What Are Nasal Drops?

Nasal drops refer to liquid preparations that are specially used in the nasal cavity of humans. Nasal drops are made of water, propylene glycol, liquid paraffin, and vegetable oil as solvents, and are usually made into solutions, but can also be made into suspensions or Emulsion. To promote absorption and prevent mucosal edema, osmotic pressure, pH and viscosity should be adjusted appropriately. The oil solution is less irritating and lasts longer, but it does not mix with nasal mucus. Nasal drops Ph should be 5.5-7.5, should be isotonic with nasal mucus, does not affect ciliary movement and secretion ion composition, such as compound nisone dragon nose drops ^[1] .

Drug Name: Nasal drops
Whether prescription drugs: Non-prescription drugs
Main indications: Rhinopathy

Dosage form: Liquid
Athletes use with caution: Inadvertent use
PH value: 5.5 7.5

Classification of nasal drops

Nasal drops

1. Vasoconstrictor. It can constrict mucosal blood vessels, eliminate nasal congestion and swelling, relieve nasal congestion, and improve ventilation, such as 1% hydrochloric acid

Nasal drops Ephedrine nasal drops.

2. Anti-allergic nasal drops. It is mainly used for patients with allergic rhinitis, such as ephedrine diphenhydramine nasal drops, ephedrine cortisone nasal drops, Kangfuxin nasal drops and so on.

3. Nasal mucosa stimulating wetting agent. It can make nasal mucosa blood vessels dilate, increase secretion, reduce dryness symptoms, and restore mucosal function. It can be used in atrophic rhinitis, such as clear cod liver oil, paraffin oil, etc., can promote mucosal wetting and exert mechanical protection.

4. Mucosal corrosive agent. Mucosal corrosives are mainly used to treat local erosion and bleeding of the mucosa, such as 5% silver nitrate and 30% trichloroacetic acid.

Nasal drops

1. Treatment of chest pain and heartache.

2. Treatment of hypertension.

3. Antiviral treatment.

4. Anti-inflammatory, antipyretic and analgesic treatments.

5. Treatment of dilated cardiomyopathy.

6. Treatment of headache.

7, antitussive treatment.

Characteristics of nasal drops

Nasal medication has the advantages of fast absorption, high bioavailability, and convenient use. It is especially suitable for drugs that are easily destroyed by the gastrointestinal tract and patients who are not easy or unwilling to take orally and injections, especially for children. The nasal administration of some drugs instead of oral or injection, especially those with poor oral or injection effects, and patients who cannot or will not take orally, has great potential in these areas ^[2] .

How to use nasal drops

When using nasal drops, patients should first clear the secretions in the nasal cavity. If there is dryness in the nasal cavity, it should be washed and soaked with warm saline before the dryness becomes soft and removed before dropping the medicine.

Two types of postures can be used when using nasal drops: one is supine and backwards, that is, the patient lies on the bed when the medicine is dropped, and a soft pillow is placed on the shoulder, so that the head is tilted back as far as possible and the nasal cavity is lower than the mouth Pharynx. When dropping medicine, the nasal drops should be 1-2 cm away from the nostrils. 3-4 drops of medicine each time. Let the medicinal solution flow down along the side of the nostril, and let the side wall of the nasal cavity buffer the medicinal solution, so as not to let the medicinal solution directly flow into the pharynx, making the bitterness unbearable. After dripping the medicine, use your fingers to press the nose a few times to make the medicine fill the nasal cavity. Then, keep the medicine dropping position for 3-5 minutes, then sit up. This method is better for patients with nasal mucositis, sacral sinusitis, ethmoid sinusitis, and frontal sinusitis. The second is the side-down side-down head type, that is, the patient lies on his side, so that the head is inclined to the side of the nasal cavity that requires medication, and the head is drooped to the shoulder, so that the head is lower than the shoulder, and then the medicine is dropped. The method of dropping medicine is the same as that described above. If both sides of the nasal cavity require dripping, then after 5 minutes of dripping from one side of the nasal cavity, tilt the body and head to the other side and then drop the medication. This method is better for patients with upper frontal sinusitis.

If two or more nasal drops are to be used at the same time, the interval between using the two drugs should be more than 3 minutes to avoid reducing the efficacy of the drug or causing adverse reactions. If both nasal drops and anti-inflammatory nasal drops can be used to shrink nasal mucosa blood vessels, the former should be used first, and the latter should be used later.

Long-term use of nasal drops can have many side effects. Therefore, the use of nasal drops is generally not more than two weeks. Infants and young children should try not to use nasal drops, so as not to affect the development of their nasal mucosa. Hypertensive patients should be cautious with nasal drops that can cause vasoconstriction of the nasal mucosa to prevent accelerated blood pressure elevation after administration. Dropping medicine into the nasal cavity is one of the main methods of treating rhinitis, sinusitis and other diseases.

