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C-6 kazim.pmd

ANNALS OF
PHYTOMEDICINE
Annals of Phytomedicine 1(2): 39-44, 2012
Formulation of solid dosage forms using natural ingredients and
novel method development for estimation of drug content
Syed Mohammed Kazim * and Mohammed Ibrahim *, **
* Nizam Institute of Pharmacy and Research Center, Deshmukhi, Pochampally, Near Ramoji Film City, Nalgonda-508284, AP, India **Asian Institute of Advance Scientific and Pharmaceutical Research, Hyderabad-500058, A.P, India. Received for publication September 7, 2012; accepted November 10, 2012 Abstract
The study is based upon the formulation of solid dosage forms, using naturalingredients and a novel method development for the estimation of individualingredients in various combination units. Tablets of analgesic drug mafenemicacid in combination with dicyclomine, a smooth muscle relaxant was prepared. Ahepatoprotective agent DL-methionine was also incorporated in the formulation.
Enhancement of bioavailability of analgesic tablets by introducing the seeds ofLallemantia royleana Benth (commonly known as Balanga) was achieved,accompanied with the estimation of the amount of methionine, incorporated in theformulation. The mathematical tool of orthogonal polynomials was implementedfor the above estimation of percentage purity of a particular ingredient in theabove complex formulation.The novel formulation is evaluated in terms of itsbioavailability by comparing the parameters like disintegration time and dissolutiontime, with that of the standard formulations. The above assessment was carriedout to establish the role of the natural disintegrant used. There are many methodsto enhance bioavailability; one of the methods is the reduction of disintegrationtime. Balanga seeds are used for the above purpose as the seeds are known tocontain plenty of mucilage within its chemical constituents. The mucilage absorbswater by imbibition and helps in tablet disintegration.
Key words: Balanga seeds, Bioavailability, Disintegration time, Orthogonal
Introduction
(i) Effect of water absorption
Disintegration: It can be defined as the process by which
The water absorbed by the tablet initiate disintegration, but the tablet breaks down or loses cohesion. It is the time required this depends on the solubility of the drug and other ingredients for the tablet to break down into aggregates. Several mechanisms of tablet disintegration have been proposed.
(ii) Swelling
Eventhough these concepts are listed separately.
Interrelationships probably occur in almost all tablet The grains of the disintegrant, particularly of starches, swell in the presence of water and exert pressure on the granulesto force them apart. Shangraw et al. (1980) reported thattablets of water insoluble drugs disintegrated faster withstarches than those of water soluble drugs due to thediminished water absorption capacity of the starches in the Author for correspondence: Professor Syed Mohammed Kazim
Nizam institute of Pharmacy and Research Centre, Deshmukhi, Imbibition is defined as the displacement of one fluid by Pochampalli, Near Ramoji Film City, Nalgonda-508284, A.P., India E-mail: s_m_kazim@yahoo.com
another immiscible fluid. This process is controlled and Tel.: +91-9866527616
affected by a variety of factors. The capillary number (Ca) and the mobility ratio (M) have the greatest importance. It isalso defined as the phenomenon by which the living or deadplant cells absorb water by surface attraction.
Porosity of tablets: It has been shown that penetration of
water into a tablet is proportional to its mean pore diameter or
porosity. The porosity and permeability of tablets decrease as
the tabletting pressure is increased, and as the porosity
decreases, the disintegration time increases. Though, no
quantitative relationships have been reported between
disintegration and penetration times, generally short
Dicyclomine hydrochloride
disintegration times are associated with rapid fluid penetrationand drug absorption. Thus, the above parameter is related Dicyclomine hydrochloride occurs as a fine, white, crystalline, directly to the absolute bioavailability of drugs (Shargel, 1999
practically odorless powder with a bitter taste. It is soluble in water, freely soluble in alcohol and chloroform, and veryslightly soluble in ether (Chananont and Hamor,1981).
Lallemantia royleana Benth (Commonly known as Balanga)
Methionine
Chemical constituents: 10.8% of fixed oil is present.
Verbenone (16.4%) and trans-carveol (9.8%) were the major
components of the oil (Braj Kishore Malavya and
Shikibhushan Dutt.,1941). The exact chemical constituents
responsible for the specific therapeutic activity are not
known. When moistened with water, the seeds become
voluminous and form translucent mucilage.
Chemical structure for DL-METHIONINE
Methionine may be one of the earliest organic substances,formed in evolution. In man, it is essential as a donor of thecritical methyl (CH ) group (Banesh,1978) and as a sulphur donor. The CH group comes from its activated form, SAM (S-adenosyl N-methionine), and goes into the formation ofimportant compounds like choline (in bile acids,phospholipids), creatine (in muscles), epinephrine (a neuro-transmitter), and carnitine (essential for oxidation of fat).
