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Controlled release formulations containing an active ingredient, preferably melatonin, and the method of preparation

a technology of controlled release and active ingredients, which is applied in the direction of medical preparations, nervous disorders, endocrine system disorders, etc., can solve the problems of high cost of controlled release formulations (or pulsatile forms) developed recently, subsequent loss of sleep induction effect,

Inactive Publication Date: 2004-03-04
AMBROS PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, a great disadvantage of those formulations is the relatively slow absorption of melatonin, often accompanied by low peripheral blood levels, with subsequent loss of the effect on sleep induction.
Additionally, the transdermal patches show limited application, because of poor compliance and the danger of leaving (forgetting to take off) the patch in the morning, and therefore having high melatonin levels during daytime (residual release from the patch), when the melatonin levels have to be very low.
On the other hand, the controlled release forms (or pulsatile forms) for oral administration developed recently are very expensive, being prepared as a various number of tablets placed in the same capsule.
Moreover, they are not suitable for the preparation of nutritional supplements, because of the use of synthetic retardants and excipients which are not allowed in nutrition and may have untoward effects.
In spite of this, up till now the exogenous administration of melatonin still presents serious problems connected with this compound's typical mode of action and its short half-life.
As previously mentioned, none of the solutions adopted up until now have resolved this problem satisfactorily.
Moreover, the existing controlled release ("pulsatile-release") formulations, are not suitable for use as nutritional supplements or as foods.

Method used

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  • Controlled release formulations containing an active ingredient, preferably melatonin, and the method of preparation

Examples

Experimental program
Comparison scheme
Effect test

example 2

Test in vitro for the Release Times of the Active Ingredients

[0059] The ready tablets, both in the pilot tests and in the experimental tests, as described above, were subjected to the following physical-chemical tests to obtain the following data:

[0060] a) weight uniformity;

[0061] b) hardness;

[0062] c) friability;

[0063] d) average content of melatonin;

[0064] e) content uniformity;

[0065] f) dissagregation;

[0066] g) time for the release of the active ingredient.

[0067] Weight uniformity, hardness, friability and disaggregation were checked by means of routine analyses according to standard procedures in the field. The average melatonin content and uniformity of content were determined by determination of the quantity of melatonin in the tablets.

Melatonin Analysis

[0068] The pilot batch samples were analysed for their melatonin content by means of direct radioimmunoassay method (RIA), using an anti-melatonin antibody (Stockgrand LTD) and 2-.sup.(125.vertline.)iodomelatonin (Amersham Inte...

example 3

Pharmacokinetics in Man (Blood and Saliva: RIA)

Materials and Methods

[0078] Subjects

[0079] Six adult subjects, 4 males and 2 females with an average age of 35 took part in the test.

[0080] The volunteers had previously been informed of the purpose of the research and received a memorandum on how it would take place. All gave verbal consent. All were healthy and had never suffered from any chronic diseases; none of them had taken any medicines for the 2 weeks prior to the test nor during the period of research.

[0081] The subjects taking part in the test took one tablet of melatonin (2 mg+1 mg) at 8.45 a.m., in two groups of three subjects. The time of administration was chosen in so as not to interfere with the normal rhythm of melatonin secretion in the 12 hours afterwards. All the volunteers were exposed to light of an intensity of >2000 Lux during the experiment.

[0082] In the first stage the determination of melatonin pharmacokinetics after oral administration was carried out by mea...

example 4

Effects on Sleep in Man

Materials and Methods

[0099] Subjects and Treatment

[0100] Ten patients (average age 56.+-.3.6 years) suffering from psychophysiological insomnia, were used in the study. All of were classified according to The International Classification of Sleep Disorders, Revised Edition, ASDA, 1997. All were informed and gave their verbal consent to take part in the study. All received case report forms to fill in the following parameters: Total Sleep Time (TST), Sleep Latency (SL), Wake After Sleep Onset (WASO), Number of Awakenings (NA).

[0101] The treatment was in "crossover" and lasted a week for every formulation. Prior / after (according to a random assignment) to the treatment with controlled release formulations containing melatonin according to this research (1+2 mg of melatonin), the subjects took standard formulations of melatonin in 3 mg tablets, followed by a washout period of three days. In both treatments the tablets were given at 22.30 hours. Then, according to...

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Abstract

A controlled release nutritional food supplement tablet having inner and an outer parts, the inner part being a slow release nucleus of melatonin and hydroxypropylmethylcellulose with the outer part being an immediate release cortex or coating of melatonin.

Description

[0001] This invention relates to new controlled release formulations containing an active ingredient, preferably melatonin, and the method of their preparation. Following their administration, the active ingredient, preferably melatonin, is released in with biphasic pattern and, in particular, rapidly during the first few minutes after its administration and later, slowly and gradually. Formulations obtained by such a process can be usefully employed in cases where controlled release of active ingredients contained in the formulation is needed, for example in disorders in the sleep / wake cycle and sleep disturbances, if they contain melatonin.FIELD OF APPLICATION[0002] This invention relates to new controlled release formulations containing melatonin, characterized by the fact that the active ingredient is released quickly at first and slowly and gradually later.[0003] Moreover, this invention relates to the use of those controlled release formulations as medicines, nutritional or he...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/20A61K9/24A61K9/54A61K31/4045
CPCA61K9/2077A61K31/4045A61K9/209A61P25/00A61P5/00
Inventor STANKOV, BOJIDAR M.
Owner AMBROS PHARMA
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