FIELD OF THE INVENTION:
The present invention relates to a liquid crystal gel for use in the production of transdermal
pharmaceutical compositions and therapeutic cosmetics that contains polyoxyethyleneglyceryl-
trioleate, propylene-glycol, iso·propyl-myristate. Specifically, the invention is
directed to compositions containing clarithromycin that are administered orally once a day.
BACKGROUND OF THE INVENTION:
Composition of Transdermal System
These designs typically consist of four layers: an adhesive layer, a semi-permeable
membrane that may act as a rate-limiting barrier, a drug reservoir, and an impermeable
backing membrane.
Transdermal delivery systems in cosmetics
Over the past 20 years, transdermal delivery systems have undergone extensive research
with the goal of breaking through the skin barrier to apply pharmaceutical and cosmetic
products more successfully. The barrier function of the skin continues to be a limiting factor
in the penetration and absorption of these actives, even though the cosmeceutical industry
has made significant progress in the development and incorporation of new and effective
actives in their products. The effects of partitioning and solubility, chemical enhancers
acting on the structure of stratum corneum lipids, and enhancement via modification of the
stratum corneum by hydration are discussed. The development of chemical compounds that
act as permeation enhancers and their mechanisms of action, as well as advancements in
suitable vehicles, such as gels, emulsions, and vesicular delivery systems, that can be used
for effective transdermal delivery.
Summary of the invention:
The transdermal system's the composition is the designs typically consist of four layers: an
adhesive layer, a semi-permeable membrane that may act as a rate-limiting barrier, a drug
reservoir, and an impermeable backing membrane.
To move between corneocytes, a molecule must also partition into and diffuse through the
estimated 4-20 lipid lamellae between each of these cells (Elias et al. 1983). This is true for
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molecules travelling via the transcellular route. Therefore, the transcellular pathway
necessitates the negotiation of numerous hydrophilic and hydrophobic domains.
Objectives of the present invention: ·
It is a primary object of the present invention to provide a colloidal systems that contain
complexes or hyaluronate that is water soluble
It is the further objective of the invention to provide a method of use for Hyaluronates or
complexes have the advantage of increasing the composition's viscosity, which improves
dosage and distribution accuracy when compared to natural skin components.
It is the ·further objective of the present invention to method of preparation of the
controlled release formulation. Active drugs that are poorly soluble in water and semipolar
media are further encouraged to be humidified by the hyaluronate or complex.The osmotic
structure effects of biopolymers, which are naturally occurring macromolecular parts of
living things, are generally also well known.
It is the further objective of the present invention to provide the Physiochemical,
pharmacological, and biopharmaceutical advantages are combined in transdermal
pharmaceutical compositions and healing cosmetics based on liquid crystal gels according to
the present invention. The compositions according to the invention are unquestiona.bly
superior to conventional vehicles based on the aforementioned benefits.
Description of the invention:
The p~esent disclosure is not pharmaceutical compositions of the invention can people have
applied a variety of substances to their skin to achieve therapeutic effects. In the present
day, numerous topical formulations hav.e been created to improve the appearance of the
skin and treat a number of conditions. With consumers' growing desire for skin that looks
healthy, there is a rising market for products that offer a variety of advantages with little
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effort. Modern consumers demand cutting-edge technological innovations with novel
formul~tions containing a variety of tested active ingredients. As a result, the development .
· of new products in the cosmetic industry is being driven by formulations that encourage
. skin permeability by actives.
, The active ingredients in· a therapeutic formulation must pass through the stratum corneum
(SC) and ·into the viable tissue after being applied to the skin. Understanding some aspects
of skin physiology and the variables affecting tran·sdermal delivery is necessary to
comprehend the transdermal delivery of actives within the structure of the skin. The barrier
function of the skin must be selectively overcome in order to deliver -beneficial ingredients
·to the skin cells effectively. The use of additives, such as chemical enhancers, is the most
popular and practical way to get around this barrier function. These substances have the
ability to "piggyback" the actives into the SC or alter the structure of the SC to make it more
permeable to the actives.
