Formulation of Oral Mucoadhesive Tablets of Pioglitazone using Natural Gum from Seeds of Pithecellobium Dulce

2015 ◽  
Vol 8 (4) ◽  
pp. 3031-3038
Author(s):  
Sudarshan Singh ◽  
Hitesha Goswami
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
Ex Vivo ◽  
Methyl Cellulose ◽  
Regulatory Issues ◽  
Pharmaceutical Excipients ◽  
Mucoadhesive Polymer ◽  
Release Drug ◽  
Mucoadhesive Tablets ◽  
Model Drug

The plant derived gums and mucilage’s comply with many requirements of pharmaceutical excipients as they are non-toxic, stable, easily available, associated with less regulatory issues as compared to their synthetic counterpart and inexpensive; also these can be easily modified to meet the specific need. The present study was undertaken to isolate mucilage from the seeds of Pithecellobium dulce (P. dulce). The mucilage isolated from P. dulce were used as a bioadhesive polymer in tablet formulation and evaluated for the parameters such as swelling, pH, and bioadhesive property like bioadhesive strength, and ex-vivo residence time. The oral mucoadhesive tablets were prepared using Pioglitazone as model drug and P. dulce seeds mucilage as mucoadhesive polymer. The prepared tablets were evaluated against existing mucoadhesive polymer such as Xanthan gum and Hydroxyl Propyl Methyl Cellulose K4M to explore its use as Pharmaceutical excipients. Swelling index of P. dulce was found to be 87.46 ± 0.11 % which was higher than Xanthan gum but lower than HPMC K4M having swelling index 73.28 ± 0.01 % and 98.88 ± 0.03 % respectively. The results showed that Bioadhesion strength of P. dulce was found to be 50.86 ± 0.03N which was higher than HPMC K4M but lower than Xanthan gum having Force of adhesion 32.81 ± 0.04N and 57.17 ± 0.01N respectively. The percentage cumulative drug release drug release of optimize batch F8 was found to be 101.71 %. So, it was concluded that the mucilage of P. dulce can be used as a pharmaceutical excipient in oral bioadhesive drug delivery systems.

Development and Evaluation of Controlled Release Mucoadhesive Tablets of Captopril

1970 ◽  
Vol 9 (3) ◽  
pp. 3318-3329
Author(s):  
Kranthi Kumar Kotta ◽  
L. Srinivas
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Xanthan Gum ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Content Uniformity ◽  
In Vitro Drug Release ◽  
Mucoadhesive Tablets

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index & desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.

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

2020 ◽  
Vol 16 (1) ◽  
pp. 43-60 ◽  
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.

scholarly journals DESIGN AND EVALUATION OF INTRAGASTRIC BUOYANT TABLETS OF VENLAFAXINE HYDROCHLORIDE

2017 ◽  
Vol 10 (5) ◽  
pp. 166
Author(s):  
Parasuram Rajam Radhika ◽  
Nishala N ◽  
Kiruthika M ◽  
Sree Iswarya S
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Xanthan Gum ◽  
Hydroxypropyl Methylcellulose ◽  
Methyl Cellulose ◽  
In Vitro Drug Release ◽  
Weight Variation ◽  
Floating Drug Delivery ◽  
Venlafaxine Hydrochloride

Objective: The present study was undertaken to prolong the release of orally administered drug. The aim is to formulate, develop, and evaluate theintragastric buoyant tablets of venlafaxine hydrochloride, which releases the drug in a sustained manner over a period of 12 hrs. Different formulationswere formulated using the polymers Carbopol 934 P, xanthan gum, hydroxypropyl methylcellulose (HPMC K100M) with varying concentration ofdrug: Polymer ratio of 1:1, 1:1.5, 1:2, in which sodium bicarbonate acts as gas generating agent, and microcrystalline cellulose as a diluent.Methods: The tablets were prepared by direct compression and evaluated for tablet thickness, weight variation, tablet hardness, friability, in vitrobuoyancy test, in vitro drug release and Fourier transform infrared spectroscopy. Formulations were evaluated by floating time, floating lag time and in vitro drug release. Dissolution profiles were subjected for various kinetic treatments to analyze the release pattern of drug.Results: It was found that drug release depends on swelling, erosion, and diffusion, thus following the non-Fickian/anomalous type of diffusion.Formulation F8 was considered as an optimized formulation for gastro retentive floating tablet of venlafaxine hydrochloride. The optimizedformulation showed sustained drug release and remained buoyant on the surface of the medium for more than 12 hrs. As the concentration of HPMCK100M increases in the formulation the drug release rate was found to be decreased. The optimized formulation was subjected for the stability studiesand was found to be stable as no significant change was observed in various evaluated parameters of the formulation.Conclusion: It can be concluded that floating drug delivery system of venlafaxine hydrochloride can be successfully formulated as an approach toincrease gastric residence time, thereby improving its bioavailability.Keywords: Venlafaxine hydrochloride, Intragastric buoyant, Floating drug delivery systems, Hydroxypropyl methyl cellulose K100M, Carbopol 934 P,Xanthan gum.