Methionine is also a component of enkephalin and variousendorphins (the painrelieving brain peptides), coenzyme A, Mafenemic Acid
heparin, biotin, and the tripeptide glutathione, an all-important Systematic (IUPAC) name 2-(2,3-dimethylphenyl) amino antioxidant and detoxifying agent. Vitamin B , B and folate, and probably magnesium are involved in methionine Mefenamic acid binds the prostaglandin synthetase receptors metabolism; and selenium, an essential trace element, needsmethionine for absorption, transportation and bioavailability COX-1 and COX-2, inhibiting the action of prostaglandinsynthetase. As these receptors have a role as a major mediator (Chaitow,1985). With low methionine levels, folate is trapped of inflammation and/or a role for prostanoid signalling in in the liver causing temporary folic acid deficiency activity-dependent plasticity, the symptoms of pain are (Anonymous,2008). Methionine is metabolised to temporarily reduced ( Cryer and Feldman,1998).
homocysteine, excess of which is believed to causeatherosclerosis by its oxidant effect (Murphy et al.,1985).
Dicyclomine hydrochloride is an antispasmodic and
This hazard is less with adequate Vitamin B which helps anticholinergic (antimuscarinic) agent available in various reconversion of homocysteine to the antioxidant (cystathione). Methionine hastens histamine breakdown and Chemically, BENTYL (dicyclomine hydrochloride) is reputedly lowers serum calcium in animals.
[bicyclohexyl]-1-carboxylic acid, 2-(diethylamino) ethyl ester, Methionine has been used to acidify urine, to antagonize hydrochloride with the following chemical structure: radiation effects and to treat paracetamol poisoning (Meredith et al.,1978) through its conversion into cysteine top and bottom is held against a 10 no. screen. Tablet is and glutathione. The average methionine dose is 1-2 g/day placed in each tube and the basket rack is positioned in a 1 liter beaker of water at 37 0C such that the tablet remains 2-5cm below the surface of liquid on their upward movement Methodology
and descend not closer than 2-5 cm from the bottom of the Extraction of balanga mucilage
beaker. A standard motor device is used to move the basketassembly ontaining the basket up and down through distance Crushed seeds were extracted by hot benzene in a large of 5-6 cm at a frequency of 28-32 cycles/min. limit specified is extraction flask, and after removal of the solvent by distillation; the crude fixed oil was left behind as a bottle green andsomewhat opalescent liquid. It was treated with animal Estimation of methionine in the pharmaceutical dosage forms
charcoal and Fuller’s earth and was ultimately obtained as by applying orthogonal polynomials
transparent light green oil(Mohammad Amini and Razavi, A novel method for the estimation of DL-Methionine in Three different formulations were prepared which are as various pharmaceutical dosage forms like tablets and syrups follows: Formulation-I was prepared according to the standardprocedure without the incorporation of balanga mucilage.
was developed. The absorbance of the solution was measured at 570 nm. Beer-Lambert’s law was observed to mucilage. Formulation-III was prepared by adding 4 g of obey in the range of 10-100 µg. In the estimation of methionine balanga mucilage. These three formulations were compared in pharmaceutical dosage forms, the quadratic polynomial by conducting the evaluation tests for tablet dosage forms coefficient was computed by measuring the fluorescence of such as weight variation, hardness, friability, disintegration the drug in 0.01N hydrochloric acid and six points equally spaced at 5nm levels on the emission spectrum from 550 to575 nm were plotted. The quadratic polynomial coefficient Formulation
was found to be linear (directly proportional) to the The conventional tablets were prepared with wet granulation concentration in the range 0.5 to 2.0µg.
technique. The active ingredients were mixed with the diluents Method - A
for about 4-5 min.Granulating agent was prepared withsoluble starch in the form of a paste. Granulation was done For quantitative analysis, mafenemic acid, dicyclomine, by mixing the mass powders to form a dough. Disintegrating methionine suspension (20 mg) was transferred to 100 ml.
agent as per the formula was dried starch and balanga calibrated flask and made up to the mark with water. In the mucilage. The mucilage was mixed along with the wet dough.
case of tablets accurately weighed powder equivalent to The dough was made to pass through a sieve of number10.