Regulations on nasal drops

1. Unless otherwise specified, the medicinal materials shall be extracted and purified in accordance with the methods prescribed for each species.

2. Common solvents for nasal drops are water, propylene glycol, liquid paraffin, and vegetable oil. Suitable antioxidants, solubilizers, preservatives or other additives can be added according to the nature of the medicinal material extract or drug. Various additives must not be irritating to the respiratory tract and mucous membranes.

3. Unless otherwise specified, if the nasal drops are aqueous solutions, the pH and osmotic pressure should be appropriately adjusted. Generally, the pH should be 5.5 to 7.5, and isotonic with nasal mucus.

4. The nasal drops should be prepared in a clean and germ-free environment and filled in a sterile, clean and dry container in a timely manner.

5. The solution-type nasal drops should be clarified without precipitation and foreign bodies. The particles in the suspension-type nasal drops should be fine and uniformly dispersed, and the precipitates should not agglomerate after being placed, and generally should not delaminate within a few minutes after shaking. Opaque nasal drops should be evenly distributed.

6. Unless otherwise specified, nasal drops should have inspection items such as relative density and pH.

7. Unless otherwise specified, the volume of each container should not exceed 10ml.

8. Unless otherwise specified, nasal drops should be sealed and stored in a cool place.

Study on Stability of Nasal Drops

According to the principle of chemical kinetics, the stability of compound dima nasal drops was studied using constant temperature and accelerated test methods. According to the Arrhenius equation, logK was used to linearly regress the inverse Kelvin temperature 1 / T to obtain the linear equation logK = -5772.1721 / T + 14.006 (n = 5). r = 0.9998, K25 can be obtained from the equation, and K25 can be used to find the time required for decomposition by 10% (t0.9) ^[3] . The half-life of dexamethasone in the nasal drops at room temperature was calculated to be 19 years, and the valid period was 2.5 years.

Effects of nasal drops on ciliary activity

Under normal circumstances, nasal ciliary activity is an important manifestation of self-cleansing of cilia. The toxicity of nasal drug delivery system to nasal ciliary is an important factor affecting nasal drug delivery. This effect determines the patient's acceptance of drugs and the effectiveness of nasal drug delivery. . The toxic effects of nasal drops on cilia of the nasal cavity mainly include the effects of drugs, additives, penetration enhancers and preservatives on the activity of cilia. Jiang Xinguo et al. Proposed a new method of the toad maxillary model in vivo, measuring the ciliary toxicity of propranolol, gentamicin sulfate, and other 8 drugs. The results show that it is not only consistent with the results of the in vitro animal model method, but also, It has the advantages of measuring the ciliary toxicity of drugs in suspensions. This method is simple, feasible, widely applicable, and reliable. It is an ideal method for evaluating nasal ciliary toxicity ^[4] .

Nasal drops drug release absorption mechanism

Nasal mucosal absorption of drugs is generally considered to be the absorption process. Drugs with Mr <1000, fat-soluble drugs are easily absorbed, high bioavailability, generally close to 100%, and blood drug concentrations are similar to intravenous injections. Some drugs that are difficult to absorb in the gastrointestinal tract (such as cefotaxime and cefazolin) can also be absorbed through the nasal mucosa. Lee et al. Reported that some low-molecular-weight peptides have certain bioavailability when administered nasally, but have peptides exceeding 27 amino acids Bioavailability <1% for nasal administration. Corbo et al. Found that the absorption of drugs with large Mr can reach 0.6% -0.8%, for example, horseradish oxidase (HRP) Mr reaches 3300, and the bioavailability can reach 0.6%, indicating that the nasal mucosa is absorbed by hydrophilic biomolecules. It is a slow transport in the intercellular space. Generally, the diameter of the nasal mucosal cell space is 0.4-0.8nm. If the diameter of the biomacromolecules is less than 0.7nm, it can be transported through the intercellular space ^[5] .

Study on Nasal Drops Nasal Mucosa Penetration Enhancer

In recent years, there have been many studies on nasal mucosal penetration enhancers. As long as there are surfactants, protease inhibitors, fatty acids, etc., their mechanism of action is mainly the following: (1) reduce the viscosity of the nasal mucosa; (2) increase Membrane fluidity and permeability; (3) Enzyme inhibitors are added to reduce degradation of peptides and protein drugs by proteolytic enzymes. However, research has found that many penetration enhancement systems have certain side effects, destroying the structure of the nasal mucosa and causing abnormal morphology of the nasal mucosa cells ^[6] .