scholarly journals DEVELOPMENT OF MUCOADHESIVE TABLET OF PENTOXIFYLLINE USING A NATURAL POLYMER FROM MANILKARA ZAPOTA LINN

Author(s):  
GNANASEKARAN JOHN SELVARAJ ◽  
ARUL BALASUBRAMANIAN ◽  
KOTHAI RAMALINGAM

Objective: The present study was designed to develop a mucoadhesive tablet of pentoxifylline using the mucoadhesive natural polymer from the plant Manilkara zapota Linn. Methods: The tablets were formulated with three different concentrations of the isolated polymer and evaluated for thickness, weight variation, friability, hardness, swelling index, mucoadhesive strength and in vitro drug release. The swelling index was indirectly proportional to the mucoadhesive polymer of Manilkara zapota (MAPMZ) concentration. Results: The tablets formulated with a high concentration of MAPMZ showed good mucoadhesion strength in 5 min contact time. The in vitro drug release studies indicated that the drug release was directly proportional to MAPMZ concentration. The release kinetics indicated that the drug release was followed the zero-order. Conclusion: The MAPMZ showed the controlled release of pentoxifylline for a period of 12 h.

2017 ◽  
Vol 9 (2) ◽  
pp. 1 ◽  
Author(s):  
Ajit Kulkarni ◽  
Trushali Mandhare ◽  
Nagesh Aloorkar

Objective: To explore a novel natural polymer, pullulan for controlling the release of fenoverine from matrix tablets and to elucidate the release kinetics of fenoverine from pullulan and HPMC matrices.Methods: In this study we formulated monolithic matrix tablets containing of fenoverine as controlled-release tablets by direct compression using pullulan, HPMC (Hydroxypropyl methyl cellulose) K4M and HPMC K100M polymers and evaluated for hardness, thickness, friability, weight variation drug content, in vitro drug release characteristics and FTIR (Fourier transform infrared spectroscopy) and DSC (Differential scanning calorimetry) study.Results: All the formulations showed compliance with pharmacopoeial standards. FTIR and DSC study indicated the absence of interaction between fenoverine and excipients. The formulation was optimized on the basis of acceptable tablet properties and in vitro drug release. The results of dissolution studies indicated that the formulation F5 [drug to polymer 1: 0.35] exhibited highest % cumulative drug release of 96.82±0.75 % at the end of 12 h. Optimised batch F5 showed super case II transport mechanism and followed zero order release kinetics. Short-term stability studies of the optimized formulation indicated that there were no significant changes observed in hardness, drug content and in vitro dissolution studies at the end of three months period. Similarity factor f2 was found to be 89, which indicated similar dissolution profiles before and after stability study.Conclusion: Based on above results we conclude that pullulan can be used as a polymer for retarding the release of drug from matrix formulations.Keywords: Pullulan, Fenoverine, Hydroxypropyl methyl cellulose, Controlled release, In vitro


INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (11) ◽  
pp. 17-23
Author(s):  
K Prakash ◽  
◽  
Y Phalguna ◽  
D. H. Narayana

The present study was aimed to develop and evaluate polycaprolactone–chitosan nanospheres of doxorubicin hydrochloride (DXO) in different drug to polymer ratios using double-emulsion solvent evaporation and solvent diffusion methods. FTIR studies showed that there was no chemical interaction between the drug and polymers. Scanning electron microscopy showed the nanospheres having a discrete spherical structure without aggregation. Prepared nanospheres were characterized for particle size, zeta potential, entrapment efficiency and in-vitro drug release kinetics. Nanospheres showed the particle size of 700±105to770±115 nm with an entrapment efficiency of 66.23±0.11% to 93.62±0.17%. The DXO content was found 76±0.12% to 91±0.36% in several batches. In-vitro drug release studies were performed using the dialysis membrane method. All the drug loaded batches were rendered sustained release over a period of 24 h.


