Enteric Dissolution Enhancement of Engineered Gastro Resistant Omeprazole Tablets using Hydroxypropyl Methylcellulose Acetate Succinate

Purposes: Aims of this study are dissolution enhancement of a poorly water-soluble drug by nano-sized solid dispersion and investigation of machenism of drug release from the solid dispersion. A drug for osteoporosis treatment was used as the model drug in the study. Methods: melting method was used to prepare the solid dispersion. Drug dissolution rate was investigated at pH 1.2 and pH 6.8. Drug crystallinity was studied using differential scanning calorimetric and powder X-ray diffraction. In addition, droplet size and contact angle of drug were determined to elucidate mechanism of drug release. Results: Drug dissolution from the solid dispersion was significantly increased at pH 1.2 and pH 6.8 as compared to pure drug. Drug crystallinity was changed to partially amorphous. Also dissolution enhancement of drug was due to the improved wettability. The droplet size of drug was in the scale of nano-size when solid dispersion was dispersed in dissolution media. Conclusions: nano-sized solid dispersion in this research was a successful preparation to enhance bioavailability of a poorly water-soluble drug by mechanisms of crystal changes, particle size reduction and increase of wet property.

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Optimization of hydroxypropyl methylcellulose and sodium carboxymethyl cellulose in buccal film salbutamol sulphate

10.36295/asro.2020.2335 ◽

2020 ◽

Vol 23 (03) ◽

pp. 33-49

Author(s):

Ni’matul Mauludiyah ◽

Devi Ayu Aprillia ◽

Viddy Agustian Rosyidi ◽

Lusia Oktora Ruma Kumala Sari

Keyword(s):

Carboxymethyl Cellulose ◽

Hydroxypropyl Methylcellulose ◽

Sodium Carboxymethyl Cellulose ◽

Salbutamol Sulphate

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Preparation and Evaluation of Gemifloxacin Mesylate Floating Matrix Tablets in Healthy Human Volunteers

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2017.10.1.8 ◽

2017 ◽

Vol 10 (1) ◽

pp. 3623-3630

Author(s):

Bhikshapathi D. V. R. N. ◽

Haarika B ◽

Jyothi Sri S ◽

K Abbulu

Keyword(s):

Drug Release ◽

Sodium Bicarbonate ◽

Polymer Concentration ◽

Hydroxypropyl Methylcellulose ◽

Matrix Tablets ◽

Physical Parameters ◽

Drug Bioavailability ◽

Floating Tablets

The purpose of present investigation was to develop floating matrix tablets of gemifloxacin mesylate, which after oral administration could prolong the gastric residence time, increase the drug bioavailability and diminish the side effects of irritating drugs. Tablets containing drug, various viscosity grades of hydroxypropyl methylcellulose such as HPMC K4M and HPMC K15M as matrix forming agent, Sodium bicarbonate as gas-forming agent and different additives were tested for their usefulness in formulating gastric floating tablets by direct compression method. The physical parameters, in vitro buoyancy, release characteristics and in vivo radiographic study were investigated in this study. The gemifloxacin mesylate floating tablets were prepared using HPMC K4M polymer giving more sustained drug release than the tablet containing HPMC K15M. All these formulations showed floating lag time of 30 to 47 sec and total floating time more than 12 h. The drug release was decreased when polymer concentration increases and gas generating agent decreases. Formulation that contains maximum concen-tration of both HPMC K15M and sodium bicarbonate (F9) showing sufficiently sustained with 99.2% of drug release at 12 h. The drug release from optimized formulation follows Higuchi model that indicates the diffusion controlled release. The best formulation (F9) was selected based on in vitro characteristics and used in vivo radiographic studies by incorporating barium sulphate as a radio-opaque agent and the tablet remained in the stomach for about 6 h.

