Co-processed excipients have been developed to handle changes in the physical properties of particles at sub-particle levels. By co-processing two excipients. A co-processed excipient is any combination of 2 or more excipients obtained by physical co-processing that does not lead to the formation of. co-processed excipients ppt. 1. 1; 2. CO-PROCESSED Presented by- Under the guidance ofMr. Bhaskar N. Bangar Dr. N. H. Aloorkar.
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In the present study an attempt has been made to evaluate Ocimum bascilium mucilage coprocessed with Mannitol as a novel super disintegrant. Coprocessed excipients were prepared by solvent evaporation method and evaluated in the formulation of mouth dissolving tablets of Terbutaline sulphate. Formulated mouth dissolving tablets were characterised for physicochemical parameters like hardness, friability, weight variation, disintegration time, drug content and in vitro drug release behaviour.
The outcomes of physicochemical evaluation of formulations showed that all developed formulations had desirable features. The coprocessed mucilage Mannitol: Mucilage exhibited disintegration within 8 sec at the concentration of 1 gm: SSG which disintegrated within 11 sec at the concentration of 1 gm: The developed excipient showed improvement in parent excipient functionalities and proving coprocessed mucilage of Ocimum bascilium to be an excellent novel super disintegrant in mouth dissolving formulation and thus it can coprocessed exploited commercially.
All Published work is licensed under a Creative Commons Attribution 4. Keywords Mouth dissolving tablet; Terbutaline sulphate; Coprocessed excipient; Ocimum bascilium ; Superdisintegrant Introduction Oral solid dosage forms are most commonly preferred dosage form due to its ease of manufacturing, user friendly nature and capital interest also. It is for this reason that most drug delivery systems are currently administered in coprocdssed form of tablets, capsules, powders, granules.
Despite their popularity, an obvious limitation of oral solid dosage form is difficulty of swallowing. The difficulty in swallowing is called as excilients. The European Pharmacopoeia describes ODTs as uncoated tablets intended to be placed in the mouth where they disperse rapidly before being swallowed as suspension and such tablets should disintegrate within 3 min [ 3 ].
FDA defines ODT as a solid dosage form which contains a medicinal substance or active ingredient which disintegrates rapidly within a matter of excipirnts when placed upon a tongue [ 4 ]. After coming in contact with saliva these formulations dissolve immediately and cporocessed a suspension that can be easily swallowed by patient. Numerous and significant changes in tablet manufacturing have occurred including transition from direct compression to wet and dry granulation.
In wet granulation and dry granulation techniques multiple, lengthy and challenging processing steps are involved leading to higher cost and time of tablet production. The direct compression technique involves the compression of a dry blend of powders that comprises drugs and various excipients.
The simplicity and low capital investment of the direct-compression process have positioned it as a preferred alternative. However, the direct compression process is highly influenced by functionality of parent excipients. To overcome these problems, the functionality of excipients can be improved by either developing new grades of excipients or modification of existing excipients.
The development of new grade of excipient is time consuming and lengthy process and requires regulatory approval as well. Developing new grades of existing excipients or combination of existing excipients is successful alternative and that can be achieved by means of coprocessing [ 5 ]. Co processing is a novel concept of processing two or more established excipients by some appropriate means to provide a synergy of functionality improvements as well as masking the undesirable properties of individual excipients.
The functionality of excipients means improvement in flow properties, compressibility, and better dilution potential. These coprocessed excipients interact at sub particle level. Particle level comprises individual particle properties such as shape, size, surface area, and porosity that reflect in bulk level by improving functionality excipients [ 6 ]. The new trend of using plant derived materials has evoked tremendous interest in pharmaceutical industry.
Diversity of their applications such as diluents, binders, disintegrants in tablet make them as alternative to synthetic excipients. Gums and mucilage are most widely used as natural excipients in pharmaceutical manufacturing. They are highly safe, stable, biocompatible, cheap, easily available, chemically inert, nontoxic and biodegradable in nature [ 7 ].
The property of mucilage like high swelling index prompted to explore its applications as disintegrating agent in tablet manufacturing [ 8 ]. The main objective of this work was exciients evaluate novel natural superdisintegrant as coprocessed ready to use excipient for direct compression in the development of mouth dissolving formulation. A comparative study was also made between coprocessed excipient developed from mucilage and coprocessed excipient developed from synthetic material.
Seeds of Ocimum bascilium were purchased from local vendor. Methods Isolation of mucilage from Ocimum bascilium: The seeds were soaked in distilled water for 12 hrs and boiled for 30 min.
The material was squeezed out using muslin cloth to remove the mark from the seeds. Acetone was added to precipitate the mucilage. The powdered mucilage was stored in desiccator until further use. The mucilage was evaluated for flow properties, Swelling index, loss on drying and FTIR coprocessex [ 910 ].
A glass funnel was secured with its tip positioned at a fixed height H above a excipifnts paper placed on a horizontal surface. The sample was poured through the funnel until the apex of the conical pile touched the tip of the funnel. It measures the unsettled apparent volume and the final tapped volume of the powder after tapping the material until no further volume changes copeocessed.