20 mg of methionine was transferred to 100 ml of calibrated The above obtained granules were dried in the hot air oven flask and made up to the mark with water. Weigh accurately for about 30 minutes at a temperature of 45 degrees. The 20 mg of the reference standards and transferred into a 250 ml above dried granules after removing the fines were lubricated calibrated flask and make up to the mark with water. Filter the with talc and aerosol. The above granules were punched into test reference standard solution, and pipette 5 ml of the test tablets using 10mm punch of concave surface (Table 1).
and reference standard into 25 ml calibrated flasks. The flasks Evaluation tests as per I.P.
are kept for 20 minutes in the boiling water along with the Hardness test
blank. The violet blue coloured chromogen having a maximumabsorbance was recorded at 570 nm. The flasks were allowed Monsanto hardness tester is used. The hardness of uncoated to cool to room temperature before being made up to mark with tablets should be between 3-7 kg/cm2 (Table 2).
water and the absorbance of the test and reference standard Friability test
solutions were read against blank at 570 nm. (Table 5).
Roche friabilator is used. 20 tablets are selected at random Method - B
and weighed. They are placed in a friabilator and operated The fluorescence readings of the standard methionine solution for 100 revolutions at 25 rpm. The tablets are dropped at a was scanned from 550 nm to 575 nm at 5 nm intervals, using distance of 6 inches with each revolution. The tablets are 0.01N hydrochloric acid as blank. The excitation wavelength then dusted and reweighed. The acceptable limit is 0.5 to 1% to measure the fluorescence reading was set at 570 nm as the excitation maxima occurred at this wavelength. The quadratic Disintegration test
polynomial coefficient was calculated for six points of 5 nm The standard pharmacoepial disintegration apparatus is used.
intervals for every segment from 550 nm to 575 nm.
It consists of 6 glass tubes that are 3 inches long, open at the P2f=(5) F -(1) F - (4) F – (4) F (-1) F + (5) F sec,7.0 min, 3 min 50 sec,4min 50 sec.and 1 min 10 sec ,2 min 18 sec, respectively. The subsequent reduction in the Where F is the value of fluorescence and the subscript disintegrating time is attributed again to the increase in the denotes the wavelength at which it is measured and the figures content of balanga. The disintegrant, particularly of in the brackets taken from standard texts on numerical mucilage’s, swell in the presence of water and exert pressure analysis. The quadratic polynomial coefficient (P2f) was more on the granules to force them apart quickly.
for the segment 550 to 575 nm and, hence, was chosen for themethod (George,1968 and Rao,1966). The amount of drug Both isomers of methionine D and L forms, gave Rf values content in the dosage form was calculated from equation 2.
0.32 and 0.40, respectively. The test sample showed thepresence of both the isomers. The violet blue chromogen Vt / Vs x Ws/ Wt x A.W/D x 100 = % of the label claim. …Eq. 2 gave linear responses on the concentration range 10-100 Where Ws and Wt are the weights of the standard drug and mcg. The recovery experiments gave 98 to 99% recovery the sample preparation.A.W is the average weight of the with 99 to 100% reproducibility by method A as shown in tablet and D the labeled drug content, all the weight being expressed in the mg. Vt and Vs are the values of quadratic Also the formulation was put on trial for the estimation of polynomial coefficient, calculated for the test and standard, percentage purity of methionine by applying orthogonal respectively, using Eq….active ingredients like asprin, polynomials to all the three formulations. The formulation 1 Ibuprofen and excipients like mannitol, parabens, sugar.
was considered as the standard and the other two formulations Essence and coloring agents did not interfere with proposed were compared with that of the standard one. The quantitative method as indicated by the quantitative recovery. The analysis for methionine in the test formulations 2 and 3 proposed method can be used for quantitative analysis of showed that the foreign absorbance’s were ignored by the application of the polynomial coefficients. The analysis was Results and Discussion
done by the application of quadratic polynomials with taking6 points into consideration.
Chemical tests of Lallemantia royleana Benth
Conclusion
Balanga powder was subjected to ruthenium red test, gavereddish pink colour, indicating the presence of mucilage in It is ascertained that natural disintegrants are far more superior the seeds. The above powder was also subjected to molisch to the synthetic ones. The disintegrant (balanga mucilage) is test formation of reddish pink ring indicates the presence of found to be absorbing water instantly, followed by its imbibition. This results in the easy break down of the tablets Evaluation of physical properties of tablets
in turn resulting in the deaggregation of all the granules.
