyance is worked with by as per disease cadence. The rule for the utilization of pulsatile drug delivery of the medications is the place where a consistent drug discharge isnt wanted. The principle for the utilization of pulsatile release of the medications is the place where a steady drug discharge isnt wanted, yet drug release must be planned in such a way that, quick medication discharge is accomplished after the lag time. Current review examined the clarifications for improvement of pulsatile drug delivery framework in accordane with body circadian rhythm, kinds of the illness during which pulsatile discharge is required, order, assessments, benefits, impediments.

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