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Formulation and Evaluation of Nelfinavir Extended Release Trilayer Matrix Tablets by Design of Experiment

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2018.11.5.6 ◽

2018 ◽

Vol 11 (5) ◽

pp. 4259-4268

Author(s):

Nirmala Rangu ◽

Gande Suresh

Keyword(s):

Controlled Release ◽

Drug Release ◽

Hydroxypropyl Methylcellulose ◽

Magnesium Stearate ◽

Zero Order ◽

Matrix Tablets ◽

Drug Dissolution ◽

Crystalline Cellulose ◽

Dissolution Profile ◽

Release Formulation

The present study was aimed to develop once-daily controlled release trilayer matrix tablets of nelfinavir to achieve zero-order drug release for sustained plasma concentration. Nelfinavir trilayer matrix tablets were prepared by direct compression method and consisted of middle active layer with different grades of hydroxypropyl methylcellulose (HPMC), PVP (Polyvinyl Pyrrolidine) K-30 and MCC (Micro Crystalline Cellulose). Barrier layers were prepared with Polyox WSR-303, Xanthan gum, microcrystalline cellulose and magnesium stearate. Based on the evaluation parameters, drug dissolution profile and release drug kinetics DF8 were found to be optimized formulation. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (DF8) was described by the zero-order and best fitted to Higuchi model. FT-IR studies confirmed that there were no chemical interactions between drug and excipients used in the formulation. These results indicate that the approach used could lead to a successful development of a controlled release formulation of nelfinavir in the management of AIDS.

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Novel Herbal Topical Patch Containing Curcumin and Arnica montana for the Treatment of Osteoarthritis

Current Rheumatology Reviews ◽

10.2174/1573397115666190214164407 ◽

2020 ◽

Vol 16 (1) ◽

pp. 43-60 ◽

Cited By ~ 1

Author(s):

Priyanka Kriplani ◽

Kumar Guarve ◽

Uttam Singh Baghel

Keyword(s):

Drug Release ◽

Factorial Design ◽

Analgesic Activity ◽

Ex Vivo ◽

Hydroxypropyl Methylcellulose ◽

Methyl Cellulose ◽

World Population ◽

Jojoba Oil ◽

Arnica Montana ◽

Transdermal Patches

Background: Osteoarthritis (OA) ranks fifth among all forms of disability affecting 10% of the world population. Current treatments available are associated with multiple side effects and do not slow down the progression of the disease. Moreover, no such effective treatment is available to date in various systems of medicine to treat osteoarthritis. Curcumin and Arnica have shown evident clinical advances in the treatment of osteoarthritis. Objective: The aim of the present study was to design, optimize and characterize novel herbal transdermal patches of curcumin and Arnica montana using factorial design. Methods: A multiple factorial design was employed to investigate the effect of hydroxypropyl methyl cellulose, ethyl cellulose and jojoba oil on elongation and drug release. Transdermal patches were evaluated by FTIR, DSC, FESEM, ex vivo drug permeation, anti osteoarthritic activity and analgesic activity. Results: Independent variables exhibited a significant effect on the physicochemical properties of the prepared formulations. The higher values of drug release and elongation were observed with the higher concentration of hydroxypropyl methylcellulose and jojoba oil. Anti osteoarthritic activity was assessed by complete Freund's adjuvant arthritis model; using rats and analgesic activity by Eddy's hot plate method, using mice. Combination patch exhibited good anti osteoarthritic and analgesic activity as compare to individual drug patches. Conclusion: The design results revealed that the combination patch exhibited good physicochemical, anti osteoarthritic and analgesic activity for the treatment of osteoarthritis in animals. More plants and their combinations should be explored to get reliable, safe and effective formulations that can compete with synthetic drugs.