The pharmaceutical composition of the invention includes a effects and mechanisms of a
number of chemical enhancers are discussed in this review, and we summarise the trends in
the creation of formulations that will improve the penetration of active ingredients into the
skin. We will first discuss the general problems with transdermal permeation in order to
better understand the potential of permeation enhancers in skin delivery systems.
A molecule moving through the transcellular pathway must partition into and diffuse ·
through corneocytes, but it must also do so in the estimated 4-20 lipid lamellae that
separate each of these cells in order to move between corneocytes. Therefore, the
transcellular route necessitates the compromise of numerous hydrophilic and hydrophobic
domains.
Diagram of the "brick and mortar" stratum corneum showing the main stratum corneum
lipids and a lamellar organisation of intercellular domains. The potential active permeation
pathways through intact stratum corneum are also demonstrated. contribution of lipids to
barrier function, modification of the lipid domain's solubility, and modification of the .SC's
ordered structure.
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The suitability of an agent for inclusion in a transdermal delivery sys,tem (TDS) is influenced
by a number of factors (Pathan and Setty 2009). These include active substance potency
(dose 50 mg/day or, ideally, 10 mg/day), low molecular weight ( 500 Daltons), high
lipophilicity (logP in the range of 1-3). a low melting point ( 200 •q, and two or. fewer
hydrogen-bonding groups. Adequate solubility in oil and water is necessary for the
membrane concentration gradient to be high.
Variations in skin structure, thickness, lipid content, perfusion rate into the dermis, and
enzyme activity are among the factors that can explain the observed differences in
transdermal permeation between individuals as well as between sites on the same
individual. Different skin types, skin temperatures, states of the skin (normal, abraded, or
diseased), areas of application, contact times, levels of skin hydration, and pretreatments of
the skin have all been linked to variations in dosage.
The pharmaceutical composition must also include one or more active drug ingredients,
such as ondansetron, terbinafine, fluconazole, metronidazole, fentanyl, nandrolone
decanoate, nestron, norethisterone, eperisone, tolperisone, vinpocetine, ketamine,
vincristine, and vinblastine, according to the present invention. In addition, a transdermal
therapy application method and a liquid crystal gel with polyoxyethylene-glyceryl-trioleate,
propylene-glycol, isopropyl-myristate, and a hyaluronate or complex are used. The two are
connected.
A surfactant is an organic compound with a polar portion and a nonpolar portion that is
surface active or capillary active. The placement of these two components being
asymmetrical is crucial. Surfactants are typ.ically used as emulsifiers, wetting agents, and
solubilizing additives in drug formulations because they significantly lower the surface
tension of water.
Organic molecules known as auxiliary surfactants have no or very little surface activity
compared to surfactants, but they can still aid in their function and help cut down on the
amount of surfactant needed. Physiologically, surfactants are identical, but at higher
concentrations, they can harm mucous membranes and the skin.
Microemulsions and microemulsion gels both have multiple components (at least three, but
usually four). Microemulsions and liquid crystals have a lot in common, but their
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compositions are different from one another. A surfactant, often in conjunction with an
auxiliary surfactant, an oil, and water make up a microemulsion. According to Nuremberg E
(Pharmacia Acta Erbetica, 65 (1990), page 105), a microemulsion is a liquid, clear,
transparent, isotropic, and thermodynamically stable system. These are made of two
immiscible or partially miscible liquids and contain at least one surfactant, preferably a
combination of two surfactants. It needs a specific combination of the three elements in
order to exist.
At room temperature, microemulsion gels hold their shape, but these viscoelastic systems
are malleable and typically have a high viscosity. These -contain an oil and water-based ·
lipophilic component along with a surfactant, an auxiliary surfactant,. and other ingredients.
They exhibit transparency or slight opacity under the microscope. Microemulsion gels are
thermodynamically stable and appropriately isotropic systems.
Natural processes result in the formation of microemulsions and microemulsion gels in a
specific ratio of auxiliary surfactants, oil, and water. Phase diagrams can be used to calculate
the relative amounts needed for the formation of the microemulsion and microemulsion
gel. These three component phase diagrams each have a region that depicts a system and
structure that corresponds to a particular relative amount of the three components.