Author(s):  
RAWOOF MD ◽  
RAJNARAYANA K ◽  
AJITHA M

Objective: The research is designed at formulating and evaluating pH-sensitive rifaximin colon-targeted tablets for targeted action in proximal colon. Method: The colon-targeted tablets are done by granulation of three levels of polymers such as Eudragit L30D, Carbopol 974P, and ethyl cellulose. The evaluation parameters such as swelling studies, drug dissolution, in vitro drug release studies, stability, and the Fourier transform infrared studies carried out for optimized formulations. Results: Physicochemical parameters of all the 27 formulations (RF1-RF27) evaluated and RF21 is chosen for further investigation based on weight variation, hardness, drug content, and swelling index. The in vitro drug release studies indicate that the optimized formulation RF21 released 98.75% drug within 24 h. The stability studies indicate that the formulation is stable. Conclusion: An effective and stable pH-dependent rifaximin colon-targeted tablet formulated for the targeted treatment of bowel syndrome.


Author(s):  
Saddam C Shaikh ◽  
Dnyaneshwar Sanap ◽  
Dipak V Bhusari ◽  
Shirish Jain ◽  
Pooja P Kochar ◽  
...  

The objective of the present study was to formulate the gastro-retentive floating tablets containing Ibuprofen, which would remain in stomach and/or upper part of GIT for prolonged period of time. Floating systems have low bulk density so that they can float on the gastric juice in the stomach. Ibuprofen is an anti inflammatory drug.  On trial and error basis formulation design was done. Four different batches of floating tablets of Ibuprofen were prepared using HPMC, Xanthan gum, and gas generating agent sodium bicarbonate and citric acid. The tablets were characterized for the pre and post compression parameters such as friability, hardness, thickness, drug content, weight variation, in-vitro buoyancy studies and 13 hrs in-vitro drug release studies and the results were within the limits. From the results obtained, it was concluded that the optimized formulation F4 desired drug release properties and floating behavior.


2020 ◽  
Vol 10 (5) ◽  
pp. 188-197
Author(s):  
Navdeep Singh ◽  
Kamya Goyal ◽  
Shivi Sondhi ◽  
Shammy Jindal

Psoriasis is an inflammatory skin disease which cause inflammation to the skin and generally the symptoms includes white or red colour of irregular skin; the patches are developed and they are commonly itchy and scaly to the skin. Barbaloin is an herbal phytoconstituent which is obtained from the plant aloe vera leaf part. In the present study hydrogels formulation batches from F1 to F10 were prepared by using carbopol 934, Xanthan gum, carbopol 940, and carbopol 71G NF as a gelling agent. The prepared formulations from F1 to F10 were evaluated for their physical appearance, Grittiness, spreadability, Homogeneity, viscosity, pH, swelling index and microscopical evaluation. The changes in each evaluation parameter were examined at multiples concentration of each polymer. The effects of gelling agent in each formulation were observed and it will help us to justify the suitable range of polymer as a single or in combination with other gelling agent. From these studies it was found to be formulation F2, F4, F7 and F10 showing good gelling properties and further these four formulations are selected for In Vitro drug release studies. By In Vitro drug release kinetics study formulation F2 and F10 showed higher release as compared to F4 and F7. Furthermore, formulation F2 and F7 had good kinetic release study and showed non fickian drug release as the n value was between 0.8-0.9. Therefore, from the above release study parameters formulation F2 and F10 show the best optimized release characterstics as compare to the selected optimized formulations F4 and F7. Keywords: Psoriasis, Barbaloin, Hydrogel, Formulation and Evaluation.


Author(s):  
P. V. KAMALA KUMARI ◽  
Y. SRINIVASA RAO

Objective: The present study was aimed to develop the formulation and in vitro evaluation of Orodispersible tablets by wet granulation method using Donepezil HCl as a model drug to enhance patient compliance. Methods: In the wet granulation method, a mixture of microcrystalline cellulose and hydroxypropyl methylcellulose were used along with superdisintegrants, i.e., croscarmellose sodium and crospovidone. The prepared granules were subjected to both pre and post-compression evaluation parameters including; FTIR spectroscopy, micromeritics properties, tablet weight variation, hardness, friability, drug content, disintegration time and in vitro drug release. Results: FTIR studies indicated that there was nointeraction between the drug and the excipients used. The formulation containing high concentration of crospovidone and mixture as the best formulation F2 based on in vitro drug release characteristics of tablet formulation. Conclusion: The results of this work suggested that orodispersible tablets of Donepezil hydrochloride with rapid disintegration time, fast drug release and good hardness can be efficiently and successfully formulated by wet granulation method.


