Composition for local tumescent anesthesia

Abstract

The present invention provides a composition for local tumescent anesthesia wherein 100 cc volume of the composition comprising 0.5-1 ml of local vasoconstrictor agent of concentration 1 mg/ml, 20-40 ml of local anesthetic agent of concentration 7.5 mg/ml; 1-2 ml of anti-fibrinolytic agent of concentration 500 mg/5 ml. The composition together generate less pain, minimize the bleeding risks and its post-operative complications, promote the tissue dissection and exerts a longer anesthetic effect. The local tumescent anesthesia composition is diluted in saline or ringer lactate solution. The composition may be employed in various surgeries selected from cosmetic surgery, plastic surgery, reconstructive surgery, head and neck surgery, ENT surgery, gynecological surgery, orthopedic surgery, proctological surgery.

Claims

1. A composition for local tumescent anesthesia, wherein 100 cc volume of the composition comprising: 0.5-1 ml of local vasoconstrictor agent of concentration 1 mg/ml. 20-40 ml of local anesthetic agent of concentration 7.5 mg/ml 1-2 ml of anti-fibrinolytic agent of concentration 500 mg/5 ml; wherein the composition together generate less pain, minimize the bleeding risks and its post-operative complications, promote the tissue dissection and exerts a longer anesthesic effect.

2. The composition for local tumescent anesthesia as claimed in claim 1, wherein said local vasoconstrictor agent is Epinephrine.

3. The composition for local tumescent anesthesia as claimed in claim 1, wherein said local anesthetic agent is Ropivacaine.

4. The composition for local tumescent anesthesia as claimed in claim 1, wherein said anti-fibrinolytic agent is Tranexamic acid.

5. The composition for local tumescent anesthesia as claimed in claim 1, wherein said composition is in the form of a liquid solution which is made in saline solution or ringer lactate solution.

6. The composition for local tumescent anesthesia as claimed in claim 1, wherein said Epinephrine is a racemic epinephrine.

7. The composition for local tumescent anesthesia as claimed in claim 1, wherein Ropivacaine has lower cytotoxicity and arrhythmogenic effects.

8. The composition for local tumescent anesthesia as claimed in claim 1, wherein said Tranexamic acid decreases the amount of bleeding.

9. The composition for local tumescent anesthesia as claimed in claim 1, wherein the composition can be employed in various surgeries selected from cosmetic surgery, plastic surgery, reconstructive surgery, head and neck surgery, ENT surgery, gynecological surgery, orthopedic surgery, proctological surgery.

Description

DETAILED DESCRIPTION OF PREFERRED EMBODIMENTS

[0020] The embodiments herein and the various features and advantageous details thereof are explained more fully with reference to the non-limiting embodiments that are illustrated and detailed in the following description. Descriptions of well-known components and processing techniques are omitted so as to not unnecessarily obscure the embodiments herein. The examples used herein are intended merely to facilitate an understanding of ways in which the embodiments herein may be practiced and to further enable those of skill in the art to practice the embodiments herein. Accordingly, the examples should not be construed as limiting the scope of the embodiments herein.

[0021] According to the present invention, it is contemplated that the composition (Reye's solution) for local tumescent anesthesia consists of combination of different components prepared in the form of liquid solution is very effective in minimizing bleeding risks. The one of the component epinephrine prominently known as adrenaline provides the local vasoconstriction effect at various sites of the infiltration. The composition includes Ropivacaine which demonstrates its function as a local anesthetic agent concomitantly provides a prolonged anesthetic and numbing effect. Another most crucial ingredient of the invention is tranexamic acid, a drug which is classified in the category of anti-fibrinolytic agents. Tranexamic acid is a substance which significantly reduces post-operative bleeding by altering selectively of the fibrinolytic system; it inhibits the formation of plasmin temporarily preventing the dissolution and degradation of fibrin clots.

[0022] In the present invention, the composition may be useful and employed in various surgeries according to this invention most preferably in cosmetic surgery, plastic surgery, reconstructive surgery, head and neck surgery, ENT surgery, gynecological surgery, orthopedic surgery, proctological surgery.

[0023] Furthermore, obtained experimental data evidence about the ability of the current composition named as Reye's solution achieves greater efficacy in reducing the bleeding episodes and its post-treatment complications with sustainable anesthetic effects. The available experimental data speaks for the surprising efficacy with usefulness in medical anesthetic treatments of the local tumescent anesthesia composition. Any references to the current composition or Reye's solution in this description should be understood as liquid solution form for its administration.