The triangle's three sides represent, respectively, the total concentration of the surfactant
and cosurfactant, the concentration of the oil phase, and the concentration of the aqueous
phase. The diagram can be used to experimentally determine the concentration range of
each component that leads to the formation of a microemulsion or microemulsion gel.
The pharmaceutical compositions of the invention provide Optical, rheological, and thermal
analysis techniques can all be used to study the properties of the microemulsion system,
including its structure, viscosity, stability, and optical isotropy or anisotropy.
Utilising a polarising microscope, the molecular arrangement (crystal-like characteristics)
can be confirmed. A high magnification image microscope connected to a computer displays
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a typical interference pattern (also known as the "Martese cloth") as evidence of the liquid
crystal state.
Rheological methods can be used to confirm ·the coalescence structure, and a relatively
straightforward method can be used to quantitatively describe the presence of liquid
crystals. In other words, a dramatic increase in viscosity occurs at a given concentration by
increasing the surfactant concentration in the solution.
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We claim:
1. Liquid crystal gel that contains polyoxyethylene-glyceryl-trioleate, propylene-glycol,
isopropyl-myristate, and hyaluronate or complex is used to make transdermal
pharmaceutical compositions and healing cosmetics. Crystal liquid gel. The
percentage of polyoxyethylene-glyceryl-trioleate in a liquid crystal gel used to make
transdermal pharmaceutical compositions and therapeutic cosmetics ranges from
26.7 to 40% (wlw) of the gel's overall weight. The liquid crystal gel in accordance
with claim 1, in which the liquid crystal gel varies. The amount of polyoxyethyleneglyceryl-
trioleate in liquid crystal gels intended for use in the production of
transdermal pharmaceutical compositions and healing cosmetics is preferably in the
range of 30-35% (w I w) of the gel's overall weight, comprising:
2. The amount of propylene-glycol added to liquid crystal gels used to make
transdermal pharmaceutical compositions and healing cosmetics ranges from 13.3 to
20% (wlw) of the gel's overall weight. The liquid crystal gel in accordance with claim
1, wherein said gel is utilised. The amount of propylene-glycol added to liquid
crystal gels used in the production of transdermal pharmaceutical compositions and
healing cosmetics is typically between 15 and 18 percent ·(wlw) of the gel's total
weight. The amount of propylene-glycol added to liquid crystal gels used to make
transdermal pharmaceutical compositions and healing cosmetics is preferably 16.7%
(wlw) of the gel's overall weight. Any one of claims 1 through 4 for liquid crystal gel,
wherein:
3. In liq.uid crystal gels for use in the manufacture
of transdermal pharmaceutical compositions and healing cosmetics, the amount of
propylene-glycol added to the gel varies in the range of 13.3 to 20% (w I w) of the
total weight of the gel The liquid crystal gel according to claim 1, wherein the liquid
crystal gel is used. In liquid crystal gels for use in the manufacture
of transdermal pharmaceutical compositions and healing cosmetics, the amount of
propylene-glycol added to the gel preferably varies in the range of 15-18% (w I w) of
the total weight of the gel. The liquid crystal gel according to claim 1, wherein the
liquid crystal gel is used. In liquid crystal gels for use in the manufacture
of transdermal pharmaceutical compositions and healing cosmetics, the amount of
propylene-glycol added to the gel is particularly preferably 16.7% (w I w) of the total
weight of the gel The liquid crystal gel according to any one of claims 1 to 4, wherein:
4. A liquid crystal gel with a polyoxyethylene-glyceryl-trioleate to propylene-glycol ratio
of 2:1 is used to create transdermal pharmaceutical compositions and therapeutic
cosmetics. Liquid crystal gel, as per any description. The amount of isopropylmyristate
added to liquid crystal gels used in the production of transdermal
pharmaceutical compositions and healing cosmetics ranges from 5 to 35% (w I w) of
the gel's overall weight.