WO2015093924A1

WO2015093924A1 - Vehicle for the administration of pharmaceutical compounds

Info

Publication number: WO2015093924A1
Application number: PCT/MX2013/000188
Authority: WO
Inventors: José de Jesús MONCADA ZUNO
Original assignee: CASTRO ALDRETE, Jorge Issac
Priority date: 2013-12-19
Filing date: 2013-12-19
Publication date: 2015-06-25

Abstract

The invention relates to a formula that uses particles of polyvinyl as a vehicle for the delivery of drugs. The invention has two main variants which can be consumed with water or injected for animals. The formula has a chemical action that improves the administration of the active substance, by combining a polyvinyl with same. The polyvinyl can serve as the preferred vehicle of the invention in order to achieve the improved results.

Description

VEHICLE FOR THE ADMINISTRATION OF PHARMACEUTICAL COMPOUNDS BACKGROUND

The administration of veterinary products is mainly against infections caused by sensitive germs. Certain type of drugs requires a minimum concentration in plasma to be able to do therapeutic affection. However, concentration is not always achieved effectively.

For this reason it is important that the vehicles with which the medicine is supplied manage to retain the active substance once they have entered the bloodstream or the tissue where they must be released.

For this reason it is important to design drug delivery vehicles that are useful for achieving acceptable vehicle concentrations. However recent inventions have presented problems for animals that are treated with novel vehicles.

In many medications, intramuscular administration develops an intense local reaction with hair loss. After subcutaneous administration, the area adjacent to the inoculation point may edematize in a mild and transient manner.

To understand how a vehicle works on a medication it is important to know the sections that form one.

A medicine is basically composed of:

1) One or several active ingredients (which really is "medicine"), which are those that produce the desired medicinal effect on the organism.

2) Inactive substances called excipient, which is the vehicle to which the active substance is incorporated to be able to administer it, since in most cases the amount of active ingredient that must be supplied is so small that we could not even take it.

i 3) Sometimes, they contain an adjuvant, which improves the biological availability of the active substance, for example, facilitating its absorption. Medications are given in doses called therapeutic at which they are effective. However, they are not without danger, they must be administered at the indicated doses and times as most are toxic at high doses. In some particular cases the optimal therapeutic dose and the toxic dose have very close values. In addition there are active ingredients that when supplied together enhance their effect when interacting.

The excipients for pharmaceutical raw materials for the production of dosage forms can be solid, liquid and semi-solid. Each having its own advantages and disadvantages. So far, polyvinyl has been used in various industrial applications without being used for a pharmaceutical formulation, having the advantage that it is stable, non-toxic and capable of containing the active substances and releasing them to achieve high concentrations, thereby the animal subject to which it was administered benefits.

The capsules do not have any more advantages when compared with the tablets as they integrate more rapidly in the presence of gastric fluids. Perhaps the only advantage is that there may be a variable absorption time. They are administered as capsules. There are some advantages, which are: Protect the drug from external agents, but not from moisture. They have a high physical resistance, it is enhanced if it is conditioned in a blister. Masks unpleasant organoleptic characteristics. Rigid capsules have a simple composition and elaboration. With the soft capsules a great accuracy in the dose is achieved. They allow controlled release systems. They have bioavailability characteristics.

Previously pharmacists received the doctor's prescription and chose the pharmacological materials to enter them into the capsules that he himself I prepared. Today it is the pharmaceutical laboratories who manufacture the capsules in special automated machines according to international standards and according to the pharmacopoeia in force in each country.

The origin of the gelatinous capsules is in the first half of the nineteenth century, its introduction is attributed to the French pharmacist Mothes, who in an attempt to mask the bad taste of some drugs used at that time, prepared jelly ampoules filled with the drug and sealed with a drop of a gelatin solution. In 1834 Mothes registered in Paris, together with the pharmacist Dublanc, the first capsule patent, the use of which extends rapidly to other countries, such as Germany and the United States. Thereafter, and since the patent restricted the production of capsules to Mothes itself, numerous attempts were made in the search for alternative materials and production methods.

The inclusion of glycerin in the formulation in order to improve the softness and elasticity of the capsules, making them more easily swallowable, is due to another French pharmacist: Taetz (1873). This modification led to the production of elastic capsules, which meant an advance in the administration of some drugs, such as fat-soluble vitamins. But it is not until 1932 when Scherer perfected the manufacturing process of these capsules, incorporating the first continuous encapsulation system. Rigid capsules as they are known today, were introduced by the Frenchman Lehuby, who, in 1846, patented them as a drug coating system. The American pharmacist Hubel contributed to the improvement in its elaboration, by introducing the use of metal punches, widely used in other industrial areas. From these works, two new pharmaceutical forms emerged, the gelatin-coated pills and the two-piece hard capsules. The first industrial scale manufacturing process for rigid capsules dates back to 1874. In 1942 the American Pharmacopoeia (USP) first collected the capsules as a pharmaceutical form.

