eDiplomaMCU: RESEARCH ENVISAGED, PLAN OF WORK, LITERATURE REVIEW : Thiocolchicoside

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Saturday, March 6, 2021

RESEARCH ENVISAGED, PLAN OF WORK, LITERATURE REVIEW : Thiocolchicoside

 

RESEARCH ENVISAGED

Thiocolchicoside is a muscle relaxant with anti-inflammatory and analgesic effects. It acts as a competitive GABAA receptor antagonist and also glycine receptor antagonist with similar potency and nicotinic acetylcholine receptors to a much lesser extent. It has powerful convulsant activity and should not be used in seizure prone individuals.

Thiocolchicoside is having a half-life of 5-6 hrs. The bioavailability of Thiocolchicoside tablets is approximately 25% absorbed with first pass metabolism and the serum concentration touches its peak within 1-2 hrs after oral administration.

Due to inherent draw backs of Thiocolchicoside an alternative drug delivery systems is needed to accomplish maximum therapeutic efficiency add to reduce dose dependent side effects and to develop patient compliance. The physicochemical properties of Thiocolchicoside like smaller dose, partial hydrophilicity, stability at GIT pH, shorter biological half-life, how molecular weight etc, makes it an ideal applicant for administration by oral route.

Hence, the attempt is to formulate sustained drug delivery system in the form of matrix tablets which will overcome inherent conventional drawbacks like poor patient compliance, shorter half-life and poor bioavailability.

Polysaccharides may always be a better alternate for the semi-synthetic polymer being non-toxic, biodegradable, and non-carcinogenic with least regulatory issues. So, the main object of proposed work is to focus on the possibilities of using this polysaccharides as Guar Gum and Okra Gum for the development of extended release drug delivery system of Thiocolchicoside.

In present, work we have tried to explore the matrixing ability of Okra Gum, and Guar Gum polymers for the development of extended release drug delivery system of Thiocolchicoside, which have very little half-life and number of adverse effects are associated with it. So it may be a good applicant for such delivery.


 

PLAN OF WORK

In the current studies it was proposed to design a matrix forming drug delivery for Thiocolchicoside. The plan of work can be outlined as follows:

1.     Literature review of research articles and patents

2.     Procurement of drug

3.     Extraction and isolation of okra gum polysaccharide

4.     Pre-formulation studies and drug analysis

Ø Characterization of drug sample

·        UV Spectroscopic analysis

·        IR Spectroscopy

·        Differential Scanning Calorimetry

Ø Solubility profile

Ø Drug excipient interaction study

5.     Formulation and Optimization of Thiocolchicoside loaded Matrix Tablet

Ø Selection of polymer and its concentration

Ø Selection of channeling agent and its concentration

Ø Comparison of formulation based on guar gum and okra gum

 

6.     Evaluation of matrix tablet

·        Pre-compression parameter

·        Angle of repose

·        Bulk density

·        Tapped density

·        Carr’s index

·        Hausner’s ratio

·        Post compression parameter

·        Hardness test

·        Friability test

·        Uniformity test

·        Drug content uniformity

·        In vitro dissolution test

7.     Data treatment of the result obtained to predict release behaviour

8.     Optimization studies for the concentration of Guar Gum

9.     Optimization studies for the concentration of Okra mucilage

10.                        Evaluation of various batchces sof matrix tablet


 

LITERATURE REVIEW

 

Murakami H et. al. (2000) had reported the long-acting matrix tablets by direct compression of the mixture of drug and poly (DL-lactide-co-glycolide) nanoparticles and to explain the effects of such factors as polymer species, mixing ratio of nanoparticles with different molecular weights, and the tablet weight on the drug release and to discuss the mechanism of drug release from matrix tablets. This structure had advantages in terms of simplicity in design and predictability of drug release rate and may be useful as an implantable dosage form.

 

Nath B. S. et. al (2000) had prepared the in vitro release date showed that 30 percent w/w total matrix component gave extended release of Theophylline for more than 8 hours. Analysis of drug release rate from the matrix system showed that the drug was released by anomalous diffusion obeying first order rate kinetics.

 

Baumgartner S et. al. (2000) had prepared the floating matrix tablets, which are designed to prolong the gastric residence time, increase the drug bioavailability and reduce the side effects of irritating drugs. The drug released from those tablets was sufficiently sustained (more than 8 h) and non-Fickian transport of the drug from tablets was confirmed.

 

AmaralM et. al. (2001) had showed that an increased amount of HPMC or hydrogenated castor oil resulted in reduced drug release, the inclusion of buffers in the HPMC matrix tablets enhanced Naproxen release. The presence of lactose on HPMC tablets did not show different result from that comprising dibasic calcium phosphate as filler. For the tablet of HCO the presence of lactose enhanced the Naproxen release rate.

 

HijareA et. al. (2004) had designed and evaluated sustained release tablets of diltiazem hydrochloride by using guar gum, sodium CMC and HPMC polymer, various physical characteristics drug-polymer interactions in vitro drug release and stability were evaluated.

 

Yunqi W et. al. (2005) had reported a optimized validated simple spectrophotometric method for determination of glucosamine released from sustained release (SR) hydrophilic matrix tablet based on reaction with ninhydrin. Determination of glucosamine release from tablet dosage form was developed based on the diketohydrindamine-diketohydrindylidene color formation. Dissolution studies of sustained release glucosamine formulations caused in reproducible dissolution profiles.

 

Kalu V et. al. (2006) had reported an okra gum was evaluated as a controlled-release agent in modified release matrices in comparison with sodium carboxymethylcellulose (NaCMC) using aspirin as the model drug. Tablets were produced by direct compression and the in vitro drug release was assessed under conditions similar to those in the gastrointestinal system for a period of 6 years. They had concluded that the okra gum is suitable for the sustained release of water soluble drugs.

ShoailM et. al. (2006) had developed a once-daily sustained release matrix table of ibuprofen using hydroxypropyl methylcellulose (HPMC) as release controlling factor and evaluated the drug release parameters as per various release kinetic models. They concluded that the drug release mechanism was found as a complex mixture of diffusion, swelling and erosion.

Corti G et. al. (2007) had reported the sustained release Matrix Tablet of metformin hydrochloride in combination with tri acetyl-cyclodextrin. They concluded that the combination of the drug with a hydrophobic cyclodextrin, such as TABCD, and its dispersion in a suitable polymeric matrix, was effective and adequately modulating the drug release rate.

Barakat N et. al. (2008) had examined the release of carbamazepine from hydrophobic and hydrophilic-hydrophobic matrix combination. Hydrophobic matrix tablets had ready by hot fusion technique, while hydrophilic-hydrophobic matrix tablets had ready by wet granulation technique. They concluded that the both matrix formulation show higher relative bioavailability of CBZ than the reference Tegretol tablet.

Praveen S. H. et. al. (2008) had developed oral controlled release matrix tablet formulations of Isoniazid using Hydroxypropyl methylcellulose (HPMC) as a hydrophilic release retardant and in-vitro release characteristics of the drug. The formulations was settled using wet granulation technology. They concluded the hydrophilic polymer like HPMC could be used as a matrix material to design CR formulations of a water-soluble drug Isoniazid with desired quality and release characteristics. The tablet manufacturing method was relatively simple and can be easily adopted in conventional tablet manufacturing units in industries on a commercial scale. A series of CR formulations of

 

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