A known volume of powder was placed in a graduated cylinder and consider as initial volume. Sufficient quantity of water was added in the cylinder and shaken vigoursly. It was placed for 24 hrs. Volume occupied by powder after 24 hrs was measured.
It is calculated as Loss on drying: Again weight of powder was measured. It is calculated as: Mucilage and dried KBR were mixed in ratio 1: Then small fraction of mixture was compressed on Automatic IR Press at pressure 10 tones to form transparent pellet.
Preparation of coprocessed superdisintegrant A blend of Mannitol- Mucilage was added to 65 ml of isopropyl alcohol in different concentrations. The contents of the beaker were stirred on a magnetic stirrer [ 11 ]. The wet coherent mass was then granulated through sieve no. It was evaluated for different flow properties and disintegration time.
Placebo tablets were prepared containing coprocessed mucilage as superdisintegrant in different concentration and evaluated for disintegration time. A comparison was made between coprocessed mucilage and coprocessed Sodium Starch Glycolate SSG which was prepared using similar method described above.
Preparation of mouth dissolving tablet The selected concentration of coprocessed mucilage was used in the preparation of mouth dissolving tablet. It was mixed with drug and other tablet excipients and compressed into tablet using flat-faced 6 mm punches on an eight-punch tablet machine Karnavati Rimek. Evaluation of mouth dissolving tablets Developed tablets were evaluated for usual tablet tests such as coproceesed variation, hardness, friability, drug content. The evaluation was carried out as described in the Pharmacopoeia [ 12 ].
Disintegration time and in vitro drug release was done by in house method.
Formulation and Evaluation of Coprocessed Excipient for Mouth Dissolving Formulation
A modified method was used to determine the disintegration time and dissolution profile of the tablets simulating the conditions similar to mouth cavity or oral cavity absorption. For this purpose, a beaker was filled with 10 ml of water. The tablet was put in the beaker and the time for the tablet to completely disintegrate into fine particles was noted. Drug excipients compatibility study The drug-excipients interaction study was carried out using method descried in Cartensen and analysis done using FTIR spectrophotometer [ 13 ].
Stability study The stability studies were carried out for the optimized formulation [ 14 ]. The protocol of stability studies was in compliance with ICH guidelines for stability testing intended for the zone IVa.
After 30 days the samples were withdrawn and characterized for weight variation, hardness, disintegration time, drug content and in vitro drug release study.
Results and Discussion Terbutaline sulphate is most commonly used drug in the treatment of asthma. Mouth dissolving formulation of Terbutaline sulphate would be useful in order to avoid swallowing problem and achieve a rapid onset of action. Requirements for a suitable tableting excipient for direct compression of ODTs are very diverse.
First of all, the excipient should have good flow properties to achieve an acceptable tableting process and second one is to produce ODTs with fast disintegrating property. The flow properties may be improved by the method of coprocessing which minimizes number of excipients and improves its functionality.
The mouth dissolving tablets should disintegrate in less than 30 seconds in a small liquid volume and should have sufficient strength in order to be handled during packaging and transportation [ 4 ]. In the present study, we successfully developed directly compressed tablets with sufficient hardness although exhibiting rapid disintegration.
The natural mucilage has been explored as super disintegrants due to its high swelling property. In addition, Mannitol is non-hygroscopic and may thus be used with moisture-sensitive ingredients. Characterization of mucilage The mucilage which was isolated from the seeds of Ocimum bascilium was evaluated for flow properties, Loss on drying and swelling index.
Results of the evaluation study have been depicted in Table 1. The angle of repose was found to be The results reveal that mucilage exhibited the fair flow properties.
The purpose of the present study was to evaluate novel superdisintegrant. Super disintegrants are generally used for developing mouth dissolving tablets which has the requirement of faster disintegration. One of the mechanisms of super disintegrant is disintegration by swelling and the mucilage showed excellent swelling property that can be used as a super disintegrant in the preparation of mouth dissolving tablet.
It has excellent swelling index that is Direct compression is highly influenced by powder characteristics such as flow ability, compressibility and dilution potential.
A material to be used for direct compression process should possess an adequate level of flow ability when blending with other ingredients in formulation to ensure a uniform die filling of a powder blend during tableting.
Coprocessed excipient having good flow ability is an important requirement for a direct compression excipient. However, the numbers of excipients that can actually fulfill such performance requirements are limited.
Several bulk powder characteristics have been employed for indirect estimation of the degree of powder flow. Table 2 depicts the flow properties before and after coprocessing. It is clear from the evaluation results that coprocessing improved the flow properties. Powder flow depends on 3 general areas: In coprocessing the substance interacted at sub particle level that comprises the particle shape, size that gives improved flow property. The fundamental powder properties such as morphology, particle size, shape, surface area, porosity and density influences excipient functionalities such as flow ability, compactability, dilution potential, disintegration potential and lubricant potential.