scholarly journals Experimental and Modeling Study of Drug Release from HPMC-Based Erodible Oral Thin Films

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 222 ◽  
Author(s):  
Alessandra Adrover ◽  
Gabriele Varani ◽  
Patrizia Paolicelli ◽  
Stefania Petralito ◽  
Laura Di Muzio ◽  
...  
Keyword(s):  
Thin Films ◽  
Drug Transport ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Franz Cell ◽  
Flow Through ◽  
Dissolution Apparatus ◽  
Model Drug ◽  
Drug Incorporation

In this work hydroxypropyl methylcellulose (HPMC) fast-dissolving thin films for oral administration are investigated. Furosemide (Class IV of the Biopharmaceutical Classification System) has been used as a model drug for in vitro release tests using three different set-ups: the Franz cell, the millifluidic flow-through device, and the paddle type dissolution apparatus (USP II). In order to enable drug incorporation within HPMC films, a multifunctional excipient, hydroxypropyl- β -cyclodextrin (HP- β -CD) has been included in the formulation, and the influence of HP- β -CD on film swelling, erosion, and release properties has been investigated. Mathematical models capable of describing the swelling and release processes from HPMC erodible thin films in different apparatuses have been developed. In particular, we propose a new model for the description of drug transport and release in a Franz cell that accounts for the effect of the unavoidable imperfect mixing of the receptor chamber.

scholarly journals Hybrid Systems Based on Talc and Chitosan for Controlled Drug Release

Materials ◽  
2019 ◽  
Vol 12 (21) ◽  
pp. 3634 ◽  
Author(s):  
Luciano C. B. Lima ◽  
Caio C. Coelho ◽  
Fabrícia C. Silva ◽  
Andréia B. Meneguin ◽  
Hernane S. Barud ◽  
...  
Keyword(s):  
Drug Release ◽  
Sol Gel ◽  
In Vitro Release ◽  
Controlled Drug Release ◽  
Therapeutic Window ◽  
X Ray Diffraction ◽  
Release Capacity ◽  
Model Drug ◽  
Drug Incorporation

Inorganic matrices and biopolymers have been widely used in pharmaceutical fields. They show properties such as biocompatibility, incorporation capacity, and controlled drug release, which can become more attractive if they are combined to form hybrid materials. This work proposes the synthesis of new drug delivery systems (DDS) based on magnesium phyllosilicate (Talc) obtained by the sol–gel route method, the biopolymer chitosan (Ch), and the inorganic-organic hybrid formed between this matrix (Talc + Ch), obtained using glutaraldehyde as a crosslink agent, and to study their incorporation/release capacity of amiloride as a model drug. The systems were characterized by X-ray diffraction (XRD), Therma analysis TG/DTG, and Fourier-transform infrared spectroscopy (FTIR) that supported the DDS’s formation. The hybrid showed a better drug incorporation capacity compared to the precursors, with a loading of 55.74, 49.53, and 4.71 mg g−1 for Talc + Ch, Talc, and Ch, respectively. The release assays were performed on a Hanson Research SR-8 Plus dissolver using apparatus I (basket), set to guarantee the sink conditions. The in vitro release tests showed a prolongation of the release rates of this drug for at least 4 h. This result proposes that the systems implies the slow and gradual release of the active substance, favoring the maintenance of the plasma concentration within a therapeutic window.

Controlled Release of Metformin Hydrochloride I. In vitro Release from Physical Mixture Containing Xanthan Gum as Hydrophilic Rate Retarding Polymer

1970 ◽  
Vol 4 (1) ◽  
Author(s):  
Mashkura Ashrafi ◽  
Jakir Ahmed Chowdhury ◽  
Md Selim Reza
Keyword(s):  
Controlled Release ◽  
Xanthan Gum ◽  
In Vitro Release ◽  
Correlation Coefficients ◽  
High Ratio ◽  
Water Soluble ◽  
Metformin Hydrochloride ◽  
Model Drug ◽  
Very High

Capsules of different formulations were prepared by using a hydrophilic polymer, xanthan gum and a filler Ludipress. Metformin hydrochloride, which is an anti-diabetic agent, was used as a model drug here with the aim to formulate sustained release capsules. In the first 6 formulations, metformin hydrochloride and xanthan gum were used in different ratio. Later, Ludipress was added to the formulations in a percentage of 8% to 41%. The total procedure was carried out by physical mixing of the ingredients and filling in capsule shells of size ‘1’. As metformin hydrochloride is a highly water soluble drug, the dissolution test was done in 250 ml distilled water in a thermal shaker (Memmert) with a shaking speed of 50 rpm at 370C &plusmn 0.50C for 6 hours. After the dissolution, the data were treated with different kinetic models. The results found from the graphs and data show that the formulations follow the Higuchian release pattern as they showed correlation coefficients greater than 0.99 and the sustaining effect of the formulations was very high when the xanthan gum was used in a very high ratio with the drug. It was also investigated that the Ludipress extended the sustaining effect of the formulation to some extent. But after a certain period, Ludipress did not show any significant effect as the pores made by the xanthan gum network were already blocked. It is found here that when the metformin hydrochloride and the xanthan gum ratio was 1:1, showed a high percentage of drug release, i.e. 91.80% of drug was released after 6 hours. But With a xanthan gum and metformin hydrochloride ratio of 6:1, a very slow release of the drug was obtained. Only 66.68% of the drug was released after 6 hours. The percent loading in this case was 14%. Again, when Ludipress was used in high ratio, it was found to retard the release rate more prominently. Key words: Metformin Hydrochloride, Xanthan Gum, Controlled release capsule Dhaka Univ. J. Pharm. Sci. Vol.4(1) 2005 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

