The oral route remains the most common route for the administration of drugs.
More particularly, the composition for the controlled-release of drugs according to the present invention expands the capacity for the controlled-release of a matrix-type polymer for controlled-release via a carbomer in which said polymer for controlled-release forms a basic frame and in which sol-gel transition occurs in accordance with a pH level.
The composition of the present invention is characterized in that it comprises: The composition for the controlled-release of drugs according to the present invention uses a carbomer which maintains the controlled-release of conventional matrix structures having polymers for controlled-release and which has sol-gel transition properties, thus preventing a sudden release of a drug caused by a collapse of the matrix structure during a late stage of elution.
In addition, the composition of the present invention uses a solubilizing agent to solve the problem of a highly insoluble drug failing to dissolve even after being released, and also uses a disintegrating agent to improve the speed of the initial release, which is the limiting factor in controlled-release preparations.
Description Drugs for controlled release composition The present invention relates to a drug for controlled release composition. Specifically, a drug for controlled release composition of the present invention is a matrix type sustained-release polymer for fulfilling the basic frame, in accordance with the pH the sol-gel transformation occurs carbonyl meoro to expand the emission control ability of the sustained-release polymer for.
The present invention is characterized by containing a solubilizer suitable for the case of poorly soluble drugs is especially subject suffering emission, and an additional disintegrating agent for a sufficient initial release.
Compared to conventional immediate release rapid release in the sustained-release preparation controlled release preparations may be due to the sustained release of drug for a period of time in the body, maintain the effective blood concentration of drug for long periods of time.
Therefore, it is advantageous to reduce the amplitude of the plasma concentration resulting from the frequent administration of a conventional formulation and thereby also can be reduced, by further reducing the frequency of administration improve the medication compliance compliance of the patient side effects.
This has already a number of ways to produce the sustained-release preparation with high effectiveness, and reliability is used, is known as a formulation which may be prepared most conveniently from the the sustained-release matrix tablets.
Sustained-release matrix tablet is generally used in the pharmaceutical industry because they can be produced by conventional manufacturing techniques and equipment, as the base from dissolving slowly out of the gastrointestinal fluids drug depending refers to a form in which dissolution.
However, the extended release matrix formulation is a matrix structure Once the breakdown is the drug is released rapidly, there is a problem that blood levels increased temporarily. In addition, when the drug itself is poorly soluble in suffering even after the collapse of matrix structure, some of the drug can be present in non-dissolved state is not economical.
In addition, there are a low nature of the initial release rate of the matrix structure side, which may rather act as a disadvantage in situations that require rapid expression. The present invention been made in view of the above problems, while prior art have the advantage of a matrix structure it is possible to, even after the collapse of matrix structure inhibiting the rapid release of the drug, sikimyeo completely solubilize the drug of suffering availability, the initial release rate It is to be the object of the present invention to provide a new and improved drugs for controlled release composition.
In another aspect, the present invention is to provide a cilostazol sustained-release tablet that can prevent the adverse effects caused by the sudden release the drug was released by the controlled release composition is appropriately controlled by another object.
In another aspect, the present invention is to provide a sustained-release tablet rebamipide to prevent the side effects of rapid release is properly controlled release by the drug release-controlling composition as another object. In another aspect, the present invention is to provide a sustained-release tablet ARI piperacillin sol to prevent the side effects of rapid release is properly controlled release by the drug release-controlling composition as another object.
Drugs for controlled release composition of the present invention to achieve the object as described above, parts by weight of the sustained-release polymer for, Carbomer Carbomer 5 to parts by weight, Solubilizing agents from 10 to parts by weight, and Disintegrating agents 30 to 70 parts by weight In that it comprises the features.
Further, the viscosity of the above-mentioned sustained release polymers may be from 50, tocps, preferably 80, tocps. In addition, the solubilizing agent may be sodium lauryl sulfate, LabrafilTM LabrafilLa bra sol LabrasolTween 60 Tween 60 or a mixture thereof, preferably sodium lauryl sulfate.
Further, the disintegrant is croscarmellose-sodium Crosscamellose-Nasodium starch glycolate Sodium starch glycolatepre-gelatinized Starch Pregelatinized Starchmicrocrystalline cellulose microcrystalline cellulosecrospovidone Crospovidonecross-linked povidoneand other commercially available polyvinylpyrrolidone polyvinylpyrrolidone, PVPlow substituted hydroxypropyl cellulose hydroxypropylcellulose, low substitutedalginate alginic acidcarboxymethyl cellulose carboxymethylcellulosecalcium salt and sodium salts, colloidal silicon dioxide Fumed silica collidal silicaguar gum guar gummagnesium aluminum silicate magnesium alumimum silicatemethyl cellulose methylcellulosepowdery cellulose, starch starchsodium alginate sodium It may be selected from the group consisting of alginateand mixtures thereof.
Further, is the content of the drug is sustained-release polymer of parts by weight of 10 to parts by weight per for, preferred may be an 20 to parts by weight. The cilostazol sustained-release tablet of the invention parts by weight of the sustained-release polymer for, Carbomer Carbomer 5 to parts by weight, Solubilizing agents from 10 to parts by weight, Disintegrating agents 30 to 70 parts by weight, and Cilostazol from to parts by weight In that it comprises the features.
The rebamipide sustained-release tablet of the invention parts by weight of the sustained-release polymer for, Carbomer Carbomer 5 to parts by weight, Solubilizing agents from 10 to parts by weight, Disintegrating agents 30 to 70 parts by weight, and Rebamipide to parts by weight In that it comprises the features.