Author(s):  
GNANASEKARAN JOHNSELVARAJ ◽  
ARUL BALASUBRAMANIAN ◽  
KOTHAI RAMALINGAM

Objective: The present study was planned to develop a mucoadhesive tablet formulation of the drug pentoxifylline using natural mucoadhesive polymer from the plant Ocimum basilicum Linn. Methods: The isolated polymer was used to formulate the mucoadhesive tablets with 3 different concentrations. The tablets were formulated by using direct compression technique and evaluated for various parameters such as thickness, friability, weight variation, hardness, mucoadhesive strength, swelling index by standard methods, and the in vitro drug release studies in USP dissolution test apparatus type-II. Results: The swelling index was indirectly proportional to the polymer concentration and the tablets with a high concentration of polymer showed better mucoadhesive strength (28.5532±0.4660). The in vitro drug release showed that the drug release was indirectly proportional to the polymer concentration. The formulation F3 showed the controlled release of drug pentoxifylline (99.84±1.86) for 10 h. The mechanism of drug release was found to be Fickian diffusion and followed the zero-order kinetics, which was proved by its highest linearity (r2) in all the formulations. Conclusion: The tablets formulated with the isolated polymer of Ocimum basilicum Linn showed the good mucoadhesive mucoadhesive property and it controlled the release of the pentoxifylline.


Author(s):  
Neeraj Agrawal ◽  
M.J. Chandrasekar ◽  
U.V. Sara ◽  
Rohini A.

A macromolecular prodrug of didanosine (ddI) for oral administration was synthesized and evaluated for in-vitro drug release profile. Didanosine was first coupled to 2-hydroxy ethyl methacrylate (HEMA) through a succinic spacer to form HEMA-Suc-ddI monomeric conjugate which was subsequently polymerized to yield Poly(HEMA-Suc-ddI) conjugate. The structures of the synthesized compounds were characterized by FT-IR, Mass and 1H-NMR spectroscopy. The prodrug was subjected for in-vitro drug release studies in buffers of pH 1.2 and 7.4 mimicking the upper and lower GIT. The results showed that the drug release from the polymeric backbone takes place in a sustained manner over a period of 24 h and the amount of drug released was comparatively higher at pH 7.4 indicating that the drug release takes place predominantly at the alkaline environment of the lower GIT rather than at the acidic environment of the upper GIT. This pH dependent sustained drug release behavior of the prodrug may be capable of reducing the dose limiting toxicities by maintaining the plasma drug level within the therapeutic range and increasing t1/2 of ddI. Moreover, the bioavailability of the drug should be improved as the prodrug releases ddI predominantly in the alkaline environment which will reduce the degradation of ddI in the stomach acid.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1130
Author(s):  
Mariana Pires Figueiredo ◽  
Ana Borrego-Sánchez ◽  
Fátima García-Villén ◽  
Dalila Miele ◽  
Silvia Rossi ◽  
...  

This work presents the development of multifunctional therapeutic membranes based on a high-performance block copolymer scaffold formed by polyether (PE) and polyamide (PA) units (known as PEBA) and layered double hydroxide (LDH) biomaterials, with the aim to study their uses as wound dressings. Two LDH layer compositions were employed containing Mg2+ or Zn2+, Fe3+ and Al3+ cations, intercalated with chloride anions, abbreviated as Mg-Cl or Zn-Cl, or intercalated with naproxenate (NAP) anions, abbreviated as Mg-NAP or Zn-NAP. Membranes were structurally and physically characterized, and the in vitro drug release kinetics and cytotoxicity assessed. PEBA-loading NaNAP salt particles were also prepared for comparison. Intercalated NAP anions improved LDH–polymer interaction, resulting in membranes with greater mechanical performance compared to the polymer only or to the membranes containing the Cl-LDHs. Drug release (in saline solution) was sustained for at least 8 h for all samples and release kinetics could be modulated: a slower, an intermediate and a faster NAP release were observed from membranes containing Zn-NAP, NaNAP and Mg-NAP particles, respectively. In general, cell viability was higher in the presence of Mg-LDH and the membranes presented improved performance in comparison with the powdered samples. PEBA containing Mg-NAP sample stood out among all membranes in all the evaluated aspects, thus being considered a great candidate for application as multifunctional therapeutic dressings.


Author(s):  
Parasuram Rajam Radhika ◽  
Nishala N ◽  
Kiruthika M ◽  
Sree Iswarya S

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.


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