scholarly journals FORMULATION AND EVALUATION OF FAST DISSOLVING FILMS OF ELETRIPTAN HYDROBROMIDE

2017 ◽  
Vol 9 (2) ◽  
pp. 59
Author(s):  
K. Pallavi ◽  
T. Pallavi
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
Guar Gum ◽  
Methyl Cellulose ◽  
Synthetic Polymers ◽  
Locust Bean Gum ◽  
Solvent Casting ◽  
Casting Method ◽  
Disintegration Time ◽  
Locust Bean

Objective: The main aim of the present research was to develop an oral fast dissolving polymeric film (FDF) with good mechanical properties, faster disintegration and dissolution when placed on the tongue.Methods: Eletriptan hydrobromide is prescribed for the treatment of mild to a moderate migraine. The polymers selected for preparing films were Pullulan, Maltodextrin (MDX), Acacia, Sodium alginate (SA), Locust bean gum (LBG), Guar gum (GG), Xanthan gum (XG), Polyvinyl alcohol (PVA), Polyvinyl pyrrolidine (PVP), Hydroxyl propyl methyl cellulose (HPMC) E5, and HPMC E15. Twelve sets of films FN1–FN12 were prepared by solvent casting method with Pullulan and combination of Acacia, MDX, SA, LBG, GG, XG, PVA, PVP, HPMC E5 and HPMC E15. Five sets of films FS1–FS5 were prepared using synthetic polymers like PVA, PVP, HPMC E5 and HPMC E15.Results: From all the prepared polymer formulations, FN2, FN8, and FS3 were selected based on disintegration time, and drug release and amongst this three FN2 was optimised based on its disintegration time (D. T). The percent drug release of the optimised film was compared with the percent release of the pure drug.Conclusion: The optimised formulation had a D. T of 16 s and a percent drug release of 97.5% in 10 min in pH 6.8 phosphate buffer and 100.6% drug release in 10 min in 0.1N HCl.

scholarly journals Low-Surfactant Microemulsions for Enhanced Topical Delivery of Poorly Soluble Drugs

2011 ◽  
Vol 14 (3) ◽  
pp. 315 ◽  
Author(s):  
Alireza Shalviri ◽  
Avinash C Sharma ◽  
Dipak Patel ◽  
Amyn Sayani
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
Colloidal Silica ◽  
Topical Delivery ◽  
Silica Gels ◽  
Poorly Soluble Drugs ◽  
Release Rates ◽  
Significant Difference ◽  
Poorly Soluble ◽  
Model Drug

Purpose: To develop and characterize low-surfactant microemulsion (ME) gels to enhance topical delivery of poorly soluble drugs. Method: Five low surfactant ME formulations were manufactured following the construction of pseudo-ternary phase diagrams. The MEs were screened for their ability to dissolve a poorly soluble new chemical entity (Model Drug X). Various viscosity imparting agents like Carbopol 934, Colloidal Silica, HPMC K100M, Lubrajel NP, and Xanthan Gum were evaluated for the manufacture of these ME gels. Each ME gel was then further evaluated for physical stability, including assessing rheological profiles. In vitro release profiles were also determined and compared to a conventional ointment. Results: Three of the five low surfactant MEs developed (ME1, ME4 and ME5) were capable of dissolving Model Drug X up to 14 fold higher than the conventional ointment formulation. ME1 and ME4 gels comprising Xanthan gum or Carbopol 934 were physically stable, while ME5 gel was stable only with Colloidal Silica. The ME5 gel with Colloidal Silica showed an irreversible increase in its elastic modulus when exposed to high temperature, indicating that the formulation would be less suitable for commercial use. The Xanthan Gum and Colloidal Silica gels yielded significantly higher release rates (8 - 10 fold) compared to a conventional ointment and formulations containing Carbopol 934. The significant difference in drug release rates between Xanthan Gum and Carbopol 934 indicated that choice of viscosity imparting agent played an important role in governing drug release from ME gels. Conclusion: ME gels were developed with low surfactant concentrations and improved formulation characteristics, which increased the solubility and subsequent release of a poorly soluble drug. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