The sustained-release tablet of the invention Ari piperacillin sol is parts by weight of the sustained-release polymer for, Carbomer Carbomer 5 to parts by weight, Solubilizing agents from 10 to parts by weight, Disintegrating agents 30 to 70 parts by weight, and Ari piperacillin sol from 20 to parts by weight In that it comprises the features.
While keeping the sustained release of a conventional matrix structure drugs for controlled release composition of the present invention has the for sustained release polymer, a sol-introduced into the carbomer with a gel conversion properties to prevent the rapid release of the drug due to the fall of the elution reviews matrix structure is.
Further, the resolution was not soluble, even after the drug is released for availability suffering problems due to the introduction of solubilizing agents, by introducing a disintegrant improves the limit of the initial release rate of the sustained-release preparation.
Figure 1 is a graph showing the dissolution test results of the non-containing solubilizing agents and disintegrating state. Figure 2 is a graph showing the dissolution test results of the solubilizing agent-containing state.
Figure 3 is a graph showing the dissolution test results of containing the solubilizer and a disintegrant state. Figure 4 is a graph showing a non-clinical trials of the present invention containing the solubilizer and a disintegrant.
Figure 5 is a graph showing a single clinical trials of the present invention containing the solubilizer and a disintegrant. Figure 6 is a graph showing the dissolution test results of another drug containing the solubilizer and a disintegrant.
Hereinafter, a detailed description of a preferred embodiment of the present invention. Further, there in the following description is described in many specific details such as concrete components, which is that the present invention without the need to be such particulars as provided to assist the overall understanding of the invention can be carried out is generally in the art who has the knowledge of it it would be obvious.
Then, in the following description of the present invention, a detailed description of known functions and configurations that are determined to unnecessarily obscure the subject matter of the present invention, a detailed description thereof will be omitted.
Drugs for controlled release composition of the present invention, parts by weight of the sustained-release polymer for, Carbomer Carbomer 5 to parts by weight, Solubilizing agents from 10 to parts by weight, and Disintegrating agents 30 to 70 parts by weight In that it comprises the features.
Agents that delay the dissolution of the pharmacological active ingredient is prepared by mixing a polymeric sustained-release, sustained-release polymer for the above in the present invention can be used both if the available polymer pharmaceutically acceptable, methyl cellulose, ethyl cellulose, hydrochloride methyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, sodium carboxymethyl cellulose and like cellulose derivatives, propylene oxide and its derivatives, polyvinylpyrrolidone, polyethylene glycol, polyvinyl alcohol, polyvinyl acetate, polyvinyl acetate phthalatethe poly may be a methacrylate, and a derivative thereof, Carbopol Carbopolpolyethylene oxide, glycerol monostearate, poloxamer and their copolymers or mixtures, and preferably hydroxypropyl methylcellulose.
Preferably may be used hydroxypropylmethyl cellulose, hydroxypropyl cellulose, methyl cellulose, polyvinylpyrrolidone, polyvinyl alcohol and its copolymers, or may be a mixture, and more preferably hydroxypropylcellulose.
The inventors have found that a sustained release using a mixture of carbomer in the general case of a sustained-release polymer for preparation required exhibit long dissolution times and constant drug elution pattern as compared to using a sustained-release polymer for a single component. It was also found that to control the elution pattern by adjusting the weight ratio of sustained release polymers and carbomer for.
The rapid dissolution of the drug may cause tachycardia, dujung feeling, headache, it is also important factor for a sustained release formulation that maintains, controls the dissolution rate constant. Hydroxy polymer for sustained release, such as methyl cellulose can secure a longer elution time by forming a matrix matrix for preventing the rapid elution of the pharmacologically active ingredient in the tablet.The title of the thesis is FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLETS OF ACECLOFENAC AND ITS PHARMACOKINETIC AND PHARMACODYNAMIC STUDIES IN ANIMAL MODEL.
Aceclofenac is a synthetic non- steroidal anti-inflammatory drug (NSAID) used in the treatment of rheumatoid arthritis, osteoarthritis and ankylosing spondylitis.
It. sustained release formulation of glimepiride. Keywords: Glimepiride, Sustained release, Matrix tablets, Wet granulation. INTRODUCTION The oral route of administration is considered as the most widely accepted route because of its convenience of self administration, compactness and easy manufacturing (Sastry et al, ; Seager et al, ).
ter-soluble drugs, the development of sustained release coated granules has a unique advantage of lessening the chance of dose dumping which is a major problem when highly water-soluble drug is formulated as matrix tablets. Most of the researchers have worked on matrix tablets and multilayered matrix tablets.
In the present study, a. In vitro release profile of Cilostazol SR tablets. Table 2. Drug release kinetic of Cilostazol SR tablet formulations. Next, the stable formula were designated for its in vivo test in rabbit.
Plasma concentration and pharmacokinetic parameters after oral administration of formulated ER matrix tablet CW5 and Cilostazol IR tablets 50mg were summarized inFigure 2andTable 3.
No sustained blood level was . The results showed probability of dose dumping from matrix tablets prepared without GC and GD. To describe the kinetics of drug release from matrix tablets, release data was analyzed according to different kinetic equations. compliance, a sustained release formulation of tramadol is developed5.
The main objective of the present work was to develop sustained release matrix tablets of water soluble Tramadol hydrochloride using different polymers viz. Hydroxy propyl methyl cellulose (HPMC) and natural gums like Karaya gum (KG) and Carrageenan (CG).