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

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.

scholarly journals IN SITU GEL AS PLATFORM FOR KETOCONAZOLE SLOW RELEASE DOSAGE FORM

2018 ◽  
Vol 10 (5) ◽  
pp. 76
Author(s):  
Methaq Hamad Sabar ◽  
Iman Sabah Jaafar ◽  
Masar Basim Mohsin Mohamed
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
High Viscosity ◽  
In Situ Gel ◽  
Alginate Concentration

Objective: The aim of this study was to formulate ketoconazole (keto) as oral floating in situ gel to slow the release of keto in the stomach.Methods: Sodium alginate (Na alginate) was used as a primary polymer in the preparation of the in situ gel and was supported by the following polymers: guar gum (GG), hydroxypropyl methylcellulose (HPMC) K4M, K15M and carbapol 940 as viscosity enhancing agents. As a consequence, and to complete the gelation process of above formulations was by adding the calcium carbonate (CaCO3). The in situ gels were investigated by the following tests: floating lag time, floating duration, viscosity, drug content, in vitro gelling studies and in vitro release study.Results: The study showed that the faster release was obtained with F1 which contained Na alginate alone. Additionally, reduction in Na alginate concentration resulted in significant increase in drug release. It was also noted that the increase in GG (viscosity enhancing polymer) concentration resulted in non-significant decrease in percent drug release and the reduction in CaCO3 concentration led to significant increase in drug release. Moreover, the release of drug was also affected by grade of viscosity enhancing polymer, the faster release was observed with the formula which contained a polymer of low viscosity (HPMC K4M) and an opposite result was with the high viscosity polymer (HPMCK15M).Conclusion: This study showed the formulation of Na alginate with GG and CaCO3, led to gain floating in situ gel and a sustained release of keto. 

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 COMPARATIVE DISSOLUTION STUDIES OF WARFARIN SODIUM TABLETS: INFLUENCE OF AGITATION RATE, DISSOLUTION MEDIUM, AND USP APPARATUS

2021 ◽  
pp. 117-123
Author(s):  
JOSE RAUL MEDINA LOPEZ ◽  
LUIS DANIEL MAZON ROMAN ◽  
JUAN MANUEL CONTRERAS JIMENEZ ◽  
JUAN CARLOS RUIZ-SEGURA
Keyword(s):  
In Vitro Release ◽  
Agitation Rate ◽  
Dissolution Medium ◽  
Dissolution Studies ◽  
Warfarin Sodium ◽  
Flow Through ◽  
Vitro Release ◽  
Comparative Dissolution ◽  
Paddle Apparatus

Objective: The aim of this study was to carry out comparative dissolution studies with warfarin sodium reference tablets under the hydrodynamic environments generated by the USP basket and paddle apparatus and flow-through cell using different agitation rates and dissolution media. Methods: Dissolution profiles were obtained with the USP basket and paddle apparatus at 50, 75, and 100 rpm and 900 ml of water as dissolution medium. After this, dissolution profiles of warfarin sodium were obtained with the USP paddle apparatus and flow-through cell method using 0.1 N hydrochloric acid, acetate buffer pH 4.5, phosphate buffer pH 6.8, and water. Spectrophotometric determination at 308 nm was carried out during 30 min. Dissolution profiles were compared with model-independent and model-dependent approaches. Results: Significant differences were found with mean dissolution time and dissolution efficiency at 50 and 75 rpm (*P<0.05). Makoid-Banakar was the best-fit model used to describe the in vitro release performance of warfarin sodium with 50-100 rpm and the USP basket and paddle apparatuses. Significant differences in all calculated parameters were found (*P<0.05) excepting percent dissolved at 30 min with 0.1 N hydrochloric acid and phosphate buffer pH 6.8. Conclusion: More research is necessary to identify the in vitro release performance of poorly soluble drugs under available USP apparatuses considering factors as agitation rate and kind of dissolution media. The knowledge of the in vitro release performance of reference drug products is important for the design of better generic formulations

FORMULATION DEVELOPMENT AND EVALUATION OF AN IN SITU OPHTHALMIC GELLING SYSTEM OF BRIMONIDINE TARTRATE AND TIMOLOL MALEATE FOR THE TREATMENT OF GLAUCOMA