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Development, Evaluation and Optimization of Osmotic Controlled Tablets of Aceclofenac for Rheumatoid Arthritis Management

Drug Delivery Letters ◽

10.2174/2210303109666181203150830 ◽

2019 ◽

Vol 9 (1) ◽

pp. 29-36

Author(s):

Bijaya Ghosh ◽

Niraj Mishra ◽

Preeta Bose ◽

Moumita D. Kirtania

Keyword(s):

Rheumatoid Arthritis ◽

Polyethylene Glycol ◽

Sodium Chloride ◽

Cellulose Acetate ◽

Hydroxypropyl Methylcellulose ◽

Release Profile ◽

Polyethylene Glycol 400 ◽

Permeable Membrane ◽

Cumulative Release ◽

The Core

Objective: Rheumatoid arthritis is a dreaded disease, characterized by pain, inflammation and stiffness of joints, leading to severe immobility problems. The disease shows circadian variation and usually gets aggravated in early morning hours. Aceclofenac, a BCS Class II compound is routinely used in the treatment of pain and inflammation associated with rheumatoid arthritis. The objective of this study was to develop an osmotic delivery system of Aceclofenac that after administration at bedtime would deliver the drug in the morning hours. </P><P> Methods: A series of osmotically controlled systems of aceclofenac was developed by using lactose, sodium chloride and hydroxypropyl methylcellulose K100M as osmogens. Cellulose acetate (2% w/v in acetone) with varying concentrations of polyethylene glycol-400 was used as the coating polymer to create semi permeable membrane and dissolution was carried out in 290 mOsm phosphate buffer. Formulation optimization was done from four considerations: cumulative release at the end of 6 hours (lag time), cumulative release at the end of 7 hours (burst time), steady state release rate and completeness of drug release. </P><P> Results: A formulation having swelling polymer hydroxypropyl methylcellulose in the core and lactose and sodium chloride as osmogens, polyethylene glycol-400 (16.39 %) as pore former, with a coating weight of 5% was a close fit to the target release profile and was chosen as the optimum formulation. Conclusion: Aceclofenac tablets containing lactose, HPMC and sodium chloride in the core, given a coating of cellulose acetate and PEG-400 (5% wt gain), generated a release profile for optimum management of rheumatoid arthritic pain.

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3 (2) Factorial Design Assisted Crushed Puffed Rice-HPMC-Chitosan based Hydrodynamically Balanced System of Metoprolol Succinate

Drug Delivery Letters ◽

10.2174/2210303110999200408122629 ◽

2020 ◽

Vol 10 (3) ◽

pp. 237-249

Author(s):

Shashank Soni ◽

Veerma Ram ◽

Anurag Verma

Keyword(s):

Drug Release ◽

Factorial Design ◽

Hydroxypropyl Methylcellulose ◽

Batch Size ◽

Metoprolol Succinate ◽

Zero Order Kinetics ◽

Two Factors ◽

Puffed Rice ◽

Model Drug

Introduction: Hydrodynamically balanced system (HBS) possesses prolonged and continuous delivery of the drug to the gastrointestinal tract which improves the rate and extent of medications that have a narrow absorption window. The objective of this work was to develop a Hydrodynamically Balanced System (HBS) of Metoprolol Succinate (MS) as a model drug for sustained stomach specific delivery. Materials and Methods: Experimental batches were designed according to 3(2) Taguchi factorial design. A total of 9 batches were prepared for batch size 100 capsules each. Formulations were prepared by physically blending MS with polymers followed by encapsulation into hard gelatin capsule shell of size 0. Polymers used were Low Molecular Weight Chitosan (LMWCH), Crushed Puffed Rice (CPR), and Hydroxypropyl Methylcellulose K15 M (HPMC K15M). Two factors used were buoyancy time (Y1) and time taken for 60% drug release (T60%; Y2). Results: The drug excipient interaction studies were performed by the thermal analysis method which depicts that no drug excipient interaction occurs. In vitro buoyancy studies and drug release studies revealed the efficacy of HBS to remain gastro retentive for a prolonged period and concurrently sustained the release of MS in highly acidic medium. All formulations followed zero-order kinetics. Conclusion: Developed HBS of MS with hydrogel-forming polymers could be an ideal delivery system for sustained stomach specific delivery and would be useful for the cardiac patients where the prolonged therapeutic action is required.

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