Furthmore, mucilage of balanga seeds also helps in the The hardness of tablets of all the three groups of formulations dissolution of the drug. The high water absorption tendency 1, 2, and 3. was measured and was found to be within the of balanga mucilage which encircles each drug particle retains range of 5.0-6.2, 4.5-5.5,3.0-4.0, respectively. The addition of water within the vicinity and promotes the drug solvation.
balanga mucilage appears to have reduced the bulk density Balanga mucilage is found to be superior to other suitable of the powder blend and subsequently granules. However, disintegrants like aerosil (silica) in terms of action, availability the reduction in hardness for formulation 3 was found to be etc. Aerosil has been found to be less preferable as a disintegrating agent because it has carcinogenic properties, The three formulation categories were subjected to it is highly expensive and furthermore it has very low density comparative studies, taking their friability into account. The which creates difficulty in granulating tablets.The mucilage friabilities of three formulations were found to be in the range of balanga is, furthermore known to have various other of 0.48-0.88%,0.46-1.0%, and 0.97-1.2%, respectively. The properties like healing, laxative, etc. The mucilage is found to increase in friability is attributed the proportionate increase be stable and does not interact with other drugs or excipients.
in the content of balanga from formulations 1-3. However, The above study needs to be conducted in much more the friability of formulation 3 is still within the acceptable elaborated way and has a lot of scope and potential in limits. The three formulations were again subjected to upgrading the formulations in drug industry. Also the method disintegration test. The disintegrating times of the three of estimating drug content by using orthogonal polynomials formulations were found to be within the ranges of 5 min 50 is much more feasible and reliable and is also precise.
Table 1: Fromulation of tablets with natural ingredients
Ingredients
Formulation-I for
Formulation-II (a) for
Formulation-II (b) for
200 tablets
100 tablets
100 tablets
(Qty in g)
(Qty in g)
(Qty in g)
Table 2: Hardness tests as per I.P
Formulation-1
Formulation-2
Formulation-3
6(kg/cm2)
(kg/cm2)
(kg/cm2)
Table 3: Friability tests as per I.P
Initialweight(W1)gm
FinalWeight(W2) gm
Friability= (W1-W2)/W1X 100
Formulation 1
Formulation 2
Formulation 3
Table 4: Disintegration tests as per I.P
Formulation-I
Formulation-II
Formulation-II
(time in min)
(a) (time in min)
(b) (time in min)
Table 5: Assay of methionine by the proposed method% amount found
Method-I
Recovery studies
Reproducibility
Standard
Formulation-1
Acknolwedgements
Chananont, P. and Hamor, T. A. (1981). Stereochemistry ofanticholinergic agents. XV. Structure of 2-(diethylamino)ethyl 1- I sincerely thank to my guide, Dr. Mohammed Ibrahim, cyclohexylcyclohexanecarboxylate hydrochloride (dicyclomine
hydrochloride) Acta Cryst, 37:1371-1375.
Principal, Nizam Institute of Pharmacy and Research Centre,for rendering his suggestions and helping me at each and Shangraw, R.F.; Mitrevej, A. and Shah, M. (1980). A new era of tablet every step of completion of this research work successfully.
disintegrants. Pharm Technol., 4:49-57.
Shargel, L. and Yu, A.B. (1999). Applied biopharmaceutics and References
pharmacokinetics (4th ed.). New York: McGraw-Hill.
Mohammad Amini, A. and Razavi, S. (2012). Dilute solution properties
of Balangu (Lallemantia royleana) seed gum: Effect of temperature,
salt, and sugar. International Journal of Biological Macromolecules,
Elsevier, 51:3.
Benesh, F.C. and Carl, G.F. (1978). Methyl Biogenesis, Bio Psychiat,
13(4):465-480.
Braj Kishore Malavya and Shikibhushan Dutt ( 1941). Chemicalexamination of the fixed oil derived from the seeds of Lallemantiaroyleana Benth. Ph.D. Thesis, Department of Chemistry, Universityof Allahabad, Allahabad, U.P. India.
Chaitow L. (1985). Amino acids in therapy. Northamptonshire, UK:Thorsons Publishers Ltd.
Cryer, B. and Feldman, M. (1998). Cyclooxygenase-1 and
cyclooxygenase-2 selectivity of widely used nonsteroidal anti-
inflammatory drugs. Am. J. Med. May, 104(5):413-421.
George, W.S and William, G.C. (1968). Statistical Methods, Oxfordand IBH. (6th edition, Indian). IBH Publishing Co. Calcutta.
Meredith, T.J. (1978). Paracetamol poisoning in children. BMJ: 2:478-
4 79
Murphy, D.R.; Wexman, M.P. and Grieco, A.J.(1985). Methionine
intolerance, a possible risk factor for coronary heart disease. JACC,
6(4):725-730.
Oluwatoyin A. Odeku, (2008), Theories of disintegration.
.pharmainfo.net/tablet-evaluation- tests/disintegration/theories-disintegration.

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