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (02) ◽  
pp. 76-78
Author(s):  
A Shirodker ◽  
◽  
S. Bhangle ◽  
R. Gude
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Formulation Development ◽  
Timolol Maleate ◽  
Release Studies ◽  
Brimonidine Tartrate ◽  
In Situ Gelling

The present study involved formulation of an in situ gelling system of brimonidine tartrate and timolol maleate for the treatment of glaucoma. Carbopol® 980 NF, xanthum gum and hydroxypropyl methylcellulose K4 M were used as polymers. The prepared in situ gelling systems were evaluated for clarity, appearance, texture analysis, pH, viscosity, rheological properties, in vitro gelation, isotonicity, drug content uniformity, in vitro release studies, microbiological evaluation, ex vivo release studies and stability testing. The results of the attenuated total reflectance spectroscopy and differential scanning calorimetry studies confirmed that there is no incompatibility between the drugs and the excipients. The formulations exhibited pseudoplastic rheology and formulation 3 showed the highest release of both the drugs from the formulation. The stability studies showed that the formulation was stable over the given period of time. Thus, it is evident that the in situ gelling system is a promising drug delivery system for the treatment of glaucoma.

LINAGLIPTIN AND GLICLAZIDE DI-LOADED EXTENDED-RELEASE NANOPARTICLES: FORMULATION AND EVALUATION

2021 ◽  
Vol 74 (9) ◽  
pp. 2315-2322
Author(s):  
Firas Aziz Rahi ◽  
Muath Sheet Mohammed Ameen ◽  
Mohammed Shamil Fayyadh
Keyword(s):  
Particle Size ◽  
Xanthan Gum ◽  
Extended Release ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Hplc Method ◽  
Electronic Microscopy ◽  
Vitro Release

The aim: This work aimed to formulate gliclazide and linagliptin extended-release nanoparticles. Materials and methods: A HPLC method was developed and validated to determine gliclazide and linagliptin at the same time without interference. The nanoparticles were prepared by emulsion solvent evaporation using two polymers, namely hydroxypropyl methylcellulose (HPMC) 4000 cps and xanthan gum. Results: Nanoparticles prepared were characterized for drug contents, production yield and entrapment efficiency, zeta potential, particle size, morphology by transmission electronic microscopy (TEM) and in-vitro release rate. The formulae GLH1, GLX1 and GHX1 showed release of linagliptin more than 75% after 8 hrs. While the only formula among the three (GHX1) showed release of gliclazide more than 80% after 8 h. So, the formula GHX1 showed acceptable release of more than 80% of both gliclazide and linagliptin after 8 h. Conclusions: The formula GHX1 which containing (0.5:1 xanthan gum: drugs) was the best nanoparticles formula which released more than 80% of both drugs after 8 h and could achieve good extended release over 24 h.

A Comparative Study on the Effect of Hydroxypropyl Methylcellulose F4M and Eudragit® E PO on the Physicochemical Properties of Taste-Masking Microparticles

2020 ◽  
Vol 859 ◽  
pp. 15-20
Author(s):  
Kanokporn Burapapadh ◽  
Napat Wattanakhejorn ◽  
Panitsupa Sukpipat ◽  
Sirapa Promchuay ◽  
Thicha Phengpinit ◽  
...  
Keyword(s):  
Bitter Taste ◽  
Diclofenac Sodium ◽  
Hydroxypropyl Methylcellulose ◽  
Taste Masking ◽  
Loading Capacity ◽  
Type Ii ◽  
Ph Responsive ◽  
Dissolution Apparatus ◽  
Model Drug ◽  
Spray Dried

The objective of this study was to investigate the effect of polymers and their content level on the taste-masking efficiency of spray-dried microparticles. Diclofenac sodium (DS) was used as a model drug, owing to its bitter taste. Hydroxypropyl methylcellulose F4M (HPMC F4M) and Eudragit® E PO were involved in the study as a hydrophilic and a pH-responsive polymer, respectively. The taste-masked DS microparticles with the drug:polymer ratios of 1:1, 1:2 and 1:4 were prepared by the spray-drying technique. The collapsed hollow sphere HPMC F4M based-microparticles was observed meanwhile spray-dried Eudragit® E PO based-microparticles were spherical. Loading capacity of both polymer based-microparticles decreased regarding to the increment of drug:polymer ratio. The Eudragit® E PO based-microparticle in the ratio of 1:4 provided the highest loading efficiency as 91.97%. According to the simplified dissolution testing, the taste-masking ability of HPMC F4M and Eudragit® E PO based-microparticles increased upon the increase of drug:polymer ratio. Drug release at the first 5 minutes from dissolution profiles, tested by type II dissolution apparatus, of the Eudragit® E PO based-microparticles was delayed compared to HPMC F4M based-microparticles. Therefore, it could be assumed that Eudragit® E PO was a promising taste-masking polymer for DS with a pleasant taste.

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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