scholarly journals Evaluation of Drug Release from Carboxymethyl Starch-Xanthan Gum-HPMC Matrix

2021 ◽  
Vol 11 (5) ◽  
pp. 27-32
Author(s):  
Amit Kumar Verma ◽  
Arun Kumar ◽  
Subbiah Ramasamy ◽  
Ajit Kumar Yadav ◽  
Rohit Kumar Bijauliya
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
Corn Starch ◽  
Methyl Cellulose ◽  
Oral Drug ◽  
Research Activity ◽  
Verapamil Hydrochloride ◽  
Carboxymethyl Starch ◽  
Verapamil Hcl ◽  
Regulatory Acceptance

The use of hydrophilic polymers from natural origin. Especially the polysaccharides have been the focus of current research activity in the design of matrix device due to their non toxic, biocompatible, biodegradable nature and broad regulatory acceptance. A large number of polysaccharides such as Carboxymethyl starch, Xanthan gum, Hydroxy propyl methyl cellulose (HPMC), Sodium Alginate etc, have been used as hydrophilic matrices to investigate release behavior of drug. In order to enrich the resources, there is a quest for new polysaccharide owing to their diverse chemical composition and functional groups are amenable to chemical modification and thus tailor made polymeric matrices are obtained which which can be used to modulate oral drug release. The objective of the study is to characterize Verapamil hydrochloride loaded matrix dosage form using hydroxy propyl methyl cellulose (HPMC), xanthan gum, corn starch as rate retarding polymer. Dosage forms were prepared using different polymers along with drug Verapamil hydrochloride. Carboxymethylation was performed. Drug release was evaluated in simulated gastric media. Addition of xanthan gum significantly retarded the burse release of drug. The retardation of drug release was found to be dependent upon the concentration. The formulation composed of HPMC K4M and CS (ARI-ARI3) followed super case transport is swelling controlled, purely relaxation controlled drug delivery. Keywords: Verapamil HCl, Natural gums, xanthan gum, HPMC, sustained release

scholarly journals Ethyl Cellulose and Hydroxypropyl Methyl Cellulose Blended Methotrexate-Loaded Transdermal Patches: In Vitro and Ex Vivo

Polymers ◽  
2021 ◽  
Vol 13 (20) ◽  
pp. 3455
Author(s):  
Muhammad Shahid Latif ◽  
Abul Kalam Azad ◽  
Asif Nawaz ◽  
Sheikh Abdur Rashid ◽  
Md. Habibur Rahman ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Transdermal Patches ◽  
Percent Moisture ◽  
Vitro Release

Transdermal drug delivery systems (TDDSs) have become innovative, fascinating drug delivery methods intended for skin application to achieve systemic effects. TDDSs overcome the drawbacks associated with oral and parenteral routes of drug administration. The current investigation aimed to design, evaluate and optimize methotrexate (MTX)-loaded transdermal-type patches having ethyl cellulose (EC) and hydroxypropyl methyl cellulose (HPMC) at different concentrations for the local management of psoriasis. In vitro release and ex vivo permeation studies were carried out for the formulated patches. Various formulations (F1–F9) were developed using different concentrations of HPMC and EC. The F1 formulation having a 1:1 polymer concentration ratio served as the control formulation. ATR–FTIR analysis was performed to study drug–polymer interactions, and it was found that the drug and polymers were compatible with each other. The formulated patches were further investigated for their physicochemical parameters, in vitro release and ex vivo diffusion characteristics. Different parameters, such as surface pH, physical appearance, thickness, weight uniformity, percent moisture absorption, percent moisture loss, folding endurance, skin irritation, stability and drug content uniformity, were studied. From the hydrophilic mixture, it was observed that viscosity has a direct influence on drug release. Among all formulated patches, the F5 formulation exhibited 82.71% drug release in a sustained-release fashion and followed an anomalous non-Fickian diffusion. The permeation data of the F5 formulation exhibited about a 36.55% cumulative amount of percent drug permeated. The skin showed high retention for the F5 formulation (15.1%). The stability study indicated that all prepared formulations had very good stability for a period of 180 days. Therefore, it was concluded from the present study that methotrexate-loaded transdermal patches with EC and HPMC as polymers at different concentrations suit TDDSs ideally and improve patient compliance for the local management of psoriasis.