The extended-release capsules are a presentation in which the drug particles are covered by substances such as resins that control the release of the drug for a longer time, which allows more time to be spaced between doses.

DESCRIPTION OF THE RELATED TECHNIQUE There are numerous classifications based on how to release the drug or on the mechanisms that govern such release. The following classification is intended to be as simple as possible, according to what appears in most of the pharmaceutical technology treaties :

• Accelerated release systems: freeze-dried oral forms

· Deferred release systems: enteric, gastro-resistant and pulsatile release systems or

Sequential.

• Extended release systems: tablets and matrix patches.

• Floating or bioadhesive systems.

The most important are described below:

1.- Accelerated release systems: these are solid forms that dissolve instantly in the oral cavity without the need for fluid administration. Examples of these systems are lyophilized tablets / tablets. In this group, different systems can be found depending on the release mechanism, such as rapid disintegration tablets in contact with saliva or orodispersible liotabs. Some cases are presented as systems that allow to increase the bioavailability of certain drugs by reducing the first-pass effect due to their sublingual or asymmetric absorption, through the oral, pharyngeal and esophageal mucosa; It must be taken into account that this has only been demonstrated in some orodispersible and specific active principles, taking into account the content of the technical data sheets and the studies provided.

2 - Deferred release systems: This group includes systems designed to release the drug in a delayed manner, which, without prolonging the therapeutic effect, allow the modification of the time or place where the release will occur. Here are the enteric cover systems that have the purpose of saving the contact of the active substance with gastric juices, well to prevent its inactivation or to prevent its gastrolesivity (example: microencapsulated aspirin). Most authors differentiate these systems from those designed for pulse release (pulsatile or sequential), where the active substance is released in several phases, usually two, one immediately and another after a certain time. In this way, it is possible to match the release of some active ingredients with certain hormonal circadian cycles3, or times of the day where it is of interest to have effective plasma concentration (Cp) of the drug. In these cases, it is intended to avoid the zero order incorporation kinetics because it is not desirable.

3.- Extended release systems: some authors also talk about controlled or sustained release. These are systems designed primarily to prolong the therapeutic effect or decrease the concentration peaks characteristic of conventional systems. These systems have been used for several decades, although innovations designed to facilitate dosage or provide a better pharmacokinetic profile continue to appear. In this sense, the change in galenic formulation is known, which allows a continuous release by presenting the active principle in a crystallized form, which dissolves slowly and continuously (example nifedipine). Osmotic systems include a drug release mechanism based on the use of tablets with a semipermeable membrane that allows the passage of water and produces the expansion of a hydrogel inside and the continuous exit of the active substance. A case that deserves special mention today is the matrix tablets due to the relevance they are reaching in the market. These are lipid, hydrophilic or insoluble polymers that allow the diffusion or release of the active ingredient in a more uniform and prolonged manner. An example of this is tamsulosin matrix tablets. This technology is also in the transdermal route of administration with fentanyl matrix patches. DETAILED DESCRIPTION OF THE INVENTION

The present invention is carried out by grinding polyvinyl solid material to reach particles less than 0.01 millimeter thick.

This material must be free of any contamination before entering the process, which can be done with any conventional process, which will not be included in this invention.

The material must be allowed to dry for two hours before being used. Subsequently it is introduced into an alcohol solution to free it from any impurity. Once the material is clean it can be included in a clean container where the pharmaceutical substance to be administered is preserved, it should be mentioned that said substance must be in a liquid state and not contain lumps.

Once the polyvinyl particles have adhered, it is necessary to let the substance stand for four hours so that it can be absorbed. SUMMARY OF THE INVENTION

Tangible effects in the improvement of plasma concentration in any mammalian animal. The formula object of this invention has two main variants that can be consumed by water or injectable for these animals. The present formula has chemical action that allows a better administration of the active substance achieved through the combination of a polyvinyl with the same.

Claims

Having described in detail and breadth, the invention of my sole and exclusive property, which I consider novel, I request and claim as my property what is contained in the following clauses: 1. A formula that is characterized by its novel composition that includes an element called a vehicle and another element called an active substance. In which the vehicle can be any compound derived from polyvinyl and the active substance any drug determined by its use as a veterinarian.

2. A variant of the first formula that uses a two-to-one composition of any polyvinyl material in relation to any active substance of veterinary drugs.

3. A variant of the first formula in which a composition is used in relation to half of a polyvinyl in relation to the active substance.

4. A variant of the first formula in which the active composition described in the preceding claims is used, which can be used as an injection in a saline suspension.

5. A variant of the first formula as described in claims one to five that can be used as an oral formula in any concentration of water that is therapeutic.