[0024] In the present invention, the composition for local tumescent anesthesia comprising epinephrine, Ropivacaine and tranexamic acid can be used in pharmaceutical preparations in combination with a pharmaceutically acceptable carrier. The components may be dissolved in the pharmaceutically acceptable carriers selected, for example 0.9% Saline Solution (100 ml) and Hartmann (Ringer's lactate) solution (100 ml). The term “carrier” applied to pharmaceutical compositions of the invention refers to an excipient or vehicle with which active components are administered. The vehicle as a carrier used must be sterile in nature to prevent the composition from microbial degradation. The composition can be employed with a 3 cc syringe and 30 G needle to get the subcutaneous layer in the tissue, it also can be injected as well in dermis; stop injection and pull back in case of bleed stain into the needle; it is forbidden to inject into the bloodstream.

[0025] Use of the composition of the present invention in the manufacture of a surgical medicament for significantly reducing bleeding risks, in usual manner comprising the step of admixing an effective amount of different components of the invention with a pharmaceutically-acceptable sterile vehicle or carrier. Reyes's solution is a mixture of elementary compounds used separately in different surgeries: cosmetical, gynecological, orthopaedical and so on, that using it together generate less pain, minimize the bleeding risks and promote the tissue dissection, leading to a safety surgery.

[0026] As disclosed herein, the dose of the components in the compositions of the present invention is determined to ensure that the amount administered continuously or intermittently will not exceed an amount determined after considering the individual conditions of a patient.

[0027] The composition is provided in the form of parenteral formulation which can be injected into the tissue imparts an excellent and appreciable behavior when administered into the body. A highly potent local anesthetic agent i.e. Ropivacaine, it is having long duration of activity and is supplied in injectable form. It is classified in the category of an amino amide, whose highly lipophilic; it has a middle lifetime from 14 min to 4 hours, it bounds to alpha 1 acid glycoprotein almost entirely with just a 6% free protein form, with an absorption and conjugation in the liver (aromatic hydroxylation transformed into 3-hydroxy-ropivacaine the 99% of all anesthetic agent) and it is excreted through the kidneys into the urine (86% approximately).

[0028] Subsequently in another embodiment, Tranexamic acid is used as an anti-fibrinolytic agent for decades for curing bleeding related complications. It has a high affinity to plasminogen and the subsequent form of plasmin reducing the effect on fibrin; after the administration it has a middle lifetime of 3 hours, it has a plasmatic protein bound of 3%, and has no free protein form. It will be excreted through the kidneys into the urine without a conjugated form (90% by the first 24 hours).

[0029] Moreover, Epinephrine which is prominently regarded as local vasoconstrictor agent is classified as a sympathomimetic amine, with a vasoconstrictor effect on alpha and beta receptors. The maximum concentration of epinephrine after a subcutaneous injection will be 20-40 minutes. It has a very short middle lifetime of 20 seconds. It will be metabolized by two enzymes, the catechol-o-methyltransferase (extra neural), and monoaminoxidase (intra neural) generating vanillylmandelic acid mostly in the liver. The principal metabolites are conjugated metanephrine (40%), vanillylmandelic acid (40%), dihydroxymandelic acid, metoxihydroxyphenylglycol and unadulterated epinephrine. The 50% of total doses will be excreted by the first 6 hours, the other 50% after next 18 hours into the urine.

Exemplary Formulations

[0030] The following exemplary formulations are given by way of illustration only and are not to be construed as limiting this invention in any way.

Formulation 1: In order to prepare Reye's Solution it combines the following components: [0031] 1 ml Epinephrine (Racemic) 1 mg/ml [0032] 40 ml Ropivacaine 7.5 mg/ml [0033] 1 ml Tranexamic Acid 500 mg/5 ml [0034] Saline Solution 0.9% q.s. 100 ml
Formulation 2: In order to prepare Reyes Solution it combines the following components: [0035] 1 ml Epinephrine (Racemic) 1 mg/ml [0036] 40 ml Ropivacaine 7.5 mg/ml [0037] 1 ml Tranexamic Acid 500 mg/5 ml [0038] Hartmann (Ringer's lactate) solution q.s. 100 ml

[0039] As mentioned, there remains the foregoing description of the specific embodiments will so fully reveal the general nature of the embodiments herein that others can, by applying current knowledge, readily modify and/or adapt for various applications such specific embodiments without departing from the generic concept, and, therefore, such adaptations and modifications should and are intended to be comprehended within the meaning and range of equivalents of the disclosed embodiments. It is to be understood that the phraseology or terminology employed herein is for the purpose of description and not of limitation. Therefore, while the embodiments herein have been described in terms of preferred embodiments, those skilled in the art will recognize that the embodiments herein can be practiced with modification within the spirit and scope of the appended claims.