DEVELOPMENT AND CHARACTERIZATION OF NOVEL SITE SPECIFIC FLOATING-MUCOADHESIVE TABLETS BEARING 5-FLOUROURACIL FOR STOMACH TARGETING.

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (09) ◽  
pp. 23-30
Author(s):  
P Bhardwaj ◽  
◽  
R Singh ◽  
A Swarup
Keyword(s):  
Drug Release ◽  
Methyl Cellulose ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Wet Granulation ◽  
Prolonged Release ◽  
Mucoadhesive Tablets

Object of present investigation was to develop and characterize such a gastroretentive tablet, which provides the synergism effect of adhesiveness and floating property for prolonged release of 5-flourouracil within the stomach. The floating mucoadhesive tablets were prepared by the wet granulation method using different ratios of hydroxy propyl methyl cellulose (HPMC K4MCR) and Carbopol 934P as polymers. The prepared floating-mucoadhesive tables were characterized for hardness, detachment stress, floating properties, swelling index and surface morphology by SEM. The in vitro drug release and floating behaviour were studied in simulated gastric fluid (SGF) at pH 1.2. Different kinetic models for drug release were as well applied. Formulations of T-9 batch were furthermore subjected to stability and in vivo radiographic studies.

Optimization of Sumatriptan Succinate Transdermal Emulgel For Treatment of Migraine

2019 ◽  
Vol 9 (01) ◽  
pp. 65-75
Author(s):  
Jagdale Swati ◽  
Maganageri Priyanka
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Factorial Design ◽  
Xanthan Gum ◽  
Ex Vivo ◽  
Oral Route ◽  
Gelling Agent ◽  
Diffusion Study ◽  
Sumatriptan Succinate ◽  
Drug Content

Purpose: Sumatriptan succinate is a BCS class III drug. Oral administration of drug suffers from poor bioavailability problem due to pre-systemic metabolism. Bioavailability for oral route is 15%, for nasal route is 17% and for parenteral route is 97%. Substantial proportion of patients suffers from severe nausea or vomiting during their migraine attack, which make oral treatment unsatisfactory. Transdermal delivery will overcome the problems of the drug giving better results to patients suffering from migraine. Methods: Oleic acid, labrafil M 1994 and transcutol P was used as oil, surfactant and cosurfactant respectively. Both the oily and aqueous phases were heated separately. Oily phase were added to the aqueous phase. Mixing of gel and emulsion in ratio of 1:1 gave emulgel. Emulsion was evaluated for globule size, zeta potential, drug content, stability etc. Carbopol 934 and Xanthan gum was used as a gelling agent. Optimization was carried by factorial design. Emulgel was evaluated for physical parameters, viscosity, drug content, bioadhesive strength, spreadability, in-vitro and ex-vivo diffusion study. Results: FE-SEM image shown spherical globules in shape with size 51.40 µm. Zeta potential showed good stability of the emulsion. FTIR and DSC studies revealed that drug and all excipients were compatible. Factorial design gave batch F7 as optimized one. ANOVA results shown that drug release and gel viscosity values are strongly dependent on concentration of carbopol 934 and xanthan gum respectively. Ex-vivo diffusion study for batch F7 through goat skin indicated 88.68±2.52 % drug release. Statistical studies showed that drug release from the optimized formulation (F7) followed First order release kinetics. Conclusion: Sumatriptan succinate emulgel act as depot of drug which releases drug in controlled manner overcoming oral route side effects.

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